CN111184696A - 一种枸橼酸托法替布缓释片及其制备方法 - Google Patents
一种枸橼酸托法替布缓释片及其制备方法 Download PDFInfo
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Abstract
本发明属于药物制剂领域，具体而言涉及一种枸橼酸托法替布缓释片及其制备方法，本发明枸橼酸托法替布缓释片包括枸橼酸托法替布、骨架材料和填充剂，其中骨架材料包括溶蚀性骨架材料和亲水凝胶骨架材料。该缓释片制备工艺简单，工艺重现性高，适合工业化大生产。
Description
技术领域
本发明属于药物制剂领域，具体而言，涉及一种枸橼酸托法替布缓释片及其制备方法。
背景技术
托法替布缓释片是一种类风湿性关节炎口服药，由辉瑞制药开发，2016年在美国上市。其化学名为其化学名称为：3-((3R,4R)-4-甲基-3-(甲基(7H-吡咯并[2,3-d]嘧啶-4-基)氨基派啶-1-基)-3-氧代丙腈，化学结构式为：
分子式为C16H20N6O，分子量为504.5，其性状为白色至灰白色粉末，在水中易溶。托法替布是一种JAK激酶抑制剂，其用于甲氨蝶呤疗效不理想或对甲氨蝶呤过敏的中度至重度类风湿性关节炎成年人患者。
专利WO2014147526A1中公开的一种枸橼酸托法替布缓释片制备是通过渗透泵的膜控制其释放，其制备包括制粒、混合、压片、半透膜包衣、老化(16h)、外包衣。这种渗透片剂生产工艺复杂，不利于产业化大生产且会产生大量废气，安全性不高。
发明内容
为解决现有技术的缺陷，发明人在研究托法替布制剂技术时发现，当枸橼酸托法替布缓释片采用溶蚀性骨架材料和亲水凝胶骨架材料联用组成时，其药物释放稳定，生物利用度高，制备工艺简单，工艺重现性高，适合工业化大生产。
本发明的目的是提供一种枸橼酸托法替布缓释片及其制备方法。
本发明提供一种枸橼酸托法替布缓释片，包括下列组分：枸橼酸托法替布、骨架材料、填充剂和润滑剂，其中骨架材料包括溶蚀性骨架材料和亲水凝胶骨架材料。
所述的溶蚀性骨架材料为山嵛酸甘油酯、单硬脂酸甘油酯、硬脂醇或硬脂酸中的一种或几种，优选山嵛酸甘油酯；亲水凝胶骨架材料为羟丙甲基纤维素、聚氧乙烯、羟丙基纤维素或聚乙烯吡咯烷酮中的一种或几种，优选羟丙甲基纤维素、聚氧乙烯中一种或多种，更优选羟丙甲基纤维素。
所述的填充剂为乳糖、甘露醇、微晶纤维素、预胶化淀粉和淀粉中的一种或几种，优选乳糖、微晶纤维素。
所述的润滑剂为硬脂酸镁或滑石粉。
所述的枸橼酸托法替布缓释片中枸橼酸托法替布、溶蚀性骨架材料、亲水凝胶骨架材料的质量比为1：0.2～4：0.5～3。
本发明还提供一种枸橼酸托法替布缓释片的制备方法，包括以下步骤：
(a)称取山嵛酸甘油酯，加热至65-70℃熔融，保温；
(b)继续保温，同时加入枸橼酸托法替布，搅拌至熔融，冷却固化，研磨，过筛，得载药颗粒；
(c)将载药颗粒与药学上可接受的辅料混合均匀，压片，即得。
具体实施方式
下面通过具体实施方式对本发明作进一步详细说明。但本领域技术人员将会理解，下列实施例仅用于说明本发明，而不应视为限定本发明的范围。所用物料或仪器未注明生产厂商者，均为可以通过市购获得的常规产品。
本发明的实施方式不仅限于下述具体实例所提供的方式。
实施例1：枸橼酸托法替布缓释片的制备：
枸橼酸托法替布缓释片处方组成：规格11mg(以托法替布计)
| 原辅料 | 用量g |
| 枸橼酸托法替布 | 8.1 |
| Compritol@888ATO | 4.05 |
| HPMC | 24.3 |
| MCC/乳糖 | 63.05 |
| 硬脂酸镁 | 0.5 |
制备工艺：
(a)称取山嵛酸甘油酯，加热至65-70℃熔融，保温；
