ABSTRACT

Packaging is designed to contain a product so that it is unable to interact with the environment. After containment protection is most important function of packaging. The product must be protected against the physical damage, loss of content or ingredients and intrusion of unwanted component of the environment such as water vapour, oxygen, dirt and light. An important role of pharmaceutical packaging is to transform the formulation into an attractive and marketable product. Pharmaceutical companies increasingly are working to improve productivity and reduce costs in their manufacturing and packaging operations. Expanding markets and innovative marketing strategies have led to an increased demand in packaging products. So many issues regarding the pharmaceutical product like stability, sell, patient compliance etc are related with the packaging and in regard to this; present review is done on the various advancements in the packaging techniques and selection of packaging material.

Keywords: Packaging, Packaging technologies, Pharmaceutical packaging 

ABSTRACT

Solubility is the phenomenon of dissolution of solid in liquid phase to give a homogenous system. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. Poorly water soluble drugs often require high doses in order to reach therapeutic plasma concentrations after oral administration. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities. Any drug to be absorbed must be present in the form of an aqueous solution at the site of absorption. The ability to increase aqueous solubility can thus be a valuable aid to increasing efficiency and/or reducing side effects for certain drugs. This is true for parenterally, topically and orally administered solutions. The solubility of drugs is defined according to (bio-pharmaceutical classification system) BCS classification system which divides drugs to different class according to its solubility. Solid dispersion is defined as dispersion of one or more active ingredients in an inert carrier or matrix known as solid dispersion. Solid dispersion reduces the particle size and changes the micro environment of the drug particle, increases the rate of dissolution and absorption and thus changes the biopharmaceutical properties of poorly water soluble drugs. The solid dispersion method, by which a drug is dispersed in a carrier to make it amorphous, is one of the pharmaceutical approaches most commonly employed to enhance bioavailability of poorly water soluble drugs. Various pharmaceutical approaches for the preparation of SDs, including co-precipitation, lyophilization, spray drying, solvent evaporation, fusion and powder mixing methods, have been reported. It’s a new and efficient technique to improve the solubility of poorly soluble drugs.

Keywords: Solubility enhancement, dissolution enhancement, carriers, mechanisms, characterization.

ABSTRACT

The last two decades have seen significant advances in the development of micro electro mechanical systems (MEMS) for use as sensors. MEMS based sensors have applications in fields of science ranging from physical and chemical sensing to biological disease diagnosis. The major advantages of MEMS sensors over conventional sensors include their potential for higher sensitivity, lower cost, smaller sample size, and label-free detection. Another important distinction is that MEMS sensors can easily be multiplexed to simultaneously detect multiple analytes. MEMS technology holds promise as the next generation of high sensitivity sensors.

Keywords: MEMS, cantilevers, microcantilevers, nanocantilevers.

ABSTRACT

Aerogel is world’s lightest material and drug delivery system. Aerogel having more than 15 entries in Guinness Book of the world’s record is very low density solid state gel which is derived by replacing the dispersion phase of gel with gas. Aerogels are prepared by sol-gel process to extract liquid component of gel through super-critical drying. This allows the liquid removed without causing the solid matrix in gel to collapse due to capillary action. Aerogel possesses some properties like lowest density, lowest optical index of reflection, lowest electric constant and highest specific surface area. Materials used for preparation of aerogel include silica, metal oxides, organic and biological polymers, carbon nanotubes etc. Both hydrophilic and hydrophobic gels can be prepared. Solvents used for preparation of gel are explosive so, they are replaced by non inflammable liquid carbon dioxide. Applications of aerogel are very wide. Aerogels are used as a composite, as an absorbent, as a sensor, as a catalyst, as a thermal insulator, for improving dissolution properties of some drugs etc.

Keywords: Aerogel, Aerogelification, Thermal insulator

ABSTRACT

Nanotechnology received a lot of attention with the never-seen-before enthusiasm because of its future potential that can literally revolutionize each field in which it is being exploited. In drug delivery, nanotechnology is just beginning to make an impact. The multidisciplinary approach of nanotechnology has opened new vistas for the development of nanoscale drug delivery systems to meet the requirements for new drug moieties. These drug moieties can either be integrated into the matrix or attached to the surface of drug delivery particles. The importance of nanotechnology in drug delivery is in the concept and ability to manipulate molecules and supramolecular structures for producing devices with programmed functions. Nanostructures like micelles, liposomes, dendrimers etc. and nanoparticles like solid lipid nanoparticles, polymeric/pegylated nanostructures, metallic nanoparticles etc. have been used to deliver drug at specific sites and reduce side effects on non target organs.

Keywords: Nanotechnology, Drug delivery system, Nanostructures, Nanoparticles, Nanosystems

ABSTRACT

Klinefelter syndrome is a chromosomal condition in which there is a presence of extra X chromosome in the males. It is characterized by small testicles, azospermia, gynecomastia, several general, craniofacial, oral manifestations and radiological manifestations. This review highlights the etiology, salient clinical features, features during the life span, other manifestations reported, oral and craniofacial radiological features, investigations, treatment, recent advancements in the management, risk factors of Klinefelter syndrome are discussed briefly.

Keywords: Klinefelter syndrome (KS), Taurodontism, Testosterone

ABSTRACT

Cancer is a general term applied of series of malignant diseases that may affect different parts of body. The main causes of cancer are alterations of DNA, mutations, damage, smoking, addiction to liquor, chewing tobacco, imbalance diet, exposure to certain chemicals (carcinogens) etc. Complementary and alternative medicine use is common amongst cancer patients. In many surveys, herbal medicines are amongst the most commonly used group of treatments. Herbal remedies are believed by the general public to be safe, cause less side-effects and less likely to cause dependency. Traditional medicine has a long history of serving peoples all over the world.  The use of herbal remedies and dietary supplements is widespread throughout the world, and use may be increasing. These are taken for a wide range of perceived benefits and treatment of specific conditions. Alternatively many herbals and dietary supplements may predispose to control in different types of cancer. In this article, we review the potential anticancer effects of herbal remedies and discuss the potential interaction between these herbal substances and conventional anticancer medications. These herbal medicines along with benefits also include some adverse effects. This review summarizes the role of some pharmaceutically important herbal medicines used in treating cancer.

Key Words: Traditional medicine,cancer,Dietary supplements, herbal remedies, potential interaction.

ABSTRACT

Peptic ulcer disease had a tremendous effect on morbidity and mortality until the last decades of the 20th century, when epidemiological trends started to point to an impressive fall in its incidence. Two important developments are associated with the decrease in rates of peptic ulcer disease: the discovery of effective and potent acid suppressants and of Helicobacter pylori. With the discovery of H. pylori infection, the causes, pathogenesis, and treatment of peptic ulcer disease have been rewritten. The inhibition of gastric acid secretion is a key therapeutic target for the ulcer diseases (viz., peptic, duodenal ulcers or that through H. pylori infection), gastro esophageal reflux disease (GERD), Zollinger–Ellison syndrome (Z-E), and gastritis. Currently this is achieved by blocking the acid secretary effect of histamine (HA) through the use of H2-receptor antagonists or the irreversible H+/K+-ATPase inhibitors, popularly referred to as proton pump inhibitors (PPIs). The incidence of ulcer diseases shows global variation and their treatment should be designed to alleviate the symptoms.

Key words: Peptic ulcer, Helicobacter pylori, Zollinger–Ellison syndrome

ABSTRACT

In traditional medicine, there are many natural crude drugs that have the potential to treat many disease and disorders, one of them is Butea monosperma (Lam.) Taub (Syn. Butea frondosa; Family Fabaceae) popularly known as 'palas', and commonly known as ‘Flame of forest’. Butea monosperma is a tree of tropical and subtropical climate found throughout the drier parts of India, often gregarious in forests, open grasslands and wastelands. It grows on a wide variety of soils including shallow, gravelly sites, black cotton soil, clay loams, and even saline or waterlogged soils. It is an erect, medium sized tree of 12-15 m high, with a crooked trunk and irregular branches. There are various species of Butea monosperma available over the world. The leaves 3 foliate, large and stipulate. Number of constituents belonging to imides, lactones, flavonoids, sterols, and alkaloids has been reported from various species of Butea. Butea monosperma is considered as a good source for products such as fodder, fuel, fibre, timber, gum or resin, dyestuff and traditionally in number of ailments. Pharmacologically Butea monosperma has been reported for various activities such as anthelmintic, anticonceptive, anticonvulsive, antidiabetic, antidiarrhoeal, antiestrogenic and antifertility, antiinflammatory, antimicrobial, antifungal, antibacterial, antistress, chemopreventive, haemaggultinating, hepatoprotective, radical scavenging, thyroid inhibitory, antiperoxidative and hypoglycemic effects and wound healing activities. The present review discusses the morphology, ethanobotany, phytochemical constituents, and traditional uses of each part of plants as well products of plant and pharmacological activities of each part of plant in details.

Keywords: Butea monosperma, morphology, ethnobotany, phytochemical, traditional uses, pharmacological properties

ABSTRACT

Hyperglycemia can be a serious problem if untreated in time. Chronic hyperglycemia that persists even in fasting states is most commonly caused by diabetes melitus, and in fact chronic hyperglycemia is the defining characteristic of the disease. Diabetes mellitus is the only non-infectious disease designated as an epidemic by the world health organization. This could have long lasting adverse effects on nation´s health and economic, especially for developing countries. the international diabetes federation(IDF) estimates the total number of people in India with diabetes to be around 50.8 million in 2010, rising to 87.0 million by 2030. The primary goal in the management of diabetes mellitus is the maintenance of blood glucose level.  Therefore, there is an urgent need to develop novel therapeutic agents without the development and progression of complications or compromising on safety. The present review provides an approach for the safe and effective treatment of diabetes melitus.

Keyword: Hyperglycemia, Hypoglycemic agents, PPARs

ABSTRACT

Solid lipid nanoparticles (SLN) introduced in 1991 represent an alternative carrier system to traditional colloidal carriers, such as emulsions, liposomes and polymeric micro- and nanoparticles. SLN are aqueous colloidal dispersions, the matrix of which comprises of solid biodegradable lipids. These lipid nanoparticles modify drug release, body distribution and kinetics of associated drugs. solid lipid nanoparticles hold great promise for reaching the goal of controlled and site specific drug delivery and hence have attracted wide attention of researchers. This review presents a broad treatment of solid lipid nanoparticles discussing their advantages, limitations, production techniques, drug incorporation, loading capacity and drug release, characterization and applications. The potential of SLN to be exploited for the different administration routes is highlighted also.

