Drug Delivery and Translational Research ( IF 5.7 ) Pub Date : 2022-06-04 , DOI: 10.1007/s13346-022-01188-5 Hao Yuan 1 , Zhengyu Zhang 1 , Liandong Hu 1
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In this study, a new gastro-floating sustained-release capsule (GFC) with levodopa (LD) and benserazide hydrochloride (BH) was successfully developed. GFCs were prepared by filling the LD and BH granules into hard capsules and coated with cellulose acetate (CA) solution as a controlled-release layer. The effects of formulation factors on the release of GFCs were conducted. The AUC0~24 (µg h/mL) of LD were 69.31 ± 3.61 (μg h/mL) and 28.87 ± 2.58 (μg h/mL) and the Cmax were 7.84 ± 0.34 (μg/mL) and 9.21 ± 1.04 (μg/mL) in the GFCs and commercial tablets respectively. The relative bioavailability of LD was 267.55 ± 34.54%. Compared with commercial tablets, the pharmacokinetic study indicated that the developed GFCs provided a better sustained-release effect and higher bioavailability than commercial tablets.
Graphical abstract
中文翻译：
提高左旋多巴生物利用度的胃漂浮缓释胶囊的研制与表征
在这项研究中，成功开发了一种新的含有左旋多巴（LD）和盐酸苄丝肼（BH）的胃漂浮缓释胶囊（GFC）。GFCs 是通过将 LD 和 BH 颗粒填充到硬胶囊中并涂上醋酸纤维素 (CA) 溶液作为控释层来制备的。研究了配方因素对 GFC 释放的影响。LD的AUC 0~24 (µg·h/mL)分别为69.31±3.61(μg·h/mL)和28.87±2.58(μg·h/mL)，Cmax在 GFCs 和商业片剂中分别为 7.84 ± 0.34 (μg/mL) 和 9.21 ± 1.04 (μg/mL)。LD 的相对生物利用度为 267.55 ± 34.54%。与商业片剂相比，药代动力学研究表明，开发的 GFCs 比商业片剂具有更好的缓释效果和更高的生物利用度。
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