The present investigation reports the formulation of resealed erythrocytes (RBCs) as carriers for the anticancer agent, 5-fluorouracil (5-FU). The preswell dilution technique was adopted for loading and various formulation conditions like preswelling point, drug concentration, time of contact, point of lysis, resealing point, incubation period and cross linking conditions were optimized. Nearly spherical RBCs with 6.9±1.014 pm size, 88% cell recovery and 43.84±1.54% drug loading were obtained after optimizat1on. The 5-FU loaded RBCs were evaluated with respect to osmotic fragility, turbulence shock studies, osmotic shock studies, In vitro 5-FU and hemoglobin (Hb) leaching. It was concluded that the loading procedure had reduced the resistance of the RBCs to osmotic and turbulence shock but the cell shape and integrity remain unaffected. Due to cross linking, stress resistance was improved and 5-FU and Hb leaching during storage were reduced. In vivo studies in healthy rats after i.v. administration of loaded RBCs showed a significant 5-FU accumulation in spleen and lungs as compared to that from plain 5-FU solution. These findings point to the potential utility of resealed RBCs as site specific carriers for improving therapy of 5-FU, especially in tumors of lungs.

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Aspirin is known to be effective in primary and secondary prevention of myocardial infarction. For this purpose aspirin release should be such that It prevents platelet thromboxane (TXA2) generation without Interfering with vascular prostacyclin (PGI2) production. Hence controlled release tablets were prepared to meet the requirements. Both In vitro dissolution and In vivo urinary excretion studies were done to ensure the effectiveness of the formulations. The study proves the usefulness of Carbopol resins for formulating aspirin tablets for minimum risk and maximum therapeutic benefit to the patient.

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Solid dispersions of meloxicam (MX) in polyvinyl pyrrolidone (PVP), hydroxy propyl methyl cellulose (HPMC), hydroxy propyl cellulose (HPC) and polyethylene glycol 6000 (PEG) and solvent deposited systems on lactose, soluble starch, microcrystalline cellulose (MCC), dicalcium phosphate (DCP), silica gel and their selected tablet formulations were investigated with an objective of enhancing the dissolution rate of MX. A marked enhancement in the dissolution rate and dissolution efficiency of MX was observed with all solid dispersions and solvent deposited systems. Among the carriers used in solid dispersions PVP gave highest enhancement (19 fold) in the dissolution rate of MX at 9:1 ratio of drug and carrier and in the case of solvent deposited systems MCC and DCP gave an improvement of 13.1 and 17.5 fold in the dissolution rate of MX respectively at 1:2 ratio of drug and excipient when compared to MX itself. The solid dispersions in PVP and HPMC and the solvent deposited systems on MCC and DCP could be formulated into tablets. These tablets, apart from fulfilling the official and other specifications, exhibited higher rates of dissolution and dissolution efficiency values.

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The essential oil from the leaves of Feronia elephantum correa (Syn. Feronia limonea(L.) Swingle, family Rutaceae), rich in methyl chavicol, has been studied for its antibacterial and antifungal activity against ten bacteria and ten fungi using filter paper disc agar diffusion technique. The oil exhibited strong to moderate activity against most of the test organisms. Bacillus subtilis, Escherchia coli, Proteus vulgaris, Pseudomonas aeruginosa, Shigella sp., Aspergillus niger, Rhizopus nodosus, Trichophyton rubrum 5Sand Trichoderma viride had remarkable susceptibility to the oil.

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Formulation of ayurvedic powder preparations into tablets may increase dosage uniformity. Application of direct compression method to ayurvedic preparations can be regarded as a major advance. In the present study, dispersible tablets of panchagni lavana were prepared by direct compression method. Panchagni lavana was subjected to preformulation studies to test the suitability of direct compression method and appropriate formulations were developed. These formulations were further evaluated for hardness, friability, weight variation, uniformity of dispersion, disintegration test and stability studies. Attempts were made to get minimum possible disintegration time by varying the concentrations of sodium starch glycolate and starch. It was found that, use of mixture of both the disintegrating agents was highly useful in the formulation of dispersible tablets of panchagni lavana. The study further revealed the usefulness of direct compression method to formulate dispersible tablets of ayurvedic preparations.

