Ophthalmic inserts of tetracycline HCI were prepared as membrane permeation controlled devices with the aim of achieving once a day administration. Drug reservoir and rate controlling membrane were prepared using different hydrophilic polymers such as HPMC, MC, PVP (K-30) and hydrophobic ethyl cellulose respectively. The ocular inserts were evaluated for their physico chemical properties, in vitro kinetics, and in vivo release characteristics. Since, the targeted zero order mode of release was observed in formulation F6 (Drug reservoir with 2% HPMC and 4% EC as rate controlling membrane), its in vivo release characteristics were evaluated using rabbits as animal models. Influence of changes in polymer composition of films over physical and in vitro release characteristics were tested using statistical tools such as ANOVA and the Students t-test. The in vitro release kinetic data was treated according to diffusion models proposed by Higuchi and Peppas in order to access the mechanism of drug release.

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The plant Cassia angustifolia vahl has been used in various diseases. The alcoholic extract of the plant was investigated for the hepatoprotective properties against carbon tetrachloride-induced liver damage. Various biochemical parameters were studied to evaluate the hepatoprotective activity of crude extract. In serum, total bilirubin, total protein, glutamate oxaloacetate transaminase (GOT) and glutamate pyruvate transaminase (GPT) were determined. In addition to these glutathione (GSH) and lipid peroxides (LPO) were determined in liver tissue and is supported by histopathological studies of liver before and after the treatment. Results of this study revealed that leaves of Cassia angustifolia could afford a significant protective action in CCl4-induced hepatocellular injury.

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Etodolac (ETO) is a nonsteroidal antiinflammatory drug (NSAID) that exhibits analgesic, antipyretic and antiinflammatory activities and is practically Insoluble in water. The solubility of ETO in four different cosolvents; ethanol, propylene glycol, polyethylene glycol 400, and glycerol, three sugars; sucrose, sorbitol, and mannitol, two hydrotropic salts; sodium benzoate and sodium salicylate, and two enhancers; Tween 80 and Brij 58 was investigated. The solubility of ETO by the used co-solvents can be arranged in the following order: ethanol>PEG 400>PG>gIycerol. Similar increase in solubility was observed with Tween 80 and Brij 58.The increase in temperature from 25 to 37° was accompanied by an increase in drug solubility at higher concentrations of co-solvents and hydrotropic solutions but the effect was insignificant with Tween 80 and Brij 58. The thermodynamic parameters calculated for some of these systems showed positive entropy and enthalpy in addition to negative free energy values suggesting high degree of randomness, endothermic dissolution and spontaneity of the solubility process. The used sugars and sodium salicylate showed no effect on ETO solubility. Based on the solubility data, a trial has been done to propose a formulation (100 mg/3 ml) for parenteral use in an aqueous solvent blend. The proposed formulation was tested physically for color, turbidity and precipitation upon storage for two months. In addition, the formulation didn't show any evidence of visible precipitation upon dilution with normal saline or 5% dextrose intravenous fluid except in low dilutions. Finally, in addition to parenteral formulation, the solubilized systems of ETO could be appreciable in the design of other liquid formulations intended for topical and oral administration of the drug.

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Recent advances in the isolation techniques, medicinal chemistry, biotechnology and the capacity for screening new drug compounds have been able to produce several lead molecules. More than likely many potential drugs have been lost because of inadequate formulation strategies during different stages of evaluation. In many cases, the loss could have been due to solubility problems. To maximize the drug potential of all molecules, there has been a renewed effort to find formulation strategies for compounds inadequately soluble in water. Many different drug delivery systems for lipid-soluble compounds have been suggested, but lipid micro sphere (LM) drug delivery system has great potential. The system is time tested, safe and stable at room temperature, easily mass-produced yet cheaper. The drug distribution and targeting can be achieved by manipulating the size, surface charge and surface legands of LM. At present, commercially available lipid micro sphere formulations are few but in future this system will find considerable share in the market.

