CN111821305A - 一种匹洛那韦利托那韦制剂及其适应症 - Google Patents

一种匹洛那韦利托那韦制剂及其适应症 Download PDF

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CN111821305A
CN111821305A CN202010082400.7A CN202010082400A CN111821305A CN 111821305 A CN111821305 A CN 111821305A CN 202010082400 A CN202010082400 A CN 202010082400A CN 111821305 A CN111821305 A CN 111821305A
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郭夏
宋雪梅
邢沙沙
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Beijing Venturepharm Technology Co ltd
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Abstract

本发明公开了匹洛那韦与利托那韦在制备用于治疗新型冠状病毒（2019‑nCoV）的药物中的用途。匹洛那韦与利托那韦的复方制剂可使新型冠状病毒（2019‑nCoV）感染的患者有效改善呼吸窘迫、咳嗽咳痰，发热等全身症状，延缓疾病进展，可以提高患者的生活质量，具有广泛的应用价值。本发明经过药物研究确定得到产品稳定性较好，用于预防和治疗新型冠状病毒的制剂。

Description

一种匹洛那韦利托那韦制剂及其适应症
技术领域
本发明涉及匹洛那韦与托那韦及其液体制剂，具体涉及一种用于预防及治疗新型冠状病毒（2019-nCoV）的制剂及其制法和适应症，属于医药技术领域。
背景技术
利托那韦是一种肽类似物抑制剂，为人免疫缺陷病毒-1(HIV-1)和人免疫缺陷病毒-2(HIV-2)天冬氨酸蛋白酶的口服有效抑制剂。洛匹那韦是一种HIV-1和HIV-2的蛋白酶的抑制剂。作为复方制剂，利托那韦可以抑制CYP3A介导的洛匹那韦代谢，从而提高血浆中洛匹那韦的药物浓度。洛匹那韦可以阻断Gag-Pol聚蛋白的分裂，导致产生未成熟的、无感染力的病毒颗粒。体外抗病毒活性洛匹那韦对于实验室HIV链和临床的HIV分离毒株分别在急性感染的淋巴母细胞系和外周血淋巴细胞显示出体外抗病毒活性。
本发明公开了匹洛那韦与利托那韦在制备用于治疗新型冠状病毒（2019-nCoV）的药物中的用途。匹洛那韦与利托那韦的复方制剂可使新型冠状病毒（2019-nCoV）感染的患者有效改善呼吸窘迫、咳嗽咳痰，发热等全身症状，延缓疾病进展，可以提高患者的生活质量，具有广泛的应用价值。本发明经过药物研究确定得到产品稳定性较好，用于预防和治疗新型冠状病毒的制剂。
利托那韦由美国Abbott实验室在世界上率先研制成功。利托那韦口服溶液于1996年3月首先在美国上市，商品名为NORVIR®在美国已经被批准上市的利托那韦制剂包括利托那韦口服溶液、利托那韦软胶囊、利托那韦片、利托那韦/洛匹那韦复方溶液、利托那韦/洛匹那韦复方片和利托那韦/阿扎那韦复方片，除利托那韦/阿扎那韦复方片由Matrix LabsLTD（美吉斯）开发外，其余均为雅培公司产品。目前国内已有雅培公司进口的利托那韦片剂、上市销售，还未有口服溶液制剂上市销售。原料药有万全万特制药(厦门)有限公司，国药准字H20040411和上海迪赛诺化学制药有限公司，国药准字H20173132上市销售。
发明内容
本发明公开了匹洛那韦与利托那韦在制备用于治疗新型冠状病毒（2019-nCoV）的药物中的用途。匹洛那韦与利托那韦的复方制剂可使新型冠状病毒（2019-nCoV）感染的患者有效改善呼吸窘迫、咳嗽咳痰，发热等全身症状，延缓疾病进展，可以提高患者的生活质量，具有广泛的应用价值。本发明经过药物研究确定得到产品稳定性较好，用于预防和治疗新型冠状病毒的制剂。
匹洛那韦与利托那韦在制备用于治疗新型冠状病毒（2019-nCoV）的药物中的用途。
匹洛那韦与利托那韦口服制剂在制备治疗新型冠状病毒（2019-nCoV）的药物中的用途。
口服制剂选自复方口服固体制剂、复方口服液体制剂。
口服制剂的有效成分为匹洛那韦与利托那韦，匹洛那韦80~200mg/片，利托那韦20~50mg/片。
复方口服液体制剂包含匹洛那韦与利托那韦、潜溶剂、稳定剂、pH调节剂。潜溶剂为乙醇、丙二醇、聚氧乙烯蓖麻油，pH调节剂为枸橼酸或柠檬酸。
复方口服固体制剂包含匹洛那韦与利托那韦、润滑剂、助溶剂、粘合剂。润滑剂为富马酸硬脂酸钠，助溶剂为司盘或吐温，粘合剂为聚维酮。
具体实施方式
实施例1
复方口服片剂以洛匹那韦200mg/片、利托那韦50mg/片，辅料加入聚维酮、山梨醇单月桂酸盐以热熔挤出工艺制备样品，继续加入富马酸硬脂酸钠压制得片芯，包衣，得终产品。
实施例2
复方口服片剂以洛匹那韦100mg/片、利托那韦25mg/片，辅料加入聚维酮、山梨醇单月桂酸盐以热熔挤出工艺制备样品，继续加入富马酸硬脂酸钠压制得片芯，包衣，得终产品。
实施例3
复方口溶液剂以洛匹那韦80mg/ml、利托那韦20mg/ml，在乙醇、丙二醇、聚氧乙烯蓖麻油的混合液中加入洛匹那韦与利托那韦搅拌至完全溶解，并用pH调节剂枸橼酸调节pH值，得终产品。
实验结果：
将实施例1-3按《中国药典》2015版稳定性指导原则进行放样，样品0天及加速3月检测结果如下。
表1 实施例0天样品检测结果
Figure 398948DEST_PATH_IMAGE001
表2 实施例加速3月样品检测结果
Figure 647527DEST_PATH_IMAGE002
试验结论：
通过实施例1-3可知，洛匹那韦与利托那韦的复方制剂中加入关键性辅料，可使所得样品稳定性良好。匹洛那韦与利托那韦的复方制剂可使新型冠状病毒（2019-nCoV）感染的患者有效改善呼吸窘迫、咳嗽咳痰，发热等全身症状，延缓疾病进展，可以提高患者的生活质量，具有广泛的应用价值。本发明经过药物研究确定得到产品稳定性较好，用于预防和治疗新型冠状病毒的制剂。

