赖氨酸布洛芬缓释液体栓的制备及体内外评价
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篇名: 赖氨酸布洛芬缓释液体栓的制备及体内外评价
TITLE:
摘要: 目的:制备赖氨酸布洛芬缓释液体栓剂,并进行体内外评价。方法:以泊洛沙姆溶液为主要基质、卡波姆为生物黏附剂、月桂氮酮为渗透剂,制备赖氨酸布洛芬缓释液体栓剂。以胶凝温度、凝胶强度、生物黏附力及体外释放度为指标筛选泊洛沙姆407(P407)-泊洛沙姆188(P188)比例和卡波姆的含量,比较所制液体栓剂与普通固体栓剂经直肠给药后在Beagle犬体内的药-时曲线和药动学参数。结果:处方中P407-P188比例为1 ∶ 1.2时缓释液体栓剂的胶凝温度为30.4~38.1 ℃,最接近直肠温度;卡波姆含量为0.8%时缓释液体栓剂的体外释放符合零级方程,相关性最好(R2=0.996)。普通固体栓的tmax为3.206 h,随后血药浓度下降明显,缓释时间不超过12 h,AUC0-∞为501.826 mg·h/L;缓释液体栓剂的tmax为8.814 h,随后血药浓度下降,缓释时间超过24 h, AUC0-∞为715.489 mg·h/L。结论:成功制得赖氨酸布洛芬缓释液体栓剂,与普通固体栓剂比较其缓控释效果更佳、体内外相关性良好。
ABSTRACT: OBJECTIVE: To prepare Ibuprofen lysine sustained-release liquid suppository, and conduct the evaluation in vivo and in vitro. METHODS: Ibuprofen lysine sustained-release liquid suppository was prepared by using Poloxamer solution as main matrix, carbomer as bioadhesive agent, laurocapram as penetrant. The ratios of poloxamer 407 (P407)-poloxamer 188 (P188) and carbomer content were screened by using gel temperature, gel intensity, biological adhesion and release rate in vitro as indexes, and the concentration-time curves and pharmacokinetic parameters of prepared liquid suppository and common solid suppository after rectal administration in Beagle dogs in vivo were compared. RESULTS: When the P407-P188 ratio was 1 ∶ 1.2, the gel temperature of sustained-release liquid suppository was 30.4-38.1 ℃, which was the nearest to the rectal temperature; when the content of carbomer was 0.8%, the in vitro release of sustained-release liquid suppository was in zero-order model, with favorable correlation (R2=0.996). The tmax of common solid suppository was 3.206 h, then plasma concentration decreased significantly, release time did not exceed 12 h, AUC0-∞ was 501.826 mg·h/L; tmax of sustained-release liquid suppository was 8.814 h, then plasma concentration decreased, release time exceeded 24 h, AUC0-∞ was 715.489 mg·h/L. CONCLUSIONS: Ibuprofen lysine sustained-release liquid suppository is successfully prepared, which shows better sustained-release effect and excellent correlation in vivo and in vitro than common solid suppository.
期刊: 2017年第28卷第10期
作者: 韩竹俊,张学娟,程锦
AUTHORS: HAN Zhujun,ZHANG Xuejuan,CHENG Jin
关键字: 赖氨酸布洛芬;缓释液体栓;释放度;药动学
KEYWORDS: Ibuprofen lysine; Sustained-release liquid suppository; Release rate; Pharmacokinetics
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