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Two UV spectrophotometric methods have been developed for the determination of celecoxib and tizanidine hydrochloride in pure and in its pharmaceutical formulations. Celecoxib having absorption maximum at 251.2 nm in 0.1 N sodium hydroxide, where as tizanidine HCI exhibiting maximum absorption at 228 nm in distilled water.

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The isocratic separation and simultaneous estimation of acetaminophen, pseudoephedrine hydrochloride, guaifenesin and dextromethorphan hydrobromide in bulk and pharmaceutical dosage forms using the technique of packed column supercritical fluid chromatography (pcSFC), has been described. Method development was based on the measurement of retention times as a function of parameters of pressure, temperature and modifier composition. An arbitrary mixture of the 4 drugs was base-line resolved on a Hypersil-Phenyl (250 x 4.6 mm) 5 pm column with a ternary mobile phase of carbon dioxide modified with 14.29% (v/v) methanol containing 1% methylamine. Detection was absorptimetric at 210 nm. The method has been fully validated and a full statistical evaluation included. Application of the method to real-time samples revealed no interferences from excipients. A comparison of the method with an HPLC method for the same assay, which appeared in literature, validated the recent proposition that pcSFC is not only a viable but also a superior alternative to HPLC for pharmaceutical analysis.

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To study the antiinflammatory activity of Elephantopus scaber in acute, sub-acute and chronic experimental models in albino rats, aerial parts of Elephantopus scaber were extracted with hydroalcoholic solvent and purified by chromatographic procedure. The compound separated was studied by carrageenan-induced hind paw oedema in rats and the paw volume was measured plethysmometrically at 0 and 3 h after injection. The compound was also subjected to turpentine oil induced granuloma pouch in rats. The pouch was opened on day 7 under anaesthesia and the exudates collected by a syringe was measured the compound was also investigated in formalin-induced oedema models in rats. Degree of inflammation was measured plethysmometrically on day 1 and 7 and compared with control and standard, diclofenac. All the drugs were administered orally. The higher dose of compound significantly reduced carrageenan-induced pedal oedema (57%) and formalin-induced pedal oedema in rats (58%). The compound also decreased exudate volume (36%) in turpentine oil-induced granuloma formation compared to control.

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A gel forming polysaccharide gum obtained from the pods of Abelmoschus esculentus was employed as a mini matrix in a new sustained release tablet formulations of furosemide (a diretic) and diclofenac sodium (a non steroidal anti inflammatory agent). Sustained release performance of the formulations was compared with formulations containing sodium carboxymethylcellulose (NaCMC, 500 mPa) in similar experimental conditions. Abelmoschus esculentus gum was as good as NaCMC in prolonging the release of furosemide and diclofenac sodium from the compressed tablets-Times for 50% (t50%) and 75% (t75%) indicated relatively faster release of furosernide in simulated intestinal fluid (SIF). Similar trends are observed in the case of diclofenac sodium. A reduction in the solubility of diclofenac sodium was observed and this was caused by the presence of sodium and potassium in SIF. These new formulations which utilize a plant hydrogel as mini matrix offer the advantage of simplicity and economy.

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Ketorolac tromethamine loaded poly (lactic acid) microspheres with different polymer composition were prepared by phase separation co-acervation induced by non-solvent addition method. The morphology of microspheres was analysed by scanning electron microscopy. The particle size distribution, studied by optical mlcroscopy, showed that particles are of uniform size. In vitro drug release profiles of these microspheres were studied using pH 7.4 phosphate buffer. The release kinetics of ketorolac tromethamine from the microspheres was evaluated by fitting the release data to the zero order, first order, Higuchi and Korsemeyer-Peppas equations. All microspheres showed initial burst release, followed by fickian diffusion of drug through microspheres. The stability of the formulations was found to be two years.

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Aqueous and ethanol extracts from the root of Momordica dioica Roxb. (Cucurbitaceae) were tested for postcoital antifertility activity in female rats. Both the extracts were found to be most effective in causing significant abortifacient activity. The extracts showed moderate estrogenic activity. Histological studies of the uterus were carried out to confirm estrogenic activity.

