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川芎嗪涂膜剂的制备及其体外经皮渗透特性研究
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| 篇名： | 川芎嗪涂膜剂的制备及其体外经皮渗透特性研究 |
| TITLE： | Preparation and Study on in vitro Transdermal Characteristics of Tetramethylpyrazine Pellicle |
| 摘要： | 目的：初步优选川芎嗪涂膜剂的制备工艺，并研究其体外经皮渗透特性。方法：采用单因素试验，以聚乙烯醇（PVA-124）、无水乙醇、甘油、吐温80、氮酮的用量为因素，采用改良的评分标准对涂膜剂基质的成膜时间、成膜性、延展性、均匀度和有无气泡等指标进行评价，优选川芎嗪涂膜剂基质处方。在优选基质处方的基础上制备含不同载药量川芎嗪（300、250、200、150、100、50mg/mL）的涂膜剂，并考察其最大载药量。采用高效液相色谱法测定川芎嗪含量，并进行方法学考察。取离体大鼠背部皮肤，对高、中、低载药量（100、75、50mg/mL）川芎嗪涂膜剂进行体外经皮渗透试验，分别于第15、30、45、60、75、90、120、150、180min时取样测定，并计算川芎嗪的渗透速率。结果：PVA-124、无水乙醇、甘油、吐温80、氮酮的用量分别为2.5g、7.0mL、1.97mL、0.07mL、0.28mL（以50mL处方量计）时的川芎嗪涂膜剂基质处方为最优；川芎嗪的最大载药量为100mg/mL。川芎嗪含量测定方法的线性范围为3.125～100μg/mL，其专属性、精密度、重复性、回收率、稳定性考察均符合要求（RSD均小于2％）；高、中、低载药量川芎嗪涂膜剂的渗透速率分别为608.42、384.19、158.20μg（/cm·2h）。结论：按优选处方制备的川芎嗪涂膜剂成膜时间短、质量稳定可靠，载药量可达100mg/mL；75mg/mL载药量的涂膜剂即可达到川芎嗪有效治疗血药浓度的渗透速率范围。 |
| ABSTRACT： | OBJECTIVE：To preliminarily optimize the preparation technology of Ligustrazine pellicle ，and to study its in vitro percutaneous permeation characteristics. METHODS ：With the amounts of PVA- 124，ethyl alcohol ，glycerin，tween-80 and azone as factors ，single factor experiment was used to optimize the Ligustrazine pellicle matrix formulation ；modified scoring standard was used to evaluate the film formation time ，film formation ability ，ductility，uniformity and the presence of bubble. On the basis of the optimal matrix formulation ，the pellicle with different loading amount of ligustrazine （300，250，200，150，100，50 mg/mL） was prepared and its maximum loading amount was investigated. HPLC method was adopted to determine the content of ligustrazine，and methodology investigation was conducted. Isolated back skin of rats were collected ，the percutaneous permeation test was conducted for high ，medium and low loading amount （100，75，50 mg/mL）of Ligustrazine pellicle. At 15，30，45，60， 75，90，120，150，180 min，the sample was taken and the permeation rate of ligustrazine was calculated. RESULTS ：When the amounts of PVA- 124，ethyl alcohol，glycerin，tween-80 and azone were 2.5 g，7.0 mL，1.97 mL，0.07 mL，0.28 mL（in terms of 50 mL formulation amount ），the optimal matrix formulation of Ligustrazine pellicle was obtained. The maximum drug loading amount of ligustrazine was 100 mg/mL. The linear ranges of ligustrazine was 3.125-100 μg/mL. The specificity，precision， reproducibility，recovery and stability investigation of content determination method of ligustrazine were all in line with the requirements（RSD＜2％）. The permeation rate of high ，medium and low loading amount of Ligustrazine pellicle were 608.42， 384.19，158.20 μg（/ cm2·h）. CONCLUSIONS ：According to the optimized formulation ，the prepared Ligustrazine pellicle had a short film forming time ，stable and re liable quality ； the drug-loading amount was up to 100 mg/mL. The pellicle with drug-loading amount of 75 mg/mL had reached the penetration rate range of effective plasma concentration of ligustrazine treatment. |
| 期刊： | 2020年第31卷第02期 |
| 作者： | 王颖，何亚楠，车逸豪，袁仕梦，赵海荣，巫秀美，杨志斌 |
| AUTHORS： | WANG Ying，HE Yanan ，CHE Yihao，YUAN Shimeng ，ZHAO Hairong ，WU Xiumei ，YANG Zhibin |
| 关键字： | 川芎嗪；涂膜剂；处方优化；大鼠；经皮渗透试验；渗透速率 |
| KEYWORDS： | Ligustrazine；Pellicle；Formula optimization ； |
| 阅读数： | 393 次 |
| 本月下载数： | 10 次 |
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