ABSTRACT

A female patient of 40 year old attended OPD of NIUM Hospital with weakness of left upper limb that prevent her from performing daily routine activities. With the intervention by Unani medicaments along with riyazat and dalk, she got satisfactory improvement. Hence forth, it can be concluded that Unani therapy for post hemiplegic weakness can be a better alternative of its management.

Keywords: Unani medicine, Riyazat, Dalak, Hemiplegic weakness

ABSTRACT

Insulin is the most effective glucose-lowering agent, which stimulates glucose uptake in skeletal muscles, myocardium, and other tissues in order to control glucose homeostasis. Is usually administered to diabetic patients through subcutaneous injection. However, the problems encountered with subcutaneous insulin injections are pain, allergic reactions, hyperinsulinemia, and insulin lipodystrophy around the injection site. Insulin if administered via the oral route will help eliminate the pain caused by injection, psychological barriers associated with multiple daily injections such as needle anxiety and possible infections. In addition, oral insulin is beneficial because it is conveyed directly to the liver, its primary site of action, via the portal circulation, a mechanism complimentary to endogenous insulin; subcutaneous insulin treatment however does not replicate the normal dynamics of endogenous insulin release, resulting in a failure to achieve a lasting glycemic control in patients. Insulin in its present form cannot be administered through oral route. Scientists have been trying hard to design an oral delivery system for insulin by applying several approaches.

Keywords: oral insulin, diabetes, insulin tablets, hyperglycemia, novel drug delivery.

ABSTRACT

Fast dissolving Tablets are disintegrating and/or dissolve rapidly in the saliva without the need for water. Some tablets are designed to dissolve in saliva remarkably fast, within a few seconds, and are true fast-dissolving tablets. Others contain agents to enhance the rate of tablet disintegration in the oral cavity, and are more appropriately termed fast-disintegrating tablets, as they may take up to a minute to completely disintegrate. Oral delivery is currently the gold standard in the pharmaceutical industry where it is regarded as the safest, most convenient and most economical method of drug delivery having the highest patient compliance. By the addition of piperine in the fast dissolving formulation, its bioavailability increases, hence dosing reduces.

Keywords: FDT, Orodispersible tablets, Fast dissolving/dispersing tablets, Melt in mouth tablets, Mass extrusion, Superdisintegrants.

ABSTRACT

Wild yams contribute significantly as diets among the hill tribes of Asia and South West Africa. The nutritional compositions are similar to the cultivated yams except presence of high fibre content and acrid principle. In addition, wild yams are a source of steroid drugs.  In the present paper, extraction and chemical structure of diosgenin, recent change in diosgenin based steroid industry, new sources of steroid, microbiological production of androstanes and chemical synthesis are discussed in addition to the distribution, botanical description, cultivation and economic uses. Conservation and use of genetic resources of wild yams in a sustainable manner has been emphasized.

Keywords: Wild yams, distribution, description, steroid drugs

ABSTRACT

The wide occurrence of benzo fused and heterocyclic fused [1,4] oxazines in bioactive natural product and pharmaceuticals have made them important synthetic targets. 2H-1,4-pyridoxazin-3-(4H)-one   has been studied intensively as important heterocyclic systems for building natural and designed synthetic compounds. They are utilized as suitable skeletons for the design of biologically active compounds, ranging from anti-inflammatory, analgesics, bacteriostatic, fungistatic and MAO inhibitors etc. Various researchers with help of organic and analytical chemistry developed 2H-1,4-pyridoxazin-3-(4H)-one using different synthetic route.

Keywords: anti-inflammatory, bacteriostatic, MAO inhibitors

ABSTRACT

The proniosomal approach helps to solve the problem regarding stability and provides higher entrapment efficiency over conventional system. Proniosomal gel is a liquid crystalline- compact niosomal hybrid which is prepared by dissolving surfactant in small amount of suitable solvent and least amount of aqueous phase. This compact gel can be converted to niosomes hydration. Proniosomes can entrap hydrophilic as well as lipophillic drugs. Proniosomal gel offers a versatile vesicle drug delivery concept with potential for drug delivery via transdermal rout. Over the last few years an inclusive research has been done over pro-vesicular approach for transdermal drug delivery. Skin has a very tough diffusion barrier inhibiting penetration of drug moiety which is rate limiting barrier for penetration of drugs. There are several approaches that deal with penetration enhancement across the skin. Vesicular and provesicular systems are promising amongst them. Vesicular systems including (niosomes, ethosomes, transfersomes and liposomes) are promising systems to cross this permeation barrier.

Keywords: Proniosomes, Niosomes, skin penetration, stability, transdermal, coacervation.

ABSTRACT

Bioavailability and Bioequivalence studies play a vital role in drug development process for new drug products and generic drugs. The main aim of abbreviated new drug application is to show that the generic drug is bioequivalent to innovator product in terms of quality, safety, and efficacy. There are several approaches to study bioequivalence and each country has its own regulations for conducting Bioavailability and Bioequivalence studies. The present review gives information about abbreviated new drug application submission and important aspects involved in bioequivalence and Regulatory requirement for various countries.

Keywords: FDA:  Food and Drug Administration, EMA: European medical agency, BA/BE: Bioavailability and Bioequivalence, AUC: Area under Curve, ANDA: Abbreviated new drug application

ABSTRACT

This review presents the numerous researches which explore the potential use of polymeric nanoparticles as carriers for a wide range of drugs for therapeutic applications. Because of their versatility and wide range of properties such as better encapsulation, control release and less toxic properties, biodegradable polymeric nanoparticles are being used as novel drug delivery systems. In particular, this class of carrier holds tremendous promise in the areas of targeted drug delivery system.

Keywords: Nanoparticles, biodegradable polymer

ABSTRACT

Eye is a window to the outside world and hence it becomes an important part of our body. Various diseases occurring in the eye cavity are difficult to treat. Some diseases require continuous use of medicine and other requires surgery. Lacrisert, Vitrasert, Mydriasert, Prosert etc. are patented technologies useful in the treatment of eye disorders. In this article brief description of various patented technologies such as Eyegiene kit, Ophtha coils, Versidoser, Microneedle, Implantable MEMS ocular drug delivery system, Ocuseal liquid bandage, Filter paper strips is given.

Keywords: Ocular drug delivery, Lacrisert, Vitrasert, Microneedle, Mydriasert.

ABSTRACT

Blood is one of the most essential components of the body. It carries out various functions that are life sustaining. Situations may arise when the requirement of blood quantity cannot be met as in case of intense injury or surgical conditions where volume of blood may not be sufficient enough to support the survival of life. In such cases there is an inevitable requirement of the source from where the requirement can be met. So, the present review focuses on such products which can be used in place of blood for supporting the life. These products are designated as Artificial Blood. Artificial blood is a product made in order to substitute Red Blood Corpuscles, with the main function of transportation of respiratory gases, Oxygen and Carbon-dioxide throughout the body as well as fill fluid volume. But the product lacks other blood related objectives including absence of cells, coagulation properties and defence mechanisms. Artificial blood products can be broadly classified into two categories: Perflourocarbon based and Hemoglobin Based Oxygen Carriers products, each being associated with its specific advantages and disadvantages. The concept of artificial blood is not only theoretical but the products have been developed and are undergoing commercial development, with some being marketed and others being undergoing clinical and preclinical trials. Besides this, other blood replacement alternatives like antigen camouflage, transgenic therapeutic proteins, platelet substitute for cancer, etc. are also employed, while stem cells, dendrimers, biodegradable micelles and blood from placental umbilical cord may serve for future investigation of blood alternatives.

Keywords: Artificial blood, perfluorocarbon (PFC), oxygen (O₂), carbon dioxide (CO₂), hemoglobin (Hb), hemoglobin based oxygen carrier (HBOC).

ABSTRACT

Now days there is need of using novel drug delivery systems to avoid side effects of conventional drug delivery systems and to achieve more significant effects from drug delivery system. Microchip is a new approach in the novel drug delivery system. It is a device act as an implant and delivers required quantity of drug on the site of action at specific time. This method is beneficial in chronic diseases which having long time therapy. Device has substrate, reservoirs, reservoir cap, microprocessors, battery, antenna, biocompatible coating etc. There are different types to deliver drug from the reservoirs. Diffusion method, electro thermal method, diamond electrophoretic method, electrochemical degradation method, polymer degradation method. By using one of these methods optimum drug can deliver.  This device having so many advantages like it stores the drug for long period of time and also protects the drug. Effective concentration of drug can be maintained in blood for long period of time. This system is more beneficial to treat chronic diseases. Chronic diseases require therapy for long period of time which improves patient non-compliance. Chronic diseases like diabetes, cancer, and osteoporosis can be treated by using microchip.There are some limitations in this type of drug delivery system which can be overcome in future research study. This type of drug delivery system can take new era in the world of medicine and technology.

