The objective of this study was to develop a novel implant containing risperidone intended for long-term treatment in Schizophrenia utilizing in vitro in vivo correlation (IVIVC) studies. Different implants (F1-F8) containing an antipsychotic drug, risperidone, were prepared using a hot melt extrusion technique by taking polycaprolactones of different molecular weights (Mwt. 15000, 45000, 80000) either alone or as their blends, and PLGA (75:25). The implants contained 40% of the drug. After fabrication, the implants were characterized for various in vitro properties such as drug release and physical strength. Prior to conducting drug release studies, optimum drug release method was developed based on IVIVC studies. An optimized formulation based on drug release and physical strength at the end of fabrication was selected from the various implants fabricated. The bioactivity, reversibility, and IVIVC of optimized formulation were determined using pharmacokinetic studies in rats. Short-term stability studies were conducted with optimized formulation. Drug release depended on polymer molecular weight. Implant fabricated using 50:50 polycaprolactone 45,000 and polycaprolactone 80,000 was considered optimized implant. Optimized formulation selected released the drug for 3-months in vitro and was physically rigid. The optimized implant was able to release the drug in vivo for a period of 3 months, the implants are reversible throughout the delivery interval and, a 100% IVIVC was achieved with optimized implant, suggesting the development of 3-month drug-releasing implant for risperidone. The optimized implant was stable for 6 months at room temperature (25°C) and 45°C. A novel implant for risperidone was successfully prepared and evaluated.

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Diabetes is associated with complications like neuropathy, nephropathy, cardiomyopathy, and retinopathy due to increased oxidative stress and serum lipids. In the present study, rosuvastatin, a HMG-CoA inhibitor, was investigated for its protective effect in neuropathy, nephropathy, and cardiomyopathy based on the lipid-lowering property along with its pleiotropic effects such as improved blood flow to the organ and antioxidant defense. Type 2 diabetes was induced in Wistar rats by single i.p. administration of streptozotocin (50 mg/kg). These diabetic rats were treated with daily doses of rosuvastatin (10 mg/kg) alone, metformin (120 mg/kg) and glimepiride (1 mg/kg) and rosuvastatin in combination with metformin (120 mg/kg) and glimepiride (1 mg/kg) for a period of 6 weeks. The biochemical parameters involved in neuropathy, renopathy, and cardiopathy were estimated. Treatment resulted in significant (P < 0.05) decrease in thiobarbituric acid reactive substances (TBARS) and increase in levels of glutathione peroxidise and catalase in brain and kidney homogenates. Significant (P < 0.05) increase in high-density lipoproteins and decrease in creatinine kinase, triglycerides, total serum cholesterol represents the cardioprotective action, whereas significant (P < 0.05) increase in the latency in the hotplate model shows the neuroprotective activity, and significant (P < 0.05) decrease in blood urea nitrogen, creatinine levels and increase in serum total protein levels suggested the renoprotective actions. The unique properties of rosuvastatin such as antioxidant defense and lipid-lowering nature might have resulted in cardio, neuro, and renoprotective activity in type 2 diabetic rats treated with metformin and glimepiride.

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Fumaria parviflora Lam. (Fumariaceae) is an annual herb found throughout the world. Traditionally it has great significance in various disorders. In folk medicine of Turkey it is used against hepato-biliary dysfunction and imported from Iran. In Charaka and Sushruta, it is recommended for treatment of fevers, blood disorders, chronic skin diseases, urinary diseases and cough. The compounds were isolated from methanolic extract of the plants by column chromatography using silica gel (60-120 mesh) as stationary phase and structure of the isolated compounds have been established on the basis of spectral data analysis and chemical reactions. Phytochemical investigation of its aerial parts led to the isolation of five new compounds characterized as (5αH,11αH)-8-oxo-homoiridolide (1), n-docosanyl-2-O-β-D-glucopyranosyl salicylate (2), 2-methyl-6-hydroxymethylenedodecan-10-oyl-12, 15-olide14-O-β-D-xylopyranoside (3), 4-oxo-stigmast-5-en-3β-ol-D-glucopyranoside (4) and salicylic acid-O-β-D-xylopyranoside (5) along with the known compounds α-D-glucopyranosyl hexadecanoate (6) and α-D-glucopyranosyl- (2 → 1ʹ)-α-D-glucopyranoside (7). The isolated compounds are useful as they will provide essential data and information for the further researchers and development of effective analytical marker for identity, purity and quality control of this traditional plant in future.

