State Key Laboratory Base for Eco-Chemical Engineering in College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao, China.
Department of Pharmaceutical Engineering, College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao, China.
Drug Dev Ind Pharm. 2020 Jan;46(1):42-49. doi: 10.1080/03639045.2019.1698597. Epub 2020 Jan 20.
The number of Parkinson's disease (PD) patients with the advanced phase and motor fluctuations is increasing. The objective of this study is developing levodopa/benzylhydrazine orally disintegrating tablets (L/B ODTs), which would provide greater convenience and ease of use than conventional tablets for these patients. In the present study, the L/B ODTs were developed successfully with an optimized formulation using response surface methodology (RSM). The direct compression technology was employed for the preparation of L/B ODTs. Considerably shorter disintegration time and faster dissolution profile were obtained under the optimum formulation with microcrystalline cellulose 25.7%, cross-polyvinylpyrrolidone 6.22% and Sodium carboxymethyl starch 5.36%. The content uniformity (%) of levodopa and benzylhydrazine was 50 ± 1.4% and 14.25 ± 0.6%, respectively. Thickness, friability, hardness and wetting time were 2.8 ± 0.05 mm, 0.46 ± 0.21%, 5.42 ± 1.1 kp and 31.2 ± 2.1 s, respectively, and all of data well comply with the General Principles of the Chinese Pharmacopeia. Mannitol of 22% in formulation could bring a pleasant taste: sweet, cool and refreshing. Almost all the volunteers felt that the ODTs had good taste, no roughness, and no gritty feeling, indicating that the ODTs prepared had good palatability, so patients will have good compliance when taking medicine.
帕金森病（PD）晚期和运动波动的患者人数正在增加。本研究的目的是开发左旋多巴/苯肼口腔崩解片（L/B ODT），与常规片剂相比，为这些患者提供更大的便利性和易用性。在本研究中，使用响应面法（RSM）成功开发了优化配方的 L/B ODT。采用直接压片技术制备 L/B ODT。在含有微晶纤维素 25.7%、交联聚维酮 6.22%和羧甲基淀粉钠 5.36%的最佳配方下，崩解时间显著缩短，溶解速度更快。左旋多巴和苯肼的含量均匀度（%）分别为 50±1.4%和 14.25±0.6%。厚度、脆碎度、硬度和润湿时间分别为 2.8±0.05mm、0.46±0.21%、5.42±1.1kp 和 31.2±2.1s，所有数据均符合《中国药典》通则要求。配方中 22%的甘露醇可带来宜人的口感：甜、凉、清爽。几乎所有志愿者都觉得 ODT 口感良好，无粗糙感，无沙砾感，说明所制备的 ODT 具有良好的适口性，因此患者在服药时会有良好的依从性。
