Antithrombotic Factors Sustained Release Matrix Tablets Of The Preparation Process, Quality Standards And Initial Intestinal Absorption Studies

Thrombus diseases concern with many subjects of clinic, it do great harm tothe health of human being, of which the death rate and cause disability dateresulting from the thrombosis of the heart and brain?ˉs blood vessel are veryhigh. Thrombosis involve artery thrombus and vein thrombus, no matter which kind,the causes of it all include the injury of the endothelial tissue of blood vesseland the activation of cruor mechanism. Kangshuansu(ISA) is a new component, which is a chemical complex of shikimene.It has good solubility and stability, and it has a high bioavailability. It?ˉspharmacodynamics research show that it has good function of anti-thrombosis andcan prevent the aggregate of blood platelet, especially it can effectivelyimprove the damage caused by cerebral ischemia, and it has no influence to thenormal cruor mechanism of organism. Therefore, Kangshuansu(ISA) as a new drugused in the treatment of thrombosis has a good prospect of application. Based on the existing research of Kangshuansu(ISA),more research about itincluding it's basic properties,pharmaceutical technology,quality standard,stability and preliminary absorption research of small intestine are studied,which laid the groundwork for the further clinic research and application.1. The complementary research about basic properties of Kangshuansu(ISA) (1) Research about Kangshuansu(ISA)'s stability at different pH. Result:It is instable in pH1??4, and in company with the decline of pH it's stabilityrundown. And it is stable in 8 hours when the pH is above 5. (2) measuring Kangshuansu(ISA)'s oil/water partition coefficient. Result:It's oil/water partition coefficient is downtrend in pH5.0～10.0 at roomtemperature, and the trend is great apparent when the pH is above 5.8 .2. The Pharmaceutical technology of Kangshuansu(ISA) sustained release matrixtablet Based on the research of Kangshuansu(ISA) tablet, some apposite technologyparametersofthetabletareestablished.Accordingtothetechnologyparameters,I filtrated the best framework material of the sustained release matrix tabletand studied the Pharmaceutical technology of it. Result: EC and HPMC is theperfect framework material, the matrix tablet made by them coincide to thetechnology parameters and can achieve ideal sustained result. The best recipeis Kangshuansu(ISA):HPMC:EC: starch:dextrin:lactose:magnesiumstearate=10:14.5:1.5:1.2:6.4:6.4:0.15 .3. The quality standard of Kangshuansu(ISA) sustained release matrix tablet The Kangshuansu(ISA) in tablet was identified by using UV and TLC; thecontent of the matrix tablet was determined by using HPLC and the content limitwas established; the release test methods and result were established. Result:The quality standard was established preliminarily. This method is stability,accurate,specificandrepeatable.Itcancontrolthequalityofthematrixtabletwell.4. The stability study of Kangshuansu(ISA) sustained release matrix tablet Quarantine period method and accelerated test were used to detect thestability of Kangshuansu(ISA) matrix tablet. Result: The samples were stableduring the testing period of 12 months at the room temperature. TheKangshuansu(ISA) matrix tablet was stable for 35 days under the temperature of40℃,60℃,the content measured up to the quality standard; and the content ofit changes very little when it put under the temperature of 80℃ for 35 days and90℃ for 15 days, it also meeted the quality standard; but when put it under thetemperature of 90℃for 15 days the content was lost seriously, and it completelylost when 35 days.5. The preliminary absorption research of small intestine about Kangshuansu(ISA) Using everted gut sac system to study the absorption characteristics ofKangshuansu(ISA),rat and rabbit were used individually. Result: (1) Theabsorption rate of Kangshuansu(ISA) in the rat's gut can achieve 8.32% at 1.25hour, but with the passage of time, the content of Kangshuansu(ISA) in the sacoutside the gut rose up. (2) The absorption rate of Kangshuansu(ISA) in therabbit's gut can achieve17.51% at 1.25 hour, but with the p...