ABSTRACT

The term “liquisolid medication” implies oily liquid drugs and solutions or suspensions of water insoluble drugs carried in suitable non-volatile solvent systems. Liquisolid compacts demonstrated a considerably higher drug dissolution rates than those of conventionally made capsules and directly compressed tablets. This was due to the increased wetting properties and surface of drug available for dissolution. This review paper highlights the application of liquisolid technique to enhance the solubility and dissolution of water insoluble drugs. This technique is appropriate for poorly or water insoluble drugs and also for immediate or sustained release formulations. This review also depicts the various formulation parameters that must be optimized before formulation the liquisolid compacts.

Keywords: Liquisolid technique; Solubility; Dissolution; Poorly; Water insoluble drugs

ABSTRACT

Hydrogel nanoparticles have gained considerable attention in recent years as one of the most promising nanoparticulate drug delivery systems owing to their unique potentials via combining the characteristics of a hydrogel system with a nanoparticle. Therefore, it seems that the pharmacy world will benefit from the hydrophilicity, flexibility, versatility, high water absorptivity, and biocompatibility of these particles and all the advantages of the NPs, mainly long life span in circulation and the possibility of being actively or passively targeted to the desired bio-phase. Several polymeric hydrogel nanoparticulate systems have been prepared and characterized in recent years, based on both natural and synthetic polymers, each with its own advantages and drawbacks. Several cross linking methods have been used in the way to form the hydrogel matrix structures. The remainder of this text presents various types of nanogels prepared and characterized, using a classification based on the type of polymeric materials used in preparation of the NPs.

Key words: Hydrogel, Nanoparticles, Hydrogel nanoparticles, Nanogels, Hydrogel.

ABSTRACT

Turmeric, derived from the plant Curcuma longa, is a gold-colored spice commonly used in the Indian subcontinent, not only for health care but also for the preservation of food and as a yellow dye for textiles. Curcumin, which gives the yellow color to turmeric, was first isolated almost two centuries ago, and its structure as diferuloylmethane was determined in 1910. Since the time of Ayurveda (1900 bc) numerous therapeutic activities have been assigned to turmeric for a wide variety of diseases and conditions, including those of the skin, pulmonary, and gastrointestinal systems, aches, pains, wounds, sprains, and liver disorders. Extensive research within the last half century has proven that most of these activities, once associated with turmeric, are due to curcumin. These include its anti-inflammatory, anti-oxidant, anti-carcinogenic, anti-mutagenic, anti-coagulant, anti-fertility, anti-diabetic, anti-bacterial, anti-fungal, anti-protozoal, anti-viral, anti-fibrotic, anti-venom, anti-ulcer, hypotensive and hypocholesteremic activities. Its anti-cancer effect is mainly mediated through induction of apoptosis. Its anti-inflammatory, anti-cancer and anti-oxidant roles may be clinically exploited to control rheumatism, carcinogenesis and oxidative stress-related pathogenesis. Thus, curcumin has the potential for the development of modern medicine for the treatment of various diseases.

Key words : Curcumin, diferuloylmethane, medicinal properties.

ABSTRACT

This review explains the recent advances in gastroretentive drug delivery systems with special focus on floating drug delivery systems. Oral controlled release (CR) dosage forms (DF) have been extensively used to improve therapy of many important medications. However, in the case of narrow absorption window drugs, this pharmaceutical approach cannot be utilized, as it requires sufficient colonic absorption of the drug (which contradicts the definition of narrow absorption window agents). On the other hand, incorporation of the drug into a CR delivery system, which releases its payload in the stomach over a prolonged time period, can lead to significant therapeutic advantages owing to various pharmacokinetic (PK) and pharmacodynamic aspects. Gastroretentive dosage forms (GRDFs) are a drug delivery formulation that are designed to be retained in the stomach for a prolonged time and release there their active materials and thereby enable sustained and prolonged input of the drug to the upper part of the gastrointestinal (GI) tract. This technology has generated enormous attention over the last few decades owing to its potential application to improve the oral delivery of some important drugs for which prolonged retention in the upper GI tract can greatly improve their oral bioavailability and/or their therapeutic outcome. This article reviews some of the latest developments in GRDF technology from a pharmaceutical point of view. It also highlights the PK and/or pharmacodynamic rationale for the development of GRDFs for certain drugs that are either absorbed in the upper GI tract or have local activity there.