Key words:  Solid lipid nanoparticles , colloidal drug carriers, homogenization, Drug Targeting.

ABSTRACT

Ayurvedic medicine is a well known treatment procedure past many years. Glycyrrhiza glabra also known as Liquorice, sweetwood, Mulhatti etc. It has well known properties such as antiviral, glucocorticoid, anti-inflammatory, antioxidant, antiulcerative, anticarcinogenic and many more. Its indications in dentistry are also well noted such as in oral lichen planus, apthous stomatitis. This herb was tried in the vesicullobullous disorder which is not well recognized. This review portrays the properties, medicinal values such as antiviral, glucocorticoid, Hypocholesterolaemic, antioxidant, toxicities, anticancer, hepatitis, gastric ulcer, hepatocellular carcinoma and dosage of this precious herb.

Keywords: Ayurveda, Liquorice, Deglycyrrhizinated Liquorice , Glycyrrhiza glabra

ABSTRACT

Drug targeting is the ability to direct a therapeutic agent specifically to desired site of action with little or no interaction with nontarget tissue. Niosomes are one of the best carriers for drug targeting. Niosomes are microscopic lamellar structures formed on admixture of non-ionic surfactant of the alkyl or dialkyl polyglycerol ether class and cholesterol with subsequent hydration in aqueous media. Niosomes are biodegradable, relatively nontoxic, more stable and inexpensive, an alternative to liposomes. Niosomes can be SUV (Small Unilamellar Vesicles), MLV (Multilamellr Vesicles) or LUV (Large Unilamellar Vesicles). The method of preparation of niosome is the based on liposome technology. The basic process of preparation is the same i.e. hydration of the lipid phase by aqueous phase. Niosomes are characterized by vesicle size, bilayer formation, number of lamellae, membrane rigidity and entrapment efficiency. A method of in-vitro release rate study includes the use of dialysis tubing. Niosomal drug delivery is potentially applicable to many pharmacological agents for their action against various diseases including cancer and leishmaniasis.

Keywords: Niosome, Surfactant, liposome, targeting.

ABSTRACT

The oral route of administration is considered as the most widely accepted route because of its convenience of self administration, compactness and easy manufacturing, in which the sustain release drug delivery replaces the conventional administration of drug by delivery system. Recently, greater emphasis has been placed on controlling the rate and or site of drug release from oral formulations for the purposes of improving patient compliance and treatment efficacy, solving problems concerning targeting of a drug to a specific organ or a tissue and controlling the rate of a drug delivery to the target site. Matrix system are favored because of they are easy to formulate, and showing better patient compliance, effective etc, than ancient drug delivery, which showing many drawbacks like repeated administration, fluctuation in drug plasma level etc.; developing oral sustained release matrix tablet with constant release rate has always being beneficial to the pharmaceutical technologist. Matrix type drug delivery systems are an interesting and promising way for developing an oral controlled release system, which will maximize the pharmacological benefits and minimize the potential side effects. The matrix tablet releases the drug in continuous manner like diffusion and dissolution controlled way. Hydrophilic polymers with high gelling capacity are of particular interest in the field of matrix tablet.

Key words: Sustained release, Oral formulations, Hydrophilic polymers, Matrix tablet.

ABSTRACT

Nails are the hard and durable epidermal appendages structurally horny in nature. Nail plate is responsible for the penetration of the drug across it. There are number of formulations with antifungal agents viz. gels, creams and oral antifungals for the treatment of transungual infections. Among these entire nail lacquers is a new concept in treating nail infections. These nail lacquers are effective as monotherapy in treatment of superficial, distal and subungual diseases. The main purpose of topical nail preparations is to protect the nail plate and enhance beauty of nails. The medicated lacquer preparations are generally used in fungal diseases. Use of this system avoids oral toxicity of anti fungal drugs. The main challenge associated with developing nail lacquers for the treatment of nail disorders is to deliver the active concentration to the site of infection which is often under nail. Penetration of topical antifungal through the nail plate requires a vehicle that is specially formulated for transungual delivery. In this article we have tried to emphasize on need to develop nail lacquer for a promising antifungal treatment. This field could be explored for the treatment of Psoriasis²⁴ and Onychomycosis.²⁴

Keywords: Antifungal, Nail, Nail lacquer, Onychomycosis, Psoriasis, Transungual.

ABSTRACT

The anthelmintic activity of fruit extracts of an Indian Medicinal plant Syzygium cuminii Linn. was evaluated on earthworms of Pheretima posthuma. This is because earthworms have anatomical and physiological resemblance with that of intestinal roundworm parasites of human beings. Here anthelmintic activity of the herb was determined by time taken for paralysis and death of earthworms after suitable treatment and comparison with standard drug piperazine citrate. The ethanol extract of Syzygium cuminii fruit at concentration of 50 mg/ml showed most pronounced activity. The results suggest that fruits of Syzygium cuminii possess anthelmintic activity. There is scope for future study on this plant.

Keywords: Syzygium cuminii, anthelmintic, piperazine citrate.

ABSTRACT

The aim of this study is to prepare gastroretentive dosage form based on the super porous hydrogel (SPH) composites using metronidazole as a model drug for eradication of H pylori.Blowing technique was used to prepare SPH composites. The latter was used as a body for the drug delivery system. The core was made from matrix granules. Four types of retardants (Beeswax, carnauba wax, ethylcellulose, and Eudragit^®RS) were used to prepare the granules by fusion for waxes and wet granulation methods for other polymers. For each retardants, two ratios (1:1 and 1:0.5 of drug: retardant) were used. Simple new method for insertion of core inside the SPH composite by using syringe with wide end opening without use of glue to close the insertion site was applied. The system was characterized by scanning electron microscopy, FT-IR. Also swelling, mechanical, and dissolution properties were studied. Scanning electron microscopic images clearly show highly porous structure and interconnected channels. FT-IR study confirmed the formation of crosslinking poly (acrylamide- sulfopropyl acrylate) SPH composites. The delivery system achieved the equilibrium swelling in about 3 minutes with swelling ratio of 10.45 ± 0.9 and penetration pressure of 483.34 ± 48.0 cm H₂O. The results showed non-significant (p > 0.05) difference between loaded and unloaded SPH composites regarding mechanical and swelling properties. A significant difference (P < 0.05) was found among the cumulative amount of metronidazole released with time depending on the nature and ratio of each retardant. It can be concluded that the proposed drug delivery system based on superporous hydrogel composite is promising for gastroretentive stomach specific delivery of metronidazole.

Key words: Superporous hydrogel composites, Gastroretentive dosage form, metronidazole

ABSTRACT

The analgesic effect of the ethanolic extract of Myristica fragrans was studied in rats using the following models; Acetic acid induce writing, Thermal test (HOT PLATE), Formalin induced pain test. The results for all the models showed dose dependent and were significant (P<0.05). The control for acetic acid induced- writhing test showed 72+0.41, the extract at dose of 200mg/kg showed 34.25 + 0.85 while dose of 500mg/kg showed 20.5+65 and Aspirin drug group showed 3.5+ 0.65. There was an increase in pain threshold for thermal induced pain at 60mm pre-treatment. For the control group, the result showed 2.59  0.08 which was significant (P<0.05). When M. fragrans was given at 200mg/kg, the result was 8.75+ 0.72 and when given at dose 500mg/kg, the reaction time was 11.75 + 0.60. For the Aspirin drug group, the reaction time was 33.30 +1.52. The formalin induced pain was inhibited in both phases i.e 0-5mins and 15-30 mins, the result was still significant for both phases. The results for the control group were 97.25+0.48 and 90.5+0.65 for 0-5mins and 15-30mins respectively. For the extract (M. fragrans) at dose 200mg/kg the result for 0-5 min was 72.75 +0.48 and for 15-30 min, it was 44.75  1.32, at the dosage of 500mg/kg, the results were 57.5  0.65 and 31.75  0.72 at 0-5min and 15-30min respectively. The results for the aspirin drug group were 52.0 + 0.41 and 22.25 + 0.63 at 0-5min and 15-30min respectively. The results indicated that the analgesic effect of Myristica fragrans houtt (NUTMEG) ethanolic extract is both peripherally and centrally significant.

Keywords: Myristica fragrans houtt, Analgesic effects, Acetic acid writhing, Thermal test, formalin pain test, mice.

ABSTRACT

In the present study, the effects of pre-treatment with catecholamine on indomethacin-induced ulcer were studied. Rats were exposed to various treatments with epinephrine and dopamine 30 minutes before ulcer was induced using NSAID (indomethacin). Experimental ulceration was induced in fasted rats using Indomethacin (40mg/kg.p.o). Four hours later after indomethacin administration, the stomachs were opened under thiopentane anesthesia and the ulcer area scored by planimetry. Sections of the stomachs were prepared for histology and stained for apoptotic cell count. Acid secretion was also studied in the control and treated animals by pylorus ligation technique. Indomethacin treatment resulted in the formation of ulcer with ulcer index of 5.0±0.5 while the pre-treatment with catecholamine significantly reduced ulceration episodes (epinephrine: ulcer index=3.0±0.7, dopamine: ulcer index=2.0±0.7, p<0.05). Total Apoptotic score in the indomethacin-induced rats’ stomachs was 19.5±0.38. This was reduced to 4.3±1.70 and 1.3±0.33 in the epinephrine and dopamine treated rats respectively. Administration of catecholamine prior to indomethacin resulted in a significant reduction in total stomach acidity from 2.381±0.042 (indomethacin alone) to 1.581±0.12 (epinephrine-treated) and 1.358±0.12 (dopamine-treated) p<0.05. However, dopamine was found to have more inhibitory influence compared to epinephrine. The results suggest an effective drug combination therapy clinically for ulcer patients placed on NSAID especially indomethacin.

Keyword: Ulcer, catecholamine, apoptosis, total acid output, indomethacin, pylorus ligation technique.

