青霉素V钾胶囊与片剂的药物动力学及相对生物利用度比较

Pharmacokinetics and bioavailability of a phenoxymethylpenicillin capsule compared to tablet

目的 :比较青霉素 V钾胶囊与片剂的药物动力学及相对生物利用度。方法 :以微生物法测定 10名健康受试者单次空腹 po青霉素 V钾胶囊和片剂 5 0 0 m g后血、尿药浓度。结果 :po青霉素 V钾胶囊和片剂后的体内过程符合二室模型 ,其平均cmax分别为 ( 8.2 2± 1.2 1)和 ( 7.71± 1.0 9) mg/ L,tmax为 ( 0 .5 5± 0 .11)和 ( 0 .5 8± 0 .17) h,T1 /2 ka为 ( 0 .2 1± 0 .0 9)和 ( 0 .2 0± 0 .0 6 )h,T1 /2β为 ( 0 .81± 0 .2 1)和 ( 0 .72± 0 .0 8) h,AUC为 ( 9.5 1± 1.0 6 )和 ( 9.5 0± 1.82 ) h· mg/ L,2 4h累积尿排出率分别为给药量的 ( 35 .33± 7.45 ) %和 ( 37.80± 5 .45 ) %。青霉素 V钾胶囊与片剂的药物动力学参数间差异无统计学意义 ( P>0 .0 5 )。结论 :青霉素 V钾胶囊的相对生物利用度为 ( 10 1.44± 9.5 9) % 。

AIM: To study the pharmacokinetics and relative bioavailability of phenoxymethylpenicillin potassium capsule compared to the tablet. METHODS: Serum and urine concentrations were measured by microbiological assay in 10 healthy volunteers with random crossover oral dose of 500 mg capsule and tablet. Pharmacokinetic parameters and bioavailabilities of 2 preparations were compared. RESULTS: The serum concentrationtime curves appeared to fit the twocompartment open model. c max were (82±121) and (771±109) mg/L; t max (055±011) and (058±017) h; T 1/2ka (021±009) and (020±006) h; T 1/2β (081±021) and (072±008) h; AUC (951±106) and (950±182) h·mg/L respectively. The urinery recovery rates within 24 h were (3533±745)% and (3780±545)% respectively. CONCLUSION: The differences of the above parameters between the capsule and tablet groups are no statistic significance (P>005). The relative bioavailability of phenoxymethylpenicillin potassium capsules was (10144±959)%. There is bioequivalence between the 2 preparations.