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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 |
| 阅读数： | 372 次 |
| 本月下载数： | 4 次 |
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