Study Of The Effects In Vitro Release Of Excipients On Water Soluble Drug Sustained Release Agent

The pharmaceutical excipients is an important part of pharmaceutical preparations, it has an important role for the maintenance of drug stability, improve efficacy, reduce toxicity. With the advancement of technology and the development of new excipients, controlled release formulations, transdermal absorption agents, targeted drug delivery formulations and other new dosage forms, new technologies are mature. Especially the sustained and controlled release formulations for its high degree of bioavailability, good patient compliance, simple process, are very popular with people. The application of new excipients can promote a new formulation of the research, development of new formulations to promote the development of new excipients. Therefore, study of the pharmaceutical excipients and their interactions on drug release in the new formulations have a great significance to promoting the development of drug formulations and excipients.In this study, we will take the hydrochloride diltiazem as the model water-soluble drug, mainly study the matrix material, like hydroxypropyl methylcellulose (HPMC), sodium carboxymethyl cellulose (CMC-Na), Eudragit L100-55 and so on and their interactions on drug release in the new sustained release matrix formulations. Study the nature and role of the excipients, promote excipients research and development, in order to get a water-soluble drug prescription model of sustained-release formulations which has a simple preparation, good in vitro release, to prepared the more water-soluble drugs into sustained-release preparations, to provide a reference and guidance to promote the development of pHarmaceutical preparations.First, choose the commercially available hydrochloride diltiazem sustained-release tablets as reference preparation to investigate the influence of dissolution media、speed and other factors on vitro release, to determine the best determination condition of drug release in vitro:the basket method,900ml distilled water as the dissolution medium.speed of 100rpm, UV 236 nm measured absorbance, calculate the cumulative release.Then make HPMC as matrix material to preparation the hydrochloride diltiazem sustained-release tablets. Investigated HPMC specifications. amount、diluent compatibility and formulation and process factors on drug release; and make HPMC as the main component of the regulation layer to preparation double layer sustained release tablets, examine the influence of HPMC on the release of double-layer skeleton preparations. Secondly,add CMC-Na into sustained-release formulations prescription, and investigated the effects of CMC-Na alone as the reinforcing material and the interaction in combination with HPMC on drug release. The results showed that the increase of HPMC viscosity and the amount of preparation or a double-layer tablets can slow the drug release, but with certain limits, and the existence of pre-release and rapid phenomenon; combination of CMC-Na as a reinforcing material can significantly slow down the drug in vitro prerelease of up to 24 hours sustained release; The tablet which has the prescription of HPMC 18.5%. CMC-Na 20% of the joint reinforcing material, Lactose 20%as thinner,3% PVP K30 as adhesive, prepared by the wet granulation have a similar in vitro release with commercially available preparations, and the preparation process is simple. easy to control quality. When added Eudragit L100-55 directly in the prescription, the release of the drug has a certain pH-dependent, can achieve the effect of enteric-coated slow release, can simplify the production process, beneficial to the control of drug quality, reduce production costs.Study and summary of this experiment to investigate the pHarmaceutical excipients, HPMC, CMC-Na, EudragitL 100-55 in the preparation as sustained release matrix, described the nature of the excipients and the interaction of each other on water-soluble drug sustained-release formulations vitro release, prepared the prescription model of sustained-release preparations, lay the foundation for the development of controlled release formulations of water-soluble drugs. Study excipient interactions that impact on the drug release can promote the wide range of applications and the development of new pHarmaceutical.