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The main aim of the study was designed to develop bioadhesive buccal patches of carvedilol (CR) and evaluate for isoprenaline-induced tachycardia. Buccal patches of carvedilol were prepared by using chitosan (CH), sodium salt of carboxy methyl cellulose (NaCMC), and polyvinyl alcohol (PVA) as mucoadhesive polymers. The solvent evaporation method was used for the preparation of buccal patches. The patches were evaluated for their physical characteristics like patch thickness, weight variation, content uniformity, folding endurance, surface pH, residence time, in vitro drug release, and in vivo pharmacodynamic study. The swelling index of the patches was found to be proportional to the polymer concentration, whereas surface pH of all the formulated bioadhesive patches was found to lie between neutral ranges. In-vitro release study shows that 94.75% drug was release in 8 hours from the patch, which containing 2% w/v chitosan. The folding endurance result shows good elasticity in all the patches.Application of buccal patches on buccal mucosa of rabbit shows a significant result in % inhibition of isoprenaline-induced tachycardia. Prepared buccal patches of chitosan, NaCMC, and PVA containing Carvedilol meet the ideal requirement for the delivery of cardiovascular drugs and inhibit the isoprenaline tachycardia.

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The purpose of this study was to investigate the effect of extraction and application of okra gum as an aqueous film coating agent. Powdered okra pods dispersed in demineralized water was heated at 80 ± 2 ^o C for 30 minutes in the presence of sodium chloride. The filtrate was successively centrifuged at 4000 rpm for 30, 60, or 120 minutes and freeze dried. The samples were used as film former at different concentrations in aqueous film coating operations. Near infrared (nIR) absorption spectra, photomicrographs, and some physicochemical properties of the coated tablets were evaluated. The okra gum samples had different nIR spectra and possessed good processing and application quality due to relatively low viscosity. A six-fold concentration of this gum from the novel extraction yielded glossy theophylline tablets within a short time. A t (18) = 2.895, P < 0.005, t critical = 1.734 were obtained for the independent analysis of the hardness of core and coated theophylline tablets. A 3.0% concentration of the okra samples at a flow rate of 3 ml/min for 100 minutes showed that F = 3.798, DF = 29, P < 0.035, F critical = 3.354 in tablet hardness among samples and F = 15.632, DF = 29, P < 0.0001, F critical = 2.152 were obtained on film thickness among tablet samples during the coating and drying operation. Novel extraction process enhanced the film coating potential of okra gum by delivering more solids on the substrate at a shorter time with improved operation efficiency.

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In the present investigation, the synthesis and antimicrobial evaluation of 1,2,4-triazolo [3,4-b][1,3,4] thiadiazine including different pharmacophores are aimed at. In this study, a series of 6-aryl-3- (3,4 -dialkoxyphenyl)-7H -[1,2,4]triazolo [3,4-b][1,3,4] thiadiazine (7a-7k) was synthesized by condensing 4-amino-5-(3,4-dialkoxyphenyl)-4H-[1,2,4]- triazole-3-thiol (6) with various aromatic carboxylic acids in the presence of phenacyl bromides through one-pot reaction. Eleven fused heterocyclic derivatives were successfully synthesized. The structures of these newly synthesized compounds were characterized by IR, ¹ H NMR and mass spectroscopic studies. All the synthesized compounds were screened for their antimicrobial evaluation. Some of the compounds exhibited promising antimicrobial activity. From the present study it may be concluded that synthesized compounds are fruitful in terms of their structural novelty and marked biological activities. These compounds could be further modified to develop potential and safer antifungal agents.

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