Keywords-microprocessor, electrophoretic, biocompatible, osteoporosis

ABSTRACT

Evaluation of the nutritive and electrolyte values of edible plants is currently essential for human nutrition and safety. This work assessed the proximate and mineral composition of the leaves of Chaya plant (Cnidoscolus aconitifolius) consumed in Niger Delta Nigeria for medicinal and nutritional purposes. Chaya is commonly known in this southern area of Nigeria as ‘hospital is too far’ or ‘ogwu obala’. The study showed that the dried leaves of the plant contain 47.03 ±1.02% of nitrogen free extract; 33.04± 3.14% of crude fibre; 7.03±0.23% of crude fat; 4.03±0.67% of crude protein, while moisture and ash made up 6.10±1.10% and 3.04±0.32%, respectively. A gram of the dried leaves yielded (in mg) 10±1.2, 20±1.6, 0.01±0.1, 100±5.3, 85±4.32, 18±2.1 and 50±2.3 of Iron, Phosphorus, Sodium, Potassium, Magnesium, Manganese and Calcium, respectively. The energy yield of the leaves was 258±4.5kcal/100 mg. These results suggested the comparative richness of the leaves in fibre, high nitrogen free extract (carbohydrate) and essential minerals. Properly prepared leaves are therefore recommended for daily consumption in order to supplement the recommended daily intake of nutrients and minerals and hence prevent nutritional and electrolyte deficiency disorders.

Keywords: Cnidoscolus aconitifolius, Nutritional, Electrolytes, Values, Niger Delta

ABSTRACT

The anti-ulcer activity of leaves of benzene and pet ether extract of cleome gynandra inn was investigated in  ethanol induced ulcer model in the male wistar albino rats. The parameters evaluated are ulcer index ,volume of gastric juice, gastric acidity, ph of gastric juice. Pet ether and benzene extract  at doses of 150 mg/kg produced significant inhibition of gastric lesion induced by ethanol induced gastric ulcer. The extract shows significant reduction in gastric volume ,and ulcer index when compared to control. The present study indicates that leaves of benzene and pet ether extract of cleome gynandra inn have potential anti ulcer activity in ethanol induced ulcer model. Further the study also implies that dietary polyphenolic phytochemical especially the flavonoid, saponins accumulated in leaves may supply substantial anti-ulcer agents, which in turn may inhibit the development of several chronic  diseases and there by provide health promoting effect.

Keywords : Cleome gynandra linn, Ethanol induced ulcer model, ulcer index

ABSTRACT

A simple, precise and economical UV Spectrophotometric method has been developed for the estimation of Tolterodine tartarate in bulk and pharmaceutical dosage form. The method is based on measurement of absorption at maximum wavelength of 283.0 nm. Linearity for detector response was observed in the concentration range of 10-50 μg/ml. The accuracy of the method was assessed by recovery studies and was found to be 99.80%. The LOD and LOQ were found to be 0.1865 and 0.5621 respectively. The developed method was validated with respect to linearity, accuracy (recovery), precision, specificity and robustness and ruggedness. The results were validated statistically as per ICH Q2 R1 guideline and were found to be satisfactory. The proposed method was successfully applied for the determination of Tolterodine tartarate in commercial pharmaceutical dosage form.

Keywords: Tolterodine tartarate, UV Spectrophotometry, validation.

ABSTRACT

A simple, fast and precise reverse phase, isocratic HPLC method was developed for the separation and quantification of perindopril and indapamide in pharmaceutical dosage form. The quantification was carried out using YMC Column (150 x 4.6mm, 3µ particle size) and mobile phase comprised of ammonium dihydrogen phosphate pH 2.5 and acetonitrile in the ratio of 60:40% v/v and degassed under ultrasonication. The flow rate was 1.0 mL/min and the effluent was monitored at 230 nm. The retention time of perindopril and indapamide were 2.4 and 4.2 min respectively. The method was validated in terms of linearity, precision, accuracy and specificity. Linearity of perindopril and indapamide were in the range of 48 to 112 μg/mL and 15 to 35 μg/mL respectively. The proposed method is suitable for simultaneous determination of perindopril and indapamide in pharmaceutical dosage form.

Key words: Perindopril and Indapamide, RP-HPLC, Validation.

ABSTRACT

The methanolic extract of Punica granatum (PUG), Glycyrrhiza glabra (GLA) and their combination (PUG-GLA) were evaluated for their wound healing activity using excision wound model in rats. Rats treated with PUG-GLA showed higher rate of wound contraction, significant decrease in epithelization period and significant increase in hydroxyproline content of granulation tissue when compared with the controls. The histological examination of treated wounds showed that the original tissue regeneration was much greater in PUG-GLA, with increase in the restoration of collagen fibers, fibroblasts, blood vessel formation and hair follicle regeneration.

Keywords: Punica granatum; Glycyrrhiza glabra; Wound healing; Excision model; Hydroxyproline 

ABSTRACT

Increase in anal resting pressure (ARP) is considered as the primary cause of chronic anal fissure (CAF). Reduction in ARP is the primary objective in treatment of CAF. Topical diltiazem is considered as first-line treatment option in CAF as surgical treatment may be associated with several post operative complications including permanent incontinence in some cases. Few studies have reported that lidocaine alone is inferior to anal dilators for pain relief in CAF which suggest that relief of internal anal sphincter is required for effective symptomatic management. The aim of this study was to evaluate whether combined treatment with diltiazem and lidocaine has any significant advantage over diltiazem monotherapy in patients with CAF. To evaluate this, 150 patients were enrolled and randomized to either treatment group. ARP, pain intensity and adverse events were recorded at various time points over 20 days study period. Fall in the mean ARP from baseline was comparable in both the study groups. However, significantly greater fall in pain intensity from baseline was observed with combined treatment with diltiazem and lidocaine, which can be attributed to the additional local anesthetic effects of lidocaine with combination treatment. No patient had any systemic or local adverse effects. Global assessment by patients and investigator was also favourable for combination treatment. We conclude that combined treatment with topical diltiazem and lidocaine is safe and effective option for pharmacological treatment of CAF, and addition of lidocaine to diltiazem significantly increases the pain relief achieved with diltiazem alone.

Keywords:  Chronic anal fissure, diltiazem, lidocaine, anal resting pressure

ABSTRACT

To synthesize and characterize novel thiazolidinone derivatives and screen them for anti tubercular activity. A series of ten 2-(substituted phenyl)-3-[{4-(1-naphthyl)-1, 3-thiazol-2-yl} amino]-5-methyl-1, 3-thiazolidin-4-ones (TM₁-TM₁₀) were synthesized from 1-acetyl naphthalene. The synthesized compound, characterized on the basis of satisfactory analytical and spectral (IR, H¹NMR, Mass and elemental) data. Studies were carried out for the synthesized compounds which were also evaluated for anti-tubercular activity by using Lowenstein-Jensen (LJ) acid medium and screening by Cup plate method. Rifampicin (Lupin) is used as standard antitubercular agents. The synthesized compounds showed good anti tubercular activity, compared to standard drugs. Two of the compounds TM₁ (Ar = 4-nitrophenyl) and TM₆ (Ar = 3-fluorophenyl) exhibited significant anti-tubercular activity, as compared to standard drug Rifampicin. We report the successful synthesis of novel thiazolidinones, as well as their spectral characterization, and anti tubercular activity which, for some, is superior to currently used anti-tubercular agents.

Keywords: Anti-tubercular activity, 1-Acetylnaphthalene, Thiazoles, Thiazolidinones

ABSTRACT

The main aim of this study was to evaluate the effect of Colgate Dental Cream on Catfish. Investigation was carried out using Catfish weighing about 475-525 g. Fishes were maintained for 24 h in the water, dissoved with 100 mg of Colgate Dental Cream.  Reduced serum total protein, albumin, glucose and urea, concomitant with a reduced concentration chloride ions were observed. Enzymes such as alanine transaminase (ALT), aspartate transaminase (AST) and alkaline phosphatase (ALP) enzyme activities were changed significantly. In addition, structural architecture of  liver, heart, gills, muscle and kidney were also changed. Biochemical and histopathological changes in the catfish were due to the fact that there was an increased demand for energy under stress to cope up with the detrimental effects of the dental cream.

Keywords: Colgate dental cream; fish; histopathology; protein; enzymes

ABSTRACT

The Unani System of Medicine also known as Greeko-Arab medicine, founded by Hippocrates is based on the concept of equilibrium and balance of natural body humours (blood, bile, black bile and phlegm). The imbalance in the quality and quantity of these humours leads to diseases whereas restoration of this balance maintains health of a person. According to Unani literature, headache is a type of pain which occurs in specified area of head and disturbs its functions. It can be due to external or internal factors. The internal factors may be maddi (involving matter) or sadah (which do not involve matter). Shaqeeqa is an Arabic word which is derived from the word ‘Shaq’ which means a part or a side, due to which it is named as Shaqeeqa. The cause of migraine is either riyah haar or imtila. In this system of medicine, the basic principle of treatment is Ilaj bil zid i.e treatment is in contrast to nature and Mizaj of the disease and is adopted in two ways i.e. observational and rational methods which are employed through diet, drugs, regimes, manipulation techniques and operations. This review aims at highlighting the concept of migraine with special reference of Shaqeeqa and its management in Unani system of medicine.

Keywords: Unani Medicine, Hippocrates, Humoral theory, Migraine, Shaqeeqa.

