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Pharmacokinetic behaviors and oral bioavailability of oridonin in rat plasma

Acta Pharmacologica Sinica 2006年第12期27卷 1642-1646页

作者： Wen XU~2 Jin SUN~2 Ting-ting ZHANG~2 Bo MA~2 Sheng-miao CUI~3 Da-wei CHEN~2 Zhong-gui HE~(2,4)2 Department of Pharmaceutics,School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China 3 Department of Pharmacy,Guangdong Pharmaceutical University,Guangzhou 510006,China DepartmentofPharmaceutics SchoolofPharmacyShenyangPharmaceuticalUniversityShenyang110016China DepartmentofPharmacy GuangdongPharmaceuticalUniversityGuangzhou510006China

Aim:To study the intravenous and oral pharmacokinetic behavior of oridonin andits extent of absolute oral bioavailability in rats.Methods:Oridonin was adminis-tered to rats via iv(5,10 and 15 mg/kg),po(20,40 and 80 mg/kg)or ip administra-tion(10 mg/kg).The concentrations of oridonin in rat plasma were determined bya high performance liquid chromatography with electrospray ionization mass spec-trometric detection(HPLC/ESI-MS)method and the pharmacokinetic parameterswere determined by non-compartmental analysis.Results:The plasma concen-tration of oridonin after intravenous administration decreased polyexponentially,and the pharmacokinetic parameters of oridonin were dose-independent withinthe examined range.Oridonin was absorbed rapidly after oral gavage with a t(max)ofless than 15 min;the extent of absolute bioavailability of oridonin following oraladministration was 4.32%,4.58% and 10.8%.The extent of absolute bioavailabilityof oridonin following intraperitoneal administration was 12.6%.Conclusion:Firstorder rate pharmacokinetics were observed for oridonin within the range of ivdoses,while the extent of absolute oral bioavailability was rather low and dose-dependent.The low and dose-dependent extent of oral bioavailability may be dueto the saturation of first-pass effects.

关键词： oridonin pharmacokinetics intravenous oral bioavailability intraperitoneal injections rats

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Photodynamic treatment of subcutaneous tumors in mice with photofrin Ⅱ and Argon ion laser

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CHINESE MEDICAL JOURNAL 1996年第1期109卷 83-88页

作者： Jyh-Sheng You Dou-Mong Hau Gung-Tung Chen Hui-Feng Huang Wang-Chi Chen I-Hsin Lin InstituteofRadiationBiology NationalTsingHuaUniversityTaiwan ChineseMedicalDepartment ChinaMedicalCollegeHospitalTaichung40421Taiwan

OBJECTIVE To investigate the combined effects of photofrin (Pf) Ⅱ and laser irradiation on mice bearing subcutaneous tumors.METHODS Ehrlish ascites tumor cells (1×107) were implanted subcutaneously into the breast area of ICR mice. The tumors, when grew up to 0.55±0.15cm3, was administered of laser irradiation (514.5nm, 112.5mW/cm2 for 11.12 min with a total energy 75J/cm2) after intraperitoneal injection of Pf Ⅱ (5, 7.5, 10 and 15mg/kg body weight) once a day for three successive days.RESULTS The mortality rate (MR120) in the tumor control was 93.7% and the mean survival time (MST120) was 46.6 days. The best therapeutic effect (50% mortality rate, 53.8% tumor control rate and mean survival time 86 days) was observed in the group treated with 7.5mg of Pf Ⅱ per kg of body weight and total irradiation energy of 75J/cm2 (112.5mW/cm2 for 11.12 min) with 514.5nm argon ion laser light.CONCLUSIONS The effect on the survival rate of tumor cells and synthetic rates of DNA, RNA and protein were obviously inhibited, as the dose of pf Ⅱ and laser irradiation increased.

关键词： Mean Survival Time intraperitoneal injections Laser radiation Argon Mortality Survival Rate Business travel Inbred ICR Mice Laser Tumours

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