More than 90% of drugs approved since 1995 have poor solubility. Also More than 40% NCEs (new chemical entities) developed in pharmaceutical industry are practically insoluble in water, The solubility and dissolution properties of drugs play an important role in the process of formulation development hence Solubility is a major challenge for formulation scientist. 1,2,3 The important aspect which may greatly affect the performance of the drug is solubility. This is an important physico -chemical property of drug, especially aqueous solubility. To exert better therapeutic efficacy or better bio-availability, the drug must be in solution state and to have drug in the solution state, it must have high dissolution rate and high solubility. Thus the bioavailability of poorly water soluble drug is often limited to its dissolution rate. A drug with poor aqueous solubility will typically exhibit dissolution rate limited absorption. Several methods have been introduced to overcome this problem.
The main objective of the present study was to enhance the solubility and dissolution rate of poorly water soluble aceclofenac using its solid dispersion with β-cyclodextrin. FTIR and DSC study was carried out to find out any incompatibility. The phase solubility of drug was carried out in 1, 2, 5, and 10% of β-cyclodextrin in distilled water. Kneading method and solvent evaporation method was use to prepared solid dispersion of aceclofenac and β-cyclodextrin. Different evaluation tests like solubility study in different solvents, PXRD and in vitro dissolution study of aceclofenac- β-cyclodextrin inclusion complex were carried out. The overall finding indicated that β-cyclodextrin is a desirable water soluble carrier, that helps in increasing solubility of drug. Due to its structural feature, β-cyclodextrin forms a good inclusion complex that decreases contact angle of drug with water molecules by increasing wetting properties. Hence, it can be concluded that, β-cyclodextrin is better water soluble carrier molecule in terms of its compatibility and increasing solubility behavior of poorly water soluble drug aceclofenac.
The present study aimed to study the protective effect of alpha- Asarone in CCL4-induced hepatotoxicity in experimental rats. The rats were randomly divided into 5 groups each containing six rats. CCL4 was given at a dosage of 0.5 mL/kg to produce hepatotoxicity, and serum AST, ALT, total bilirubin, and albumin, as well as hepatic hydroxyproline (HP), reduced glutathione (GSH), and malondialdehyde (MDA), cytokines, and NO, were assessed. CCL4 treatment resulted in a decrease in body weight and an increase in liver weight in rats, while treatment with α- Asarone resulted in normal body and liver weight. Serum AST, ALT, total bilirubin, HP, GSH, MDA, and cytokines were increased in CCL4 treated rats. α- Asarone-treated rats showed a reduction in oxidative stress as well as inhibited the release of cytokines in dose dependent manner and showed protection against hepatotoxicity. From the study, we conclude that, α- Asarone has a protective effect against the hepatotoxicity induced by CCL4. Keywords: CCL4; Hepatotoxicity; ALT; oxidative stress; α- Asarone; Cytokine.
The present paper describes simple and sensitive, reversed phase high performance liquid chromatography (RP-HPLC) method developed for the determination of tapentadol hydrochloride in bulk and in its tablet dosage form. Chromatographic separation was achieved by using phenomenex C18 column, 250×4.6 mm, 5 μm as stationary phase. Mixture of acetonitrile: water (80:20 V/V) was used as the mobile phase and the pH was adjusted into 7.0 using orthophosphoric acid, at a flow rate of 0.7 mL/ min. Tapentadol standard shows maximum absorption in UV at 272 nm. The method was linear over the concentration range of 5-25 μg/mL. The method was validated statistically and recovery study was performed as per ICH guidelines. The analytical recovery obtained was 98-119%. As per validation data it was found that method is specific, robust and precise within the described concentration range. The described RP-HPLC method was successfully employed for the analysis of a commercial brand of tapentadol hydrochloride tablets.
Present study was aimed to investigate the protective of Spermacoce hispida in Cisplatin induced nephrotoxicity using in vivo model. S. hispida was collected and extract of plant was prepared in different solvents and prepared extracts was used for phytochemical scrrening. Nephrotoxicity in rats was induced by a single intraperitoneal injection of Cisplatin at a dose of 5 mg/kg. S. hispida extract in different solvent at the dose 100 mg/kg used to find protective activity. Blood urea nitrogen (BUN), serum creatinine, oxidative stress, a proinflammatory cytokine, NO, and histological alteration was measured to estimate the therapeutic ability of S. hispida. BUN, creatinine, and inflammatory cytokine levels in rats were increased by Cisplatin but decreased by S. hispida treatment for 14 days. Besides, S. hispida treatment decreased oxidative stress and nitric oxide in Cisplatin-treated rats. Cisplatin treated rats shows altered structure of kidney tissue; meanwhile S. hispida normalizes the structure of kidney tissue. From this study, we conclude that S. hispida has nephroprotective activity by inhibiting the oxidative stress and NO production in rats from nephrotoxicity. Keywords: Spermacoce hispida; Cisplatin; oxidative stress; Cytokine; Nitric oxide.
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