International Journal of Pharmaceutical Sciences and Drug Research

249-253

Authors: Himanshu A Acharya*, Rakesh P Patel

Hydralazine hydrochloride has a half-life of 2 to 4 hours with an oral bioavailability of 26-50%. Since hydralazine has a demethylating effect on various suppressor genes, it can be used in various types of cancer to support chemotherapy. The purpose of this study was to optimize and evaluate floating tablets of hydralazine hydrochloride designed to prolong the gastric residence time and to provide controlled release of the drug for 24 h. The floating tablets of hydralazine hydrochloride were prepared by the wet granulation method. Polymers of hydroxy propyl methyl cellulose (HPMC K100M), HPMC K15M, carbopol 940 and sodium bicarbonate were used as the release retarding agents. This study investigated utility of a 3-factor, 3-level Box-Behnken design and optimization process for floating tablet of Hydralazine with 5 replicates of center points. Amount of HPMC K4 (Hydroxy Propyl Methyl cellulose), amount of sodium bicarbonate were selected as the independent variables whereas total floating time (TFT), T90, % cumulative drug release at 24 hours, and T20, Q1 were selected as dependent variables. Non-Fickian diffusion release transport was confirmed as the release mechanism for the optimized formulation and the predicted values agreed well with the experimental values. Drug excipient compatibility studies were investigated by FTIR, DSC and XRD. The produced tablets exhibited good floating time and controlled drug release over a period of 24 h. The resultant data were critically analyzed to locate the composition of optimum formulations. All predicted values of response variables of optimized formulation demonstrated close agreement with the experimental data during optimization procedure.

259-264

Authors: Susheel Thakur*, Nisha Thakur, Niladry Shekar Ghosh

Arthritis is the condition which is associated with inflammation of a joint, pain, swelling, and stiffness. Drug delivery to the target site remains a challenge due to ineffective drug delivery system. An attempt has been made to formulate and evaluate micro-emulgel for the effective drug delivery in the treatment of Arthritis. Micro-emulgel was loaded with Curcumin and Tinospora cordifolia to enhance bioavailability of extracts which have been widely used in the treatment of arthritis. Micro-emulgel was prepared by emulsion-solvent diffusion method using carbopol 940P as a gelling agent. Micro-emulsion was formulated using Liquid paraffin oil as oil phase; Tween 80 and Span 20 as surfactant and co-surfactant respectively. FTIR studies proved the compatibility between drug, excipient and carbopol. The Prepared micro-emulgel was subjected to various parameters such as pH, rheological studies, spreadability, thermodynamic stability tests, drug content, electro conductivity, and in-vitro release studies. The pH of all formulations was found near to the skin pH value. Viscosity and spreadability of F1 optimized formulation was found to be 146.5×103 cPs and 2.24 g×cm. From the in vitro drug release study, it was revealed that sustained release of formulation last up to 18 hours. F1 formulation showed the highest drug release of Curcumin (92.37%) and Tinospora cordifolia (90.75%). SEM images showed the diameter of oil globules of Micro-emulgel were in range of 1.50 to 2.13µm. Drug release kinetics showed the zero order drug release from the optimized F1 formulation. From the stability studies, F1 formulations had an excellent physical stability.

269-274

Authors: G. Rajeswari Gopal1*, G.I. Anuja2, P.G. Latha2, A. Jayakumaran Nair1, A. Gangaprasad4, P.R. Sudhakaran1, D. Muraleedharan3, G.M. Nair1

In the present study the roots and leaf ethanolic extracts of Chassalia curviflora were screened for their anti hepatotoxic and anti oxidant effects in experimentally induced liver injury by carbon tetra chloride. Liver serum marker enzymes as well as antioxidant enzymes mainly superoxide dismutase, catalase and glutathione levels were determined. The plant root and leaf ethanolic extracts at 50, 100, 200 mg concentrations significantly (**P ≤ 0.05) reduced the elevated serum hepato specific enzyme [serum glutamate pyruvate transaminase (SGPT), serum glutamate oxaloacetate transaminase (SGOT), serum alkaline phosphatase (SAKP), serum bilirubin (SB)] and cholesterol levels induced by CCl4. Antioxidant enzymes such as superoxide dismutase (SOD), catalase (CAT) and non enzymatic reduced glutathione (GSH) levels were increased whereas malondialdehyde (MDA) level was reduced by the extracts. Compared to the leaf extract, root extract significantly reduced serum hepato parameters and increased the levels of anti-oxidant enzymes in a dose dependent manner. The results were comparable to that of silymarin, reference drug used for the study. The histopathological studies also supported the biochemical findings. Acute toxicity studies revealed that it is safe for pharmacological uses upto 2000mg/kg. The present study scientifically validated the traditional use of plant root in hepatoprotection.