Compound Danshen Sustained-release Tablets

The project was aimed at the complication, muti-composition, muti-target and muti-level of the effective material foundation in the famous complex prescription in pharmacopeia, i.e. Compound Danshen. And it was directed against the difficult sustained-release drug form study of the complex prescriptions, which is how to develop and evaluate. In the study of the compound sustained-release drug form, the muti-subject combination method of nuclear techniqe, biology and pharmacology was applicated. In detail, with the help of 45Ca determination of transmembrane inflow, extraction with defferent polar solvent and resin adsorption techniqe, using the experience of modern sustained-release techniqe, the selection, preparation, quality standard stability of the effective part of Compound Danshen were studied systematically. With the foundation of above, the prescription ratio, preparation procedure and the sustained-release evaluation of the effective part of Compound Danshen Sustained-release Tablet were completed. As a result, the sustained-release tablet with perfect effect has been made. Furthermore, as the methods and indexes of intracorporal and extracorporeal sustained-release evaluation had been studied deeply, it has laid a solid foundation for the study and development of the new drug form of Chinese medicine, i.e. the sustained-release drug form. With the combination of 45Ca determination of transmembrane inflow and extraction with defferent polar solvent, the effective part selection experiment shows that the liposoluble and hydrosoluble part of Danshen and the total saponin part of Sanqi are all effective significantly. And Tanshinone II A, Danshensu, Protocatechuic alalelehyde, Notoginsenoside Ri, Ginsenoside Rbl and Borneolum Syntheticum are all effective composition.Taking them as the evaluation indexes, the procedure of effective part were studied with orthogonal test. The quality standard of the effective part was given in such aspects, i.e. nature, identification, examination, content determination(60%) and Ca2+ antagonism.Their stability was also -2- detected. The safety of the Prescription was comfirmed by 45Ca determination of transmembrane inflow. The tablet procedure was studied in such aspects, i.e. compressing method, the category and ammount of HPMC, binder and malactic with monofactorial test. Then Compound Danshen Sustained-release Tablet was made, which can release composition 12 hours continuously. The extracorporeal indexes including composition release level and Ca2~ antagonism of sustained-release tablet were detected. The intracorporal indexes including blood-serum and artery circle were detected also. The result of the test shows that Compound Danshen Sustained-release Tablet can possess the characteristics of 12-hour-sustained-release-tablet. Meanwhile, the pharmacokinetics of effective composition has been primarily studied. There are 2 innovation points in the project. One is that the new research mode of the compound sustained-release form of Chinese medicine has been producuced. The mode is 搒electionand preparation of the effective part 梡rocedure study of sustained-release form梒omprehensive evaluation of sustained-release effect? The other is that 45Ca determination of transmembrane inflow technique has been firstly used in the effective part selection and comprehensive evaluation of sustained-release effect of the Chinese medici...