Key words: Floating drug delivery systems, single unit, multiple units, gastric resident time, Expandable Systems

ABSTRACT

There are several species of trypanosomes, which are single-celled organisms. Some affect primarily animals, but some are a significant cause of human illnes. Trypanosomes are transmitted by insect bites; Chagas disease is transmitted by bites of the reduviid bug. It is estimated that 16 to 18 million people are infected with T. cruzi and that 30 to 40 percent will develop heart symptoms as a result of their infection. In parts of the world where Chagas disease is endemic, most notably South America, the disease is the largest single cause of cardiovascular death. Chagas disease is very rare in the United States; only eight cases have been reported, and all of these in Latin American immigrants.Conditions resulting from Chagas disease also include atrioventricular block, which is a failure of the normal conduction of the electrical impulses which control the heartbeat. Eighteen of the 25 patients with Chagas disease were under treatment for heart disease prior to their proper diagnosis. In one case, a patient had been treated for 10 prior to the diagnosis.

Keyword:- Mal de Chagas-Mazza, Chagas, Trypanosomes cruzi, American trypanosomiasis, Brazilian Trypanosomiasis, heart disease.

ABSTRACT

Colloidal Drug Delivery system is an advancing technology expected to bring revolutionary changes in the field of pharma and health sciences including drug delivery, diagnostics and treatment. The advancement in colloidal drug delivery systems helps in preparing newer formulations which become useful for treatment of tuberculosis. Development of Metered dose inhaler (MDT) and Directly Observed Therapy (DOTS) also proves to helpful in treatment of tuberculosis. Various colloidal drug delivery systems liposomes, niosomes, nanoparticles and microparticles proves to be a successful tool for tuberculosis treatment. One of the preparations like microemulsions results in theimprovement of bioavailability of the drugs. Similarly corticosteroids also found to be an interesting tool here because corticosteroids reduced the risk of pleural thickening in tuberculosis patients. These various colloidal drug delivery systems minimize the problems of conventional therapy like poor penetration, drug resistance, systemic toxicity and also main the improved drug delivery. This article describes the applications of various formulations along with their future aspects in treatment of tuberculosis.

Keywords: Tuberculosis, Liposomes, Nanoparticles, Niosomes, DOTS.

ABSTRACT

This community based study assessed the prevalence of obesity and associated factors among age group between 16 to 75 years. The obese and overweight subjects were from age group from 31 to 45 year which was 42.42% and 28.78% respectively and most of them were in sedentary jobs. Obese and overweight dipsomaniac smokers were from the age group46-60 year which was 90%. Prevalence of hypertension and diabetes among overweight elderly was observed in this study.

Key words: Obesity, Overweight, Dipsomaniac, Hypertension, Diabetes

ABSTRACT

A simple, rapid and economical spectrofluorimetric method for estimation of Celecoxib, a selective COX-2 inhibitor, in bulk and solid dosage forms was developed in the present study. Celecoxib shows maximum excitation intensity at 245 nm and maximum emission intensity at 382 nm which is used in this study. The linear regression equation obtained by least square regression method, was Int =0.253*Conc. (in ng/ml) +34.80. The method provides a linear response across a quantization range of 250ng/ml to 4000ng/ml. The developed method was employed with a high degree of precision and accuracy for the estimation of total drug content in three commercial capsule formulations of Celecoxib. The results of analysis were treated statistically, as per International Conference on Harmonisation (ICH) guidelines for validation of analytical procedures. The results were found to be accurate, reproducible and free from interference.

Keywords: Celecoxib; Spectrofluorimeter; Recovery Studies

ABSTRACT

A simple and sensitive high performance thin layer chromatography (HPTLC) method has been developed for the quantitative estimation of Tadalafil in its single component tablet formulation (20 mg). Tadalafil was chromatographed on silica gel 60 F₂₅₄ TLC plate using chloroform: methanol (9:1, v/v) as mobile phase. Tadalafil showed Rf value 0.78 + 0.008 and scanned at 285 nm using a camag TLC scanner 3. The method was validated in terms of linearity (100 – 800 ng/spot), precision (intra-day variation, 0.38 to 0.81% and inter-day variation, 0.45 to 1.90%), accuracy (100.3 ± 0.76) and specificity. The limit of detection and limit of quantification for Tadalafil were found to be 28.11 ng/spot and 93.45 ng/spot, respectively. The developed method was successfully used for the assay of Tadalafil tablet formulation. The method was found to be simple, sensitive, specific, accurate and precise and can be used for the routine quality control testing of Tadalafil in tablet dosage form.

