CN106924210A - 一种含有帕布昔利布的胶囊剂及其制备方法 - Google Patents
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Abstract
本发明涉及一种含有帕布昔利布的胶囊剂及其制备方法，属于药物制剂技术领域。本品可与来曲唑联用，适用于晚期乳腺癌患者。所述的胶囊剂含有帕布昔利布、稀释剂、崩解剂和润滑剂，其中帕布昔利布的质量比例为10％～40％，稀释剂的质量比例为30％～80％，崩解剂的质量比例为1％～10％，润滑剂的用量为0.5～5％。此外，本发明还公开了一种帕布昔利布胶囊剂的制备方法，采用本发明所述的方法制备的帕布昔利布胶囊剂具有工艺操作简单，特别适宜于工业化生产，制备得到的帕布昔利布胶囊剂稳定性好、溶出度好。
Description
技术领域
本发明涉及一种帕布昔利布胶囊，具体来说，一种含有帕布昔利布的胶囊剂。本发明还涉及帕布昔利布胶囊剂的制备方法。采用本发明所述的方法制备的帕布昔利布胶囊剂具有工艺操作简单，特别适宜于工业化生产，制备得到的帕布昔利布胶囊剂稳定性好、溶出度好。
背景技术
乳腺癌是女性最常见的恶性肿瘤之一，发病率占全身各种恶性肿瘤的7～10％，在妇女中仅次于子宫癌，它的发病常与遗传有关。乳腺癌的病因尚未完全清楚，研究发现乳腺癌的发病存在一定的规律性，具有乳腺癌高危因素的女性容易患乳腺癌。乳腺癌的早期发现、早期诊断，是提高疗效的关键。手术治疗和化疗为乳腺癌的常见治疗方法。抗乳腺癌新药帕布昔利布(palbociclib)是一种高度选择性的CDK4/6抑制剂，其作为一种口服的细胞周期素依赖性激酶4/6的抑制药物，主要通过抑制CDK4/6活性来阻止细胞由G1期到S期进而抑制DNA的合成。帕布昔利布胶囊由辉瑞公司研发，规格有75mg、110mg和150mg。帕布昔利布胶囊剂于2015年在美国批准上市，与诺华来曲唑合并用药，作为一线疗法用于先前未接受过系统治疗的雌激素受体阳性(ER+)、HER2阴性晚期乳腺癌绝经后女性。
国内关于帕布昔利布的化合物专利有许多，包括CN104910149A，CN103200822，CN1835951B等，关于帕布昔利布的制剂专利有CN104887641A，其阐述了帕布昔利布胃漂浮片的组成及制备方法。目前未发现有关于帕布昔利布的制剂专利，本发明提供一种含帕布昔利布的胶囊剂及其制备方法。
发明内容
本发明的目的是提供一种帕布昔利布胶囊及其制备方法，制备工艺操作简便，重现性好，溶出性好，制剂稳定性好。
本发明涉及一种帕布昔利布胶囊，具体来说，其包含帕布昔利布、稀释剂、崩解剂和润滑剂。其中帕布昔利布的质量比例为10％～40％，稀释剂的质量比例为30％～80％，崩解剂的质量比例为1％～10％，润滑剂的用量为0.5～5％。
上述稀释剂选自甘露醇、预胶化淀粉、微晶纤维素和乳糖中的一种或多种。
上述崩解剂选自交联羧甲基纤维素钠、羧甲基淀粉钠和低取代羟丙基纤维素中的一种或多种。
上述润滑剂选自硬脂酸镁、二氧化硅和硬脂富马酸钠的一种或两种。
上述稀释剂选自甘露醇、微晶纤维素和乳糖中的一种或多种。
上述崩解剂选自交联羧甲基纤维素钠和羧甲基淀粉钠的一种或两种。
上述润滑剂选自硬脂酸镁和二氧化硅中的一种或两种。
以上所述的帕布昔利布胶囊，其特征在于其各成分组成为：原料药的质量比例为15％～35％，稀释剂的质量比例为40％～75％，崩解剂的质量比例为2％～8％，润滑剂的质量比例为1％～4％。
以上所述的帕布昔利布胶囊，其特征在于，所述的帕布昔利布胶囊由以下步骤制备而成：
(1)将原料药粉碎过100目筛；
(2)将原料药与稀释剂、崩解剂和润滑剂混合均匀，干法制粒，过筛；
(3)向上述混合物中加入润滑剂，混合均匀后，灌装胶囊。
以上所述的帕布昔利布胶囊用于治疗晚期乳腺癌患者，属于药物制剂领域。
实施例
本发明通过以下实施例和对比实施例详细阐述本发明，所述实施例不应被认为是局限性的。
实施例1：制备实施例
制备工艺：
1、将原料药粉碎过100目筛；
2、将原料药与微晶纤维素、乳糖、羧甲基淀粉钠、二氧化硅和1/2量的硬脂酸镁混合均匀，干法制粒，过20目筛；
3、向上述混合物中加入剩余量的硬脂酸镁，混合均匀后，灌装胶囊。
实施例2：制备实施例
制备工艺：
1、将原料药粉碎过100目筛；
2、将原料药与微晶纤维素、乳糖、羧甲基淀粉钠、硬脂酸镁和1/2量的二氧化硅混合均匀，干法制粒，过20目筛；
3、向上述混合物中加入剩余量的二氧化硅，混合均匀后，灌装胶囊。
实施例3：制备实施例
制备工艺：
1、将原料药粉碎过100目筛；
2、将原料药与微晶纤维素、乳糖、羧甲基淀粉钠和2/3量的二氧化硅混合均匀，干法制粒，过20目筛；
3、向上述混合物中加入剩余量的二氧化硅，混合均匀后，灌装胶囊。
