Garnett W R, Levy B, McLean A M, Zhang Y, Couch R A, Rudnic E M, Pellock J M, Belendiuk G W
Department of Pharmacy, Virginia Commonwealth University Medical College of Virginia, Richmond 23298-0533, USA.
Epilepsia. 1998 Mar;39(3):274-9. doi: 10.1111/j.1528-1157.1998.tb01372.x.
A new capsule dosage form of carbamazepine (CBZ) has been developed, consisting of three different types of beads (immediate-release, extended-release, and enteric-release) that may be taken sprinkled on food or swallowed for easy administration. We compared the pharmacokinetics of the extended-release dosage form of CBZ (Carbatrol capsules) twice daily with the conventional immediate-release formulation of CBZ four times daily.
The randomized, double-blind, two-way, cross-over study was conducted at two sites, with a planned sample size of 24 adult patients with epilepsy. Each treatment was administered for 2 weeks. At the end of the 2-week period, blood samples were obtained hourly for a 24-h period.
The 90% confidence intervals (CI) of the ratio of the means of the extended-release formulation twice daily to the immediate-release formulation four times daily were within the range of 0.80-1.25 for each of the pharmacokinetic parameters for CBZ and for the summation of CBZ and CBZ-epoxide (CBZ-E). There was no difference in the frequency of seizures between treatment (p = 0.103).
Our results demonstrate that extended-release CBZ twice daily was bioequivalent to immediate-release CBZ four times daily, with regard to CBZ levels and summation of CBZ and CBZ-E levels, based on the pharmacokinetic parameters evaluated. Substituting one formulation for the other did not cause patients to have a significant change in seizure frequency.
已研发出一种新的卡马西平（CBZ）胶囊剂型，它由三种不同类型的微丸（速释、缓释和肠溶）组成，可以撒在食物上服用或直接吞服，便于给药。我们比较了卡马西平缓释剂型（Carbatrol胶囊）每日两次与传统卡马西平速释制剂每日四次的药代动力学。
该随机、双盲、双向、交叉研究在两个地点进行，计划样本量为24名成年癫痫患者。每种治疗给药2周。在2周疗程结束时，在24小时内每小时采集血样。
对于卡马西平以及卡马西平和卡马西平-环氧化物（CBZ-E）总和的每个药代动力学参数，每日两次缓释制剂与每日四次速释制剂均值之比的90%置信区间（CI）在0.80 - 1.25范围内。治疗之间癫痫发作频率无差异（p = 0.103）。
我们的结果表明，基于所评估的药代动力学参数，就卡马西平水平以及卡马西平和卡马西平-环氧化物水平总和而言，每日两次缓释卡马西平与每日四次速释卡马西平生物等效。用一种制剂替代另一种制剂不会使患者癫痫发作频率发生显著变化。
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