Evaluation Of Quality Consistency Of Tirofiban Hydrochloride Injection

Tirofiban Hydrochloride (TH), N-(butylsulfonyl)-O-(4-(4-piperidinyl) but yl-L-tyrosine monohydrochloride monohydrate, is a nonpeptide glycoprotein (GP) Ⅱb/Ⅲa receptor antagonist which can exhibit the aggregation of platel et. Combining with heparin, TH can prevent acute ischemic syndromes in p atients with unstable angina and non-Q-wave myocardial infarction and also be suitable for people who experienced atherosclerotic plaque excision. Qu ality by Design, in order to improve the quality of Tirofiban Hydrochloride injection which is self-developed, we detailed studied the quality of Tirof iban Hydrochloride (API),the composition of prescription, formulate the p reparation procedure and the quality of Tirofiban Hydrochloride injection in this task. The main research contents are as follows:1、the fundamental research of Tirofiban Hydrochlorid injectionThe fundamental research of Tirofiban Hydrochlorid injection consists of two aspects. One is the study of Tirofiban Hydrochlorid API; the other is the study of excipients used to Tirofiban Hydrochlorid injection.2、Study on the processing technique of Tirofiban Hydrochloride injecti onIt is reported that the key factor causing the different quality between the original product and imitation was preparation technology. Hence, we d etailed researched the preparing technology. Firstly, we determined the form ulation of Tirofiban Hydrochloride injection based on the commercially avai lable products prescription. Then studied the critical process parameters, sue h as the pH range of the solution, the consμmption of activated carbon, t he conditions of sterilisatio.3、the quality study of Tirofiban Hydrochloride injectionConsulting the related standards of Tirofiban Hydrochloride injection, we focused on studying the specific items of Tirofiban Hydrochloride inject ion, such as the determination of related impurities, the contents of Tirofib an and the isomeride of Tirofiban Hydrochloride. The detection method of related impurities was as follows:mobile phase A was acetonitrile, mobile phase B was a mixture of0.025M phosphate buffer, adjusted to pH6.8wi th triethylamine, and acetonitrile in the ratio of4:1(v/v). The following gra dient programme was employed:T(min)/B(v/v):0/100,10/95,20/94,20/94,30/81,50/81,55/100. We detected the contents of Tirofiban by the mobile phase of a mixture of0.025M phosphate buffer, adjusted to pH6.8with tr iethylamine, and acetonitrile in the ratio of78:22(v/v). The isomeride of Ti rofiban Hydrochloride was detected by hexyl hydride-isopropanol-methyl ale ohol-ethanediamine-ice vinegar (300:400:300:3:3).4、The quality study of self-developed and the commercially productsIn order improve the quality of AND A in our country, SFDA publishe d the document about evaluating the quality between self-developed and the commercially products. We did the follow tasks in order to ensure the dif ference between self-developed and the commercially products:(1)compared the difference between Tirofiban Hydrochloride injection and its commercia lly product in pH, the content of impurities and appearance characters.(2) o bserved if the results of compatibility test between Heparin Sodiμm Injectio n and Tirofiban Hydrochloride injection in accordance with commercially pr oduct (3) compared the difference between Tirofiban Hydrochloride injection and its commercially product under the conditions of stability test...