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Antitubercular Fixed Dose Combinations (FDCs) containing rifampicin (RIF) along with Isoniazid (INH), And/or pyrazinamide (PZ) and/or ethambutol (ETB) ensure better patient compliance and help to minimize development of resistance to the drugs by M. tuberculosis. However, poor bioavailability of RIF In these FDC formulations is a subject of much concern for the last three decades. Poor bioavailability of RIF could lead to faulty treatment and to the drug resistance. WHO and IUATLD have now sounded a caution that antitubercular FDC formulations should be used only if the bioavailability of RIF has been demonstrated convincingly. It has been suggested that probable physical factors responsible for the variable bioavailability of RIF include particle size, crystalline nature, nature of excipients and lack of GMP. However, nine of these explanations are found to be satisfactory. During the last few years, sufficient data has been generated, independently, in two Indian research laboratories, indicating that in the acidic medium of the stomach, RIF degrades to form an insoluble and inactive 3-formyl rifamycin SV, an aldehyde, involving a distinct catalytic role of INH. An elegant reaction mechanism has been proposed for the impaired bioavailability of RIF from FDC formulations containing INH. With a better understanding of the interaction of RIF and INH in the acidic medium, it should now be possible to formulate a stable FDC with acceptable and reproducible bioavailability of RIF.

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The systemic absorption of propranolol hydrochloride (PHL) delivered through rabbit oral mucosa was studied. Drug-loaded buccoadhesive films of varying compositions with unidirectional drug release were applied to rabbit oral mucosa and inhibition of isoprenaline-induced tachycardia was achieved. In vitro drug release followed zero-order kinetics. The ex vivo mucoadhesivity tests using rabbit small intestinal mucosa on an in-house fabricated apparatus yielded correlation between film composition and rnucoadhesivity. Selected batches of placebo films showing good bioadhesion and oral mucosal compatibility in human volunteers could form a basis of propronalol delivery through this route to avoid first pass metabolism.

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Microencapsulation by ethylene vinyl acetate copolymer (EVA) and the resulting microcapsules were investigated. EVA microcapsules of indomethacin were prepared by an emulsion solvent evaporation method employing various proportions of coat and core materials and chloroform as solvent for the polymer EVA. The microcapsules are spherical, discrete and free flowing. Microencap-sulation efficiency was in the range of 87-99% lndomethacin release from the microcapsules was slow and extended over more than 12 h and depended on coat: core ratio, wall thickness and size of the microcapsules. Drug release was diffusion controlled and followed first order kinetics. Good linear relationships were observed between wall thickness and release rate and T50 (time for 50% release) values. Some microcapsules fulfilled the official (USP XXIII) dissolution rate test specification of indomethacin extended release capsules. Differential scanning calorimetry (DSC) indicated no Interaction between the coat polymer (EVA) and the core (indomethacin).

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A series of antiinflammatory 4,5-diarylpyrroles was subjected to quantitative structure activity relationship analysis. The effect of structural modification in 4,5-diarylpyrroles on their COX-2 inhibition potential was analysed by quantitative structure activity relation (QSAR) analysis using the software Cerius2 3.5. Special emphasis was laid on various electronic, spatial and thermodynamic descriptors at the minimum energy conformation. Out of several electronic, spatial and thermodynamic descriptors investigated on the COX-2 inhibitory potential of substituted 4,5-diarylpyrroles, PMI, ROG and MR showed appreciable correlation with COX-2 inhibitory potential. These investigations will further help in rationalizing the design of new molecules.

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The objective of the present study is to develop an instrumental method, which is more accurate than the physical method that is followed in Indian Pharmacopoeia. A simple and sensitive spectrophotometric method has been developed for the estimation of iron as an impurity in pharmaceutical raw materials. In this method wine red color complex formed between iron and 1-3-diphenyl-4-carboethoxy pyrazole-5-one (DPCP) was measured at 525 nm. Beer's law was found to obey in the concentration range 0.5-10 μg/ml. Sandell's sensitivity and standard deviations were found to be 0.0483 μg/cm2 and±0.035 respectively.

