| 张美玲,朱佳滨,王路,等.帕利哌酮缓释片的制备[J].中国海洋药物,2024,43(1):47-53. |
| 帕利哌酮缓释片的制备 |
| Preparation of paliperidone sustained-release tablets |
| 投稿时间：2022-11-21 修订日期：2023-01-09 |
| DOI：10.13400/j.cnki.cjmd.2024.01.006 |
| 中文关键词: 帕利哌酮 缓释片 体外释放 |
| English Keywords:paliperidone sustained-release tablets in vitro release |
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| 中文摘要: |
| 目的 制备骨架膜控型帕利哌酮缓释片，针对制剂处方和制备工艺进行筛选，并考察其体外释放特性。方法 通过检索原研制剂处方和其他仿制药等相关信息，选择以海藻酸钠（SA）、羟丙甲纤维素（HPMC）和聚氧乙烯（PEO）等缓释材料作为凝胶骨架片芯进行研究，筛选不同种类缓释材料及不同比例用量，以确定片芯处方；然后，筛选包衣材料和用量以确定包衣处方；同时，通过考察包衣老化温度和老化时间等，确定缓释片的制备工艺。结果 经过优化，确定片芯以SA和HPMC K100LV CR质量比为1：1作为亲水凝胶骨架，以无水乳糖作为填充剂，硬脂酸镁作为润滑剂；缓释衣膜以乙基纤维素水分散体Surelease、HPMC SH-E3和枸橼酸三乙酯（TEC）作为包衣材料，包衣体系为乙基纤维素（EC）：HPMC：TEC=80：20：15，同时确定老化工艺为：采用包衣锅设备，于55-60 ℃条件下老化3 h。结论 成功制备骨架膜控型帕利哌酮缓释片，制剂处方和制备工艺合理，且体外溶出曲线介于参比制剂（RLD）和对照制剂溶出曲线之间，通过一致性评价的可能性更高。 |
| English Summary: |
| Objective To prepare matrix membrane controlled sustained release tablets of paliperidone, optimize the formulation and preparation process, and investigate its release characteristics in vitro. Methods By searching the relevant information of the original formulation and other generic drugs, the sustained-release materials such as sodium alginate (SA), hydroxypropyl methylcellulose (HPMC) and polyoxyethylene (PEO) were selected as the gel skeleton core for research, and different kinds of sustained-release materials and different proportions of dosage were selected to determine the core formulation. Then, the coating materials and dosage were optimized to determine the coating prescription. At the same time, the preparation process of sustained-release tablets was determined by investigating the coating aging temperature and aging time. Results After optimization, SA and HPMC K100LV CR with a mass ratio of 1:1 were selected as the hydrophilic gel skeleton, anhydrous lactose was used as the filler, magnesium stearate was used as the lubricant. The sustained-release film was coated with ethyl cellulose aqueous dispersion Surelease, HPMC SH-E3 and triethyl citrate (TEC). And the coating system was ethyl cellulose (EC): HPMC: TEC=80:20:15. At the same time, the aging process was determined as follows: aging for 3 hours at 55-60 ℃ with coating machine. Conclusion The matrix membrane controlled sustained release tablets of paliperidone were successfully prepared. The formulation and preparation process were reasonable. The dissolution curve in vitro was between that of reference listed drug (RLD) and that of reference preparation, so it would be more likely to pass the consistency evaluation. |
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