乳剂型凝胶剂预混辅料的初步研制(1)
[摘要]该实验旨在研究乳剂型凝胶剂预混辅料。以最为常用、成本低廉和工艺简单等为标准筛选辅料和设计配方。采用星点设计-效应面法进行实验设计，以主观评分为指标，使用Design-Expert 8.0.6 Trial 进行数据拟合与分析，绘制三维效应曲面图和二维等高线图。结果确定最佳范围为A(卡波姆940)：0.05～0.065 g；B(蓖麻油)：1.00～1.12 mL；C[聚氧乙烯脱水山梨醇单油酸酯(吐温-80)]：0.15 mL。选取最佳配方为卡波姆 0.057 5 g，蓖麻油 1.1 mL，吐温-80 0.15 mL。对制得的基质进行了初步稳定性评价和一些流变学特性如黏度、触变性的考察。并以此最佳配方为基质，分别以98%芦丁、98%盐酸小檗碱和98%盐酸小檗胺为主药制备乳剂型凝胶制剂，以0.9%生理盐水为接收液，1 h内3种制剂的透皮量均在1%以下。可见，该基质具有发展成为预混辅料的潜力。该配方制得的乳剂型凝胶基质具有较好外观，具有一定的稳定性、较好黏度和触变性，在1 h内无皮肤刺激性。
[关键词]预混辅料； 乳剂型凝胶剂； 星点设计-效应面法； 体外透皮性实验
, 百拇医药
[Abstract]The purpose of this paper was to study the pre-mixed materials of emulsion gel. Accessories were screened and formula was designed with the most common use， low cost and simple process as the standards. Experiments were designed by central composite design-response surface methodology (ccd-rsm). 8.0.6 Trial Design-Expert was used for data processing and analysis， and subjective scores were used as the index to draw the three-dimensional effect surface and 2D contour maps. It was determined that the optimal ranges were A (carbomer 940)： 0.05-0.065 g； B (castor oil)： 1.00-1.12 mL； C (poly polysorbate-80)： 0.15 mL. The optimal formula was as follows： carbopol 0.057 5 g， castor oil 1.1 mL， polysorbate-80 0.15 mL. The formulated substrate was studied on its preliminary stability and rheology characteristics， such as viscosity and thixotropy. Then with the optimal formula as substrate， emulsion type gel was prepared respectively with 98% rutin， 98% berberine hydrochloride， and 98% berbamine hydrochloride as the main component. With 0.9% normal saline as the absorption solution， the results showed that the ransdermal flux of the three formulations of 1 h was all less than 1%. The results indicated that this substrate had the potential to be developed into a premixed material. The emulsion type gel matrix made from this formula had a good appearance， stability to certain extent， appropriate viscosity and thixotropy， and showed no skin irritation in 1 h.
, 百拇医药
[Key words]premixed materials； emulsion gel； ccd-rsm； transdermal experiment
預混辅料和凝胶剂都是现如今极为热门的研究领域。根据主药的性质选择最合适的辅料，不仅需要大量的实验，还需大量时间和成本；若有一种预混辅料，能与多种主药均制得较好制剂，可以很大程度上节约研发的时间和经济成本，为制剂提供便利。预混辅料作为新辅料开发中最简单、最节约时间和成本的方式，面对的将是一个广阔的世界市场。凝胶剂中水性凝胶剂研究最多，油性凝胶剂用于皮肤会带来油腻感，适用药物范围也较窄。而乳剂型凝胶基质兼有乳剂和凝胶的一些特性，洁白、细腻、富有光泽、极易涂布和洗除、无刺激且稳定，适用范围广，极具市场应用价值。
经过大量预实验筛选以及文献数据分析[1-5]，本实验以卡波姆940、蓖麻油、聚氧乙烯脱水山梨醇单油酸酯(吐温-80)为主要成分，利用星点设计-效应面法考察配方中各成分含量对基质质量的影响，通过外观评价，筛选最佳配方。并通过体外透皮实验，考察其1 h内的透皮量，证明其具有发展成新型乳剂型凝胶预混辅料的潜力。, http://www.100md.com(邱仁杰 黄艺钟 王秀丽)
[关键词]预混辅料； 乳剂型凝胶剂； 星点设计-效应面法； 体外透皮性实验
, 百拇医药
[Abstract]The purpose of this paper was to study the pre-mixed materials of emulsion gel. Accessories were screened and formula was designed with the most common use， low cost and simple process as the standards. Experiments were designed by central composite design-response surface methodology (ccd-rsm). 8.0.6 Trial Design-Expert was used for data processing and analysis， and subjective scores were used as the index to draw the three-dimensional effect surface and 2D contour maps. It was determined that the optimal ranges were A (carbomer 940)： 0.05-0.065 g； B (castor oil)： 1.00-1.12 mL； C (poly polysorbate-80)： 0.15 mL. The optimal formula was as follows： carbopol 0.057 5 g， castor oil 1.1 mL， polysorbate-80 0.15 mL. The formulated substrate was studied on its preliminary stability and rheology characteristics， such as viscosity and thixotropy. Then with the optimal formula as substrate， emulsion type gel was prepared respectively with 98% rutin， 98% berberine hydrochloride， and 98% berbamine hydrochloride as the main component. With 0.9% normal saline as the absorption solution， the results showed that the ransdermal flux of the three formulations of 1 h was all less than 1%. The results indicated that this substrate had the potential to be developed into a premixed material. The emulsion type gel matrix made from this formula had a good appearance， stability to certain extent， appropriate viscosity and thixotropy， and showed no skin irritation in 1 h.
, 百拇医药
[Key words]premixed materials； emulsion gel； ccd-rsm； transdermal experiment
預混辅料和凝胶剂都是现如今极为热门的研究领域。根据主药的性质选择最合适的辅料，不仅需要大量的实验，还需大量时间和成本；若有一种预混辅料，能与多种主药均制得较好制剂，可以很大程度上节约研发的时间和经济成本，为制剂提供便利。预混辅料作为新辅料开发中最简单、最节约时间和成本的方式，面对的将是一个广阔的世界市场。凝胶剂中水性凝胶剂研究最多，油性凝胶剂用于皮肤会带来油腻感，适用药物范围也较窄。而乳剂型凝胶基质兼有乳剂和凝胶的一些特性，洁白、细腻、富有光泽、极易涂布和洗除、无刺激且稳定，适用范围广，极具市场应用价值。
经过大量预实验筛选以及文献数据分析[1-5]，本实验以卡波姆940、蓖麻油、聚氧乙烯脱水山梨醇单油酸酯(吐温-80)为主要成分，利用星点设计-效应面法考察配方中各成分含量对基质质量的影响，通过外观评价，筛选最佳配方。并通过体外透皮实验，考察其1 h内的透皮量，证明其具有发展成新型乳剂型凝胶预混辅料的潜力。, http://www.100md.com(邱仁杰 黄艺钟 王秀丽)