ABSTRACT

To study the effects of ethanolic extracts of Vernonia amygdalina(VA) and Ocimum gratissimum (OG)on the testes of diabetic rats, thirty-two male rats were used. Control consisted of eight (8) rats which served as non- diabetic control, receiving sodium citrate daily. The remaining rats were injected intraperitoneally with streptozotocin(65mg/kg) to induce diabetes. The rats confirmed diabetic were randomly divided into three experimental groups (1, 2 and 3) made up of eight rats each. Group 1 received 6IU/kg of insulin. Group 2 was given 100mg/kg body weight of Vernonia amygdalina and 200mg/kg body weight of Ocimum gratissimum combined daily. Group 3 served as the diabetic control and was given distilled water. The entire investigation lasted for 6 weeks. Results revealed typical testicular architecture in the normal control. Diabetic control exhibited alteration of germinal epithelium, distortion of seminiferous tubules as well as vacuolation of seminiferous tubules. The effects of the extracts on diabetic rats’ testes showed improvements compared to the diabetic control group. It is therefore safe to speculate that the extracts of these plants used especially when combined exert some significant improvement in combating the adverse effects of diabetes on the testes of male rats.

Keywords: Vernonia amygdalina, Ocinum gratissimum, insulin, ethanolic extract, streptozotocin,diabetic, rats.

ABSTRACT

Nasal delivery protects drugs like salbutamol sulphate (SS) from hepatic first-pass metabolism. The study aimed to formulate mucoadhesive sodium alginate (SA) microspheres loaded with (SS) by emulsion cross-linking, with mucoadhesive polymers, for potential nasal delivery by-passing first-pass metabolism. Relevant physichochemical properties, in vitro release and irritation in rabbits were investigated. Stirring rate and cross-linking time affected microsphere parameters. Microspheres were spherical in shape, discrete, with smooth and porous properties favorable for intranasal absorption with high drug-loading of 78.7 %. Mixed-polymers microspheres exhibited higher degree of swelling. Kinetic analysis of release data showed a case II release kinetics for alginate microspheres, and anomalous mechanism for other mixed-polymers formulae. Pronounced sustained drug release over 8 hours was exhibited upon incorporation of Carbopol^® 934 and Hydroxypropyl methyl cellulose. The formulated microspheres showed high swelling ability and good mucoadhesion, offering a good potential for future in vivo study to confirm safety and avoidance of first-pass metabolism.

Keywords: Mucoadhesive microspheres; nasal; salbutamol sulphate; sodium alginate

ABSTRACT

This study was conducted to determine the probable suppressive role of certain grape components on detrimental effects of lipid peroxidation which accompanied with liquid storage of roosters' semen. A total of 60 White Leghorn roosters, 32 weeks of age, randomly divided into 6 groups of 10 roosters each were used in this experiment. Semen samples for each treatment group were collected on a weekly basis during the whole experiment period which lasted 10 weeks. Treatment groups were as follows: T1 = fresh semen (control group); T2 = semen diluted 1: 1 with Lake diluent (LD) alone; T3 = semen diluted with LD and supplemented with 4 ml of grape flavonoids; T4 = semen diluted with LD and supplemented with 4 ml of grape phenols; T5 = semen diluted with LD and supplemented with 4 mg of grape seed proanthocyanidins extract (GSPE); and T6 = semen diluted with LD and supplemented with 4 ml of grape juice concentrate (GJC). Results revealed that after 1, 7 and 14 d in vitro storage, the supplementation of roosters' semen diluent with certain grape components (T3, T4, T5 and T6) resulted in significant (p< 0.05) improvement in mass and individual motility of spermatozoa in comparison with control group (T1) and significant improvement in regard to percentages of live spermatozoa and normal spermatozoa and acrosomes compared with T1 and T2 groups. Besides, T3 and T5 groups surpasses all other treatments involved in the present study as concerns all of semen traits involved in the present study. In conclusion, grape components especially flavonoids and GSPE gave a good suppression against the detriments of lipid peroxidation during in vitro storage of roosters' semen for up to 14d.

Key words: Grape constituents, semen quality, storage ability, roosters' semen

ABSTRACT

The purpose of the present investigation was to enhance the dissolution properties and bioavailability of a poor water soluble drug (Glibenclamide) by matrix-type transdermal films. Eudragit S 100 (Ed S100) and Hydroxypropylmethyl cellulose (HPMC) were used individually or in mixtures to formulate the transdermal devices by solvent casting method. The physicomechanical evaluation of the polymer matrices was performed. The prepared films showed good physicomechanical characteristics as Ed S100 percent increased, where HPMC lowered these characters. In-vitro release studies of ideal films were evaluated and the results revealed that the amount of Glibenclamide released was affected to great extent by the polymer type and also the solvent used. HPMC films showed high release rates of the drug where Ed S100 retards and control the drug release rates. HPMC mixtures with Ed S100 in 1:1 ratio released about 100% of the drug after 6 hours. In vivo evaluation of the prepared films was investigated by testing the hypoglycaemic effects of the drug after transdermal application to diabetic rats. The observed results simulated that obtained after oral administration of Glibenclamide in a dose of 5 mg/kg. The obtained results revealed a good promise of using Glibenclamide via transdermal route which could be of excellent benefit when oral route is unavailable.

Keywords: Glibenclamide, Film devices, Tensile strength, Transdermal, Blood Glucose. 

ABSTRACT

In the southern and southwestern parts of Nigeria, xylopia aethiopica is much acclaimed to possess nutritional properties for the control of diverse or definite physiological processes and were evaluated and compared based on the folklore methods of the finished medicinal products and practices. Result showed variability and statistically significant differences in the percent composition of the detected bio-active phyto-mineral elements and suggested that the novel hydro-alcoholic formulations, specifically, hydro-methanolic, potentiated the stimulation of the phyto-minerals and ranked: hydro-methanolic (60.8%), > hydro-ethanolic (21.3%), > methanolic (11.81%) > ethanolic (6.15%). Evident in hydro-methanolic formulation, it can be a good source of the following micro-minerals: iron (32.7%), magnesium (10.2%), manganese (8.9%), calcium (7.6%), potassium (0.69%), zinc (0.36%), sodium (0.28%), phosphorus (0.08%) and lead (0.001%). The percent proximate composition ranged: carbohydrate 72.6 to 77.7, protein 12 to 14.7, fiber 2.99 to 6.0, ash value 2.5 to 3.9, lipid/fat 1.47 to 2.3, and moisture content 0.98 to 1.96. While the anti-nutrients detected were: tannin 87%, oxalate 12.03%, hydrogen cyanide 0.93%, and phytate 0.08%.  The findings of this study provided importantly that xylopia aethiopica can ameliorate natural healing and scientific credence on the rationale of the folklore hydro-alcoholic methods, particularly, hydro-methanolic formulations in processing and dispensing the finished bio-active products from which our understanding of the safety, effectiveness and quality of finished nutritional or medicinal products and practices may emerge.

Keywords: Xylopia aethiopica, proximate composition, anti-nutrients, hydro-alcoholic solvent, electrolyte profile.

ABSTRACT

The present experimental research work was undertaken to determine the analgesic and anti-inflammatory activities of novel xylopia aethiopica formulations based on folklore methods used in Nigeria for the management of chronic severe painful conditions on eggwhite induced paw oedma in both sex of albino wistar rats using the pain models of Randall and Selitto (1957) as adopted by Ugo Basile (Italy). Analgesic and anti-inflammatory activities of the different analgesia models at doses as low as 0.5mg/ kg & 2mg/ kg respectively were evaluated against the standard analgesic drug Piroxicam, at dose of 20mg/ kg. The analgesic and anti-inflammatory activities was dose, and sex dependant: females appearing to endure more pains than males and in the ratio 2:1; suggesting that xylopia aethiopica is efficacious in ameliorating pains .The results from the study demonstrated strong anti- nociceptive than anti-inflammatory activities and as evidenced the bioactive constituents of hydro-alcoholic formulations, particularly, hydro-methanolic, potentiated the effects which resonated with the local use of finished products and practices for medicine purposes. Studies with the pure samples are on the way in order to understand the precise mechanisms of action.

Key words: Analgesic & anti-inflammation activity, Piroxicam, xylopia aethiopica, hydro-alcoholic formulation, paw oedema, sex.

ABSTRACT

A reaction between Moxifloxacin HCl and FeCl₃ solution in slightly acidic medium was studied. It gave brown colour complex having maximum absorbance at 407.0nm. The reaction is selective for Moxifloxacin HCl with 0.00024µg/uL and different concentration of FeCl3 was applied.  The color reaction obeyed Beer’s law from 0.01 µg /µL to 0.00018 µg/µL of FeCl₃ solution having concentration 0.1ug∕uL and relative standard deviation 0.026%.The quantitative estimation of moxifloxacin HCl in blood sample is also studied.

Key Words: Moxifloxacin, UV-Visible Spectrophotometer, Ferric Chloride, Beer’s law, Color reaction, Analytical method

ABSTRACT

In the present study, a series of N-[5-(phenyl)-1,3,4-thiadiazole-2-yl] benzamide and N-[5-(phenyl)-1,3,4-thiadiazole-2-yl] acetamide were prepared by refluxing with benzoyl chloride and acetyl chloride with 5-phenyl-1,3,4-thiadiazole-2-amine. 5-phenyl-1,3,4-thiadiazole-2-amine were prepared by oxidative cyclization of thiosemicarbazone (through condensation of aromatic aldehyde and thiosemicarbazide). The structure of new compounds prepared during present investigation have been authentically established by their IR,¹H-NMR and Mass spectral studies. The antibacterial and antifungal activities of thiadiazole derivatives also reported. Some of these derivatives exhibit significant antimicrobial activity.

Key words:  Thiosemicarbazone, Thiadiazole, antibacterial, antifungal.

ABSTRACT

Most of pregnant women take prescription or non-prescription drugs during pregnancy. In general, unless absolutely necessary, drugs should not be used during pregnancy because it can affect the fetus .The aim of this study was to evaluate the patterns of drug prescriptions to pregnant women in tertiary care hospital. It was a cross-sectional descriptive study conducted at MediCiti Institute of Medical Sciences, a tertiary care hospital of Medchal, Hyderabad. Prescriptions given to outpatients and inpatients pregnant women attending the antenatal clinics were collected. A simple questionnaire was used to gather information. The drugs were classified according to the pharmacological class and their teratogenic potential. The most frequently prescribed drugs were oral iron, folic acid preparations, antacids, antibacterials and analgesics. Majority were in accordance with WHO criteria for rational use of drugs except for prescription by generic names. Average number of drugs per encounter was 3.5, most common route of administration was oral. Most commonly used drugs were iron, folic acid. Most common antibiotic prescribed was amoxicillin. Most common condition for which drugs were prescribed was cough, backache and fever. All the prescribed drugs were available in hospital pharmacy in sufficient quantities.

Keywords: Pregnancy, drugs, prescription, rational usage.

