黄依韵,何慧怡,蒋少鸿,肖婷,陆瑞斌,胡巧红,王晓明
HUANG Yiyun,HE Huiyi,JIANG Shaohong,XIAO Ting,LU Ruibin,HU Qiaohong,WANG Xiaoming

• 1:广东药科大学药学院

摘要(Abstract)：

目的制备雌二醇超分子有机原位凝胶,并考察处方工艺对其体外释药性能的影响。方法以凝胶因子棕榈酰-苯丙氨酸甲酯为载体材料,考察凝胶因子用量、抗凝剂的种类及用量等因素对凝胶形成的影响。建立雌二醇有机原位凝胶体外释放的高效液相分析方法,在恒温气浴振荡器中用动态透析法研究凝胶中雌二醇的释放特性并评价各组分对药物释放的影响。结果雌二醇有机原位凝胶的最优处方为:雌二醇3.5 mg,注射用大豆油1 mL,凝胶因子棕榈酰-苯丙氨酸甲酯300 mg,N-甲基吡咯烷酮0.6 mL。影响本制剂体外释放的主要因素是抗凝剂的种类及凝胶因子的用量,考察范围内的抗凝剂用量对体外释放影响不大,最优处方制得的凝胶可持续释放72 h以上。结论雌二醇有机原位凝胶可持续性低剂量释放药物,是理想的新型长效制剂。
OBJECTIVE To prepare the in situ organogel of estradiol,and evaluate its in vitro release. METHODS Estradiol in situ organogel was prepared by using the N-palmityl-L-phenylalanine methyl ester( C_(16)-L-Phe-OMe) as the carrier,factors such as the amounts of C_(16)-L-Phe-OMe and the type of anti-gelling solvents were inverstigated. HPLC analysis methods of in vitro release was established,releasing characteristic of estradiol from the in situ organogel was investigated using dynamic dialysis technique in vapourbathing constant temperature vibrator,and the effect on drug release of each component was evaluated. RESULTS The formulation of estradiol in situ organogel was optimized as follows: the amount of estradiol was 3.5 mg,soybean oil for injection was 1 mL,C_(16)-L-Phe-OMe was 300 g·L~(-1),and the type and amount of anti-gelling solvent was 0.6 mL of NMP. The type of anti-gelling solvent and amount of gelator had significant influence on the in vitro release. In contrast,the amount of anti-gelling solvent had only marginal influence on the in vitro release. The optimal formulation could release sustainably more than 72 h. CONCLUSION The estradiol in situ organogel prepared can achieve sustained release and is expected to be an ideal new long-term agent.

关键词(KeyWords)： 雌二醇;凝胶因子;有机原位凝胶;体外释放
estradiol;gelator;in situ organogel;in vitro release

Abstract:

Keywords:

基金项目(Foundation): 广东药科大学“创新强校工程”资助项目(2016KQNCX083);; 广东药学院省级大学生创新创业训练计划项目(201510573023)

作者(Author): 黄依韵,何慧怡,蒋少鸿,肖婷,陆瑞斌,胡巧红,王晓明
HUANG Yiyun,HE Huiyi,JIANG Shaohong,XIAO Ting,LU Ruibin,HU Qiaohong,WANG Xiaoming

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