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《Chinese Journal of Clinical Pharmacy》 2010-06
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Effect of pH regulators on the oral bioavailability of scutellarin in rats

LI Yuping~1,ZHANG Libin~1,TIAN Feifei~2,WENG Weiyu~2(1 Department of Pharmacy,Shanghai Pulmonary Hospital, School of Medicine,Tongji University,Shanghai 200433,China;2 School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China)  
AIM To evaluate the effect of pH regulators on the oral bioavailability of scutellarin in rats.METHODS The plasma concentration of scutellarin,the primary active ingredient in breviscapine,was determined by an HPLC-UV method.Rats received the following 3 treatment regimens at an oral dose of 40 mg·kg~(-1)(calculated with reference to scutellarin):(A) breviscapine suspension without pH regulators;(B) pre-administration with sodium bicarbonate -citric acid buffer(pH 6.2),then breviscapine suspension without pH regulators;(C) breviscapine suspension adjusted to pH 6.2 with sodium bicarbonate-citric acid buffer.RESULTS The relative bioavailability to treatment regimen A was 183.1%and 162.4%for treatment B and C,respectively.No significant difference in AUC_(0→t) between treatments regimen B and regimen C was observed.In treatment regimen A,about 1-2 h of lag time was observed for each rat, while scutellarin was absorbed rapidly and reached the first peak concentration within 15 min in treatment regimen B and regimen C.The profile of the solubility of scutellarin versus pH showed that scutellarin was poorly soluble at low pH and the solubility rose as the pH increased.CONCLUSION The pH value is an important influencing factor in absorption of scutellarin after oral administration.Pre-administration and co-administration of pH regulators to elevate gastric pH could increase the solubility of scutellarin,which result in shorter lag time and higher bioavailability in rats.
【CateGory Index】: R285.5
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