Posted by admin on May 31, 2020 in |
Eplerenone is a poorly soluble drug that belongs to class II biopharmaceutical classification system. It is a selective aldosterone receptor antagonist, which binds to the mineralocorticoid receptor and blocks the binding of aldosterone, thereby decreases the sodium resorption and subsequently increasing water outflow. This leads to a decrease in blood pressure and used in congestive heart failure. The aim of the present study was to improve the solubility, dissolution and permeability properties of Eplerenone by liquisolid compacts, thereby enhancing oral bioavailability. Different formulations of Liquisolid were developed by dissolving the drug in mixture of Transcutol HP: Capmul MCM and Cremophor EL: Capmul MCM (Non-volatile liquid; 1:1 ratio), converting this liquid medication using carriers as fujicalin and neusilin and coating material as syloid FP 244. The results showed that Liquisolid formulation exhibited significantly higher drug dissolution rate compared to pure drug as well as marketed formulation. The plasma concentration-time profile of healthy Wister rats indicated that the oral bioavailability of optimized formulation has been significantly improved compared to pure drug...
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Posted by admin on May 31, 2020 in |
The present work is focused on the formulation of Febuxostat fast dissolving tablets by lyophilization technique using natural starch extracted from Sterculia foetida seeds. Starches were extracted using the alkali method, i.e., sodium hydroxide at 0.1%, 0.25%, and 0.5% concentrations and water from Sterculia foetida seed powder. These starches were evaluated for phytochemical and physicochemical tests. Tablets were prepared using Febuxostat, Sterculia foetida seed starch, and croscarmellose sodium in various concentrations using direct compression technique. Various pre and post-compression parameters were performed along with in vitro drug release studies, characterization studies like FTIR, DSC, SEM, XRD, and accelerated stability studies. Phytochemical tests revealed the presence of only starch in all the extracts. The starch prepared from 0.1% sodium hydroxide (SFS2) showed the best physicochemical properties. From in vitro dissolution studies, it was observed that formulations FS6 and FS12 containing 15% w/w of SFS2 and 15% w/w of croscarmellose sodium respectively showed faster disintegration and enhanced dissolution rate compared with other formulations. Febuxostat tablets were further prepared by lyophilization technique....
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Posted by admin on May 31, 2020 in |
The present investigation deals with the assessment of neuroprotective effect Leucasa spera in streptozotocin (STZ) induced Alzheimer’s disease (AD) in rats. AD was induced by administering STZ (3 mg/kg, ICV) on day one and 3rd day after surgery. Surgery was performed on anesthetized rats with the help of the stereotaxic apparatus. STZ induced AD rats were treated with ethanolic extract of Leucasa spera (100, 200, and 400 mg/kg, p.o.) for 28 days. Effect of Leucasa spera root in AD rats was assessed by estimating the alteration in the behavior (Y maze apparatus and single trail passive avoidance) and biochemical parameter in the brain tissue {Oxidative stress parameters (SOD, CAT, and LPO), amyloid β peptide (Aβ) and acetylcholinesterase (AchE). Treatment with Leucasa spera shows significant (P<0.01) increased in the % of alteration in the behavior and step-through latency in Y maze task and single-trial passive avoidance test compared to AD rats. Leucasa spera significantly (P<0.01) decreases the AchE in the brain tissue compared to AD rats, whereas treatment with Leucasa...
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Posted by admin on May 31, 2020 in |
Objective: In the present study to enhance solubility and in vitro dissolution of poorly aqueous soluble drug Famotidine by preparing solid dispersions using the Kneading method. Methods: Solid dispersions of the drug were prepared by the kneading method using Kollidon and Povidone K30 (as a carrier). Eight different drugs: Carrier ratios were prepared by Factorial design taking three factors, i.e., the concentration of Famotidine (X1), Kollidon (X2), and Povidone K30(X3). Results: DSC, FTIR spectroscopy, powder X-ray diffraction (XRD), and SEM studies were used to characterize solid dispersions. In vitro release was carried out using the USP II dissolution apparatus. Multilinear regression analysis was applied to develop a mathematical model to estimate cumulative drug release. The batch F4 was found to be best batch as it showed maximum solubility and in-vitro dissolution after 30 min. Improvement in the dissolution behavior of solid dispersion batches was observed due to the conversion of a crystalline form of drug to amorphous form as confirmed by DSC, FTIR studies, and X-RD studies. SEM photographs...
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Posted by admin on May 31, 2020 in |
An attempt was made to formulate and evaluate Fexofenadine HCl loaded chitosan nanoparticles using biodegradable polymers such as chitosan and sodium tripolyphosphate as a crosslinker in different ratio and proportions. In this formulation, Fexofenadine HCl was selected because of wide range of its use in treatment of skin allergy in the form of coated tablet and pediatric suspension. Different formulations of Fexofenadine HCl loaded chitosan nanoparticles were prepared containing 0.5%, 0.75% of chitosan and 0.5% STPP as crosslinker using ionic gelation technique. Nanoparticles were characterized for particle size determination, Polydispersity index, Zeta potential, % Entrapment Efficiency and in-vitro release study and Scanning Electron Microscopy. For the formulations F6-F10, no yield was formed which might be due to an insufficient amount of crosslinker to form the nanoparticles. F2 was selected as the best formulation to be incorporated into the gel base using carbopol 934P in different concentrations of 0.5%, 0.75%, and 1%. The formulated gels were evaluated in case of viscosity, spread ability, in-vitro release study, kinetic and skin irritation...
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