CAJ | 학술논문

目的：了解国产舒他西林胶囊的相对生物利用度，评价其生物等效性。方法：10名健康志愿者随机交叉po单剂量750mg国产舒他西林胶囊和进口片剂后，采用HPLC测定血浆中的血药浓度。结果：口服国产舒他西林胶囊和进口片剂后，利用HPLC测得血浆中药物浓度舒巴坦分别在(38.66±10.39)min和(36.68±11.37)min达到峰值(3.45±2.63)mg.L-1和(4.21±3.67)mg.L-1；氨苄西林分别在(26.13±5.98)min和(28.00±7.54)min达到峰值(7.11±2.19)mg.L-1和(7.46±2.79)mg.L-1。血药浓度曲线下面积舒巴坦分别为(629.98±177.34)mg.min.L-1和(687.78±225.44)mg.min.L-1；氨苄西林分别为(693.87±192.15)mg.min.L-1和(708.87±202.48)mg.min.L-1。经药动力学程序计算拟合后，发现氨苄西林和舒巴坦在体内的过程符合一级吸收和消除的二室模型。国产舒他西林胶囊的相对生物利用度舒巴坦为95%(81%～118%)，氨苄西林为99%(81%～115%)两药的主要药代动力学参数无显著性差异(P＞0.05)。结论：国产舒他西林胶囊和进口片剂具有生物等效性。
목적：료해국산서타서림효낭적상대생물이용도，평개기생물등효성。방법：10명건강지원자수궤교차po단제량750mg국산서타서림효낭화진구편제후，채용HPLC측정혈장중적혈약농도。결과：구복국산서타서림효낭화진구편제후，이용HPLC측득혈장중약물농도서파탄분별재(38.66±10.39)min화(36.68±11.37)min체도봉치(3.45±2.63)mg.L-1화(4.21±3.67)mg.L-1；안변서림분별재(26.13±5.98)min화(28.00±7.54)min체도봉치(7.11±2.19)mg.L-1화(7.46±2.79)mg.L-1。혈약농도곡선하면적서파탄분별위(629.98±177.34)mg.min.L-1화(687.78±225.44)mg.min.L-1；안변서림분별위(693.87±192.15)mg.min.L-1화(708.87±202.48)mg.min.L-1。경약동역학정서계산의합후，발현안변서림화서파탄재체내적과정부합일급흡수화소제적이실모형。국산서타서림효낭적상대생물이용도서파탄위95%(81%～118%)，안변서림위99%(81%～115%)량약적주요약대동역학삼수무현저성차이(P＞0.05)。결론：국산서타서림효낭화진구편제구유생물등효성。
OBJECTIVE：To observe the relative bioavailability of domestic sultamicillin and evaluate the bioequivalence between the domestic capsule and the imported tablet.METHODS:The pharmacokinetics of sultamicillin capsule was determined following a single oral dose of 750mg give to 10 volunteers in an open randomized crossover study.Drug concentration in plasma was assayed by HPLC method.RESULTS:The sulbactam peak levels in plasma averaged(3.45±2.63) and (4.21±3.67)mg.L-1 at (38.66±10.39)and(36.68±11.37)min,respectively.The ampicillin peak levels in plasma averaged(7.11±2.19)and(7.46±2.79)mg.L-1 at(26.13±5.98)and(28.00±7.54)min,respectively.The AUC were (629.98±177.34) and (687.78±225.44)mg.min.L-1for (693.87±192.15) and (708.87±202.48)mg.min.L-1 for domestic capsule and improrted tablet respectively.The concentration-time courses after medication conformed to a 2-compartment open model with a first order obsorption.The sulbactam bioavailability of domestic capsule was 95%(81%～118%),the ampicillin bioavailability of it was 99%(81%～115%) compared with the standard preparation.The pharmacokinetic parameters between two products had no significant difference (P＞0.05).CONCLUSION:The two formulations were of bioequivalence.