【摘要】：目的建立體內(nèi)外相關(guān)性良好的醋酸曲普瑞林緩釋微球體外加速釋放方法。方法殘留法測(cè)定該藥微球在大鼠體內(nèi)的釋放行為;分別考察表面活性劑、pH值、乙醇濃度、溫度、轉(zhuǎn)速和防腐劑濃度對(duì)體外加速釋放的影響,調(diào)整釋放條件并建立加速釋放方法,進(jìn)行體內(nèi)外相關(guān)性研究。結(jié)果確定體外加速釋放條件為:以15%乙醇溶液(含0.06%吐溫80和0.1%苯扎氯銨)為釋放介質(zhì),釋放溫度為55℃,振搖頻率為200 r/min;在此條件下該藥微球30 h釋放達(dá)到87.35%,相當(dāng)于微球在體內(nèi)釋放30 d,且體外加速釋放結(jié)果與體內(nèi)釋放數(shù)據(jù)相關(guān)性良好(y=0.8845x+12.4510,R2=0.9938)。結(jié)論所建立的醋酸曲普瑞林微球體外加速釋放方法與體內(nèi)釋放行為相關(guān)性良好,采用此法可快速有效評(píng)價(jià)該藥微球釋放行為。
[Abstract]:Objective to establish an accelerated release method of triprrelin acetate sustained release microspheres in vitro and in vivo. Methods the release behavior of the microspheres in rats was determined by residue method, and the effects of surfactants, pH value, ethanol concentration, temperature, rotating speed and preservative concentration on the accelerated release in vitro were investigated, the release conditions were adjusted and the accelerated release method was established to study the correlation in vitro and in vivo. Results the accelerated release conditions in vitro were determined as follows: 15% ethanol solution (containing 0.06% Tween 80 and 0.1% benzalkonium chloride) was used as the release medium, the release temperature was 55 鈩，

本文編號(hào)：2517003