局部的碘苷脂质体凝胶治疗单纯疱疹:制药和临床意义。

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赛斯AK, Misra Umrigar D

局部的碘苷脂质体凝胶治疗单纯疱疹:制药和临床意义。

制药开发工艺。2004年8月,9 (3):277 - 89。

PubMed ID
15458233 (在PubMed
]
文摘

碘苷的制备方法的优化(IDU)脂质体的逆相蒸发(牧师)方法是由三个变量在三个层次(3(3))的阶乘设计。三个独立变量选择体积的有机相(x1)、水相的体积(x2),和药物中胆固醇/磷脂酰胆碱/摩尔比率(x3)。27批IDU脂质体被牧师准备方法和受到评价药物滞留比例(PDE),大小和粒度分布。减少多项式方程导出了数据的多元回归PDE和转换后的值的三个独立变量。等高线图3 - 1(低)的固定汇率水平,0(媒介),1(高)的主要贡献变量(x3)绘制x1和x2之间按预定PDE理解独立变量的物理意义。脂质体凝胶是由分散优化IDU脂质体在2% w / w和5% w / w (HPMC K4M)凝胶基地,含有1% w / w IDU(分别LIG-1和LIG-2)。药物保留的百分比(PDR)研究优化批14 (Lipo-14)和LIG-1 LIG-2进行了在三个不同的储存条件(2 - 8摄氏度,25 + / - 2度,和37摄氏度)。比较扩散研究LIG-1和PIG-1 LIG-2 PIG-2 (1% w / w IDU组件的脂质体分散在2% w / w w / w和5% HPMC K4M凝胶基地,分别),分别通过人类尸体的皮肤。比较双盲临床试验研究优化LIG-2凝胶进行了八周,与20日PIG-2单纯疱疹患者相比(每个1型单纯疱疹病毒和HSV-2 10位病人,分为两组每个5例)。批14 (Lipo-14)被发现最大PDE的74.4%。PDR研究显示最大药物保留2 - 8度c PDR显著增加(p < 0.05)观察LIG-1和LIG-2与Lipo-14相比三个温度。 In the diffusion studies, a significant (p<0.05) flux reduction; 3.5 times in LIG-1 when compared with PIG-1 and 2.3 times in LIG-2 when compared with PIG-2 was observed. Approximately 2.2- and 2.5-fold increase in skin drug retention in LIG-1 and LIG-2, respectively, was determined. A double blind clinical study demonstrated an approximately 2.0- and 1.6-fold increase in average percentage improvement in healing of the lesions in patients suffering from HSV-1 and HSV-2 diseases, respectively, when treated with LIG-2 compared with PIG-2. However, complete removal of lesions was not observed. Local side effects such as itching, burning, inflammation in HSV-1 and HSV-2, and burning micturation in HSV-2 associated with the use of PIG-2 were reduced considerably with the use of LIG-2. The findings of this investigation establish the role of the derived equation and plotted contour plots in predicting the values of independent variables for preparation of IDU liposomes by the REV method. The study also demonstrated that IDU liposomal gels retain more drug when compared with plain liposomes at all temperatures for the period of three months, while maximum PDR was found at refrigeration temperature. The skin retention of IDU was enhanced due to its entrapment in the liposomal vesicles. The clinical study suggested the improvement of therapeutic efficacy of IDU entrapped in liposomes in treatment of HSV-1 and HSV-2 patients.

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