Claims (6)

1.匹洛那韦与利托那韦在制备用于治疗新型冠状病毒（2019-nCoV）的药物中的用途。
2.匹洛那韦与利托那韦口服制剂在制备治疗新型冠状病毒（2019-nCoV）的药物中的用途。
3.如权利要求2所述的用途，其中所述口服制剂选自复方口服固体制剂、复方口服液体制剂。
4.如权利要求2所述的用途，其中所述的口服制剂的有效成分为匹洛那韦与利托那韦，匹洛那韦80~200mg/片，利托那韦20~50mg/片。
5.如权利要求3所述的用途，其中所述的复方口服液体制剂包含匹洛那韦与利托那韦、潜溶剂、稳定剂、pH调节剂；潜溶剂为乙醇、丙二醇、聚氧乙烯蓖麻油，pH调节剂为枸橼酸或柠檬酸。
6.如权利要求3所述的用途，其中所述的复方口服固体制剂包含匹洛那韦与利托那韦、润滑剂、助溶剂、粘合剂；润滑剂为富马酸硬脂酸钠，助溶剂为司盘或吐温，粘合剂为聚维酮。
CN202010082400.7A 2020-02-07 2020-02-07 一种匹洛那韦利托那韦制剂及其适应症 Pending CN111821305A (zh)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114668737A (zh) * 2022-03-02 2022-06-28 乐普制药科技有限公司 一种用于治疗新型冠状病毒含有利托那韦微丸的复方双层片剂

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114668737A (zh) * 2022-03-02 2022-06-28 乐普制药科技有限公司 一种用于治疗新型冠状病毒含有利托那韦微丸的复方双层片剂

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Application publication date: 20201027