發(fā)布時間：2018-04-22 13:44

  本文選題：西羅莫司 + 自微乳給藥系統(tǒng)�。� 參考：《中國醫(yī)院藥學(xué)雜志》2017年17期

【摘要】：目的:提高自微乳緩釋片中西羅莫司(SRL)的穩(wěn)定性。方法:考察SRL在不同pH條件下的穩(wěn)定性,再利用檸檬酸或蘋果酸調(diào)節(jié)自微乳的pH并制備緩釋片,利用鋁塑材料對自微乳緩釋片進行包裝,考察在高溫、高濕和強光照射條件下SRL的含量變化。結(jié)果:SRL原料藥在高溫、高濕和強光照射條件下穩(wěn)定,市售片中的SRL含量僅在強光照射下少量降低,而自制自微乳緩釋片中的SRL在高溫和強光照射試驗下均不穩(wěn)定。自微乳的堿性環(huán)境可能是導(dǎo)致SRL高溫不穩(wěn)定的主要原因,測定發(fā)現(xiàn)SRL穩(wěn)定的pH為4.5~5.8。利用蘋果酸和檸檬酸均可提高自微乳中藥物的高溫穩(wěn)定性,使(40±2)℃條件下,緩釋片中藥物的含量達到98%以上。蘋果酸的吸濕性導(dǎo)致片重增加,表面有濕潤感,因此確定選用0.20%的檸檬酸作為pH調(diào)節(jié)劑。光照對自微乳緩釋片中的藥物有不利影響,采用鋁塑包裝(內(nèi)含暗黑色避光層),可使SRL含量由94.06%提高至99.37%。綜合應(yīng)用0.20%檸檬酸和鋁塑包裝所得的SRL自微乳緩釋片在高溫、高濕和強光照射條件下,10 d時的含量均在99%以上。結(jié)論:經(jīng)鋁塑包裝的含0.20%檸檬酸的SRL自微乳緩釋片,在高溫、高濕、強光照射條件下均具有良好的穩(wěn)定性。
[Abstract]:Objective: to improve the stability of sirolimus SRL in self-emulsion sustained release tablets. Methods: the stability of SRL under different pH conditions was investigated. The pH of self-microemulsion was adjusted by citric acid or malic acid and sustained release tablets were prepared. The change of SRL content under high humidity and strong light irradiation. Results under the conditions of high temperature, high humidity and strong light irradiation, the content of SRL in commercial tablets decreased only slightly, while the SRL in self-made self-microemulsion sustained release tablets was unstable under high temperature and strong light irradiation. The alkaline environment of the self-microemulsion may be the main cause of the instability of SRL at high temperature. It was found that the stable pH of SRL was 4.5 ~ 5.8. Both malic acid and citric acid could improve the high temperature stability of the drug in the microemulsion, and the content of the drug in the sustained-release tablets could reach more than 98% at 40 鹵2 鈩，

本文編號：1787485