ABSTRACT

A simple reverse phase liquid chromatographic method has been developed and subsequently validated for simultaneous determination of Ofloxacin and Ornidazole in infusion dosage form. The separation was carried out using a mobile phase containing methanol and buffer (equal proportion of 0.01M orthophosphoric acid and 0.01M sodium phosphate monobasic dihydrate) with pH 4.00 adjusted by 20% of triethylamine in the ratio of 60:40 v/v. The column used was HiQ Sil C₁₈ (150 mm x 4.6 mm i.d, 5 µ) with flow rate of 1 mL / min using UV detection at 300 nm. The described method was linear over a concentration range of 1.25-10 µg/mL (r²>0.9991) for Ofloxacin and 3.12-25 µg/mL (r²>0.9992) for Ornidazole. Separation was achieved within 5 min. The mean % recovery was found to be 99.94% for Ofloxacin and 100.27 % for Ornidazole. The limit of detection (LOD) for Ofloxacin and Ornidazole were found to be 0.146 and 0.25 µg/mL respectively. Whereas the limit of quantification (LOQ) for Ofloxacin and Ornidazole was 0.44 and 0.77 µg/mL respectively. The results of the study showed that the proposed RP-HPLC method is simple, rapid, precise, accurate and cost effective which is useful for the routine determination of Ofloxacin and Ornidazole in bulk drug and in its infusion.

Keywords: Infusion, Ofloxacin, Ornidazole, RP-HPLC

ABSTRACT

A Simple, Sensitive, and rapid reverse phase high performance liquid chromatographic method has been developed for the determination of Bosentan monohydrate in bulk and tablet Dosage Forms. Chromatographic separation was achieved on a Zorbax SB-Phenyl (150×4.6 mm), 3.5 µm make: Aglient column with a 30:70 mixture of 0.02M sodium dihydrogen phosphate and HPLC grade Methanol as mobile phase, detection was at 225 nm, oven temperature is 30°C, injection volume is 20µL, flow rate is 1.5 mL/min and the expected retention of Bosentan monohydrate peak is about 5.2 minutes. Response was a linear function of concentration in the range 2-0.01 µg/mL for Bosentan monohydrate; correlation coefficiencent was 0.9999, respectively.LOD and LOQ for Bosentan monohydrate were found 0.01 µg/mL and 0.03 µg/mL based on signal to noise ratio(S/N). Accuracy (recoveries 90-98%) and reproducibility were found to satisfactory.

Key words: Bosentan monohydrate, S/N ratio, RP-HPLC method and validation.

ABSTRACT

The proposed method is a simple, accurate, precise, specific and rapid method for the simultaneous estimation of dextromethorphan hydrobromide (DXM) and chlorpheniramine maleate (CPM) in bulk and syrup formulation. Stationary phase consist of Eclipse-XDB C18 column(150×4.6mm, 5μm) and mobile phase with gradient mode consisting of phosphate buffer (adjusted to pH 3.0 with o-phosphoric acid): acetonitrile (80:20 v/v) was used. The flow rate was set at 1.0 ml/min and UV detection was carried out at 272 nm. The retention time of DXM and CPM were 9.05 min and 7.53 min respectively. The % recovery of DXM and CPM was found to be 99.58 ±1.33 and 98.24 ±1.97 respectively. DXM and CPM drugs were found to be linear over the concentration range of 2-50 µg/ml and 0.8 - 20 µg/ml respectively. The proposed method can be useful in the quality control of DXM and CPM in bulk drug and drug products. 

Keywords: Chlorpheniramine maleate, Dextromethorphan hydrobromide, RP-HPLC, Validation.

ABSTRACT

In the present study, the polyherbal antidiabetic nutraceutical formulation was screened for its safety and efficacy using albino wistar rats (130-150gm). The formulation consists of Gymnema sylvestre, Trigonella foenum-graecum, Allium cepa, Curcuma longa, Phyllanthus amarus, Tinospora cordifolia, Eugenia jambolana, Cinnamomum zeylanicum. The safety of the formulation was studied by acute toxicity studies according to Organisation for Economic Co-operation and Development (OECD) guidelines and efficacy was studied by using streptozotocin induced diabetes model at 45 mg/kg b.w. The test drug did not show any signs of toxic­ity or mortality up to 5000 mg/kg which was fixed as the cut off point for the maximum tolerated dose.  Antidiabetic activity was screened in streptozotocin induced diabetic rat model for 21 days using glibenclamide 1.5 mg/kg as standard and parameters like blood glucose level and weight variation were studied. After 21 days treatment the mean blood glucose level of the formulation, dose 1 (500mg/kg) treated group showed 142.50±1.11mg/dl, the formulation, dose 2 (250mg/kg) treated group showed 210.66±2.96 mg/dl, the standard group showed 137.66±2.10 mg/dl, Control group 433.33±9.89mg/dl, Normal group 94.83±0.30 mg/dl respectively and at a dose of 500mg/kg body weight. The formulation showed significant increase in the body weight. Therefore, the results indicated that the polyherbal neutraceuticals formulation is an efficacious and safer antidiabetic/ oral hypoglycemic formulation in Type II diabetes.

Keywords: Nutraceutical formulation, acute toxicity study, streptozotocin, antidiabetic activity.

ABSTRACT

Barlaria buxifolia Linn is one of the medicinal plants well documented traditionally in Ayurveda system of medicine and is highly valued in modern medicine owing to the presence of alkaloids, flavonoids, tannins, phenolic compounds, steroids. The plant is reported to contain phenol, flavonoid and tannin; phenolic and flavonoids compounds are reported to possess antioxidant and hence the plant may be used as organ protective. Keeping this in view, the plant was analysed for total phenol, flavonoid and tannin content. Catechol, quercetin and tannic acid reagents were used as standards for calibration of total polyphenols, flavonoids and tannins respectively. The quantification of total polyphenol, falvonoid and tannin content showed 14.65mg/gm catechol, 26.80mg/gm quercetin and 11.32mg/gm tannic acid equivalent respectively, the study indicates that the leaves of Barlaria buxifolia Linn exhibits the highest flavonoid, phenolic and tannin content. It can be used potentially as a readily accessible source of natural antioxidant.

Key words: Catechol, Phenol, Flavonoid, Quercetin and Tannin, Barlaria buxifolia Linn

ABSTRACT

Herbal remedies are very common all over the world and herbal medications are dispensed by apothecaries. Herbal remedies are seen by some as a treatment to be preferred to chemical medications which have been industrially produced. The medicinal values of plants are dictated by their phytochemical and other chemical constituents. Medicinal herbs have been an essential part of human society since the civilization started. They are boon of nature to cure a number of ailments of human beings. In the present study phytochemical screening for the presence of various phyto compounds of Ailanthus excelsa using Acetone Chloroform, n-Hexene & Distilled water has been carried out and was assayed for in-vitro antidermatophytic activity against human pathogenic fungi viz: Microsporum gypseum & Trichophyton mentagrophytes. Results obtained revealed that maximum eight phytocompounds among nine tested, has been observed in the Chloroform solvent extract followed by seven by Acetone & n-Hexene and the least six by aqueous extract. Further the antidermatophytic activity against human dermatophytes has revealed the Inhibition in the mycelial weight of test organisms, and the maximum 57.14% inhibition has been observed in the mycelial weight of Trichophyton mentagrophytes at 2:5 concentration ratio, whereas the maximum 34.88% inhibition ion Microsporum gypseum has further being observed. In the present study it has been observed that Trichophyton mentagrophytes is susceptible among the pathogens whereas Microsporum gypseum is resistant to the selected plant species extract.

Key words: Herbal remedies, Phytocompounds, Susceptible & Resistant.

ABSTRACT

Two simple and sensitive ion-pairing spectrophotometric methods have been developed for the assay of saxagliptin in pure form and in tablet dosage form. The developed methods involve formation of yellow colored chloroform extractable ion-pair complexes of the drug with Bromocresol Green (BCG) and Bromothymol Blue (BTB) in acidic medium. The extracted complexes showed absorbance maxima at 420, 415 nm for BCG, BTB, respectively. Beer’s law is obeyed in the concentration ranges 10-50 μg ml^-1 in both methods with molar absorptivity of 3.164 x 10³, 4.305 x 10³, L mole^-1 cm^-1 for BCG and BTB, respectively. These methods have been successfully applied for the assay of drug in tablets. Results of analysis were validated statistically and through recovery studies.

Keywords: Saxagliptin, extractive spectrophotometry, tablet analysis.

ABSTRACT

Gymnema sylvestre has been extensively evaluated for its in vitro and in vivo activity against diabetes mellitus. The leaves of the shrub Gymnema sylvestre contain a complex of pentacyclic triterpenes known as gymnemic acids that have been reported as potential therapeutic agents in the treatment of diabetes. The present study reveals the relationship between the structure and function of the medicinally important constituents of this plant. To understand the binding mechanisms of these active constituents, molecular modelling studies has been performed with dipeptidyl peptidase-4, protein tyrosine phosphatase 1B, sodium potassium ATPase, aldose reductase and glycogen synthase kinase-3β as target proteins using XP docking program of Glide, version 9.2, Schrödinger suit. These constituents showed favourable interactions with the amino acid residues at the active site, their by substantiating their proven efficacy as antidiabetic agents. The present study also gives an insight to the probable herb-drug interaction and reason for sudden hypoglycemic shocks that may occur on concurrent administration of Gymnema extract and synthetic drug, Glimepiride, for the treatment of diabetes.

Keywords: diabetes mellitus, docking, Gymnema sylvestre, gymnemagenin, glimepiride, Glide, in silico herb-drug interaction.

ABSTRACT

Acne is an inflammatory disease of sebaceous follicles of skin. The present study was conducted to formulate and evaluate the topical anti acne formulation of coriander oil with penetration enhancer. The antibacterial activity of Coriander oil against Propionibacterium acne and Staphylococcus epidermidis was investigated using disc diffusion method and minimum inhibitory concentration was determined by agar dilution method. The topical formulations were developed using menthol as the penetration enhancer and tested for physical parameters, drug content uniformity, spreadibility, extrudability and in-vitro diffusion. The results showed that coriander oil showed the MIC values of 1%v/v and 1.1%v/v against P.acne and S. epidermidis respectively. It was reveled from the results that all the formulations showed the increased zone of inhibition for both of the bacteria. The formulations with the addition of penetration enhancer showed the increased drug content as well as the invitro release which increased with increase in the concentration of menthol. The formulation  Fo₁₁ showed the drug content (98.9%), invitro- diffusion (98.2%) and maximum stability among all the formulations. So it is the potent formulation to be further developed for treatment of acne.

