盐酸普萘洛尔凝胶的制备与处方优化

发布时间：2018-04-19 07:20

本文选题：盐酸普萘洛尔 + 凝胶　；参考：《中国药房》2015年01期

【摘要】：目的:为了避免口服给药可能发生的肝脏首关效应及全身不良反应,制备盐酸普萘洛尔凝胶,并进行处方优化。方法:以水溶性氮酮为渗透促进剂,羟丙甲纤维素K4M为凝胶基质制备盐酸普萘洛尔凝胶。单因素考察法筛选盐酸普萘洛尔凝胶处方中的主药浓度、p H、保湿剂等;以8 h的累积渗透量和稳态渗透速率为指标,采用星点设计法对水溶性氮酮和羟丙甲纤维素K4M的浓度进行优化,并对最优处方进行验证。结果:最优处方为盐酸普萘洛尔3 g、水溶性氮酮1.64 g、丙二醇10 g、羟丙甲纤维素K4M2.61 g、甘油10 g、羟苯乙酯0.1 g,加水至100 g,p H为5.0~6.5;所制凝胶8 h的累积渗透量和稳态渗透速率分别为290.10μg/cm2、36.90μg/(cm2·h)。结论:成功制得渗透效果较好的盐酸普萘洛尔凝胶。
[Abstract]:Aim: to prepare propranolol hydrochloride gel and optimize its formulation in order to avoid the possible hepatic first-pass effect and systemic adverse reaction in oral administration of propranolol hydrochloride.Methods: propranolol hydrochloride gel was prepared with water-soluble azone as penetration promoter and hydroxypropylcellulose K4M as gel matrix.The main concentration of propranolol hydrochloride gel, humidifier and so on were screened by single factor method, and the cumulative osmotic capacity and steady osmotic rate of 8 h were taken as the index.The concentration of water-soluble azone and hydroxypropylcellulose K4M was optimized by star design, and the optimum formulation was verified.Results: the optimal formulation was propranolol hydrochloride 3 g, water-soluble azone 1.64 g, propylene glycol 10 g, hydroxypropyl cellulose K4M2.61 g, glycerol 10 g, hydroxyphenylethyl 0.1 g, adding water to 100g / g, and the cumulative osmotic capacity and steady-state osmotic rate of the gel were 290.10 渭 g 路cm ~ (2 +) ~ 36.90 渭 g/(cm2 路h, respectively.Conclusion: propranolol hydrochloride gel with good osmotic effect was successfully prepared.
【作者单位】：南京军区福州总医院药学科;福建卫生职业技术学院;
【基金】：福建省科技计划项目(No.闽财指〔2011〕671) 福建省中青年教师教育科研项目(No.JB13322)
【分类号】：R943

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