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FORMULATION AND EVALUATION OF TOPICAL MICROEMULGEL LOADED WITH TERBINAFINE HCL MICROEMULSION

机译:特比萘芬盐酸盐微乳负载的局部微乳的制备与评价

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The aim of the present study was to investigate the potential of a micro-emulgel formulation for topical delivery of Terbinafine. Terbinafine showed highest solubility in propylene glycol among the available oil phase. Tween 80 and polyethylene glycol 400 were used as surfactant and co-surfactant respectively. Using pseudo-ternary phase diagram 1:2 ratio of surfactant: co-surfactant was selected. Using Central Composite Design thirteen formulations with varying ranges of Smix and oil phase were prepared. Final formulation was selected on the basis of transmittance. From optimization plot it was concluded that 27.93% of Smix and 6.51% of oil phase gave maximum transmittance. Then, optimized formulation was used to prepare final microemulgel of terbinafine. Thirteen gel formulation from varying concentration of carbopol 934 and hydroxypropylmethyl cellulose was prepared and evaluated for extrudability, spread ability, drug content, in-vitro drug release, rheological study and in-vitro antifungal activity against Teniapedis. Formulations with suitable consistencies were selected and optimization was done on the basis of drug release and ex-vivo permeation study in goat skin. Formulation with 0.45gm of carbopol 934 and 0.3gm of HPMC showed better drug release and skin permeation than other formulations. This formulation was further compared with marketed terbinafine ointment and was found to give enhanced drug release and permeation.
机译:本研究的目的是研究微乳胶制剂对特比萘芬局部给药的潜力。在可用的油相中,特比萘芬在丙二醇中的溶解度最高。吐温80和聚乙二醇400分别用作表面活性剂和助表面活性剂。使用拟三元相图,选择表面活性剂:助表面活性剂的比例为1∶2。使用Central Composite Design,制备了十三种具有不同范围的S mix 和油相的配方。根据透射率选择最终配方。从优化图中得出结论,S.mix 的27.93%和油相的6.51%给出了最大透射率。然后,使用优化的配方制备特比萘芬的最终微乳胶。制备了13种来自不同浓度的carbopol 934和羟丙基甲基纤维素的凝胶制剂,并对其挤出性,铺展能力,药物含量,体外药物释放,流变学研究和针对Teniapedis的体外抗真菌活性进行了评估。选择具有合适稠度的制剂,并根据药物释放和离体在山羊皮肤中的渗透研究进行优化。与其他配方相比,用0.45 gm的carbopol 934和0.3 gm的HPMC配制的药物释放和皮肤渗透性更好。将该制剂与市售的特比萘芬软膏进行了进一步的比较,发现该制剂具有增强的药物释放和渗透性。

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