Nowadays, the use of natural polymers as an alternative to synthetic gastro-retentive polymers is increasing. Such natural raw materials are highly biocompatible and biodegradable with no or significantly fewer side effects and are economical too. The main aim of this research work was to design a gastro-retentive tablet of Captopril by using Maize Stem Pith (MSP) powder and Jowar Stem Pith (JSP) as novel natural low-density polymers and also to sustain the drug release for up to 12 hours. Our objective behind this research is to prepare the gastro-retentive tablet, evaluate it for floating behavior, and to achieve the sustained release effect for at least 12 hours. The novelty of this research work is that MSP powder and JSP powder possesses low density. Thus, gastro-retentive tablets with a low-density (floating) approach can be prepared at a very lost cost compared to the currently marketed formulation. Gastro-retentive tablets of Captopril were designed by using MSP and JSP powder. Using design-expert® version 13, the formulations were prepared using a 32-complete factorial design. The gastro-retentive tablet showed good floating behavior and dissolution pattern, which sustains the release of the drug for up to 12 hours. The optimization study using a contour plot and response surface plot suggested that formulation R9 is an optimized batch among all batches. The current research indicated that there is an increase in floating time with a corresponding decline in the dissolution rate of the tablet as the concentration of MSP powder and JSP powder increases. The optimized formulation R9 consists of MSP powder and JSP powder at 12% and 8 %, respectively, in combination with HPMC (K-100M), and has proven excellent floating behavior and expected drug release pattern. Therefore, MSP powder and JSP powder could be used as suitable low-density novel polymers to design gastro-retentive tablets of Captopril.
Disulfiram is widely prescribed to discourage alcoholics from drinking alcohol. The effectiveness of oral disulfiram as a treatment for alcoholism is severely limited due to its poor bioavailability and poor patient compliance. To minimize the failure of the orally administered drug, efforts have been made to prepare alternative dosage form of subcutaneously implantable disulfiram pellets or tablets. In the present study an attempt has been made to design and evaluate a disulfiram implant using plain drug. The disulfiram implants have been formulated by direct compression and the effect of parameters like pH of site of administration (6.0 and 7.4) and sterilization were studied on in-vitro release of implantable disulfiram pellets. In- vitro release has been studied by vial and rotary flask shaker methods. The release kinetic mechanism from all the formulation was found to be zero order. The in vitro release data of all the formulations was compared with that of marketed disulfiram implant (Esperal). In contrast to other formulation in vitro release from marketed formulation appeared to be independent of hydrodynamics of diffusion (volume of dissolution media and agitation speed). The present study had revealed that, in-vitro drug release from implants is unaffected by pH of site of administration and gamma ray sterilization. Both the methods (Vial Method & Rotating Flask Method) of in vitro dissolution testing are found significantly different for formulations prepared in laboratory but not for marketed formulation, indicating the different mechanism of release of marketed formulation.
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