Tjandrawinata Raymond R, Setiawati Effi, Putri Ratih Sofia Ika, Yunaidi Danang Agung, Amalia Fawzia, Susanto Liana W
Dexa Laboratories of Biomolecular Sciences, Cikarang, Indonesia.
PT Equilab International, Bioavailability and Bioequivalence Laboratory, Jakarta, Indonesia.
Drug Des Devel Ther. 2014 Sep 4;8:1249-55. doi: 10.2147/DDDT.S69326. eCollection 2014.
The current study was conducted to find out whether two oral preparations of 300 mg gabapentin (the test and reference capsules) were bioequivalent.
This was a randomized, single-blind, crossover study under fasting condition, with a 7-day washout period, which included 37 healthy adult male and female subjects. After an overnight fast, subjects were given, orally, one capsule of the test drug or of the reference drug. Blood samples were drawn immediately before taking the drug, then at 20 and 40 minutes, and 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 15, and 24 hours after dosing, to evaluate pharmacokinetic parameters of the single dose administration, ie, the area under the plasma concentration-time curve (AUC) from time zero to 24 hours (AUCt), AUC from time zero to infinity (AUC(inf)), the peak plasma concentration of the drug (Cmax), time needed to achieve Cmax (tmax), and the elimination half-life (t1/2). The plasma concentrations of gabapentin were determined using validated high-performance liquid chromatography with ultraviolet detection.
The geometric mean ratios (90% confidence interval) of the test drug/reference drug for gabapentin were 103.15% (90.38%-117.72%) for AUCt, 103.53% (90.78%-118.07%) for AUC(inf), and 108.06% (96.32%-121.24%) for Cmax. The differences in tmax and t1/2 values between the test and reference drug products for gabapentin were not statistically significant. Light-headedness, nausea, and headache were encountered during the study, but they were all mild and well tolerated. The 90% confidence intervals of the test/reference AUC ratio and Cmax ratio of gabapentin were within the acceptance range for bioequivalence.
The two preparations of gabapentin 300 mg capsule were bioequivalent, thus both can be used interchangeably in the clinical setting.
开展本研究以确定两种300毫克加巴喷丁口服制剂（受试胶囊和参比胶囊）是否生物等效。
这是一项在禁食条件下进行的随机、单盲、交叉研究，洗脱期为7天，纳入了37名健康成年男性和女性受试者。经过一夜禁食后，受试者口服一粒受试药物胶囊或参比药物胶囊。在服药前即刻、服药后20和40分钟以及1、1.5、2、2.5、3、4、5、6、8、10、12、15和24小时采集血样，以评估单剂量给药的药代动力学参数，即从0至24小时的血浆浓度-时间曲线下面积（AUCt）、从0至无穷大的AUC（AUC(inf)）、药物的血浆峰浓度（Cmax）、达到Cmax所需时间（tmax）以及消除半衰期（t1/2）。采用经过验证的高效液相色谱-紫外检测法测定加巴喷丁的血浆浓度。
加巴喷丁受试药物/参比药物的几何平均比值（90%置信区间）为：AUCt为103.15%（90.38%-117.72%），AUC(inf)为103.53%（90.78%-118.07%），Cmax为108.06%（96.32%-121.24%）。加巴喷丁受试药物和参比药物产品在tmax和t1/2值上的差异无统计学意义。研究期间出现了头晕、恶心和头痛，但均为轻度且耐受性良好。加巴喷丁受试/参比AUC比值和Cmax比值的90%置信区间在生物等效性的可接受范围内。
两种300毫克加巴喷丁胶囊制剂生物等效，因此在临床环境中两者可互换使用。