(b)继续保温，同时加入枸橼酸托法替布，使用电动搅拌器搅拌30min以上至熔融，迅速放入冰水混合物中固化，待完全固化后，研磨，过80目筛，得载药颗粒；
(c)将载药颗粒与处方量的HPMC、MCC/乳糖(过100目筛)、硬脂酸镁混合均匀，压片，Φ8mm冲压片，控制硬度40-60N范围内。
实施例2：枸橼酸托法替布缓释片的制备：
枸橼酸托法替布缓释片处方组成：规格11mg(以托法替布计)
| 原辅料 | 用量g |
| 枸橼酸托法替布 | 8.1 |
| Compritol@888ATO | 8.1 |
| HPMC | 8.1 |
| MCC/乳糖 | 75.2 |
| 硬脂酸镁 | 0.5 |
制备工艺：同实施例1。
实施例3：枸橼酸托法替布缓释片的制备：
枸橼酸托法替布缓释片处方组成：规格11mg(以托法替布计)
| 原辅料 | 用量g |
| 枸橼酸托法替布 | 8.1 |
| Compritol@888ATO | 24.3 |
| HPMC | 24.3 |
| MCC/乳糖 | 42.3 |
| 硬脂酸镁 | 1 |
制备工艺：同实施例1。
实施例4：枸橼酸托法替布缓释片的制备：
枸橼酸托法替布缓释片处方组成：规格11mg(以托法替布计)
| 原辅料 | 用量g |
| 枸橼酸托法替布 | 8.1 |
| Compritol@888ATO | 8.1 |
| HPMC | 16.2 |
| MCC/乳糖 | 67.1 |
| 硬脂酸镁 | 1 |
制备工艺：同实施例1。
对比例1枸橼酸托法替布缓释片，商品名XELJANZ XR，规格：11mg来源：辉瑞制药
制备工艺：同专利WO2014147526A1。
实施例5：枸橼酸托法替布缓释片的释放度测定
释放度的方法如下：取样品，照释放度测定法(中国药典2015版四部制剂通则0931第二法)+沉降篮的装置，溶出介质为pH6.8磷酸盐缓冲液900ml，转速为50转；以不同时间取样，在线过滤。在286nm处检测。计算片剂的释放度。。
各实例释放结果：
实施例5的实例1-4结果显示：枸橼酸托法替布缓释片采用Compritol@888ATO和HPMC双骨架材料联合使用时，药物12h内平稳释放且释放完全，且可以获得同渗透片剂释放曲线较一致的释放。
Claims (6)
1.一种枸橼酸托法替布缓释片，其特征在于，包括下列组分：枸橼酸托法替布、骨架材料、填充剂和润滑剂，其中骨架材料包括溶蚀性骨架材料和亲水凝胶骨架材料。
2.权利要求1所述的枸橼酸托法替布缓释片，其特征在于：溶蚀性骨架材料选自山嵛酸甘油酯、单硬脂酸甘油酯、硬脂醇或硬脂酸中的一种或几种，优选山嵛酸甘油酯；亲水凝胶骨架材料选自羟丙甲基纤维素、聚氧乙烯、羟丙基纤维素或聚乙烯吡咯烷酮中的一种或几种，优选羟丙甲基纤维素、聚氧乙烯中一种或多种，更优选羟丙甲基纤维素。
3.权利要求1所述的枸橼酸托法替布缓释片，其特征在于，所述的填充剂选自乳糖、甘露醇、微晶纤维素、预胶化淀粉和淀粉中的一种或几种，优选乳糖、微晶纤维素。
4.权利要求1所述的枸橼酸托法替布缓释片，其特征在于，所述的润滑剂选自硬脂酸镁或滑石粉。
5.权利要求1-3所述的枸橼酸托法替布缓释片，其特征在于，枸橼酸托法替布、溶蚀性骨架材料、亲水凝胶骨架材料的质量比为1：0.2～3：0.5～3。
6.权利要求1-5任一所述的枸橼酸托法替布缓释片的制备方法，该方法包括以下步骤：
(a)称取山嵛酸甘油酯，加热至65-70℃熔融，保温；
(b)继续保温，同时加入枸橼酸托法替布，搅拌至熔融，冷却固化，研磨，过筛，得载药颗粒；
(c)将载药颗粒与药学上可接受的辅料混合均匀，压片，即得。
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