ABSTRACT

Tamoxifen Citrate (TC), an antiestrogenic drug, is used in both pre and post menopausal breast cancer treatment in women. One of the major causes of its poor bioavailability is attributed to its poor aqueous solubility. In this study an effort has been made to improve the aqueous solubility of the hydrophobic drug using methods like cosolvency and micellisation. Cosolvents (ethanol, polyethylene glycol-400), and surfactants [polyoxyethylene sorbitan monooleate (Tween-80), Poloxamer-407 and Poloxamer-188] were tested for their solubilizing potential. Solubility enhancement approaches showed variable degrees of increase in solubility of TC. Solubility studies with different concentrations of Ethanol and PEG-400 at 37°C showed that higher efficiency of increasing solubility by cosolvency was achieved with ethanol (6.10 fold) than that with PEG 400 (5.62 fold) while in case of varying concentrations of surfactants (tween 80, Poloxamer 188 and Poloxamer 407). Poloxamer 407 exhibited maximum potential in solubilizing TC in water (7.1 fold). However, among the solubilizing techniques and solubilizing agents used, micellization with polysorbate 80 as surfactant was found to be the most effective. Data suggests that using simple techniques, improvement of solubility of TC can be attained which may help in improving its poor bioavailability.

Keywords: Tamoxifen citrate, bioavailability, cosolvent, surfactant, micellisation, Poloxamer.

ABSTRACT

The aim of the study is to prepare solid lipid Microparticle (SLM) dispersion of aceclofenac for the treatment of inflammation and allied condition. SLM prepared by melt emulsification & solvent evaporation methods were characterized by Malvern instrument for particle size and particle size distribution and zeta potential analysis. The particle size of dispersion was further confirmed by scanning electron microscopy (SEM) studies. IR study of pure drug, Stearic acid and drug loaded solid lipid Microparticle were performed. In-vitro release study was performed on modified franz diffusion assembly which showed that drug release maximum 79.86% in 24 hours.

Keywords; Aceclofenac, Solid lipid Microparticle (SLM), Microparticle, Lipid Microparticle

ABSTRACT

Poorly, water soluble drugs such as cefuroxime axetil offer challenges in developing a drug product with adequate bioavailability. The main objective of present study was to prepare a lipid based self-microemulsifying drug delivery system to improve the oral bioavailability of cefuroxime axetil. The liquid self - microemulsifying drug delivery system consisted of cefuroxime axetil, Lutrol E 400, Labrasol and Gelucire 44/14. Initially liquid self - microemulsifying drug delivery system were characterized for clarity, rate of emulsification and drug loading capacity. The optimized formulation characterized for the zeta particle sizer, Differential scanning calorimetrystudies. In vitro results of self - microemulsifying drug delivery system and cefuroxime axetil were shown that the rate of drug dissolution from lipid based self-microemulsifying drug delivery system was significantly higher than commercial tablet and as well as pure drug. The results demonstrate the potential use of self - microemulsifying drug delivery system as a means of improving solubility, dissolution thereby it may enhance the bioavailability of cefuroxime axetil.

Keywords: Cefuroxime axetil, lipid based formulation, Self – microemulsifying drug delivery system.

ABSTRACT

Some chalcones (2a-2n) were synthesized by the condensation of various substituted benzaldehydes and unsubstituted/4-bromo acetophenone by using Claisen-Schmidt condensation. This is a comparative study of synthesizing compounds by conventional as well as non-conventional microwave irradiation in a commercially modified microwave oven. The research is focused on the remarkable reaction rate enhancement by the use of various non-conventional microwave irradiations which minimizes the time and solvents in reactions. Variety of functional groups such as nitro, chloro, dimethylamino, methoxy and methyl survived under the reaction conditions. The structures of newly synthesized compounds have been established on the basis of IR, ¹H NMR spectral data and elemental analysis. The synthesized compounds were screened for analgesic and anti-inflammatory activity.

Keywords: 4-bromoacetophenone, chalcone, analgesic, anti-inflammatory

ABSTRACT

To compare the bioavailability of two tablet formulations of Balofloxacin 100 mg in adult, male, healthy human subjects under fasting conditions.The study was conducted as an open label, balanced, randomized, two-period, two-sequence, two treatment, single dose cross over study to determine the bioequivalence of two tablet formulations of Balofloxacin 100 mg in 24 healthy, adult, male, human subjects under fasting conditions. Serial blood samples were collected at 0, 0.5, 1.0, 1.50, 2.0, 2.50, 2.75, 3.0, 3.25, 3.50, 3.75, 4.0, 4.50, 4.75, 5.0, 6.0, 8.0, 10.0, 12.0, 16.0, 24.0, 36.0, 48.0h during each study period. A washout period of 7 days was given between two study periods. 90% confidence interval(CI) for the ratio of logarithmic transformed pharmacokinetic parameters Cmax, Tmax, AUC0-t and AUC 0- ∞ were used to determine bioequivalence. The data of 23 subjects was analyzed in the study. Tmax (hrs),  Cmax (µg/ml),  AUC 0-t  and AUC0-∞ (µg.h/ml) for test formulation were 1.174±0.535 , 852.431±361.274, 4682.785±1616.552 and 5375.882±1727.286 and that of reference formulation were 1.033±0.428, 850.238±312.422, 4447.628±1240.125 and 5125.723±1304.619 respectively. The 90% CI for the T/R ratios of  log transformed  Cmax, AUC0-t and  AUC 0-∞ were 89.58%-108.19%, 98.86%-109.88% and 97.70%-110.01% respectively. The two tablet formulations of Balofloxacin 100mg (both test and reference) met the  requisite bioequivalence criteria (80-125%) .

Keywords: Bioequivalence, Balofloxacin, Urinary Tract Infection

ABSTRACT

Cyclosporin A (CsA) is a potent immunosuppressant acting mainly on T lymphocytes by blocking intracellular processes of T cell activation. Gingival overgrowth (GO) is a well-documented side effect associated with the systemic use of cyclosporin A, an immunosuppressive drug extensively used for the prevention of organ transplant rejection, as well as in the treatment of immuno-related disorders. It would appear from both human and animal models that plaque-induced inflammatory changes have a significant part in the pathogenesis of such a disease. Gingival overgrowth is a clinical condition that poses functional and aesthetic problems. This article describes a case of cyclosporin A induced gingival overgrowth and its management.

Keywords: cyclosporin A, gingival overgrowth, immunohistochemistry, gingivectomy

ABSTRACT

A simple rapid, sensitive, selective and reproducible reversed- phase high-performance liquid chromatographic method has been developed and validated for the simultaneous estimation of embtricitabine and tenofovir in pure and Pharmaceutical dosage form. In present work a simple, sensitive and specific method (RP-HPLC assay, stability indicating RP-HPLC) has been developed for the simultaneous estimation of embtricitabine and tenofovir in pure and Pharmaceutical dosage form. A phenomenex BDS C18, column having 5 µm particle size and 150 mm x 4.6 mm in length and gradient mode, with mobile phase containing  potassium dihydrogen phosphate (pH3.0, adjusted with O-phosphoric acid) and  acetonitrile in the ratio of 96:4. The flow rate was 1.0ml/min and effluents were monitored by UV detector at 254nm. The retention times of emtricitabine and tenofovir is 3.1±0.1 & 6.1±0.1 min was recorded at 254nm. The method is linear and the correlation coefficient was found to be 0.999. The method was validated for linearity, precesion, accuracy, solution stability, ruggedness, and post degradation studies were performed. Recoveries from formulations were between 98.3 and 99.5%. The results of specificity studies indicated no interference from excipients, impurities, and degradation products under various stress conditions and assured that the peak response was due to a single component only. Hence, the present method is cost-effective, faster, and can be used for the routine analysis of these drugs in pure and formulations.

Keywords: RP-HPLC method, Embtricitabine, Tenofovir Validation and Stability studies

ABSTRACT

The article describes strategy for masking the intensely bitter taste of Azithromycin Dihydrate(AZT) by using complexation with Kyron T-134. The resinates prepared with drug-Kyron T-134 ratio (1:3) at pH 8, gave maximum drug loading. Suspension containing, resinate showed more than 90% in-vitro drug release within 45min. Prepared formulation showed good stability and retention of palatable taste. Thus, the “patient-friendly dosage form” of bitter drugs, especially for pediatric, geriatric, bedridden, and non cooperative patients, can be successfully formulated using this technology.

Keywords: Azithromycin Dihydrate, taste masking, Kyron T-134.

ABSTRACT

Ixora pavetta Andrews, (var.: I. Parviflora Vahl.) is a small tree or evergreen shrub belongs to the family Rubiaceae, and is used for many ailments, especially for the treatment of to treat chronic wounds, urinary diseases, skin infection, pulmonary troubles, liver disorder, hair tonic, sedative, diuretic, diarrhoea, dysentery, leucorrhoea and veneral diseases. Preliminary phytochemical screening of ethanol exract of I. pavetta leaf showed the presence of alkaloids, flavonoids, tannins and saponin glycoside. In the analgesic activity, ethanol extract provoked a significant reduction of the number of writhes in acetic acid-induced writhing response, also significantly reduced the licking time in both phases of the formalin test and highest analgesia in hot-plate test (P < 0.01) compared to the control group. The anti-inflammatory effects were investigated employing the both carrageenan and arachidonic acid -induced hind-paw oedema in rats and results of the study revealed the extract to have significant (P<0.05) anti-inflammatory effects at a dose of 400 and 600 mg/kg p.o., rats in both the models. The antipyretic activity was evaluated using Brewer’s yeast induced pyrexia in rats and the extract showed significant lowering of body temperature in rats at doses of 400 and 600 mg/kg p.o., and no promising results with 200 mg/kg dose level. These findings suggest that ethanol extract of I. pavetta leaves possess potent anti-inflammatory, analgesic and antipyretics effects.

