Preparation of Ibuprofen Lysine Sustained-release Liquid Suppository and Its Evaluation in vivo and in vi-tro / 中国药房

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 af-ter rectal administration in Beagle dogs in vivo were compared. RESULTS:When the P407-P188 ratio was 11.2,the gel tempera-ture 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.