【摘要】：目的:制備鹽酸氟西汀醇質(zhì)體凝膠劑并考察其體外經(jīng)皮滲透特性。方法:采用乙醇注入法制備鹽酸氟西汀醇質(zhì)體,以包封率和粒徑為指標(biāo),利用正交設(shè)計(jì)優(yōu)化處方和制備工藝,對(duì)其粒徑及包封率、Zeta電位進(jìn)行評(píng)價(jià),并以卡波姆940為基質(zhì)制備醇質(zhì)體凝膠。采用透皮擴(kuò)散儀,大鼠離體皮膚進(jìn)行體外透皮實(shí)驗(yàn),HPLC測(cè)定藥物濃度并計(jì)算藥物累積滲透量、穩(wěn)態(tài)透皮速率。結(jié)果:制得的鹽酸氟西汀醇質(zhì)外觀呈淡藍(lán)色,平均粒徑為(77.3±1.49)nm,包封率為(60.4±1.76)%,鹽酸氟西汀醇質(zhì)體凝膠體外經(jīng)皮滲透速率為(5.13±0.78)μg·cm-2·h-1,是普通凝膠劑和對(duì)照凝膠的1.31和4.31倍。結(jié)論:鹽酸氟西汀醇質(zhì)體凝膠劑制備工藝簡單可行,質(zhì)量穩(wěn)定可控,能明顯促進(jìn)鹽酸氟西汀的經(jīng)皮滲透。
[Abstract]:OBJECTIVE: To prepare fluoxetine hydrochloride ethosome gel and investigate its transdermal permeability in vitro. METHODS: Fluoxetine hydrochloride ethosome was prepared by ethanol injection method. The encapsulation efficiency and particle size were taken as the index. The formulation and preparation technology were optimized by orthogonal design. The particle size, encapsulation efficiency and Zeta potential of the gel were evaluated. Carbomer 940 was used as the matrix to prepare the gel. Preparation of ethosome gel. In vitro transdermal test was carried out on rat skin by transdermal diffusion apparatus. The drug concentration was determined by HPLC and the cumulative penetration and steady-state transdermal rate were calculated. The transdermal permeation rate in vitro was (5.13+0.78) UG cm 2 h 1, which was 1.31 and 4.31 times higher than that of normal gel and control gel.
【作者單位】： 南京中醫(yī)藥大學(xué)藥學(xué)院;中國人民解放軍第102醫(yī)院全軍心理疾病防治中心藥物研究室;江蘇省中藥高效給藥系統(tǒng)工程技術(shù)研究中心;南京市中藥微丸產(chǎn)業(yè)化工程技術(shù)研究中心;中國人民解放軍第102醫(yī)院藥劑科;
【基金】：江蘇高校優(yōu)勢(shì)學(xué)科建設(shè)工程資助項(xiàng)目
【分類號(hào)】：R943

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本文編號(hào)：2240611