Keywords: acne vulgaris, antibacterial activity, coriander, penetration enhancer , in-vitro activity.

ABSTRACT

An attempt has been made in the present research to formulate periodontal inserts of  Satranidazole (STZ) to increase residence time and prolong drug release. The periodontal inserts were prepared using chitosan, a natural biodegradable polymer. Chitosan inserts containing Satranidazole (10%, 20% and 30% to the weight of polymer) were prepared by solution casting method using 1% v/v acetic acid in water. Further inserts containing 30% Satranidazole were cross-linked by exposing to the vapours of 2% v/v glutaraldehyde in water for two different time period of 2 and 4 hours to retard the release of drug. FTIR and DSC studies revealed that there was no interaction between drug and polymers. The inserts were then evaluated for their physicochemical parameters like uniformity of thickness, weight, folding endurance, % moisture loss, tensile strength; drug content and in vitro drug release studies.  In vitro drug release data indicated that the films showed an initial burst release followed by sustained release of the drug. The drug-loaded films that were not cross linked had released the drug up to 10 days and the films which were cross linked for different duration showed a progressive fall in the release of the drug and extended up to 18 days.

Keywords: Satranidazole, cross-linking, chitosan, periodontal insert.

ABSTRACT

In present study, a novel series of 6-bromo-2,7,8-trichloro-3-(3’-phenyl-4’,5’-dihydro-1H-pyrazol-5’-yl)quinoline_(a-i). These novel synthesized entities were elicited by IR, ¹H NMR, ¹³C NMR, C,H,N Analyzer and mass spectra. The entities produced in laboratory were screened with strains of bacteria and fungi like Staphylococcus aureus, Bacillus Megaterium, Proteus vulgaris, Escherichia coli, and Aspergillus niger respectively. Out of nine different entities synthesized five derivatives showed excellent antibacterial activity and rest of them showed moderate antimicrobial activity.

Keywords: antifungal agents, pyrazolines, antibacterial agents, chalcones

ABSTRACT

The present study was aimed to evaluate the effect of ellagic acid on physical and biochemical parameters and histopathological changes in tissues of streptozotocin (STZ) - induced diabetes in wistar rats. Diabetes was induced in wistar rats by single intraperitoneal injection of STZ (45mg/kg body weight). STZ-induced diabetic rats showed a significant increase in kidney weight, food intake, water intake, blood urea, serum uric acid and creatinine and a significant decrease in body weight, liver weight, plasma total protein and albumin when compared to normal rats. Oral administration of ellagic acid (50 and 100 mg/kg) in STZ-induced diabetic rats for a period of 35 days significantly improved body weight and reduced food intake and water intake when compared with diabetic control rats. Ellagic acid administration in STZ-induced diabetic rats restored the liver and kidney weight and also the biochemical parameters to near normal when compared to diabetic control rats. The results of the present study clearly show the preventive role of ellagic acid in STZ-induced diabetic rats. Results obtained from histopathological studies also supported the anti-diabetic effect of ellagic acid in STZ- induced diabetes.

Keywords: Diabetes Mellitus, Flavonoids, Ellagic Acid, Antioxidant, Insulin.

ABSTRACT

The present study aims at the formulation of a floating drug delivery system of an antiulcer drug nizatidine using different grades of HPMC (K100, K4M, K15M & K100M) and an effervescent agent i.e. sodium bicarbonate. It was found that the release rate of nizatidine from tablet formulations prepared from HPMC K100LV was very high as compared to that from formulations containing higher viscosity grades namely K4M, K15M and K100M. In the current study, it was also found that overall rate of drug release tends to decrease with increase in concentration of HPMC. These observations are in agreement with the results reported in literature i.e. with the increase in polymer concentration and viscosity grade, the viscosity of gel layer around the tablet also increases leading to enhanced diffusional path length for the drug to follow and thus limits the release of active ingredient.

Keywords: Nizatidine, gastroretentive, floating drug delivery, sustained release

ABSTRACT

Armodafinil is very slightly soluble in water; hence the drug may be slowly or incompletely dissolved in the gastro intestinal tract. So the rate of dissolution and therefore its bioavailability is less. In the present study an attempt has been made to prepare immediate release tablets of Armodafinil by using different superdisintegrants (croscarmellose sodium, pregelatinized starch and Avicel pH 101 to increase the rate of drug release from dosage form or the dissolution rate and hence its bioavailability. The prepared granules and tablets were evaluated for their physiochemical properties and in-vitro dissolution study was conducted for the prepared tablets. The in-vitro dissolution studies shows the release in the following order of superdisintegrants is croscarmellose sodium> Pregelatinized starch> Avicel P^H 101. It was concluded that the immediate release tablets with proper hardness, disintegration time and with increase rate of dissolution can be made using croscarmellose sodium as superdisintegrants (F9). The formulation F9 was selected as an optimized formulation for stability study and the in-vitro dissolution study showed that was no difference in percent of drug released between 1^st month and 3^rd month sample.

Keywords: Armodafinil, Immediate release tablets, Superdisintegrants, Magnesiumsterate

ABSTRACT

In the present study, novel co-processed superdisintegrants were developed by solvent evaporation method using crospovidone and croscarmellose sodium in the different ratios (1:1, 1:2 & 1:3) to formulate mouth dissolving tablet formulations of Meloxicam. The poor aqueous solubility of Meloxicam makes its absorption as dissolution rate-limited and thus delay onset of action. Mouth dissolving tablets of Meloxicam were prepared using the above co-processed superdisintegrants and evaluated for different parameters. Effect of co-processed superdisintegrants (such as crospovidone and sodium starch glycolate) on wetting time, disintegrating time, drug content and in-vitro release parameters have been studied. Based on in vitro dispersion time (approximately 19 sec), promising formulation CP1 was tested for in-vitro drug release pattern. Among the designed formulations, the formulation (CP1) containing 4% w/w of co-processed superdisintegrant (1:1 mixture of crospovidone and sodium starch glycolate) found as the best formulation based on drug release characteristics. From this study, it can be concluded that dissolution rate of Meloxicam could be enhanced by tablets containing co-processed superdisintegrant.

Keywords: Meloxicam, mouth dissolving tablets, direct compression, co-processed superdisintegrants, croscarmellose sodium, crospovidone.

ABSTRACT

Depression is an affective disorder characterized mainly by change in mood and is associated with significant morbidity and mortality. A number of drugs are used for treatment but their adverse effects compromise the therapeutic effects. Thus search for an agent with minimal adverse effects and maximum therapeutic benefit is going on.  In Asia, Camellia sinensis (CS) popularly known as green tea is widely used as a beverage and has been reported to have antioxidant property.On this basis, the present study was designed to evaluate the antidepressant activity of Camellia sinensis on albino mice. The antidepressant effect of Camellia sinensis was examined using two behavioral models, the forced swim test (FST) and tail suspension test (TST) in albino mice. The effect ofethanolicextract of Camellia sinensisin three different doses (3.3, 16.5 and 33mg/kg) was compared with the standard antidepressant, imipramine (10mg/kg).  Antidepressant effect was studied both on acute and chronic administration (14 days) of Camellia sinensis. Acute and chronic treatment with Camellia sinensis reduced duration of immobility in FST in a dose dependent manner. In TST acute treatment with Camellia sinensis reduced duration of immobility at 3.3 & 16.5 mg/kg; whereas on chronic treatment CS reduced duration of immobility at 3.3 & 33 mg/kg. Acute & chronic treatment with Camellia sinensis produced antidepressant effect in both FST & TST models of depression in mice.

Keywords: Anti-depressants;camellia sinensis; forced swim test; tail suspension test

ABSTRACT

An ethanolic extract of Tinospora malabarica (Menispermaceae) was studied for its effects on growth in two malignant cell lines including a Human Melanoma cancer cell lines (A 375) and Skin cancer cell lines (A 431) using MTT assay. In these cell lines studied, the extract decreased cell viability, inhibited cell proliferation, and induced cell death in a dose dependent manner. The ethanolic extract of T. malabarica showed good cytotoxicity and IC50 value of 49.87μg/mL and 112.54 µg/mL respectively. It could be a reliable source of potent pharmacophore for treatment of disease like cancer.

Keywords: Tinospora malabarica, Ethanol extract, Melanoma cancer and Skin cancer.

ABSTRACT

The present investigation was carried out for phytochemical profile from aerial parts of methanolic extracts of Stephania wightii by using Liquid Chromatography-Electronic Spray Ionization-Mass spectrometry (LC-ESI-MS). The results confirmed the presence of eighteen compounds in the crude extract and the pharmacological activities of the identified compounds were listed. The presence of various bioactive compounds justifies the use of the whole plant for various ailments by traditional practitioners.

Keywords: Liquid chromatography, mass spectrometry, Stephania wightii, aerial parts and bioactive compounds

ABSTRACT

A series of 4-[2-(4-chlorobenzyl)-4-oxoquinazoline-3(4H)-yl)benzoyl] derivatives  were synthesized. The synthesized compounds were characterized by IR, NMR and Mass spectral data. The synthesized compounds were screened for their antioxidant activity by DPPH (1-1-diphenyl 2-picryl hydrazyl) radical-scavenging method and Ferric reducing antioxidant power (FRAP) assay. The synthesized 2,3-disubstituted-3H-Quinazolin-4-one derivatives exhibited moderate to good Anti oxidant activity. Among those Compounds C-GY,C-GU,C-TP, and C-TY were found to be the most potent compound with Promising Anti-Oxidant activity.

Keywords: Amino acids, Quinazolin 4(3H)ones, antioxidant, DDPH,FRAP method.

ABSTRACT

Dissolution is a valuable qualitative tool to asses the biological availability and batch to batch consistency. Discriminative dissolution mediums are highly desirable to differentiate the dissolution profiles of two identical products which are varied in their composition, formulation technique, manufacturing process and site of manufacturing. The objective of present investigation is to develop discriminative dissolution medium for valsartan by using two different marked formulations named as VALZAAR and VALENT. The dissolution studies were performed in four dissolution mediums (0.1N HCl (pH 1.2), pH 4.5 acetate buffer, pH 6.8 phosphate buffer and distill water) at three different agitation speeds (50, 75,100 RPM). Model independent approaches such as difference factor (f₁) and a similarity factor (f ₂) were used to compare dissolution profiles. Among all the cases in pH 6.8 phosphate buffer at 100 rpm drug releases at faster rate and best suited to maintain sink conditions. Irrespective of other cases pH 4.5 acetate buffer at 50 rpm was considered as a discriminative dissolution medium because of its lesser similarity factor and higher difference factor. From the present experimental investigation the rate of dissolution was found to be influenced by pH of the dissolution medium and speed of the agitation. The usage of 4.5 acetate buffer at 50 rpm was found to be a discriminative dissolution medium for valsartan tablets.

