Pharmacokinetic profile of carbamazepine and its metabolites on Javanese and Chinese ethnics in Indonesia

Indonesian Journal of Pharmacy

Mulyadi Djojosaputro¹  A. Aziz Hubeis²  Sugiyanto³  M. Ismadi⁴ 

[1] Bagian Farmakologi, Fakultas Kedokteran, Universitas Gadjah Mada, Yogyakarta,;Fakultas Farmasi, Universitas Airlangga, Surabaya;Fakultas Farmasi, Universitas Gadjah Mada, Yogyakarta;Fakultas Kedokteran, Universitas Gadjah Mada Yogyakarta;

关键词: Carbamazepine;    Javanese;    Chinese;    pharmacokinetics;    epilepsy;   

DOI  :  http://dx.doi.org/10.14499/indonesianjpharm0iss0pp1-7

来源: DOAJ

【 摘 要 】

Carbamazepine(CBZ)isananticonvulsantwidelyusedforepilepsy treatment. However, it is difficulttoestablish suitable dosageregimensforthis drug because of the variation on its pharmacokinetics profiles. A lot of evidences indicatethatethnicdifferencesmayaffectpharmacokineticsandhencedosage requirements. The study was conducted to document pharmacokinetic profile of CBZanditsmetabolitesonJavaneseandChineseethnicsinIndonesia.The study was carried out in 26 Javanese and 24 Chinese ethnics healthy volunteers, Bloodsampleswerecollectedserially.Carbamazepineanditsmetabolites wasassayedbyHPLC.Theresultsshowedthatnosignificantdifferences inpharmacokineticparameterswereobservedbetweenbothethnics.The valuesofAUC0-~, Cmax,Tmax,andt1/2 CBZonJavaneseethnicare652.44± 254.79µg/mL.h,8.93±3.58µg/mL,11.53±2.16h,and43.70±12.50h respectively,whileonChineseethnicare830.27±809.57µg/mL.h,13.29± 17.46µg/mL,9.97±2,90h,and41.27±13.50h,respectively.However,a significantinterindividualvariationinCBZmetabolismwasobservedinboth ethnicsasshownin itslargevariation in metabolicratio.Themetabolic10,11-epoxideCBZandtrans-10,11CBZconcentrationratioonJavaneseethnic are 0.07 ± 0.03 and 0.13 ± 0.14, while on Chinese ethnic are 0.35 ± 0.99 and 0.14± 0.11. Itcanbeconcluded,thatthePharmacokineticofCBZandits metabolitesonJavenesethnicisnotdifferentcomparedtoChineseethnic.In addition, thereisasignificantinterindividualvariationinpharmacokinetics profile on both ethnics.

【 授权许可】

Unknown