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A drug utilisation evaluation of ranitidine was conducted in a 300-bed government hospital. Baseline audit was done in selected wards of the hospital over 30 days, which identified 228 patients receiving ranitidine. The main reasons for prescribing ranitidine were prophylaxis against non-steroidal antiinflammatory drugs (21%) and pain in the epigastrium (16%). In 20% of the cases, the reason for prescribing ranitidine was unknown. A questionnaire on ranitidine usage was developed and the responses from all the doctors of the hospital were obtained. Guidelines for ranitidine usage in the hospital were framed and officially circulated among doctors in the hospital. Another 30-day audit was carried out in the same wards where baseline audit was performed, during which 145 in-patients were identified to be taking ranitidine. Prophylactic use of non-steroidal antiinflammatory drugs decreased to 13% and only in 10% of the cases reason for prescribing ranitidine was unknown. More than 30% reduction of overall in-patient ranitidine usage was noticed during the study period compared to a similar period from the previous year. The program brought about rational changes in ranitidine prescribing and awareness among doctors regarding cost-effective usage of drugs.

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This paper deals with the development of a mathematical model to predict the baseline enantioseparation and to customize chiral HPLC analysis using factorial experimental design. An attempt is made to establish quantitative relationship between chromatographic separation variables and the response factor (resolution). The significance of the chromatographic factors and adequacy of the model developed was checked using F-test and coefficient of determination (R2) respectively. The trends of important effects of chromatographic factors on chiral resolution have been presented in graphical form. The study suggests that factorial design is a potential tool to customize chiral HPLC analysis.

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Chemical examination of the whole plant of Swertia alternifolia yielded four xanthones, 2,8-dihydroxy- 1,6-dimethoxyxanthone, 1,8-dihydroxy-3, 5d-i methoxyxanthone, 1,2,6,8-tetrahydroxyxanthone and 1,5,8 trihydroxy-3-methoxyxanthone. These compounds were characterlsed by chemical and spectral methods. These compounds were Isolated for the first time from this plant.

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Antimicrobial resistance is a serious global issue. Since only empirical therapy with antibiotics is widely followed in India, it is helpful that the treating doctors haw information on the prevalence of microbial resistance to the commonly prescribed antibiotics for various infections. A study of the prevalence of antimicrobial resistance among respiratory tract isolates was conducted in a secondary care Government hospital in Tamil Nadu in order to gauge the existing level of antimicrobial resistance. Out of 154 isolates obtained, 138 possessed seven types of pathogenic microorganisms. This study has revealed that there exists a high level of resistance to penicillins like ampicillin, methicillin and cloxacillin and the first generation cephalosporin, cephalexin. Third generation cephalosporins, ceftriaxzone and ceftazidime, were effective against the organisms isolated.

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Association constants for the binding of six drugs to serum albumin have been studied in the absence and presence of paracetamol using ultraviolet absorption spectroscopic technique. Paracetamol is found to influence the binding behaviour of other drugs by non-competitive interference involving structural changes in the albumin molecule. Significant increase in the concentration of free drug has been observed for metronidazole and promethazine hydrochloride in the presence of paracetamol. Ratio of association constants in the presence and absence of paracetamol can be used as a guide to the modified design of dosage forms in the presence of paracetamol.

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EPZ10, a supported reagent catalyst, offers an environmentally benign and a commercially viable alternative to the conventional Friedel-Crafts catalyst, anhydrous AICI3. Aluminium chloride is mainly associated with unacceptable levels of waste and by-products. With EPZ10, the aqueous effluent from quenching is eliminated and acidic gaseous emissions are limited to those produced from the reaction mixture itself. It can be filtered off from the process, and may be reused, depending on the reaction type and temperature. It is also reported to give higher yields as compared to the corresponding reactions using AICI3. In this article, synthesis of three alkylbenzenes using EPZ10 as the catalyst is discussed.

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