Keywords: Ixora pavetta Andrews; analgesic; anti-inflammatory; antipyretic

ABSTRACT

The potential of guar gum as a film coating material for colon targeted delivery of raupyabhasma is assessed in this study. The granules was prepared by mixing raupyabhasma, guar gum and xanthan gum which was coated by guar gum and pH-sensitive polymer eudragit FS30D sequentially around drug-loaded granules. The outer eudragit FS30D coating defends the system against gastrointestinal environment and dissolves rapidly in distal small intestine, where a lumen pH of over 7 triggers the dissolution of the enteric polymer. The inner guar gum coating works as a time-controlled retardant and offers additional protection of the granules until it is degraded by microbes at the proximal colon. In vitro results indicate that guar gum followed by eudragit FS30D coating is a feasible coating material to achieve colon specific drug delivery.

Keywords: Colon targeting, Microbially triggered drug delivery to colon, Polysaccharide based drug delivery, Colon targeted drug delivery, Silver nanoparticles, Bhasma etc.

ABSTRACT

Solvent extraction of iron (III) from hydrochloric, sulphuric, nitric and perchloric acid solutions with Tri-n-butylamine (TBuA) in benzene has been studied. The extractions are nearly quantitative from all the acid solutions. The optimum conditions for extraction were established from the study of the effect of several variables like concentration of amine, metal ion, acidity, foreign ions etc. Attempts are also made to strip iron from the organic phase with 1.0M H₂SO₄. The extracted species are identified.  The method has been applied for the determination of iron in tap water as well as ferrochrome slag.

Keywords: Solvent extraction -iron (III) - Mineral acid  - Tri-n- Butyl amine [TBuA]  - Slag

ABSTRACT

Heterocyclic compounds have gained immense importance in human life because of their variety of applications, particularly these compounds have been successfully tested against several diseases and therefore have acquired medicinal importance. Titled Bis-Pyrazoles have been synthesized by condensation of phenyl hydrazine hydrochloride and hydrazine hydrate respectively with Bis-chalcone dibromides in pyridine medium. All compounds have been evaluated for their in vitro growth of inhibitory activity against one Gram-positive strain Staphylococcus aureus and three Gram-negative strains like Escherichia coli, Proteus mirabilis and Salmonella typhi using paper disc-method. The culture medium was nutrient agar medium. Most of the titled Bis-pyrazoles are more or less effective against these microorganisms. Hence for treatment of diseases these Bis-pyrazoles can be used by test pathogens only when they do not have any toxic and other side effects.

Keywords: 1, 1 Bis- {2- hydroxy-3-(1΄- phenyl / H-5΄-Aryl-pyrazol 3΄-y1) – 5 methyl phenyl} methanes, Antimiorobial activity.

ABSTRACT

A simple, precise, economical and accurate difference spectroscopic method has been developed for the valacyclovir in bulk and in pharmaceutical dosage form. The proposed method is based on the principle that valacyclovir exhibits two different chemical forms that differs in the absorption spectra in acidic and basic solution. The absorptions were measured in acidic and basic solution separately against reagent blank. Valacyclovir has exhibited maximum absorbance at 252 and 262nm in acidic and basic solution respectively. Difference in absorbance between these two maxima was calculated to find out the amplitude. The amplitude plotted against concentration showed linear response in the concentration range of 0.5 – 2.5μg/mL with linear regression value 0.999. The proposed method was applied to pharmaceutical formulation and the common excipient present in the formulation does not interfere in the analysis of the drug. The method was validated as per ICH guidelines and statistical results of analysis were found to be satisfactory.

Keywords Valacyclovir, difference spectrophotometry, overlay spectra, tablet dosage form, validation.

ABSTRACT

The solubility of a substance becomes especially important in the pharmaceutical field because it often represents a major factor that controls the bioavailability of a drug substance. Moreover, solubility and solubility-related properties can also provide important information regarding the structure of drug substances, and in their range of possible intermolecular interactions. For these reasons, a comprehensive knowledge of solubility phenomena permits pharmaceutical scientists to develop an optimal understanding of a drug substance, to determine the ultimate form of the drug substance, and to yield information essential to the development and processing of its dosage forms.

Keywords : Development, Drug Substance, Solubility, Pharmaceutical Field.

ABSTRACT

In view of an increasing interest in developing plant derived insecticides as an alternative to chemical insecticides, this study was undertaken to assess the larvicidal potential of  Erythrina indica root and leaf extracts  against two medically important species of mosquito vectors, Aedes aegypti  and Culex quinquefasciatus. Larvicidal activity of methanol, aqueous, ethyl acetate, chloroform and petroleum ether extracts of leaf and root of Erythrina indica were tested against the early fourth instar larvae of A.aegypti and C. quinquefasciatus. Fourth instar larvae of A. aegypti and C. quinquefasciatus were used for assessing the larvicidal activity. A number of 125 larvae were exposed in five replicates of 25 larvae each. Experiments were maintained at 28±1° C, 65±2% relative humidity. The mortality data were subjected to probit analysis to determine the lethal concentrations (LC₅₀ and LC₉₀) to kill 50 and 90 per cent of the treated larvae of the respective species. Among the leaf and root extracts studied for mosquito larvicidal activity, both root and leaf extracts showed the moderate activity. The chloroform extract of the root was moderatively effective against the larvae of C. quinquefasciatus and A. aegypti; the respective values for LC50 and LC90 were 125.55, 118.90 ppm and 375.27, 354.03 ppm. The methanol extract of the leaf was also moderatively effective against the larvae of  C. quinquefasciatus and A. aegypti with respective LC50 and LC90 values 126.60, 126.76 ppm. The finding of the present investigation revealed that the leaf and root extract possesses remarkable larvicidal activity against two medically important vector mosquitoes C.quinquefasciatus and A. aegypti. So this present ecofriendly paradigm proves the efficacy of E.indica as an botanical larvicide.

Keywords: Aedes Aegypti, C. quinquefasciatus, Erythrina indica, Larvicide, Mosquito, Phytochemical

ABSTRACT

Systemic sclerosis (SSc) is a multisystem autoimmune disease characterized by fibrosis and vasculopathy. It is a rapidly progressing disease and wide spreading dysfunctioning of various organs includes kidney, gastro intestinal, cardiovascular systems and etc. Annual incidence is 19 per million, and prevalence is 19-75 per 100,000, with a female: male ratio of 3:1, and 8:1 in mid to late childbearing years. Incidence is twice as high among African Americans. The data was collected from in-patient record book in the Deportment of Dermatology in a tertiary care hospital in India for a period of March 2011 to February 2013. A total of 180 patients were recorded in the in-patient record book of the Department of Dermatology in a tertiary care hospital for a period of March 2011to February 2013. Among the patients of systemic Sclerosis the dominating age groups were 21 to 30 years and 31to40 years. In the study most of the females 144 (80%) patients out of 180, males 36 (20%) patients out of 180 are having Systemic sclerosis disease. The female/male ratio of disease is 4:1.

Keywords: Systemic Sclerosis, Auto immune disorder, Epidemiology, Prevalence in a tertiary care hospital, Female/Male ratios.

ABSTRACT

The present investigation was carried out to develop colon targeted drug delivery system which consists of chitosan-chondroitin sulphate interpolymer complex as a binder containing rifaximin in the core coated with Eudragit E-100 and Eudragit RL-100.The  chitosan-chondroitin sulphate interpolymer complex was characterized by Fourier Transform Infrared Spectroscopy. In vitro release studies of coated tablets were carried out for 2 h in pH1.2 HCl buffer, 3h in pH 7.4 phosphate buffer and 19 h in pH6.8 phosphate buffer in the presence and absence of rat caecal content. A drug release of 27.13% was observed with uncoated tablets in HCl buffer pH 1.2, 80.56% of drug release in phosphate buffer pH 7.4 and 99.23% was observed in phosphate buffer pH6.8. Also tablets coated with Eudragit E-100 and Eudradgit RL-100 with different coat weight showed less than 10% of drug release in the stomach whereas same tablets showed 23.22%, 15%, 13.39%, 12.83% release of drug in pH 7.4 phosphate buffer and 73.26%, 75.91%, 72.23%, 71.93% release of drug in pH 6.8 phosphate buffer. Histopathology of rat colon after administration of Eudragit E-100 and Eudradgit RL-100 coated tablets containing chitosan-chondroitin sulphate interpolymer complex revealed marked reduction in acetic acid induced colitis in test group.