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The particulate form of albumin has been regarded as a potential carrier of drugs for either site-specific localization or their local application into autonomically discrete sites. Various formulations of metronidazole loaded albumin microspheres were prepared by heat stabilization process and chemical stabilization process. Effect of stirring rate on size distribution, effect of albumin concentration, effect of cross linking agent on microspheres were the parameters investigated Angle of repose, drug content, in vitro and in vivo release rate studies were also carried out. In vitro release profile for formulations containing metronidazole-loaded albumin microspheres with cross linking agent shows slow sustained release up to 24 h.lt also obeys first order kinetics. The studies conducted in rabbits confirm sustained release. Hence albumin microspheres prepared by the heat stabilization process and chemical stabilization process could be used for the treatment of hepatic amoebiasis where the sustained action is needed.

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The cardioprotective effect of Abana, a polyherbal formulation on serum lipid and lipoprotein profile in isoproterenol-induced myocardial Infarction was studied in rats. The levels of total cholesterol, ester cholesterol, free cholesterol, phospholipid, triglycerides, low density lipoprotein (LDL), very low density lipoprotein (VLDL) and free fatty acids Increased significantly while high density lipoprotein (HDL) was decreased in the serum of isoproterenol administered rats. Polyherbal formulation Abana, showed marked reversal of these metabolic changes Induced by isoproterenol.

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Bioequivalence studies are performed to demonstrate that two pharmaceutically equivalent products are equal in rate and extent of absorption in vivo. Following on from developments in the pharmaceutical industry and government mandates in the 1970's and 1980's and since the early 1990's, average bioequivalence has served as the international standard for demonstrating that two formulations of drug product will provide the same therapeutic benefit and safety profile when used in the marketplace. Population (PBE) and Individual (IBE) bioequivalence has been the subject of Intense international debate since methods for their assessment were proposed in the late 1980's. Guidance has been proposed by the Food and Drug Administration of the United States government for the implementation of these techniques in the pioneer and generic pharmaceutical industries. Implementation of these techniques may follow a data collection period to evaluate the operating characteristics, efficiency, and metrics involved in PBE and IBE assessment. The history of bioequivalence will be described, and various techniques and study designs for in vivo bioequivalence assessment will be provided. Part One of this series will develop the ideas behind bioequivalence and discuss development of average bioequivalence. Part Two of this series will describe the implementation of average bioequivalence in industry and the development of population and individual bioequivalence.

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Two simple and sensitive spectrophotometric methods (A and B) In the visible region have beer1 developed for the determination of cefotaxime sodium (CFTS) in bulk and in dosage forms. Method A is based on the reaction of CFTS with nitrous acid under alkaline conditions to form a stable violet colored chromogen with absorption maximum of 560 nm and method B is based on the reaction of CFTS with 1,10-phenanthroline and ferric chloride to form a red colored Chromogen with the absorption maximum of 520mm.The color obeyed Beer's law in the concentration range of 100-500 μg/ml for method A and 1.6-16 μg/ml for method B, respectively. When pharmaceutical preparations containing CFTS were analysed, the results obtained by the proposed methods are in good agreement with the labeled amounts and are comparable with the results obtained using a UV spectrophotometric method.

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A simple and accurate method for the Simultaneous estimation of losartan potassium (LP) and hydrochlorthiazide (HZ) has been developed-The method employs simultaneous equations to estimate these drugs. In methanol, losartan potassium and hydrochlorthiazide showed maximum absorbance at 236 and 270 nm respectively. Losartan potassium and hydrochlorthiazide obeyed Beer Lambert's law in the concentration range from 2-20μg/ml and 1-50μg/ml, respectively. The results of analysis have been validated statistically and by recovery studies.

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A sulphydryl plant protease obtained from the latex of Ficus hispida Linn was purified by chromatography on Sephadex g-200 upto 36-fold with a yield of 5.22% after initial purification by DEAE-cellulose chromatography. Molecular weight of the protease was estimated by Sephadex G-100 gel filtration and found to be around 23,700 daltons. The Michaelis constant (Km) with substrates haemoglobin and N-α-benzoyl-DL-arginine-p nitroanllide (BAPNA) was 1.25 mM and 0.83 mM, respectively. The activating and inhibiting effect of some chemical agents on the protease activity of the enzyme was also studied.