Keywords: Tadalafil, HPTLC, validation, tablet

ABSTRACT

Pantoprazole Sodium sesquihydrate is a proton pump inhibitor that belongs to group benzimidazole, used for the treatment of ulcers in duodenum and gastric, which was degraded in stomach .Thus, the purpose of the study is to formulate a dosage form which is coated by coating polymer(s) which passed the acidic medium and exhibit significant effect in intestine and cures ulcers. An attempt was made to formulate micro particles with two coating polymers: Eudragit L-100 & Cellulose acetate phthalate as well as using of mucoadhesive polymers will release drug in controlled manner. Thus, these different types of micro particles was characterized in terms of Particles size, Mucoadhesive efficiency, Entrapment efficiency, In-vitro as well as In-vivo studies.

Key words: - Pantoprazole, Coating polymers, Mucoadhesive polymers

ABSTRACT

The present manuscript describe simple, sensitive, rapid, accurate, precise and economical spectrophotometric method for the simultaneous determination of Ofloxacin and Cefpodoxime proxetil in combined tablet dosage form. The method is based on the simultaneous equations for analysis of both the drugs using methanol as solvent. Ofloxacin has absorbance maxima at 297 nm and cefpodoxime proxetil has absorbance maxima at 236.2 nm in methanol. The linearity was obtained in the concentration range of 2-12 μg/ml and 4-24 μg/ml for Ofloxacin and Cefpodoxime proxetil, respectively. The concentrations of the drugs were determined by using simultaneous equations at both the wavelengths. The mean recovery was 99.63 ± 0.47 and 99.57 ± 0.36 for Ofloxacin and Cefpodoxime proxetil, respectively. The method was successfully applied to pharmaceutical dosage form because no interference from the tablet excipients was found. The suitability of this method for the quantitative determination of Ofloxacin and Cefpodoxime proxetil was proved by validation. The proposed method was found to be simple and sensitive for the routine quality control application of Ofloxacin and Cefpodoxime proxetil in pharmaceutical tablet dosage form. The results of analysis have been validated statistically and by recovery studies.

Key words: Cefpodoxime proxetil, Ofloxacin, recovery, simultaneous equations method, tablet, validation.

ABSTRACT

Schiff Base derivatives are important class of compounds. They possess different types of Biological activities like antibacterial, antiviral, anti HIV, antifungal etc. Schiff base derivatives are prepared by the condensation of aldehyde and amine and these compounds are characterized by chemical and instrumental methods. Their important biological properties have been investigated.

Key words: Schiff Base derivatives, Biological study, pyrimidine derivatives, Hydrazone derivatives

ABSTRACT

The objective of present study is to improve the dissolution rate of Acyclovir a poorly water soluble drug by solid dispersion technique using a water soluble carrier, PEG-6000, urea, mannitol. The solid dispersions are prepared by physical method, co-grinding method and solvent evaporation method. The prepared solid dispersions showed an enhancement in dissolution rate and solubility compared to plain drug. In vitro release profiles of all SDs were comparatively evaluated and also studied against pure acyclovir. Faster dissolution was exhibited by solid dispersion containing 1:4 ratio of drug: PEG-6000. The increase in dissolution rate of the drug may be due to increase in wettability, hydrophilic nature of the carrier and due to reduction in drug crystallinity. The prepared solid dispersion was subjected for % practical yield, drug content, infrared (IR) spectroscopic, differential scanning calorimetry (DSC). FT‐IR spectra revealed no chemical incompatibility between drug and PEG-6000.Drug– polymer interaction was investigated using differential scanning calorimetry (DSC) studies.