Keywords: Valsartan, Dissolution medium, Difference factor , Similarity factor, Dissolution efficiency

ABSTRACT

Lornoxicam is comparatively a new non-steroidal anti-inflammatory drug, which is selective cyclooxygenase-1 and 2 (COX 1 and 2) inhibitors. Lornoxicam is a non steroidal anti-inflammatory drug that exhibits its anti inflammatory, analgesic and anti pyretic activities in animal models and it is presently available in the market only as tablet dosage form. It is preferred in the treatment of adults with osteoarthritis, acute pain rheumatoid arthritis, postoperative dental pain and primary dysmenorrhoea. The present study was undertaken with an intention to develop a stable and effective parenteral formulation, containing the drug Lornoxicam. Lornoxicam is a light sensitive and insoluble water soluble drug but unstable at higher temperature in water. So the effects of various co solvents in the solubility of  Lornoxicam have been evaluated. Lornoxicam was tried with co solvents such as PEG-400, β-cyclodextrin and Sodium Lauryl sulphate. The drug was made into injection formulation for administered as a SVP. Various batches of Lornoxicam injection formulation were prepared in order to assess the influence of heat, light, atmospheric oxygen and antioxidant on the stability of the drug and the formulations were also subjected to accelerated stability test. Out of all trials, formulation containing Sodium Lauryl sulphate was found to be more soluble, stable and passed all tests satisfactorily.

Keywords: Lornoxicam, osteoarthritis, β-cyclodextrin, dysmenorrhoea, Sodium Lauryl sulphate

ABSTRACT

The aim of this study is to find the usage of antimicrobials in hospital section and to study the frequency of morbidity and mortality. The present study was undertaken to screen rational use of antimicrobials in inpatient department (IPD). Prescriptions from medicine, surgery, obstetrics (OBG) were collected over a period of nine months. Prescriptions containing antimicrobial drugs were analyzed for appropriateness in dose, dosage, duration of therapy. In our study we found that, out of 362, 179 were males and 189 were females. In that most commonly Cephalosporinns 142 (39.22%), Quinolones 128 (35.35%), Antiprotozoal 63 (17.40%) followed by Macrolides, Aminoglycosides, Penicillines, and Anthelmentics were prescribed. Our findings indicate an urgent need for the establishment of proper guidelines, dissemination of information to practitioners and supervision of antimicrobial usage in low income countries like India. Irrational and unnecessary drug use can be expensive and harmful leading to resistance.

Key words: Antimicrobials, Prescription, Health Care

ABSTRACT

The changes in polyphenols and caffeine alkaloid compositions of black tea, due to the variations of fermentation temperature were investigated. Black tea was manufactured by fermentation at various temperatures such as 26^oC (Control) 30^o, 36^o and 40^o where the tea leaves were fermented initially for 45-50 minutes at an private factory. During this oxidation process, withered and rolled leaf looses its green colour acquiring copper red to brown colour. Drying terminates these biochemical changes and remove moisture thereby the colour of fermented leaves turns from copper red to black and fermentation is arrested. Total polyphenols content were determined colorimetrically using Folin-Ciocalteau method and caffeine was isolated from all the samples by Liquid-Liquid extraction using chloroform. The results showed that increase in fermentation temperature significantly increases caffeine content whereas polyphenols content showed a great reduction at 30^o, 36^o and 40^o. However further studies are needed to evaluate the organoleptic characters such as taste and aroma.

Keywords: Black tea, fermentation, polyphenols, caffeine, yield difference.

ABSTRACT

E. littorale (Chota-kirayat or Chota–chirayata) is a glabrous perennial herb belongs to family Gentianaceae. It is traditionally used as antidiabetic, urinary astringent, antiperiodic, anthelmintic, anti-inflammatory, laxative and carminative. It possesses antioxidant, antimicrobial, antiedematologinic. antitumour activities. The present study deals with the pharmacognostical evaluation of Enicostemma litorale Blume. The physicochemical parameters like ash and extractive values were determined. The fluorescence analysis was observed both under ordinary light and UV light. The phytochemical analysis on extract was done by using different solvents and revealed the presence of steroids, terpenoids, alkaloids, phenolic compound, quinine, flavanoid, Tannin and Amino acid and identified by the basis of IR and gas chromatography-MS. The results of this study could be useful in setting some diagnostic indices for identification and preparation of the monograph of the plant.  

Keywords: Phytochemical, Pharmacognosy, E.littorale, IR, GC- MS

ABSTRACT

A rapid and sensitive High Performance liquid chromatography (HPLC) method has been developed and validated. The analyte was extracted from human plasma by simple precipitation technique. Nifedipine was used as the internal standard. A Princeton C₁₈ column provided chromatographic separation of the analyte. A simple, selective, rapid, precise and economical reverse phase High Pressure Liquid Chromatographic method has been developed for the estimation of Lercanidipine in human Plasma. The method was carried out on a Princeton C₁₈ (250 mm x 4.6 mm i.d., 5µ) column with a mobile phase consisting of acetonitrile: Water (adjusted to pH 3.5 using orthophosphoric acid) (55:45 v/v) at a flow rate of 1.0 ml/min. Detection was carried out at 235 nm. The retention time of Lercanidipine Nifedipine, was 5.31, 10.00 min, respectively. The proposed method has been validated with linear range of 5.0-250.0 ng/ml for Lercanidipine. The precision and accuracy values are within 10%. The overall recovery of Lercanidipine was 96.4 %. The developed and validated method was applicable for the pharmacokinetics studies.

Keywords: Lercanidipine, HPLC, Validation

ABSTRACT

In the present study, antifertility effect of ethanolic extract of Cassia fistula leaf on the fertile male albino rats was studied. The sperm count was significantly decreased when treated with extract. Similarly, the sperm vitality, sperm motility were also decreased after the treatment of Cassia fistula extract. The abnormalities of sperm were also increased in the Cassia fistula extract treated rats. Thus the C. fistula may be used as a male antifertility agent.

Keywords: Male antifertility activity; Cassia fistula leaves

ABSTRACT

Urolithiasis in its different forms is a frequently encountered urological disorder. For many years it has been at the forefront of urology. In the present study ethanolic extract of whole plant of Saccharum spontaneum (Linn.) was studied for its antiurolithiatic activity against most common type of renal stone i.e. calcium oxalate. Lithiasis was induced in rats by fed with a calculi-producing diet (CPD: commercial diet mixed with 3% glycolic acid) for 28 days. Glycolic acid treated rats showed significant increase (p < 0.05) the activities of oxalate synthesizing enzymes such as glycolic acid oxidase (GAO) in liver and lactate dehydrogenase (LDH) in serum, urine kidney and liver Administration of the ethanolic extract of S.spontaneum (200mg and 300/kg b.wt.dose^-1 day^-1oral^-1) has significantly ameliorated to near normalcy in the curative group.. The results of the present study confirmed that S.spontaneum can be used as a curative agent for urolithiasis.

Keywords: Urolithiasis, Saccharum spontaneum, glycolic acid, glycolic acid oxidase, lactate dehydrogenase,

ABSTRACT

The aerial parts of plant contain a number of medicinally important compounds. The present study was carried out to extract the flavonoid rich fraction from the aerial parts of Hemidesmus indicus Linn. R. Br. and identified the phytochemicals presents in the flavonoid rich fraction of aerial parts of Hemidesmus indicus Linn. R. Br. & determined the total flavonoid contents and antioxidant potential of obtained favonoid rich fraction of Hemidesmus indicus Linn. R. Br. Total flavonoid content was estimated by Aluminium Chloride colorimetric method and the flavonoid content was 0.406 % TFC (Total Flavonoids Contents) in grams of Quercetin equivalent. Antioxidant activity was evaluated by DPPH method and IC₅₀ value of flavonoid rich fraction of aerial parts of Hemidesmus indicus Linn. was found to be 21.39 µg/ml.

Key words: Total flavonoids, Aluminium chloride, Antioxidant activity, DPPH, IC₅₀ value.

ABSTRACT

To evaluate the use of tricyclic antidepressants, selective serotonin reuptake inhibitors and benzodiazepines in elderly patients aged over 60 years. Prospective, cross sectional, descriptive type of study was carried out in the general medicine department of a 640 bedded multispecialty tertiary care teaching hospital, South India. Benzodiazepines were prescribed in 79.6% patients, selective serotonin reuptake inhibitors in 12.3% and tricyclic antidepressants in 8.27%. The study identified 81.7% inappropriateness in prescriptions. Initiation of treatment with high dose after admission contributed to 32.6% while prescribing without proper indication accounted for 31.7%. Significant reduction of inappropriateness (48%) was observed during the post implementation phase, especially in the number of prescriptions of tricyclic antidepressants. The initial dose of alprazolam was reduced to 0.25 mg in all elderly patients. Prescribing benzodiazepines without proper indication reduced from 31.7% to 22%. Long acting benzodiazepines were not prescribed during this phase. The study demonstrated an overall improvement in the prescribing pattern of tricyclic antidepressants, selective serotonin reuptake inhibitors and benzodiazepines in elderly patients.

Key Words: Antianxiety agents, tricyclic antidepressants, selective serotonin reuptake inhibitors, benzodiazepines, elderly, prescriptions.

ABSTRACT

An aqueous extract of the leaves of Eclipta alba (Astraceae) was obtained by cold maceration process and tested for it antimicrobial activity against Fusarium species to ascertain preservative potential in food products. The screening was performed against Fusarium oxysporum and Fusarium subglutinans by agar plate disc diffusion method at 50 µg/ml and 100 µg/ml concentrations. The results were interpreted by Kirby-Bauer standard and indicated that the extract showed significant antimicrobial property against Fusarium species, however, predominant activity was found against Fusarium oxysporum.

Keywords: Eclipta Alba, Aqueous extract, Antimicrobial, preservative, Fusarium species.