Keywords: chitosan, chondroitin sulphate, Eudragit E-100, Eudradgit RL-100, rifaximin    

ABSTRACT

The purposes of the present study were: 1).To study the relationship between different concentrations of the chiral enhancer D-Limonene (D-LM) on the solubility of individual enantiomer and racemate Timolol maleate (TM). 2). To study the preferential enhancement of D-LM upon S-TM, R-TM, and racemate across the hairless mice skin. For solubility studies, excess of R-, S-, or racemate with wide-range of different concentrations of D-LM were prepared.  Samples were agitated, centrifuged and filtered and analyzed by HPLC using chiral column at 294nm.  For skin transport studies, formulations containing 0.5% solutions of S-TM, R-TM, or racemate in buffer solution with predetermined concentrations of D-LM were studied. Samples of 1-ml were withdrawn and quantitatively analyzed for their TM contents.  The steady-state fluxes (Jss), permeability coefficients and the enhancement factor were calculated. In solubility studies, D-LM significantly enhances solubility of all forms of TM in a concentration dependent manner.  In permeation studies, presence of D-LM significantly enhances the flux values of both enantiomers and racemate.  However, D-LM immensely increased all permeability characteristics of the S-isomer compared to those of R-isomer. Solubilities of all forms of TM were found to be a single-valued function of D-LM concentration. Moreover, addition of D-LM has enhanced the transport of S-, R-TM enantiomers and that of racemate across hairless mice skin.  For all tested formulations, the overall permeability characteristics of the therapeutically active TM (i.e., S-TM) were superior results obtained with the R-TM either as enantiomer or racemate.

Keyword: Timolol, Terpene, Chiral, Enhancer, D-Limonene, Enantioselective

ABSTRACT

In the present study, ethanolic and aqueous fruit extracts of Thespesia populnea were tested against the head louse pediculus humanus capitis. A filter paper diffusion method was conducted for determining the potential pediculocidal activity. The results revealed that plant extracts possess excellent anti lice activity. Results were well comparable with benzyl benzoate.

Key words: Thespesia populnea, Anti lice activity, Filter paper bioassay, Head louse.

ABSTRACT

The colon drug delivery system has gained recent importance in delivery of the drug to the colon. These system facilitate the delivery of the drug to the colon and mainly releases the drug in the colonic environment and thereby reduces various side effects of conventional dosage forms like lower dose is required and hence lowering the side effects caused by higher doses. In the present study natural polysaccharide approach is employed and sesbania gum powder was used as a carrier for delivery of the drug to the colon . Satranidazole was selected as a drug of choice because it is most potent nitroimidazole derivative and clinically useful against common protozoa, it is twice as effective as other nitroimidazoles against amoebiasis. Colon targeted tablet of satranidazole can maintain minimum inhibitory concentration for desired duration in fewer doses with fewer side effects. The aim of the present research work is to develop core tablets of satranidazole and compression coated with different ratios of sesbania gum powder. All the formulations were then subjected for evaluation and were tested for hardness, drug content uniformity an in vitro drug release studies. The compression coated formulation CCS 2 released less than 5% of satranidazole drug in the physiological environment of stomach and intestine, when the dissolution studies was further continued in simulated colonic fluids the compression coated tablets with 150mg of sesbania gum powder released another 70% of satranidazole in the colon after degradation by colonic bacteria at the end of 12 hrs.

Keywords: Satranidazole, compression coated, Microbially triggered, polysaccharides, colon targeted tablets.

ABSTRACT

The different solvent extracts of Scleroderma bermudense belongs to the family Sclerodermataceae collected from semi evergreen forest region (13˚51'56.30"N, 75˚03'12.50"E) which is located in Haniya, Hosanagar taluk, Shimoga district, Karnataka was subjected to phytochemical analysis for secondary metabolites and antifungal screening by agar well diffusion method against plant and human pathogenic fungi viz., A. alternate, A. flavus, A. solani, A. tomentosa, C. capsici, C. dematium, C. lindemuthianum, F. oxysporum, F. solani, M. gypseum, T. equinum, T. kanei, C. albicans, C. indicum, C. krusei, C. merdarium, C. zonatum, E. floccosum and T. rubrum. Extracts were found to contain steroids, saponins, glycosides, flavonoids and phenols. The extract also showed significant antifungal activity against C. albicans, C. indicum, C. merdarium, F. oxysporum, C. dematium, T. equinum, A. flavus C. capsici, F. solani, C. kruesi and C. lindemuthianum, whereas least activity showed against A. solani, M. gypseum and does not showed inhibition zone against A. alternate, A. tomentosa. T. kanei, C. zonatum, E. floccosum and T. rubrum. However, the activity was less than the standard Clotrimazole, Fleuconazole, Mancozeb and Captan. The extract shows increasing inhibitory activity with increase in concentration (12.5%-100%).While comparing the solvent studied, petroleum ether and methanol extracts showed highest response in resisting microbial growth than chloroform.

Keywords: Scleroderma bermudense, Phytochemistry, Antifungal activity, Pathogens, Wild mushrooms, Western Ghats.

ABSTRACT

The aim of this study was to prepare Diclofenac potassium (DP) microspheres by using Double Emulsion-solvent evaporation method with ethyl cellulose (EC) and Eudragit polymers. An attempt was made to formulate a sustained release dosage form of diclofenac potassium, to minimize frequent dosing as well as reducing or eliminating local side effects by avoiding the drug release in the upper gastro-intestinal tract Poly vinyl alcohol containing 2% (w/w) span 80 was the external phase and polymer -drug solution was the internal phase. EC and Eudragit were used to encapsulate diclofenac potassium. By using different formulation variables, six different formulations (F1, F2, F3, F4, F5, & F6) were prepared. The resulting microspheres obtained, were more spherical in shape and showed more entrapment efficiency. The size of the microspheres varied between 346-695 μm and as high as 96.24% loading efficiency for Eudragit and 82.34% for EC was obtained. In vitro release study was carried out in 0.1 N hydrochloric acid solution (pH 1.2) for first 2 hours followed by in phosphate buffer solution (pH 6.8) for next 4 hours. After first 2 hours of dissolution in 0.1 N hydrochloric acid, EC microspheres released 23% of drug and Eudragit released 7% of drug. The formulations were found to be effective in providing controlled release of drug for a longer period of time.

Keywords: microsphere, diclofenac potassium, eudragit, ethyl cellulose, entrapment efficiency.

ABSTRACT

The present investigation has been undertaken with aim to formulation and evaluation of etoricoxib gel with different gelling agent and different penetration enhancer. Etoricoxib is highly selective cyclooxygenase-2 (COX-2) inhibitor. In this present study gel with carbopol, HPMC and Na-CMC as gelling agent prepared with different penetration enhancer like propyl glycol, oleic acid. Menthol oil. Formulation were evaluated for pH, stability study, spreadibilty, extrudabilty, bioadhesive (ex-vivo), skin irritation, viscosity, appearance and In-vitro drug diffusion. The formulation of Etoricoxib topical gel was prepared using carbopol, HPMC and Na-cmc in three batches A, B and C. With the consideration of all formulation characteristic and parameter we selected batch-A formulation for further study of anti-inflammatory and anti-analgesic activity. It was concluded that the Etoricoxib gel formulation containing carbopol with increase concentration of propyl glycol 10% and 2% oleic acid (OA) was suitable for topical application and it shows comparable result with market product and shows much better result of formulation, anti-inflammatory and anti-analgesic activity.

Keywords: Etoricoxib, topical gel, Carbopol, HPMC, Sodium CMC, Propyl glycol, Oleic acid, Anti-inflammatory activity, Anti-analgesic activity.

ABSTRACT

A new series of Mn(II), Co(II), Ni(II), Cu(II), Cr(III) and Fe(III) complexes with tetradentate unsymmetrical Schiff base ligand derived from o-hydroxyacetophenone, 5-chloro-2-hydroxyacetophenone and ethylenediamine have been reported. The complexes have been characterized by elemental analyses, magnetic susceptibility measurements, electronic and infrared spectra and thermogravimetric analyses. The ligand and its complexes were screened for their antimicrobial  activities against the bacteria Staphalococcus aureus, Bacillus Subtilis, Salmonella typhimurium and Escherichia coli and fungi Aspergillus oryzae and Fusarium species. The results indicated that the complexes exhibited good antimicrobial activities.

Keywords: Unsymmetrical Schiff base, Transition metal complexes, Antimicrobial activity.

ABSTRACT

Most of the synthetic drugs which induce side effect during overdose. The natural compounds are playing important role to reducing side effects of the synthetic drugs and also increase the immunity of recipients. The objective of the present study is to investigate the compatibility between Paracetamol as a synthetic compound with Spirulina as a natural compound.  The Paracetamol and Spirulina mixture were prepared in different ratio 1:1 (w/w) (Paracetamol: Spirulina), 1:2 (w/w) (Paracetamol: Spirulina) and 2: 1 (w/w) (Paracetamol: Spirulina). These samples were stored at different temperature (5 ˚C, 15 ˚ C, 30 ˚ C and 40 ˚ C) for one month. For every week samples were taken in the mixtures and the quantification of Paracetamol by using reversed phase liquid chromatography and estimation of chlorophyll A, B, total chlorophyll and total carotenoids in the mixture by using UV spectrophotometer. There was no significant loss of Paracetamol, chlorophyll, and carotenoids in their mixture. Both Paracetamol and Spirulina were stable under different temperature. Therefore it conclude that Paracetamol and Spirulina were compatible when mixed in a ratio of 1:1(w/w), 1:2 (w/w) and 2:1 w/w) 

Keywords: Paracetamol, Spirulina, RP-HPLC, UV spectrophotometer

ABSTRACT

The aim of the present study was to investigate the chemical composition of Spirulina subjected to different solvent extraction (acetone, methanol and ethyl acetate) by using soxhlet methodology and the extracts were analysis by Gas chromatography coupled with mass spectrophotometer (GC-MS) using DB-5 capillary column. During GC-MS analysis, it was observed that fatty acid components are present in their extracts. In acetone extract, totally forty compounds were identified and heptacosane (17.25%), hexacosane (17.04%), heneicosane (14.47%), pentacosane (13.22%) and Nonacosane (11.29%) as major components. Thirty five compounds were identified in methanol extract and the major compounds are n-Hexadecanoic acid (19.9%), Cyclononasiloxane octadeca methyl (7.81%) and phytol (6.53%). Thirty components were identified in ethyl acetate extract and dodecane (17.35%), heptadecane (15.31%), sufurous acid butyl heptadecyl ester (11.31%) and n-hexadecanoic acid (4.26%) most abundant in ethyl acetate extract.