Key words: Solid dispersions, carriers, solubility enhancement, poorly soluble drugs, bioavailability

ABSTRACT

The present work describes the development of stability indicating assay method for Diacerein and Aceclofenac in their combined dosage form that would provide helpful information to the manufacturers. Stress studies were conducted on the drug substance and product under the ICH prescribed stress conditions viz. hydrolysis, oxidation, humidity, photolysis, thermal stress. The separation of the drug from its degradation products, trials were made by taking acetonitrile: water, acetonitrile: phosphate buffer, acetonitrile: phosphoric acid in various blends. Separation was achieved using C-18 column and a mobile phase comprising of Acetonitrile: Phosphoric acid 0.1 M (61: 39) at a flow rate of 1.5 mL/min. The detection wavelength was 260 nm. The drug showed sufficient decomposition under alkaline hydrolysis (0.05 N NaOH), acidic hydrolysis (0.05 N HCl), neutral hydrolysis (distilled water), and oxidative hydrolysis (6% H₂O₂). The drug was found to be moderately sensitive to humidity studies (75 % RH), photochemical studies (UV 254 nm), and thermal studies (60⁰C). Recovery studies were also carried out for both the drugs and the mean percent recovery were found to be 100.69 for diacerein and 99.15 for aceclofenac. Mean percent estimation in marketed formulation gave 99.63% for diacerein and 100.04% for aceclofenac. The above method was validated for accuracy, precision, ruggedness, limit of detection, limit of quantitation and was found to be satisfactory for routine analysis of diacerein and aceclofenac in their combined dosage form in the presence of their degradation products.

Key words: Aceclofenac, Diacerein, Stress Degradation, Stability Indicating, Validation

ABSTRACT

Quantitative estimation of Trapidil and its pharmaceutical dosage form by HPLC, HPTLC and UV spectroscopy methods was developed. In the RP-HPLC method, the drug was resolved using a mobile phase phosphate buffer: acetonitrile (30:70%v/v) with pH adjusted to 3.5 using phosphoric acid on C₁₈ column in isocratic mode. The retention time of trapidil was found to be 3.195 min.  In HPTLC method, the chromatograms were developed by using a mobile phase Methylene chloride: Methanol:  ammonia (8.5:1:0.5 v/v) on precoated plate of silica gel 60F₂₅₄ and quantified by densiometric absorbance mode at 312nm. The Rf value of Trapidil was 0.28. In the UV method, trapidil was quantified at 221nm in acetronitrile. Recovery studies of 98.8-101.14%, percentage relative standard deviation (%RSD less than 2%) and correlation coefficient (linearity range) that developed methods were accurate and precise. These methods can be employed for the routine analysis of tablets containing trapidil.

Key words: Trapidil, RP-PHLC, HPTLC, UV spectrophotometry, validation

ABSTRACT

Gymnosporia montana belonging to the family Celastraceae commonly known as Vikalo.  It is a shrub or tree growing wild in dry areas and is commonly found in Gujarat. It is widely used in treating sore, ulcer, gastro-intestinal disorders, toothache, and dysentery. The dried powder of leaf of Gymnosporia montana was subjected to the phytochemical screening for the presence of various phytoconstituents like alkaloids, flavonoids, saponins, tannins, anthraquinones, and carbohydrates, etc. Effectiveness of methanolic extracts of leaf of Gymnosporia montana was evaluated (100, 200 and 300 mg/kg; p.o.) against carrageenan-induced rat paw edema, and cotton pellet-induced chronic inflammation. Further, methanolic fraction of the plant was also evaluated (200 mg/kg; p.o.) in tail flick model using rats as well as acetic acid-induced writhing response using mice. Pretreatment with methanolic fraction showed significant (p<0.05) anti-inflammatory activity at 3 h when compared with the control group. Further, it also significantly (p<0.05) reduced the increase in the weight of cotton pellet when compared with the control group and results were comparable with that of diclofenac (standard) treated group of animals. Pretreatment with methanolic fraction significantly (p<0.05) prolonged the reaction time in rats in tail flick model as well as reduction in the number of mouse abdominal constrictions following acetic acid administration when compared with the control group. It can be thus concluded that the methanolic fraction of leaf of Gymnosporia montana showed significant anti-inflammatory activity and analgesic activity in experimental animals.