ABSTRACT

There is a growing demand for herbal cosmetics in the world market and they are invaluable gifts of nature. Therefore, the basic intention of the present study was to design a proper formulation contain the flower extract of Butea monosperma (FEBM) with improved physical parameter. To accomplish this intention the herbal gel was prepared and subjected to evaluation of the various parameters. The cosmetic gel formulation was designed by using ethanolic extract of FEBM in varied concentration (0.5, 1 and 1.5%) using carbapol 940 as gelling agent and evaluated for various parameters. The study was also undertaken to evaluate the stability of gels. The prepared gels were evaluated for various physicochemical parameters such as physical observation, homogeneity, pH determination, viscosity, spreadability, extrudability, drug content, rate of drug permeability, stability as per ICH guidelines and HPTLC fingerprint profiles. All developed gels showed good homogeneity with absence of lumps. All gels were found to be stable with respective to their pH, viscosity and drug content. The extrudability and spreadability were also found to be less variant after stability study. The gels of Butea monosperma are radically permeable from skin of rats as demonstrate by the in-vitro permeation study. However, further preclinical studies of gel need to evaluate further confirming the reported biological activities. There is also need to evaluate effects especially in human phase, would be beneficial to assess its usefulness more exactly.

Keywords: Butea monosperma, gel, physicochemical properties, in-vitro permeation, stability.

ABSTRACT

The objective of the present study was to formulate a solid self micro emulsifying of drug delivery system (SMEDDS) for oral administration to improve the solubility and bioavailability of Lamotrigine. Solubility was determined in various oils, surfactants and cosurfactants. Ternary phase diagrams were constructed to evaluate the micro emulsification existence area. The optimized formula is obtained by factorial design employed as statistical tool.  The optimal formulation consists of 20% Capmul MCM C₈, 55% Labrasol , 25% Tween 80 was adsorbed on carriers Aerosil200, Microcrystalline cellulose (MCC) .The solid SMEDDS are characterized by globule size analysis, and drug release studies of formulations are compared with plain drug. The pharmacokinetic study in rats for the optimized formulation was performed and compared to plain drug powder. SMEDDS have significantly increased the Cmax and area under the curve (AUC) of Lamotrigine compared to powder (P < 0.001). Thus, this self-micro emulsifying drug delivery system should been effective oral dosage form for improving oral bioavailability of Lamotrigine.

Key Words: Solid self-microemulsifying drug delivery system, Globule size, Dissolution, Oral bioavailability

ABSTRACT

The structural and therapeutic diversity coupled with commercial viability of small heterocyclic molecules has fascinated organic and medicinal chemist. So, a great deal of research was carried out in the field of heterocyclic containing sulphur and nitrogen, because of their immense biological importance. The thiadiazole derivatives posses’ different pharmacological and biological activity. Hence, the search for never effective antimicrobial agents is imperative. It focuses on the problems of cross resistance and better activity against variety of infections. The majority of 1, 3, 4-thiadiazoles are based on the cyclisation of thiaosemicarbazide derivative incorporating this basic structural unit. The structure of new compounds prepared during present investigation has been authentically established by their IR, ¹H NMR and Mass spectral studies. The antimicrobial activity of thiadiazole derivatives also reported some of these derivatives exhibit significant and broad spectrum antimicrobial activity. All the synthesized compounds were screened for antibacterial activity against Bacillus subtilis, Bacillus pumilus, E coli and Pseudomonas aureginosa by Disc diffusion method using ciprofloxacin as a standard against Gram positive and Gram negative bacteria.

Key Words: Thiadiazole, Thiosemicarbazide, Antimicrobial, Cyclization, Screening 

ABSTRACT

The aim of this study is to enhance the solubility of poorly water soluble drugs via the mixed hydrotrophic solid dispersion strategy using ibuprofen as a model drug because Ibuprofen is absorbed after oral administration, it is critical to improve the dissolution rate to enhance the bioavailability, due to its low water solubility. Solid dispersions were prepared by mixed hydrotrphic method. In vitro dissolution studies showed remarkable improvement in solubility and drug dissolution profile of these new ibupro­fen solid dispersions over pure ibuprofen. It was observed that dissolution rate of ibuprofen enhanced to a great extent by solid dispersion technique using citric acid and urea as a hydrotrophic agents.The results indicates that mixed hydrotrophic solid dispersion may serve as a successful strategy for enhancing solubility of poorly water soluble drugs.

Keywords:  Mixed Hydrotrophic solid dispersions, Solubility, Drug release study, Dissolution

ABSTRACT

Salvadora persica L. (family- Salvadoraceae) is an evergreen small tree commonly known as Pilu, Jal and toothbrush tree. It is used in the treatment of pain, low fever, toothache, nose trouble, piles, scabies, inflammation, scurvy, gonorrhoea, chest disease and boils.  The present study was undertaken to evaluate the antinociceptive activity of the successive extracts (chloroform, ethyl acetate, ethanol and aqueous extracts) of powdered leaves of Salvadora persica L. at the dose of 500 mg/kg b. w. using eddy’s hot plate method. The results of the statistical analysis showed that chloroform and ethyl acetate extracts have significant antinociceptive activity. From the results of antinociceptive effects it can be concluded that the chloroform extract of the powdered leaves of Salvadora persica has shown significant activity (P < 0.05) at 30 min and significant activity (P < 0.01) at 60 and 120 minutes. The ethyl acetate extract has shown significant activity (P < 0.01) at 30, 60 and 120 minutes when compared to the control group. While the standard drug (Morphine Sulphate) shown significant activity (P < 0.01) at 30, 60, 120 and 180 minutes. Other successive extracts (ethanol and aqueous extracts) could not produce the significance of the difference from the control as antinociceptives. Hence present investigation reveals the antinociceptive activity of chloroform and ethyl acetate extracts of leaves of Salvadora persica L

Key Words: Salvadora persica L. antinociceptive activity, chloroform and ethyl acetate extracts

ABSTRACT

Olmesartan medoxomil is an angiotensin II antagonist used as an antihypertensive drug which has poor oral bioavailability. Hence, an attempt was made to prepare and evaluate mucoadhesive buccal films containing Olmesartan medoxomil as model drug. Various mucoadhesive buccal films were prepared by employing HPMC alone, and in combination with Eudragit RL100, Carbapol 934, Ethyl cellulose were prepared by solvent casting method using ethanol , water and acetone as solvents, tween 80 as solubilising agent and glycerine as plasticizer. The prepared mucoadhesive buccal films were evaluated for their physic-chemical parameters such as thickness uniformity, weight uniformity, folding endurance, drug content , surface pH, swelling index, bioadhesion, percentage moisture loss and uptake, vapor transmission rate. The formulations exhibited good results. In – vitro drug release studies were conducted for OLM loaded films in phosphate buffer (pH 6.8) solution. The drug release was in the range of 67 to 90 % in 6hrs.. Stability studies were carried out with selected formulation. In- vivo release was evaluated in rabbits by patch test and it showed good correlation with the in-vitro release data. Drug release was found to be diffusion following zero order as per kinetic studies.

Keywords: Mucoadhesive buccal films,Omedoxomil, HPMC, Carbopol 934, Eudragit, Ethyl cellulose, swelling study, Bioadhesion, in – vitro release, in-vivo study.

ABSTRACT

Different formulation technologies intended for gastro retentive dosage form were investigated and patented over the years. The aim of this study was to formulate, optimize and evaluate the gastro retentive floating tablet of stavudine. The developed technology induces a low density dosage form containing high concentration of active pharmaceutical ingredient (API). In the present work, the in-vitro sustained release of stavudine from matrix of tablet containing HPMC K100M and Xanthan gum as release retardant polymers has been studied. Sodium bi-carbonate and citric acid are used as gas generating agents. The tablets were prepared by direct compression method. The tablets eroded upon contact with the release medium 0.1N HCl and  the relative importance of floating lag time,% swelling index and % drug release patterns varied significantly with the concentration of polymers. Optimization was done by using design expert 8.0.4.1 and optimized formulation F6 of stavudine floating tablet shows no significant change in hardness, drug content, floating lag time and % cumulative drug release pattern after the stability period of 3 months at 40⁰c/75% relative humidity.

Key-words- Stavudine, HPMC, Xanthan gum, floating tablet, in vitro buoyancy.

ABSTRACT

A series of novel schiff bases containing N-benzyl piperidine moiety (1a-d) were synthesized by the reaction of N-benzylpiperidine-4-carbaldehyde with suitable aromatic amines. And synthesized schiff bases were converted to a series of novel 4-thiazolidinones (2a-d) by the reaction of Schiff base with mercaptoacetic acid. The chemical structures of the synthesized compounds were confirmed by using spectroscopic and chemical analysis techniques. All the above compounds were screened for their antimicrobial activity against some selected pathogenic microorganism. Good level of antimicrobial activity has been displayed by both categories of compounds against tested pathogenic microorganism. Thiazolidinone derivatives (2a-d) showed higher activity than schiff base derivatives (1a-d).

Keywords: N-benzylpiperidine-4-carbaldehyde, 4-Thiazolidinone, antimicrobial activity, Schiff base, Heterocyclic compounds, N-benzyl piperidine moiety.

ABSTRACT

A simple, rapid, novel and normal phase chiral HPLC method has been developed for the separation of S-Silodosin from R-Silodosin and quantitative determination of S-Silodosin enantiomer in Silodosin bulk drugs. The proposed method was based on normal phase chromatographic separation on Polysaccharide-Based Chiral Stationary Phase, Chiral pak AS-H column (250mm ×4.6mm i.d.; particle size,5µ) at a temperature of 28°C using a mobile phase consisting of n-Hexane, Ethanol and Diethyl amine (600 : 400 : 0.1 v/v/v) at a flow rate of 1mL.min^-1 with an injection volume of 10μL. Quantitation was achieved with UV detection at 270 nm based on peak area with linear calibration curves. The elution times of S-Silodosin and R-Silodosin were 5.0 min and 6.0 min respectively. In this proposed chiral HPLC method, the resolution between S-Silodosin and R-Silodosin was found to be greater than 1.5. The developed method was validated with respect to linearity, accuracy, precision, solution stability, ruggedness, robustness, limit of detection and limit of quantification. The recovery obtained for S-isomer was in between 102.2 % and 104.4%. The detection limit obtained for S-isomer was 0.04µg.mL^-1 and the quantification limit was 0.13µg.mL^-1 respectively. Linearity was performed for the S-isomer from LOQ to 150%. The correlation coefficient obtained for S-isomer was more than 0.999. The solution stability of Silodosin bulk drug was determined and the compound was found to be stable up to 48 hrs. As the method has less run time (10 min), it can be useful in quality control laboratories for routine analysis.

