In Vitro and In Vivo Evaluation of Proniosomes Containing Celecoxib for Oral Administration
In Vitro and In Vivo Evaluation of Proniosomes Containing Celecoxib for Oral Administration
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DOI：
10.1208/s12249-009-9364-5
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发表时间：
2010-03-01
影响因子：
3.3
通讯作者：
Nasr, Mohamed
中科院分区：
文献类型：
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作者：
Nasr, Mohamed
本研究的目的是制备塞来昔布前体，并评价前体制剂对人体口服生物利用度的影响。开发了一种新的用于水溶性差的药物如塞来昔布的前体给药系统，并进行了体内外研究。以胆固醇、司盘60和磷酸双十六烷基酯为原料，采用顺序喷雾法制备了前体，其摩尔比分别为1：1：0.1。塞来昔布前体类囊泡的平均包封率约为95%。与纯药物粉末相比，所制备的前体显示出塞来昔布溶出的显著增强。在人类志愿者中研究了200 mg单剂量塞来昔布前体制剂和常规市售塞来昔布胶囊的生物利用度。所获得的结果表明，与常规胶囊相比，前体制剂显著改善了塞来昔布的吸收程度。前体制剂相对于常规胶囊的平均相对生物利用度为172.06 +/-0.14%。塞来昔布作为前体胶囊给药时，其平均Tmax延长。两种塞来昔布制剂的K-el和t（1/2）值之间无显著差异。结论：塞来昔布前体口服给药系统具有良好的生物利用度。
The objectives of this research were to prepare celecoxib proniosomes and evaluate the influence of proniosomal formulation on the oral bioavailability of the drug in human volunteers. Anew proniosomal delivery system for a poorly water-soluble drug such as celecoxib was developed and subjected to in vitro and in vivo studies. Proniosomes were prepared by sequential spraying method, which consisted of cholesterol, span 60, and dicetyl phosphate in a molar ratio of 1:1: 0.1, respectively. The average entrapment percent of celecoxib proniosome-derived niosomes was about 95%. The prepared proniosomes showed marked enhancement in the dissolution of celecoxib as compared to pure drug powder. The bioavailability of 200 mg single dose of both celecoxib proniosomal formulation and a conventional marketed celecoxib capsule was studied in human volunteers. The obtained results show that the proniosomal formulation significantly improved the extent of celecoxib absorption than conventional capsule. The mean relative bioavailability of the proniosomal formulation to the conventional capsule was 172.06 +/- 0.14%. The mean T-max for celecoxib was prolonged when given as proniosomal capsule. There was no significant difference between the values of K-el and t(1/2) for both celecoxib preparations. In conclusion, the proniosomal oral delivery system of celecoxib with improved bioavailability was established.