Home Contact Us 中文 English
Yourlocation:Home >News> Experimental study on the gastric floating sustained - release tablets of trimebutine maleate

Experimental study on the gastric floating sustained - release tablets of trimebutine maleate

Time:2017/8/2 17:32:58

Trimebutine maleate is a new type of gastrointestinal function regulator, because it is weak acid, pKa value of 6.25, in acidic media solubility than distilled water and alkaline medium solubility. It acts directly on the stomach smooth muscle, so to extend its retention time in the stomach to avoid premature emptying into the small intestine, can increase its strength and improve bioavailability. Trimebutine maleate  tablets (100mg / tablets) need to take 3 times a day, each 1-2 tablets. The development of trimebutine maleate floating sustained-release tablets designed to reduce the number of patients taking medication to improve patient compliance. Before the prescription, the apparent equilibrium solubility, wettability, apparent oil / water partition coefficient and powder properties of the product were studied. The orthogonal test was used to select the auxiliary materials from the drift time as the effect index, and the critical relative humidity of the excipients was measured, which provided reference for the environmental humidity of the tablet and the storage conditions of the tablets. The compatibility of drugs and excipients was studied. The results showed that the apparent equilibrium solubility of the product in acidic medium was slightly hygroscopic and its apparent oil / water partition coefficient increased with the increase of pH value and poor mobility. Orthogonal test screening of the excipients and drug compatibility is good. The effects of preparation process on release and floating properties were investigated. On the basis of single factor optimization, the best prescription is selected by using the multi - index optimization method, such as the overlapping contour method and the effect surface method, and the minimum deviation is proved by the overlapping contour method. The evaluation of gastric floating sustained-release tablets in vitro is the focus and difficulty. In vitro determination of floating properties of drugs in the stomach may be poor floating effect and lead to the failure of scientific research. During the experiment, it was found that the traditional release degree measuring device was not suitable for the special preparation. It was mainly reflected in the adhesion of the tablet after the floating of the tablet, the fluid force of the release medium and the mechanical force of the rotating shaft. In this study on the basis of other studies, the design of the release of the preparation of the device, the results show that feasible and convenient. The zero - level dynamics of the release curve, the first - order kinetics and the gray prediction model of the non - equal - spaced sequence are fitted to show that the Weibull distribution is the most suitable. The preliminary study on the floating mechanism confirms that the expansion of the floating sheet is mainly axial, and the floating capacity depends on the proportion of the water absorption and weight ratio and the expansion ratio. Increasing the expansion ratio is lower than the water absorption weight gain ratio, by reducing the pressure of the compression method to improve the floating performance is limited. The results showed that the moisture absorption was more than 5% in the humidity sensitive and high humidity (92.5%) environment, and the floating performance was decreased. Therefore, the inner packaging was made of aluminum plastic aluminum. Accelerated and long-term trials show that the stability of this product is still, long-term stability and pre-clinical pharmacokinetics to be further studied.