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首页> 外文期刊>Veterinarski glasnik >Predicting absorption and pharmacokinetic profile of carbamazepine from controlled-release tablet formulation in humans using rabbit model
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Predicting absorption and pharmacokinetic profile of carbamazepine from controlled-release tablet formulation in humans using rabbit model

机译：使用兔模型从控释片剂中预测卡马西平的吸收和药动学特征

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Controlled-release (CR) pharmaceutical formulations offer several advantages over the conventional, immediate release dosage forms of the same drug, including reduced dosing frequency, decreased incidence and/or intensity of adverse effects, greater selectivity of pharmacological activity, reduced drug plasma fluctuation, and better compliance. After a drug product has been registered, and is already on market, minor changes in formulation might be needed. At the same time, the product has to remain effective and safe for patients that could be confirmed via plasma drug concentrations and pharmacokinetic characteristics. It is challenging to predict human absorption and pharmacokinetic characteristics of a drug based on the in vitro dissolution test and the animal pharmacokinetic data. Therefore, the objective of this study was to establish correlation of the pharmacokinetic parameters of carbamazepine (CBZ) CR tablet formulation between the rabbit and the human model, and to establish in vitro in vivo correlation (IVIVC) based on the predicted fractions of absorbed CBZ. Although differences in mean plasma concentration profiles were notified, the data concerning the predicted fraction of drug absorbed were almost superimposable. Accordingly, it can be concluded that rabbits may be representative as an in vivo model for predicting the pharmacokinetics of the CR formulation of CBZ in humans.
机译：与相同药物的常规立即释放剂型相比，控释（CR）药物制剂具有多个优势，包括降低给药频率，降低不良反应的发生率和/或强度，降低药理活性的选择性，降低药物血浆的波动，以及更好的合规性。在药品注册后并已投放市场后，可能需要对配方进行细微更改。同时，该产品必须对患者保持有效和安全，这可以通过血浆药物浓度和药代动力学特征得到证实。根据体外溶出度试验和动物药代动力学数据预测药物的人体吸收和药代动力学特征具有挑战性。因此，本研究的目的是建立卡马西平（CBZ）CR片制剂在兔和人体模型之间的药代动力学参数的相关性，并根据预测的吸收CBZ分数建立体外体内相关性（IVIVC） 。尽管通知了平均血浆浓度分布的差异，但有关药物吸收的预测分数的数据几乎是可叠加的。因此，可以得出结论，兔子可以作为预测CBZ的CR制剂在人体内的药代动力学的体内模型的代表。

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