首页> 外国专利> FORMULATION AND EVALUATION OF POLOXAMER-407 AND HPMC K 15 M BASED THERMOSENSITIVE SOL-GEL TRANSITION SYSTEM OF DORZOLAMIDE HYDROCHLORIDE

FORMULATION AND EVALUATION OF POLOXAMER-407 AND HPMC K 15 M BASED THERMOSENSITIVE SOL-GEL TRANSITION SYSTEM OF DORZOLAMIDE HYDROCHLORIDE

机译：基于泊洛沙姆-407和HPMC K 15 M的热敏性溶胶-凝胶转变体系的研究与评价

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In the present invention, we have disclosed thermosensitive sol-gel transition system of Dorzolamide hydrochloride for glaucoma treatment. The developed sol- gel transition system effectively formed gel at physiological temperature 37� C. with sustained appearance upto 8 hours after instillation in cul de sac. The developed formulation contains 0.5 % Dorzolamide Hydrochloride as effective to minimise intra ocular pressure although it is % th dose of marketed formulation. The thermosensitive property of developed formulation is due to poloxamer 407 polymer in the range of 16-20 % w/v where as sustained release property is due to viscosity enhancer polymer HPMC K 15 M in the range of 0.5 - 1% w/v. We evaluated 0.01 % v/v benzalkonium chloride as effective preservative in developed formulation. Optimized formulation successfully sustained release of drug upto 5 hours in ex vivo goat corneal permeability study. Comparative in vivo study in normotensive rabbits showed that optimized formulation sustained therapeutic effect upto 8 hours. Table 1 : The composition of developed thermosensitive sol - gel phase transition system Dorzolamide Poloxamer 407 HPMC K15M Benzalkoniumm chloride Sodium Chloride Puri. Water Hydrochloride (%w/v) (%w/v) (%w/v) (%v/v) (%w/v) q.s.(ml) Fl 0.5 16 0.5 0.01 0.5 10 F2 0.5 16 0.75 0.01 0.5 10 F3 0.5 16 1.0 0.01 0.5 10 F4 0.5 18 0.5 0.01 0.5 10 F5 0.5 18 0.75 0.01 0.5 10 F6 0.5 18 1.0 0.01 0.5 10 F7 0.5 20 0.5 0.01 0.5 10 F8 0.5 20 0.75 0.01 0.5 10 F9 0.5 20 1.0 0.01 0.5 10

机译：在本发明中，我们已经公开了用于青光眼治疗的盐酸多佐酰胺的热敏溶胶-凝胶转变系统。发达的溶胶-凝胶过渡系统可在37°C的生理温度下有效地形成凝胶，并在注入死囊后长达8小时持续出现。所开发的配方含有0.5％的盐酸多佐胺，可有效降低眼内压，尽管它是市售配方的％剂量。所开发配方的热敏性能归因于泊洛沙姆407聚合物在16-20％w / v的范围内，而缓释性能归因于粘度增强剂聚合物HPMC K 15 M在0.5-1％w / v的范围内。我们评估了0.01％v / v的苯扎氯铵作为开发配方中的有效防腐剂。在离体山羊角膜通透性研究中，优化的配方成功地将药物持续释放长达5小时。在血压正常的兔子中进行的体内比较研究表明，优化的制剂可维持长达8小时的治疗效果。表1：已开发的热敏溶胶-凝胶相变系统Dorzolamide Poloxamer 407 HPMC K15M苯扎氯铵氯化钠Puri的组成。盐酸盐水（％w / v）（％w / v）（％w / v）（％v / v）（％w / v）qs（ml）Fl 0.5 16 0.5 0.01 0.5 10 F2 0.5 16 0.75 0.01 0.5 10 F3 0.5 16 1.0 0.01 0.5 10 F4 0.5 18 0.5 0.01 0.5 10 F5 0.5 18 0.75 0.01 0.5 10 F6 0.5 18 1.0 0.01 0.5 10 F7 0.5 20 0.5 0.01 0.5 10 F8 0.5 20 0.75 0.01 0.5 10 F9 0.5 20 1.0 0.01 0.5 10

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公开/公告号IN2014MU02680A

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公开/公告日2016-03-18

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申请/专利号IN2680/MUM/2014
发明设计人 DR CHANDRAKANT RAJARAM KOKARE;MR ROHAN KRISHNA BARSE;MR UMESH DILIP LADDHA;DR AMOL AMBADAS TAGALPALLEWAR;
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申请日2014-08-21
分类号A61K31/416;
国家 IN
入库时间 2022-08-21 14:25:21

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