Posted by admin on Nov 30, 2019 in |
In the present research, newly developed hydrotropic solid dispersion technique utilizing the use of aqueous solvent was developed, to avoid the utilization of organic solvent and all together declining their toxicity. This technology was employ intended for preparing the dispersion of Eluxadoline by using new hydrotropic agent sodium caprylate with using different ratio. Prepared formulations were evaluated by Solubility study, Fourier transforms infrared spectroscopy, X-Ray Diffractometry, Drug content analysis, and in-vitro drug release study. Based on the evaluation of hydrotropic solid dispersion concluded that the concept or technology of hydrotropic solid dispersion method is a novel, nontoxic and as well cost-effective technique for the rationale of enhancing the aqueous solubility of substance and bioavailability of poorly water-soluble drugs. The improvement within solubility and dissolution of Eluxadoline is a clear sign. It can be able to use in the future for more poorly water-soluble drugs to enhance solubility and also which having low bioavailability is a major...
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Posted by admin on Nov 30, 2019 in |
Allium cepa L. has known potent antidiabetic effects due to several of its constituents, including kaempferol -3-O-β-D-6”-(p-coumaroyl) glucopyranoside (kaempferol). This preliminary work was aimed at preparing oral hard gelatin capsules of kaempferol obtained from Allium cepa L. In order to obtain more potent hypoglycemic activities, lower side effects with good patient compliance over the crude extract kaempferol were isolated from Allium cepa L. and formulated into capsule dosage form. The capsules were prepared by filling hard gelatin capsule shells with blends of kaempferol with excipients which included Avicel® PH102, agglomerated lactose®, Primogel®, Ac-Di-Sol®, maize starch, stearic acid, and talc. The blends were evaluated for their micrometric properties such as bulk densities, tapped densities, Hausner’s quotients, compressibility indices, true densities, flow rate and angle of repose. Prepared capsules were evaluated for weight variation, disintegration time, content uniformity, dissolution profiles and antidiabetic properties in alloxan-induced diabetic rats with distilled water and glibenclamide respectively as negative and positive controls. The capsules were of good properties with disintegration time (2.75 ± 0.22 –...
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Posted by admin on Nov 30, 2019 in |
Purpose: Helicobacter pylori (H-pylori) infection has been commonly associated with gastric ulcers. Lepidium sativum (L. Sativum) is an herbaceous edible plant, botanically related to mustard and watercress with remarkable pharmacological features. In this study, we investigate the anti-microbial and anti-oxidant effect of L. sativum seed methanolic extract in-vitro and correlate this with the gastroprotective potential of this extract against H-pylori–induced gastric ulcer in an in-vivo model. Methods: L. sativum extract was quantified for phenolic compounds using high-performance liquid chromatography, and the anti-microbial and anti-oxidant activities of the extract were evaluated in-vitro. Furthermore, an in-vivo rat model was assessed in order to explore the effect of L. sativum extract against H. pylori-induced gastric ulcer in-vitro. Results: The L. sativum extract exhibited significant antioxidant and anti-microbial activities against different pathogenic organisms. In vivo, L. sativum extract reduced the ulcer index, increased the percentage of ulcer inhibition, halted lipid peroxide and triggered anti-oxidant markers. Moreover, it suppressed inflammatory and apoptotic markers. The histopathological results for L. sativum treated rats showed the amelioration...
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Posted by admin on Nov 30, 2019 in |
A simple, accurate and precise UPLC method was developed and validated for dissolution testing of Lamivudine, Tenofovir disoproxil fumarate and Efavirenz in tablet dosage form. The separation was achieved under optimized chromatographic condition on an Acquity UPLC BEH (50 mm × 2.1 mm, 1.7 μm) column with mobile phase consist of 20 mM potassium dihydrogen phosphate buffer pH 2.5: acetonitrile with gradient elution at a flow rate of 0.37 mL/min using 35 °C column oven temperature with UV detection at 260 nm. The method was validated as per ICH and USP guideline and the values were found to be within the limits. So, the proposed method was found to be simple, linear, accurate, precise, robust and...
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Posted by admin on Nov 30, 2019 in |
A new series of hydroxamic (5a-5j) and carboxylic acid analogs (4a-4j) based on the 1, 3, 4-thiadiazole scaffold was designed and synthesized to explore its potential as new antitumor agents. The chemical structures of the compounds were confirmed based on TLC, IR, 1H NMR, and 13C NMR analysis. Molecular docking studies showed that the target compounds correctly dock into the binding pocket of histone deacetylase inhibitor (PDB Code 1w22 reference compound), while their bioavailability / drug-likeness was predicted to be acceptable. The predicted physicochemical were compared with those of a reference compound. Biological results revealed that the structural modifications proposed significantly affected inhibitory potency as well as selectivity for HDAC inhibitors. Most target compounds were significantly more active specifically 5a, 5b, 5e with IC50 values in the low micromolar or, the most active compounds in the series. Selected compounds were tested on the viability of MDA-MB-231 (breast cancer cell) and K562 (chronic myelogenous leukemia cell), A549 (human lung cancer), PC3 (Prostate cancer cell lines) using MTT...
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