Keywords: Spirulina, GC-MS, acetone, methanol, ethyl acetate

ABSTRACT

The field of patient’s drug safety has been receiving great deal of attention, since adverse drug reaction has been recognized as hazards of drug therapy. Adverse drug reactions are a great cause of concern to the healthcare professionals, patients and the pharmaceutical industry. However, may times it goes undetected and ignored by the patients and healthcare professionals. Hence we took a prospective observational study to analyse the Adverse Drug reactions among all patients admitted in general medicine department in Justice KS Hegde Charitable Hospital, Mangalore. The study was carried out for a period of eight months from September 2012 to April2013. The suspected adverse drug reactions were later analysed for their causality, severity and preventability by using the different adverse drug reaction assessment scales. A total of 640 cases has been followed and 47 Adverse Drug Reactions has been reported from the 40 patients during the study period. Male predominance was noted over females in case of total number of patients. Majority Adverse Drug Reactions were in the age group 70-79(31.91%). The most common class of drugs involved in adverse drug reactions is Antibiotics (17.39%) followed by Antihypertensive 7(15.21%). The most common system involved in adverse drug reaction is Digestive system (19.36%) followed by dermatological system (13.04%). Out of the 47 adverse drug reactions reported, 53% were probable, 45% were possible and 2% were unlikely. The severity assessment done by using the Hartwig and Seigel scale indicate that majority of the ADRs were ‘Mild’ followed by moderate and severe respectively. The preventability assess shows that most of ADRs are Probably Preventable 28(59.57%) followed by Not preventable 16(34.04%) and definitely preventable 3(6.38%). Monitoring and reporting of adverse drug reactions in the hospital is one of the best method to identify the causality between exposure to the drug and the occurrence of adverse drug reaction. Proper education and training to the healthcare professional’s towards ADR reporting will have a positive attitude towards continuous reporting and improving patient safety.

Keywords: Adverse Drug Reaction (ADR), prospective observational, Causality, Severity, Preventability, Predisposing factors.

ABSTRACT

Tablet is the most popular dosage form of all existing dosage forms , but in some cases due to the large size of dosage forms, in case of uncooperative, pediatric and dysphasia patients, it may create  problems, to overcome this , a new form of dosage form is developed, which is known as fast dissolving tablets or mouth dissolving tablets. These dosage forms are also used to attain instant higher concentration of drug in body for immediate actions. Gliclazide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). Fenugreek seed powder was added to this formuation because of  its various pharmacological benefits as well as its self disintegrating property. Mouth dissolving tablets were prepared using direct compression method .Formulations were optimized to develop tablets having minimum possible disintegration time. Tablets were evaluated for hardness, weight variation, friability, wetting time, disintegration time and stability. The main objective of the present research is formulation and evaluation  of mouth dissolving tablets of gliclazide which is an antidiabetic drug ,containing fenugreek seed powder as disintegrating agent.

Keywords : mouth dissolving tablets, gliclazide, fenugreek seed powder, solid dispersion, evaluation.

ABSTRACT

Pyrazinamide being a 1^st line of defense against tuberculosis is very effective for the first 2 to 3 months of treatment and helps to eradicate a major portion of the strain. But due to its increased use, there are adverse effects such as hepato-toxicity and other dose related side effects. The amount of drug used in formulation is high i.e. 500mg to 1gm. Another major disadvantage is resistance of the bacteria leading to DR-TB (drug resistant tuberculosis). The main objective of this study is to decrease the amount of drug needed for formulation and to avoid hepato-toxicity. Pyrazinamide drug formulation was prepared into a niosomal dosage form by modified ether injection method, using various concentrations of polymer and keeping cholesterol content constant. Characterization was carried out and vesicle size determination showed that the formulated vesicles were in the range of 110-350nm. FTIR results showed that drug and polymers were compatible. Drug content and entrapment efficiency were calculated using UV-spectroscopy at 268nm. In-vitro release studies were carried out for all formulations and it was seen that Span-80 formulation had the highest percentage release when compared to other formulations. The drug release was subjected to various kinetic models and it was observed that all formulations followed zero order kinetics. It can be concluded that all these polymers can be used for the successful formulation of Pyrazinamide niosomes and the surfactant that is most apt was found to be Span-80 in the ratio 1:3 as compared to other polymers in various ratios.

Keywords: Pyrazinamide, tuberculosis, hepato-toxicity, drug resistant tuberculosis, niosomes.

ABSTRACT

This study is retrospective study to the culture and sensitivity test that done in the laboratory of  Al-Sadr hosp. in 2012 , during this period about 2664 C&S tests for all types of infection this includes (1033 for  urine), (790 t for blood),  (250 ts for  ear swab )and (591 ts for sputum) There is a completely irrational use of antibiotics in al-Sadr teaching hospital in Maysan –Iraq because there is no  a clear strategy for the treatment of different infections so they use antibiotics as a prophylaxis for all patients specially Ampiclox and Claforan or ceftriaxone  , but in fact there is about 14% only of patient that are suspected to be infected have a bacterial growth according to culture and sensitivity tests .Also there is only 0.4% of microorganisms that cause infection in that hospital sensitive to penicillin due to increase the antimicrobial resistance due to the overuse and misuse of antibiotics specially Ampiclox. Also the antibiotics cost is very high compared to other hospital in the neighboring countries  penicillins and most of cephalosporins are no longer  drug of choice for most of bacterial infections including staphylococcus bacterial infections in Iraq due to excessive use of them most of the medical problems that thought to be caused by bacterial infections, they are not. Only about 14% of them are caused by bacteria there is no critical need for antimicrobial prophylaxis for most of cases

Keywords: irrational antibiotic, antibiotics resistance, culture and sensitivity test, cost of antibiotics.

ABSTRACT

Sepsis is a leading cause of mortality in critically ill patients especially in burn unit. Delay in diagnosis and initiation of antibiotics treatment have been shown to increase mortality. This study aimed to find out a novel septicemia biomarker, more practical and easy. 48 patients had been admitted into burn unit during 4 months, 22 patients of them (46%) were complained of septicemia. HDL (high density lipoproteins) had been measured for patients in admitted to burn unit every other day to measure the correlation of HDL concentration and septicemia. HDL was a very good indicator for septicemia due to the wide range of normal value (40-60 mg/dl).Number of patients was 48 patients, 22 of them developed septicemia about 46%. 11 patients of the 22 patients are died (50%). Also it is clear to notice that all patients died were with (HDL = <5); 1 or 2 days before dying, all patients with HDL < 15 were with a positive blood culture, and all patients with septicemia when their HDL value increased 5 scales are cured of the infection, i.e. from < 5 to 10 for example. It is very important to find that patients with HDL value < 15 with abnormal triglyceride value (more than 200) were with high risk of developing septicemia  HDL value in burn unit is the best biomarker for septicemia and it seems to give a map for the severity of infection and accurate time of initiation and stopping of antibiotics treatment.

Key words: HDL, septicemia, burn, Maysan and Iraq.

ABSTRACT

Mannich bases of sparfloxacin were synthesized from the reaction of 5-acetylamino-1-cyclopropyl-7-(3΄,5΄-dimethyl-piperazin-1-yl)-6,8-difluoro-4-oxo1,4-dihydro-quinoline-3-carboxylic acid with formaldehyde and several isatin derivatives. The structures of the synthesized compounds were elucidated from the IR, ¹H NMR, ¹³C NMR and FAB Mass data. The synthesized compounds were evaluated for the antibacterial, antitubercular and anticancer activity. The compounds showed good activity against Gram-positive bacteria and moderate activity against tested Gram-negative bacteria. The MIC for the compounds against M. tuberculosis H₃₇Rv strain was <6.25 µg/mL while the IC₅₀ values against cancer cell lines SW480, HeLa, A549 and HepG2 was in the range of 18.31- >50 µg/mL. The most potent compound in this series 3c exhibited enhanced antibacterial activity than sparfloxacin against S. aureus, Bacillus Sp while the anticancer activity was in the range of 18.31- 23.61 µg/mL.

Keywords : Sparfloxacin, Mannich bases, Isatin, Antibacterial, Antitubercular, Anticancer.

