曲安奈德微乳透皮凝胶的优选。

Q3 Medicine
Swati Jagdale, Bhagyashree Chaudhari
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引用次数: 9

摘要

背景:曲安奈德是一种长效皮质类固醇,用于治疗关节炎、湿疹、牛皮癣和引起炎症的类似疾病。曲安奈德的半衰期为88分钟。如多项专利所述,长期口服与消化性溃疡、腹胀和溃疡性食管炎等胃肠道不良反应有关。微凝胶具有稳定性好、载药量大、缓释可控等优点,尤其适用于半衰期短的药物。目的:优化曲安奈德微凝胶经皮给药工艺。方法:测定曲安奈德在各种油脂、表面活性剂和助表面活性剂中的饱和溶解度。构造了伪三元相图,确定了透明微乳的区域。对微乳液的粒径(FE-SEM, zetasizer),透光率,pH,粘度,电导率等进行了评价。通过实验设计对微乳液凝胶进行优化。以Carbopol 971P和HPMC K100M为自变量。微乳液凝胶的体外和离体参数进行了评价。结果:以油酸、月桂醇催化裂化剂和丙二醇配制微乳液。PDI为0.197,表明微乳液为单分散。32因子设计以F8批次为最优。设计专家建议药物释放;凝胶粘度和生物黏附强度是影响透皮给药的三个重要因素。F8经卵膜释放率为92.62.16±1.22%,经山羊皮释放率为95.23±1.44%,符合korsmemeyer - peppas释放模型。结论:优选出一种稳定、有效的曲安奈德缓释透皮微乳。这将是一种很有前途的工具,可以提高曲安奈德的生物利用度,减少给药频率。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Optimization of Microemulsion Based Transdermal Gel of Triamcinolone.

Background: Triamcinolone is a long acting corticosteroid used in the treatment of arthritis, eczema, psoriasis and similar conditions which cause inflammation. Triamcinolone has half-life of 88min. Prolonged oral use is associated with gastrointestinal adverse effects as peptic ulcer, abdominal distention and ulcerative esophagitis as described in various patents. Microemulgel offers advantage of better stability, better loading capacity and controlled release especially for drug with short half life.

Objective: Objective of the present study was to optimize microemulgel based transdermal delivery of triamcinolone.

Method: Saturated solubility of triamcinolone in various oils, surfactants and co-surfactants is estimated. Pseudo-ternary phase diagrams were constructed to determine the region of transparent microemulsion. Microemulsion was evaluated for globule size (FE-SEM, zetasizer), % transmittance, pH, viscosity, conductivity etc. Design of experiment was used to optimize microemulsion based gel. Carbopol 971P and HPMC K100M were used as independent variables. Microemulsion based gel was evaluated for in-vitro as well as ex-vivo parameters.

Results: Microemulsion was formulated with oleic acid, lauroglycol FCC and propylene glycol. PDI 0.197 indicated microemulsion is mono-disperse. 32 factorial design gave batch F8 as optimized. Design expert suggested drug release; gel viscosity and bio-adhesive strength were three significant dependant factors affecting the transdermal delivery. F8 showed drug release 92.62.16±1.22% through egg membrane, 95.23±1.44% through goat skin after 8hr and Korsmeyer-Peppas release model was followed.

Conclusion: It can be concluded that a stable, effective controlled release transdermal microemulgel was optimised for triamcinolone. This would be a promising tool to deliver triamcinolone with enhanced bioavailability and reduced dosing frequency.

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来源期刊
Recent patents on anti-infective drug discovery
Recent patents on anti-infective drug discovery Medicine-Pharmacology (medical)
CiteScore
2.40
自引率
0.00%
发文量
1
期刊介绍: Recent Patents on Anti-Infective Drug Discovery publishes review articles on recent patents in the field of anti-infective drug discovery e.g. novel bioactive compounds, analogs & targets. A selection of important and recent patents on anti-infective drug discovery is also included in the journal. The journal is essential reading for all researchers involved in anti-infective drug design and discovery.
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