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The in vitro Antimicrobial activity of a new guggul preparation has been investigated against Staphylococcus aureus, Staphylococcus epidermidis, Pseudomonas aeruginosa, Proteus vulgaris, Alcaligenes faecalis, Serratia marcesens, Escherichia coli, Micrococcus glutamicus, Bacillus thermodenitrificans, Bacillus subtilis, Bacillus pumilus. The preparation containing a 5:10 proportion of guggul and coconut oil showed more antimicrobial activity than other preparations. Guggul and coconut oil when tested alone failed to show any antimicrobial activity.

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A simple and sensitive spectrophotometric method for the determination of terazosin in pure and dosage forms is proposed. The drug forms a stable green chromogen with ferric chloride and potassium ferricyanide, exhibiting maximum absorption at 740 nm. The chromogen obeys Beer - Lambert's law in the concentration range of 1-1 0 μg/ml.

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In search of new potent NSAIDs, It was considered of interest to investigate a 3D QSAR analysis of some antiinflammatory 3,5-di-tert-butyl-4-hydroxystyrene derivatives. To investigate relationship molecular shape analysis has been used as a 3D QSAR formalism. Molecular modelling software Cerius2 was used to study 3D QSAR. The analysis resulted In the following 3D QSAR equation which can be used for prediction of antiinflammatory activity of new molecules. log (BA) = 0.827(0.283) Fo + 0.007 (0.002) Energy - 0.489(0.156) ROG - 0.114(0.038) DIPOLE + 3.756 n=17 r2=0.762 r=0.873 f=9.604 s=0.197 press=0.921 cvr2=0.622 bsr2=0.764

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The fatty acid composition of lipid constituents of seventeen species of marine sponges from the Orissa coast have been studied by GLC. Most abundant are saturated fatty acids. Among the unsaturated acids, oleic acid occurs in 40% of the species investigated. Six polyunsaturated fatty acids were noted in different species. Docosahexaenoic acid (ω3 PUFA) is present in two species in large quantities. The sponges, Plakina monolopha and Callyspongiasp. which have shown antimicrobial activity are found to have >80% oleic acid.

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The possible role of skin cholesterol in modifying the percutaneous permeation of indomethacin was studied by employing lovastatin, an inhibitor of cholesterol synthesis. The decreased cholesterol content of solvent perturbed skin was maintained till 24 h by topical application of lovastatin (1.125 mg/cm2). Solvent perturbed-lovastatin treated viable skin excised after 24 h produced enhanced in vitro permeation of indomethacin. The time for 75% reduction in edema was significantly less in rats with perturbed-lovastatin treated skin as compared to that with normal skin.

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The mechanism of interaction of five phenothiazine derivatives with serum albumin was investigated using fluorescence spectroscopy. It was found that phenothiazine ring common to all drugs makes major contribution to interaction. However, the nature of alkyl amino group at position 10 influences the protein binding significantly. Binding affinities could be related to parachor values of drugs. Fluorescence intensity data in the presence of additives showed that hydrophobic Interactions play a significant role. Stern-Volmer plots indicated the presence of a static component in the quenching mechanism. Results also showed that both tryptophan residues of protein are accessible to drug molecules. The high magnitude of the rate constant of quenching Indicated that the process of energy transfer occurs by intermolecular interaction forces and thus drug binding site is in close proximity to tryptophan residues of BSA.

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Hydrotropically gelled maize starch (HTGS) was investigated as granulating agent for preparing tablets of diclofenac sodium. Granular and tablet properties were determined and compared with those obtained using conventionally prepared starch paste (THSP). Both types of granules could be compressed into satisfactory tablets with a mean disintegration times of 13 min 5's and 7 min 42 s, respectively, for HTGS and THSP. However, tablets prepared with HTGS gave faster dissolution (88% in 70 min), whereas the other type gave 77% in the same time in phosphate buffer of pH 7.2. Hydrotropically gelled starch exhibited good stability even after storing for one month where as conventionally prepared starch paste was spoilt within 24 h.

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Aibendazole-chloranilic acid complex In dioxane was analysed spectrophotometrically. The optimum conditions for the complexation were determined. The stoichiometry for the complex was found to be 1:1 through Job's methods of continuous variation. Benesi- Hildebrand equation was used in the determination of the association constant, molar absorptivity and hence free energy for the complex was calculated.

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