ABSTRACT

Oral drug delivery has been known for decades as the most widely utilized route of administration among all the routes. United State Food and Drug Administration (FDA) defined ODT as “a solid dosage form containing medicinal substance or active ingredients which disintegrate rapidly usually within a matter of second when placed upon the tongue. Propranolol is a nonselective beta-adrenergic blocker and is almost completely absorbed following oral administration. However , most of drug is undergoes high first-pass metabolism by the liver and on average, only about 25% of propranolol reaches the systemic circulation. The present study investigated to development of novel fast dissolving tablet of Propranolol HCL which was by first pass metabolism, provide rapid onset of action and increasing the bioavailability of the drug. The fast dissolving tablets were prepared by Direct compression method by using different superdisintegrant like Crosspovidone, crosscarmellose sodium, sodium starch glycolate etc. The advantage of this formulation is such that in case of hypertension attack patient can take the drug without the usage of water. Therefore the main objective of the present work is to develop orodispersible tablets of Propranolol hydrochloride to improve bioavailability, disintegration time, dissolution efficacy and patient compliance.

Keywords: Superdisintegrants, Orodispersible tablets, Disintegration time, Direct compression, Propranolol hydrochloride

ABSTRACT

Ethnic communities inhabiting Jharkhand state are living in true harmony with nature. They entirely depend on plants and plant resources for their livelihood. Plants use in tribal belt is as diverse as the ethnic diversity. The paper focuses on lesser known nutraceutical plants, usually  not known to the modern society but form an important dietary part of the ethnic people and provide them both nutritional and health security. These vegetables are lesser known and under-utilized resources, which are rich both in nutrients and secondary metabolites, providing nutritional and health security (nutraceutical). These plant resources grow their own, thrive easily on inhospitable conditions without any input, give new taste and are free of chemical pesticides and insecticides. In view of the large scale utilization of land area in the name of various kinds of developmental activities there is an urgent need of enlisting wild nutraceutical potherbs and documentation of their therapeutic uses before it is too late. The present paper describes 35 plants species which are widely consumed amongst ethnic communities.

Keywords: Ethnic communities, Under-utilized, Potherbs, Secondary metabolites, Nutraceutical, Pesticides. 

ABSTRACT

A pestle and mortar-assisted solvent-free condensation of salicylaldehyde and 2-aminopyridine efficiently afforded a NO donor Schiff base ligand in high yield. This is an environmentally benign method, as satisfactory results were obtained in solvent free conditions with excellent yields, short reaction time, and operational simplicity in the experimental procedure. Copper(II) complex of this ligand were synthesized. Schiff base ligand and its complex were characterized by their melting point, elemental analysis, IR and ¹H NMR spectra. In addition, DNA-binding properties of the metal complex were investigated using absorption spectroscopy, viscosity measurements and thermal denaturation methods. The DNA photoclevage experiment shows that, the complex act as effective DNA cleavage agent.

Keywords: Green synthesis; Schiff base; Metal complexes; DNA binding; DNA photocleavage.

ABSTRACT

The aim of present study,  To formulate and characterized  proniosome contain flurbiprofen in a gel formulation for the treatment of rheumatoid arthritis and enhanced skin targeted effect, sustained & prolonged drug release, enhanced skin bioavailability by using different type of non ionic surfactant & cholesterol. The batches were designed using Box Behnken Design and prepared by coacervation phase separation method. Optimized formulation (PNGopt) showed drug entrapment efficiency of 74.46% and particle size 215nm. In-vitro drug release from PNGopt was found to be 84.15 in 24 hrs. The In-vitro drug release was best explained by zero order kinetics as the plot showed highest linearity and release was governed by Quasi Fickian diffusion.

Keywords: Proniosomes, Flurbiprofen,Brij93,in-vitro release, Stability  studies

ABSTRACT

Chitosan, a linear binary heteropolysaccharide, composed of β-1, 4-linked glucosamine (GlcN) with various degrees of N-acetylation of GlcN residues. It is a non-toxic, biocompatible and biodegradable natural polymer of high molecular weight (~500,000 kDa). The degree of deacetylation (DD) and molecular weight (MW) are two fundamental parameters that can affect the properties and functionality of chitosan. HPMC is the dominant hydrophilic vehicle used for the preparation of oral controlled drug delivery systems. Hydrophilic polymers are widely used in controlled release systems due to their favorable functionality. Enhancing the mobility of the polymer chains and diffusing of the drug out from such polymer matrices could be done by inclusion of different types of excipients at different concentrations. The present manuscript describes the attempt undertaken to develop the matrix tablet of Aceclofenac along with different grades of chitosan and HPMC as a copolymer & to study effect of it on the swelling behavior and the drug release pattern.

Keywords: chitosan A, B, C, D and E, Aceclofenac, HPMC, drug release, swelling

ABSTRACT

Plants are known to be associated directly or indirectly with the needs of human since time immemorial. In addition to the basic needs, i.e. food, shelter and clothing, plants are utilized for fodder, fuel, timber, tannins, colors, oils and medicines etc. History reveals that uses of plants as medicine is known in different parts of  the world, especially in India there are evidences which suggest its therapeutic role since Rig Veda. There are 32 ethnic communities in Jharkhand, which constitute about 33% of total population. They have their own self-managed traditional system for primary health care (Horopathy).Women are traditionally using herbal medicines for the remedy of different types of gynecological problems. In the present investigation 30 plants species have been reported on the basis of ethno-medicinal information extracted from ethnic communities. All the parts of plants, like root, bark, leaf, flower, fruit and  tubers are used as medicines, either preparation from single plant is used as drug or in some cases decoction or paste are made with more than one herb.  There is very wide scope for the pharmacological studies of the reported plants in future. 

Keywords: Horopathy, Therapeutic, Ethnic communities, Gynecology, Pharmacology 

ABSTRACT

The crude methanol extract of leaf of Tiliacora acuminata Miers as well as organic solvent (n-hexane, carbon tetrachloride and chloroform) fractions and methanolic fraction (aqueous) were subjected to screening for total phenolic content, antioxidant, cytotoxic, thrombolytic and antimicrobial activity. In total phenolic content analysis, the n-hexane soluble fraction of leaf was found to contain highest amount of phenolic content (TPC, 132.18 mg/gm of dry weight of extract, expressed as gallic acid equivalents). In the DPPH assay, the n-hexane soluble fraction of leaf displayed the highest free radical scavenging activity with IC₅₀ value 64.54 μg/ml as compared to 27.5 μg/ml produced by butylated hydroxyl toluene.  A positive correlation was evident between total phenolic content and free radical scavenging activity of T. acuminata having correlation coefficient (R²) of 0.91. In cytotoxicity screening, the crude methanol extract of leaf demonstrated strong cytotoxic activity with LC₅₀ value of 2.40 μg/ml as compared to 0.451 μg/ml produced by vincristine sulphate. During assay for thrombolytic activity, the crude methanol extract revealed 32.5% lysis of clot while standard streptokinase and water, used as positive and negative controls, demonstrated 70.4% and 3.62% lysis of clot, respectively. In antimicrobial assay by disc diffusion method, all the samples exhibited moderate to significant antimicrobial activity (zone of inhibition = 10.0-20.0 mm) against all the test organisms. Among all the samples, the carbon tetrachloride soluble fraction displayed strong antimicrobial activity against Escherichia coli (20.0 mm).

Keywords: Tiliacora acuminata, Total Phenolic Content, Cytotoxicity, Antioxidant, Thrombolytic, Antimicrobial.

ABSTRACT

The voltammetric reduction behaviour of Lorazepam has been studied by using d.c polarography, cyclic voltammetry (CV) and differential pulse polarography (DPP) in Britton-Robinson buffers of the pH ranging from 2.0 to 12.0. DPP has been developed for the quantitative estimation of Lorazepam in different pharmaceutical formulations (Tablets) without any prior separation using standard addition method. A single step reduction wave/peak is found to be irreversible and diffusion controlled. Kinetic parameters such as transfer coefficient, diffusion coefficient and heterogeneous forward rate constant values are evaluated and reported. On the basis of the experimental results, a reduction mechanism is proposed for Lorazepam.

Key words: Lorazepam, Reduction behaviour, Mechanism, Analysis, Pharmaceutical formulations

ABSTRACT

Hepatic targeting of Concanavalin A appended myristoyl chitosan nanoparticles containing Epirubicin. Myristoyl chitosan was synthesised by reacting native chitosan with myristoyl chloride and  degree of acylation was determined by Ninhydrin assay. Nanoparticles of chitosan and myristoyl chitosan were prepared by ionic gelation and the method was optimised for processing parameters based on particle size, zeta potential and entrapment efficiency (EE). The nanoparticles of chitosan and myristoyl chitosan were conjugated with concanavalin A by incubation and the conjugation was confirmed by zeta potential measurement. The surface morphology of the optimized formulation was checked with the help of SEM and was further studied for organ distribution studies in Wistar rat model. Myristoyl chitosan synthesised was confirmed by FT-IR studies. Degree of acylation was found out to be 42.2 ± 2.7%. The optimized Con A conjugated nanoparticles prepared by chitosan (Ch17) and myristoyl chitosan (MCh17) was found to be spherical in shape with particle size 244.4nm and 275.8nm, zeta potential of 0.307mV and 0.133mV, entrapment efficiency 45.01±1.32% and 40.10±1.23% respectively. In vitro drug release (PBS 7.4) from Ch17 was 93.02±1.66% and followed Higuchi model, while release from MCh17 was 68.53±2.27% and followed Peppas model. Both the formulation were stable for 1 month at the temperature of 2-8^oC. In vivo liver uptake of MCh17 nanoparticles was 93.6±10.11% while it was  87.0±7.55% with Ch17. Epirubicin loaded MCH17 nanoparticle showed high uptake by liver with concomitant reduction in blood level of Epirubicin in comparison to  Ch17 nanoparticles.