Key words: R-Silodosin, S-Silodosin, Polysaccharide-based chiral stationary phase, High performance liquid chromatography and Method validation. 

ABSTRACT

Melasma is a cosmetic problem that sometimes cause great emotional suffering. One survey showed that melasma was associated with a significant impact on health related quality of life. It is defined as a disorder of pigment metabolism characterized by sharply demarcated, blotchy, brown maculae, usually symmetrical on the cheeks, forehead, sometimes on the upper lip and neck. In Unani Medicine, it is mentioned that Kalf is due to black bile homour and charred blood parts, which oozes out of capillaries and get accumulated under the skin. The present study was a Randomized, parallel group, comparative clinical trial. The present research was done to evaluate and to compare the clinical efficacy of a topical application made up of powdered cuttlefish bone and lemon juice along with oral Cascuta reflexa capsule which was compared with another group that is oral placebo with same topical application. The efficacy of the treatment was evaluated by MASI, skin color shades chart, Patient’s Global Assessment,  Patient’s Satisfaction Index and DLQI. Assessment of safety was done by clinical assessment, patients’ complains about any adverse effects i.e. itching, inflammation, rashes, eruptions etc., DLQI and laboratory parameters such as LFT, KFT, CBC and Hb%. At the end of the treatment all the efficacy parameters showed significant improvement when compared with baseline in both the groups; however the difference between the groups was not statistically significant. Thus, topical application had promising effects in melasma.

Key words- Kalf, Unani formulation, hyper pigmentation, MASI, cuttlefish bone 

ABSTRACT

The objective of this research work was to prepare sustained release matrix tablets of doxofylline. Doxofylline is a  xanthine bronchodilator having reduced affinity for A₁ & A₂ adenosine receptors. Different grades of hydrophilic polymers( HPMC K4M, HPMC K15 cps, HPMC K100 M, Sodium carboxymethylcellulose) and hydrophobic polymer (ethyl cellulose) were used. FTIR study shows that drug and other excipients are compatible with each other. Tablets were prepared by wet granulation technique using non-aqueous solvent IPA and PVP K90D as a binder. Under stage I of preliminary study, tablets were formulated using polymers alone. In stage II polymers were used in combination, with an objective of sustaining release up to 12 hrs. The effect polymer concentration on drug release profile was  investigated. The amounts of HPMC K100 M & NaCMC were selected as independent variables. The results of  final batches indicated that a low concentration of HPMC K100 M & high amount of Sodium CMC favours sustained release of doxofylline from matrix tablets. Accelerated stability study for 8 weeks  confirmed that the best selected formulation F 15 was stable

Keywords: Doxofylline , matrix tablets, HPMC, Sodium CMC, Sustained release tablets.

ABSTRACT

A simple, rapid and specific UV spectrophotometric method with good sensitivity was developed and validated for the simultaneous determination of tamsulosin and finasteride in bulk and pharmaceutical formulations. In methanol, the lambda max of finasteride and tamsulosin was fixed as 235 and 225nm respectively, using a Shimadzu UV–Visible spectrophotometer (model UV-1800) with quartz cells. In this proposed method both these drugs obeyed linearity individually and in mixture within the concentration range of 1- 10 μg ml^-1 for tamsulosin and 12.5 - 100 μg ml^-1 for finasteride, with a correlation coefficient value of  0.9992 and 0.9994 for tamsulosin and finasteride respectively. The low relative standard deviation values indicate good precision and high recovery values indicate accuracy of the proposed method. The proposed method had been applied to the determination of drugs in commercial formulations. Assay results were in good agreement with label claim. The method was validated according to the ICH guidelines.

Keywords: UV spectrophotometric method, finasteride, tamsulosin, simultaneous determination. 

ABSTRACT

Water soluble drugs if not formulated properly, may release the drug at a faster rate and produce a toxic concentration on administration. Captopril belongs to the class I of biopharmaceutical classification system (BCS) has short half life (~2hrs) shows dose dumping, burst and stability in acidic pH of stomach. In this study HPMC K15M and Compritol 888 ATO alone and in combination different proportions using physical mixture and solid dispersion method to prepare floating matrix tablet. The tablets were evaluated for appearance, weight variation, hardness, friability, floating lag time, duration and integrity of matrices, In-vitro and In vivo drug release kinetics. IR spectra, thermal behavior and X-ray diffraction pattern of selected solid dispersions were carried out indicating no degradative changes. The rate of release of Captopril from floating matrix tablets containing physical mixtures was found to be affected by the concentration of Compritol 888 ATO increase in the concentration decrease the release. Among the formulations containing solid dispersions of drug with Compritol888 ATO (SPC3c’’) give retardation of drug release (t_90% >12) for extended time. All formulations indicated diffusion exponent (n) values in the range 0.4 to 0.6 suggesting Fickian diffusion. The values of ‘n’ increased with increase in concentration of lipid polymers suggesting a shift in the mechanism of drug release from Fickian to anomalous. All formulations show initial burst release which may due to high water solubility of Captopril. The X-Ray photographs indicated the residence of tablet in stomach for about 5hs.

Keywords: Compritol888 ATO; X-ray diffraction; Solid dispersions

ABSTRACT

A new reverse phase high performance liquid chromatography (RP-HPLC) method for the quantitative determination of Sitagliptin in human plasma was developed and validated as per US-FDA guidelines. The drug was spiked in the plasma and extracted with mobile phase by precipitation method. The extracted analyte was injected into an INTERSIL C18 column (150 mm × 4.6 mm, 5μm), maintained at ambient temperature and effluent was monitored at 267 nm. The mobile phase consisting of acetonitrile: methanol: buffer (2:3:5 v/v). The pH of the mobile phase was adjusted to 4.0 by using O-phosphoric acid. The flow rate was maintained at 1.0 mL/min. The developed method shows high specificity for sitagliptin. Calibration curve was plotted with a range from 25-125µg/mL (r²>0.9994). The lower limit of quantification (LLOQ) was found to be 25μg/mL. The method was validated for parameters like accuracy, precision, recovery, linearity, range, stability and sensitivity. This RP-HPLC method is suitable for determining the concentration of sitagliptin in human plasma and it was applied to routine analysis for determination of the Sitagliptin from dosage form during pharmacokinetic study.

Keywords: Sitagliptin, RP-HPLC, Human plasma, Validation.

ABSTRACT

Mucoadhesive microspheres of metformin hydrochloride (HCL) were successfully developed by emulsification /evaporation techniques to achieve the optimum effect for prolong duration of time. All the prepared formulation was subjected to different type of evaluation like, practical yield, particle size, entrapment efficiency, in vitro release study, in-vitro kinetic study and percentage of mucoadhesion. Particle size was determined by image microscope and the average particle size of prepared formulation was found in the range of 90.32±1.8  to 154.55±0.20 μm for all batches .Cumulative percent drug release was found to be maximum for F4 and F9 (90.88±0.59 and92.10±0.414). Formulation F1,F2,F3,F4,F5,F7,F9 show Zero order releases profile and other formulations like, F6 show Hixon, F8 show Higuchi , F 10 show First order kinetic. All the batches showed good in vitro mucoadhesive property. It was also found that the prepared formulations not showing any interaction .The satisfactory result of different evaluatory parameters, reflect that the experimental study will prove to be a effective delivery system.

Keywords :- Mucoadhesion. , Entrapment efficiency, in-vitro kinetic study

ABSTRACT

A simple and economical Q-Absorbance spectrophotometric method has been developed for the simultaneous estimation of cefixime and moxifloxacin in their synthetic mixture. The method is based on Q‐absorption Ratio method using two wavelengths, 293.6 nm (λmax of Moxifloxacin) and 276 nm (Isoabsorptive point). Methanol was used as a solvent in the method. Both drugs showed linearity in the range of 4‐14 μg/mL in the methods. The method was validated statistically and recovery studies were carried out. The proposed method was found to be simple, economical, accurate, and reproducible. It can be applied for routine analysis and quality control of both drugs in their combination drug products.

Keywords: Cefixime, Moxifloxacin, Spectrophotometric, Q-absorption Ratio Method

ABSTRACT

The present manuscript describes simple, sensitive, rapid, accurate, precise and economical Q-absorbance ratio method for the simultaneous determination of diclofenac sodium and tolperisone hydrochloride in bulk and synthetic mixture. Absorbance ratio method uses the ratio of absorbances at two selected wavelengths, one which is an isoabsorptive point and other being the λ-max of one of the two components. Tolperisone hydrochloride and diclofenac sodium show an isoabsorptive point at 267 nm in methanol. The second wavelength used is 255 nm, which is the λ-max of tolperisone hydrochloride in methanol. The linearity was obtained in the concentration range of 2-20 μg/ml for both tolperisone hydrochloride and diclofenac sodium. The concentrations of the drugs were determined by using ratio of absorbances at isoabsorptive point and at the λ-max of tolperisone hydrochloride. The method was successfully applied to pharmaceutical dosage form because no interference from the synthetic mixture excipients was found. The suitability of this method for the quantitative determination of tolperisone hydrochloride and diclofenac sodium was proved by validation. The proposed method was found to be simple and sensitive for the routine quality control application of tolperisone hydrochloride and diclofenac sodium in synthetic mixture or pharmaceutical dosage form. The results of analysis have been validated statistically and by recovery studies.

Keywords: Diclofenac sodium, Tolperisone hydrochloride, Recovery, Absorbance ratio method, Isoabsorptive point, Validation

ABSTRACT

An accurate and precise stability-indicating RP-HPLC method has been developed and validated for the analysis of Erlotinib HCl in tablet dosage forms. The method was developed on a Qualisil Gold C18 (250×4.6mmi.d, 5μm particle size) analytical column using methanol: water in the ratio of 58:42(v/v) as the mobile phase. The instrumental settings were flow rate 1mL/min, column temperature 23^oC and the detection wavelength of 246nm using a Photo Diode Array (PDA) detector. The method is linear over a range of 5-50μg/ml. The LOD and LOQ values were found to be 0.81μg/mL and 2.466μg/mL respectively. Erlotinib was exposed to acidic, alkaline, oxidative, photolytic, thermal stress conditions and these stressed samples were analyzed by the proposed method. The drug product was completely separated from the degradants which indicates that the method is specific.

Key-words: ErlotinibHCl, RP-HPLC, Stress degradation studies.