College of Pharmacy and Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, Republic of Korea.
GL PharmTech Corp, Seongnam, Republic of Korea.
Drug Des Devel Ther. 2020 Jan 30;14:445-456. doi: 10.2147/DDDT.S222505. eCollection 2020.
Novel three-layered (TL) tablet systems were compared with both monolithic matrix (MM) formulations and a commercial immediate-release (IR) capsule to develop once-a-day (OAD) pregabalin tablets.
The physical properties of the TL tablets, including dissolution and swelling rates, were compared with those of the MM tablets and the pharmacokinetic parameters of the TL tablet were compared with those of an IR capsule in beagles and humans.
Our results indicated that the same amount of a hydrophilic polymer in the formulations had similar dissolution profiles at 12 h, regardless of the tablet geometry. However, the degree of tablet swelling differed, with larger amounts of polymer in the tablets showing a greater degree of swelling. In addition, TL tablets swelled more rapidly compared with MM tablets. For the pharmacokinetic study of the TL tablet, the beagles demonstrated absorption results similar to those of an IR capsule, whereas the humans demonstrated low total absorption compared with an IR capsule. The time of the peak plasma concentration at 6 h in the fed state of humans coincided with the results of the study on beagles.
The novel TL tablet system of pregabalin may prove to be helpful in developing improved formulations with better continuous drug absorption for OAD administration.
新型三层（TL）片剂系统与单片基质（MM）制剂和一种商业即时释放（IR）胶囊进行了比较，以开发每日一次（OAD）普瑞巴林片剂。
TL 片剂的物理性质，包括溶出度和溶胀率，与 MM 片剂进行了比较，TL 片剂的药代动力学参数与比格犬和人体内的 IR 胶囊进行了比较。
我们的结果表明，在 12 小时时，制剂中相同量的亲水性聚合物具有相似的溶出曲线，而不管片剂的几何形状如何。然而，片剂的溶胀程度不同，片剂中聚合物的含量越多，溶胀程度越大。此外，TL 片剂比 MM 片剂膨胀得更快。对于 TL 片剂的药代动力学研究，比格犬的吸收结果与 IR 胶囊相似，而人体与 IR 胶囊相比总吸收较低。在人体进食状态下，6 小时时的血浆峰浓度时间与比格犬的研究结果一致。
新型普瑞巴林 TL 片剂系统可能有助于开发更好的制剂，以改善 OAD 给药的持续药物吸收。