Keywords: Chitosan, Concanavalin A, Epirubicin, Liver targeting, Myristoyl chitosan, Nanoparticles.

ABSTRACT

In this study, a simple, sensitive and highly accurate ultraviolet spectrophotometric method has been developed and validated for determination of atenolol in bulk and pharmaceutical formulations. The method is based on the measurement of the absorbance of atenolol solution in methanol: phosphate buffer pH 6.8 (10:90) at 224 nm in the wavelength range of 200 - 400 nm. Beer’s law was obeyed in the concentration range of 5-25 µg/mL. The slope, intercept and correlation coefficient were also calculated. Results of percentage recovery shows that the method was not affected by the presence of common excipients in tablets. The developed method was validated in terms of accuracy, precision, linearity, limit of detection, limit of quantification which proves suitability of proposed method for routine estimation of atenolol in bulk and pharmaceutical formulations.

Keywords: Atenolol, Spectrophotometry, Estimation, Tablets.

ABSTRACT

Carica papaya Linn., (Family: Cariaceae) is a very well known plant which is found in various parts of India. The main aim of this study is to assay the wound healing activity of ethanolic extract of C. papaya leaf by using healthy rats of both sex and almost same age. Three types of models namely excision wound, incision wound and burn wounds which was created on dorsal part of saved rats using a metal rod heated to 80-85⁰ C and exposed for 20 seconds. The effects of ethanolic extract of C. papaya leaf on wound healing were observed by the rate of wound closure, period of epithelialisation and finally wound breaking strength. Povidone iodine ointment (5% w/w) is used as reference for excision and incision wounds models. During this study, it is observed that animals treated with C. papaya ethanolic extract, shows wound healing at a faster rate by comparing with animals treated with povidone iodine ointment. Similarly in burn wound healing study Silver-sulfadiazine used as reference drug for activity comparison and the efficacy of treatment was evaluated based on reduction of burn wound area. The ethanolic extract treated animals showed significant reduction in the burn wound area when compared with control groups. The result of the present study offers pharmacological evidence on the folklore use of C. papaya leaves for healing wounds including burns.

Keywords: Carica papaya, Wound healing activity, Excision wound, Incision wound, Povidone ointment.

ABSTRACT

The present work objective are to investigate the wound healing activity of some indigenous plant’s (Ipomoea Carnea  and N.Oleander Linn) leave extracts in Wister Albino Rats using two different models Viz., excision and incision model. In the form of an ointment with two concentrations (5% and 10% w/v ointment of methanolic leave extract in simple ointment base). Higher concentration of both concentrations of the methanolic extracts showed significant response in both the wound types tested when compared with the control group. From both the plants 10 % w/v ointment of plant Ipomoea carnea leave extracts on topically showed more significant activity than other test compounds. Nitrofurazone ointment (0.2%w/w) used as standard.

Keywords- Methanol extract, I. Carnea, N. Oleander Linn, Excision, Incision, Nitrofurazone.

ABSTRACT

Quetiapine Fumarate is a antipsychotic agent indicated for treatment of Schizophrenia and Bipolar disorder. Quetiapine Fumarate is BCS Class II drug which is  poorly water soluble and may show dissolution limited absorption. Hence to improve dissolution rate and bioavailability, Solid dispersion of Quetiapine Fumarate by Solvent Evaporation method were prepared using 1:1, 1:2, 1:3, 1:4 and 1:5 ratios of Quetiapine Fumarate and Polyvinyl Pyrrolidone K30(PVP K30). The solid dispersion (SD) was characterized for physical appearance, solubility, FTIR, DSC, XRD studies and in vitro dissolution studies. FTIR study revealed that there was no drug-carrier chemical interaction in Solid dispersion. DSC studies revealed that, the peak observed for the melting of Quetiapine Fumarate is found to be absent in SD with PVP K30 carrier. XRD studies suggested that there has been a large change in the nature of Quetiapine Fumarate in the solid dispersion. Solubility of Quetiapine Fumarate from SD increased in distilled water. The drug content was found to be high and uniformly distributed in the formulation. The in vitro dissolution studies were carried using USP type II (paddle) type dissolution apparatus. The prepared Solid dispersion showed marked increase in the dissolution rate of Quetiapine Fumarate than that of pure drug. The Solid dispersion with PVP K30 (1:5) by Solvent evaporation method showed faster dissolution rate as compared to other Solid dispersions. It is concluded that dissolution of the Quetiapine Fumarate could be improved by the Solid dispersion.

Keywords: Quetiapine Fumarate, bioavailability, Solid dispersion, dissolution.

ABSTRACT

Nateglinide, an oral hypoglycemic agent is having disadvantage of low systemic bioavailability, poor absorption in upper intestinal tract, and short biological half life (1.5hr) for increasing the resident time of this drug in stomach spray drying technique used for preparation of mucoadhesive microspheres consist of different polymers like Hydroxypropyl Methycellulose (HPMC), Hydroxypropyl cellulose (HPC), Polyvinylpyrrolidone (PVP), Sodium alginate and ethyl cellulose with Nateglinide. The surface morphology and particle shape were studied by scanning electron microscope (SEM). The microspheres were evaluated for their micro encapsulation efficiency. The micro encapsulation efficiency of microspheres evaluated. Mucoadhesive microspheres prepared were spherical in shape, size in the range of 2.6-5μm.In vitro drug release performed for all the formulation and in vivo study of optimum formulation (F3) and pure Nateglinide in normal healthy rabbits performed. The micro encapsulation efficiency was in the range of 76.75 % - 89.36 % and microspheres of formulations (F1, F2, F3, F4, F6, and F7) have shown good mucoadhesive property. F3 had shown significant hypoglycaemic effect upto period from 5 hrs to 19 hrs, whereas pure Nateglinide showed the reduction of 39.85% after a period of 3hrs and reached normal with in 6.5hrs.

Keywords: Sustained Release, Nateglinide, Spray Drying, Mucoadhesive Polymers

ABSTRACT

Wounds are the result of injuries to the skin that disrupt the other soft tissue. Healing of a wound is a complex and protracted process of tissue repair and remodeling in response to injury. Various plant products have been used in treatment of wounds over the years. Wound healing herbal extracts promote blood clotting, fight infection, and accelerate the healing of wounds. Phytoconstituents derived from plants and identified and screened for antimicrobial activity, and the ratio was selected for the preparation of ointment. The in vitro assays are useful, quick, and relatively inexpensive. The wound healing efficacies of various herbal extracts have been evaluated in CAM assay in in-vitro model. CAM  was used to assess the angiogenic activity of polyherbal formulation. Angiogenesis plays an important role in wound healing and newly formed blood vessels comprise 60% of the repair tissue. Neovascularization helps hypoxic wounds to attain the normoxic conditions.  The CAM assay was done in prepared Polyherbal formulation , control and standard. As shown in the figure below the Prepared polyherbal formulation possess the good growth of blood vessels as compared to control and standard. This observation indicates that the developed veterinary polyherbal formulation has good angiogenic property. Improved angiogenesis, therefore, would be contributing significantly to wound healing activity of polyherbal formulation.

Keywords: CAM, Polyherbal formulation

ABSTRACT

This  study was  focused over  the  designing  of sustained  release  HPMC  K100M  micropellet dosage form for  Ibuprofen which is an anti-inflammatory agent and broadly used for treating mild and severe pains. The approach of this study was to make a comparative evaluation among polymers  &  excipients  and  to  assess  the  effect  of  physicochemical  nature  of  the  active ingredients on the drug release profile. The prototype micropellets were obtained using drum pelletizer at 300 rpm. Percentage of water in binding liquid, i.e. IPA, is varied from 95 to 99% and  the effect  over  various parameters,  such as  particle size,  entrapment,  bulk  density and particle  shape,  were observed. Concerning the results of prototype preparation of Ibuprofen micropellets  were  prepared  using  HPMC  K100M,  as  release  retardant,  in  three  different concentrations i.e. 16.7%, 33.3% & 50%. Formulated micropellets showed particle size in the range of 275-284µm, bulk density (0.74-0.82 g/ml), % yield (25.9 -58.3%) & % entrapment (32.8-34.3%). Formulations showed the   maximum   desirability 0.996. Dry suspension formulation  parameters  such  as  pH  (5.15),  Viscosity  (450  cps),  Redispersibility  (5)  & Sedimentation volume (0.46 ml), was  found in  range. Formulation           PIH   were selected as the best   optimized  formulation  and  evaluated  for  In-vivo  parameters,  results  inferred  good sustainability with p>0.0001. Formulated micropellet showed sustained in-vitro dissolution rate, due to optimized polymer concentration. The micropellets were stable at 40°C±2°C/75%±5% RH as per ICH guidelines, after 3 months.

Keywords: Ibuprofen, micropellets, factorial design, HPMC K100M, pelletizer, NDDS