Keywords: Gymnosporia montana, anti-inflammatory, Vikalo 

ABSTRACT

In traditional medicine Calotropis gigantean Linn is a well-known plant in the traditional medicine of Rajasthan. Asclepiadaceae is used in folk medicine for pain, burns, eczema, skin diseases (Ring worm), Anti-bacterial and anti-fungal and wound-healing activities. Based on its traditional use, this plant was selected for evaluation of its wound healing potential. Preliminary wound healing activity was performed on different extracts and based on the findings; Petroleum ether, chloroform, methanol and distilled water extract was selected for further studies. The extract of Calotropis gigantean Linn promoted wound-healing activity significantly in all the three wound models studied. Topical application twice a day for 16 days significantly increased the wound contracting ability of the extract ointment (5% and 10%) and it was comparable to the reference standard nitrofurazone ointment in the excision wound model. The tensile strength in healing of incised wounds and dead space wound was found to be significantly higher in the group of animals treated with extract ointments (5% and 10%) and extracts (200mg/kg body weight) respectively. To investigate the effects of Calotropis gigantean Linn on wound healing activity in rats by excision, incision and dead space wound healing models in rats.

Key words: Calotropis gigantean Linn, Excision wound model, Tensile strength Incised wounds, Dead space wound.

ABSTRACT

The objective of designing a dosage form is to achieve predictable therapeutic response to a drug included in a formulation which is capable of large scale manufacture with reproducible product quality. In order to ensure quality of product various features are required, like chemical and physical stability, preservation against microbial contamination, uniformity of dose of drug, acceptability to users including prescriber and patient, as well as suitable packing, labeling, and validation. The present research work focused on prospective process validation for the gliclazide 40mg tablet. Tablet was manufactured by wet granulation method. Formulation of tablet using Maize Starch, Avicel Ph 102, PVP-K30, sodium starch glycolate, Purified Talc, Aerosil 200 and  Magnesium stearate. Uniformity of dry mixing is excellent in 10min because % RSD found to be 0.4267-0.9021%. Granulating agent was prepared of desired consistency. Drying time 30 min is sufficient to achieve LOD 2-3%. Evaluation parameter of sizing shows effective LOD, % fine, BD & CI. Lubrication stage uniformity was achieved with 10min because % RSD found 0.8320-1.032% and flow properties was satisfactory. Compression machines optimum speed (20RPM) was satisfactory for effective compression. Based on results at each of the stages for the specified parameters it is concluded that gliclazide tablets can be effectively prepared with the desired specification & reproducible quality standards.

Keywords: Prospective Validation, Gliclazide, Tablet.

ABSTRACT

Piroxicam is a non-steroidal anti-inflammatory drug, classified in the Biopharmaceutics Drug Classification system as a Class II drug with low solubility and high permeability. It demonstrates a slow and gradual absorption via the oral route and has a long half-life of elimination, rendering a prolonged therapeutic action and a delayed onset of anti-inflammatory and analgesic effect. The basic objective of the present study is to formulate and evaluate the fast dissolving tablet of Piroxicam. Study proposes the use of a Sodium Satrch Glycolate (SSG) alone to prepare solid dispersion of piroxicam and comparison of its in-vitro dissolution with pure piroxicam. Fast Dissolving tablets can be prepared by conventional direct compression method using solid dispersion of superdisintegrants which shows rapid rate of disintegration. For better Hardness, less friability, faster wetting time and less moisture uptake combination of both MCC and Mannitol are required in the formulation.

Key Words: Fast dissolving tablet, Piroxicam, Sodium starch Glycolate (SSG)

ABSTRACT

In the present research paper, anticonvulsant Sodium valproate tablets were prepared using two different disintegrating agents in different ratio. Acrycoat-L-100 polymer was used as an enteric coating material. The tablets were formulated using direct compression method. Further post formulation parameters like hardness, friability, weight variations and content uniformity were studied. The results suggested, that the prepared enteric coated tablets specifics all the criteria of the standard formulation as per specified in monographs.

Keywords: Sodium valproate, anticonvulsant, polymer, enteric coated

ABSTRACT

In the present communication, finger print of two ethano-botanically important Anisomeles species has been developed. A sensitive and reliable densitometric High Performance Thin Layer Chromatography (HPTLC) method has been developed for the quantification of quercetin, β-sitosterol, stigmasterol, catechin and ovatodiolide present in Anisomeles indica and Anisomeles malabarica.  Chromatographic analysis was performed using methanol, chloroform, acetone and ethanol extract of these plants were developed in the different solvents such as toluene, chloroform, ethyl acetate, methanol at various proportions. Detection and quantification of all phytoconstituents was done by densitometric scanning at different wavelengths. These finger prints would be helpful in the standardization of these species.

Key words: HPTLC, Anisomeles indica, Anisomeles malabarica, phytoconstituents, standardization