Studies On The Methods Of Dissolution And Drug Release Of The National Drug Standards

ObjectiveDissolution and drug release examination is an effective indicator of controlling the solid preparations quality, and it can be used to evaluate the quality of drugs, to guide the development of new dosage forms, and to ensure product quality and curative effect after the changing of preparation process, and can also predict the preparations’bioavailability in vivo and evaluate the uniformity of dosage units. In recent years, more and more preparations that need for the dissolution and drug release examination have been contained in all Pharmacopoeia, which can be seen that the dissolution and drug release examination plays an important role in controlling and improving the quality of preparations, but the premise is to establish a scientific、reasonable and operational execution dissolution and drug release method. Currently, dissolution and drug release method of "Chinese Pharmacopoeia"2010edition exists many incomplete places, and need for further revisions. This project aims to establish a scientific and rational appendix dissolution and drug release method, as well as study the relative products’dissolution or release test,which can improve some solid preparation quality of Chinese Pharmacopeia, reduce the gap between the Chinese and foreign Pharmacopeia. This method can not only be the real effective in vitro test of monitoring the solid preparation quality,but also can meet the need for production research and supervision.Methods1. The research of dissolution method. Firstly, to revise the incompatible and improper places in the dissolution test from the apparatus. And make experimental study on the fiber—optical chemical sensor dissolution test(FOCSDT) system. It indicates that there is no difference between the FOCSDT and ordinay dissolution apparatus by comparing the datas of FOCSDT on-line results and UV results of manual sampling. So this method can be introduced into Chinese pharmacopeia as the official methods.Secondly, to amend the difference between ChP2010and ChP2005from the procedure aspects combined with the foreign pharmacopeia. Finally, According to the revised dissolution method, using multiple dissolution profile study to evaluated the in vitro dissolution consistency of famotidine tablets.2. The research of drug release method. To revise the paddle over disk appratus for the transdermal patches. The method is useing the ChP disk and USP disk respectively in the same conditions to take experiment on the same batch sample, and compare the experimental data. The results discover that the size of ChP disk was too big, the ratio of solution volume under the disk is very large. It has a big influence on the accuracy of determination results, when the test solution concentration upper and lower the disk don’t reach a balance. So the author advises to contract the size of ChP disk, and use the rotating-cylinder method to measure the preparation that the paddle over disk unapplicable. Then to develope a scientific and reasonable quality criteria for the release of Gliclazide Sustained-Release Tablets according to the method of dissolution studies in the Project of Drug quality Re-evaluation in Japan, and investigate release test of several domestic generic drugs using the proposed standardResultsTo amend the incompatible place of dissolution and drug release test combining with the foreign pharmacopeia and establish a scientific and rational dissolution and release method. And on this basis, to research the quality consistency evalution of Farmotidine tablets and improvement of release test of quality critera of Gliclazide sustained-release tablets through the multiple dissolution or release curves. The results indicate that the method can not only assess the quality of generic drugs and the original druge objectively, but can also be used for generic drug quality control and standard research.ConclusionA scientific and rational dissolution and release method is the guidance of all product standards that need for dissolution and release test. And based on a rigorous method, the dissolution and release test can better distinguish the differences of preparation process and reflect the uniformity of preparations, and then improve its inner quality.