实施例4：制备实施例
制备工艺：
1、将原料药粉碎过100目筛；
2、将原料药与微晶纤维素、乳糖、交联羧甲基纤维素钠和1/2量的硬脂酸镁混合均匀，干法制粒，过16目筛；
3、向上述混合物中加入剩余量的硬脂酸镁，混合均匀后，灌装胶囊。
试验例1：帕布昔利布胶囊的外观检查
照中国药典2010版制剂通则中胶囊剂的外观检查，胶囊剂应整洁，不得有粘结、变形、渗漏或囊壳破裂等现象，并应无异臭。检查结果见表1。
试验例2：溶出度试验
测定法：取本品，照溶出度测定法(中国药典2010年版二部附录XC第二法)，以37℃、900mL 0.1M盐酸为溶出介质，转速为50rpm，依法操作，经30min时，取样检测并计算每粒胶囊的溶出量。检查结果见表1。
试验例3：稳定性实试验
取本发明实施例1～4样品，按照中国药典2010年版中附录XIXC原料药与药物制剂稳定性试验指导原则，铝塑泡罩包装后进行加速稳定性考察，条件为40℃±2℃、RH75％±5％，并于放置后的0月、1月、2月、3月和6月取样，考察其稳定性，结果见表2。
表1 帕布昔利布胶囊试验结果
表2 帕布昔利布胶囊稳定性试验结果
试验结果表明本发明制备的样品溶出性好，稳定性好。
已采用实施例对本发明作了阐述。应当理解的是，实施例仅仅是为了举例说明本发明而已。在不偏离本发明的保护范围的前提下，本领域技术人员可依据本发明设计出替换和改进方案，均应被认为是在本发明的保护范围内。
Claims (10)
1.本发明涉及一种帕布昔利布胶囊，具体来说，其包含帕布昔利布、稀释剂、崩解剂和润滑剂。其中原料药的质量比例为10％～40％，稀释剂的质量比例为30％～80％，崩解剂的质量比例为1％～10％，润滑剂的用量为0.5％～5％。
2.根据权利要求1所述的帕布昔利布胶囊，其特征在于，所述的稀释剂为甘露醇、预胶化淀粉、微晶纤维素和乳糖中的一种或多种。
3.根据权利要求1所述的帕布昔利布胶囊，其特征在于，所述的崩解剂为交联羧甲基纤维素钠、羧甲基淀粉钠和低取代羟丙基纤维素中的一种或多种。
4.根据权利要求1所述的帕布昔利布胶囊，其特征在于，所述的润滑剂为硬脂酸镁、二氧化硅和硬脂富马酸钠中的一种或多种。
5.根据权利要求2所述的帕布昔利布胶囊，其特征在于，所述的稀释剂为甘露醇、微晶纤维素和乳糖中的一种或两种。
6.根据权利要求3所述的帕布昔利布胶囊，其特征在于，所述的崩解剂为交联羧甲基纤维素钠和羧甲基淀粉钠中的一种或两种。
7.根据权利要求4所述的帕布昔利布胶囊，其特征在于，所述的润滑剂为硬脂酸镁和二氧化硅中的一种或两种。
8.根据权利要求1所述的帕布昔利布胶囊，其特征在于其各成分组成为：原料药的质量比例为15％～35％，稀释剂的质量比例为40％～75％，崩解剂的质量比例为2％～8％，润滑剂的质量比例为1％～4％。
9.根据权利要求1所述的帕布昔利布胶囊，其特征在于，所述的帕布昔利布胶囊由以下步骤制备而成：
(1)将原料药粉碎过100目筛；
(2)将原料药与稀释剂、崩解剂和润滑剂混合均匀，干法制粒；
(3)向上述混合物中加入润滑剂，混合均匀后，灌装胶囊。
10.根据权利要求1所述的帕布昔利布胶囊用于治疗晚期乳腺癌患者，属于药物制剂领域。
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| CN201510999542.9A Pending CN106924210A (zh) | 2015-12-29 | 2015-12-29 | 一种含有帕布昔利布的胶囊剂及其制备方法 |
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| CN108066312A (zh) * | 2017-12-29 | 2018-05-25 | 山东裕欣药业有限公司 | 一种帕博西尼药物组合物及其制备方法 |
| EP3434272A1 (en) * | 2017-07-25 | 2019-01-30 | Sanofi | Combination comprising palbociclib and 6-(2,4-dichlorophenyl)-5-[4-[(3s)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7h-benzo[7]annulene-2-carboxylic acid |
| WO2019056163A1 (zh) * | 2017-09-19 | 2019-03-28 | 浙江华海药业股份有限公司 | N-甲酰基帕博西尼及其制备方法和用途以及帕博西尼制剂及其质量控制方法 |
| WO2020207441A1 (zh) * | 2019-04-12 | 2020-10-15 | 杭州华东医药集团新药研究院有限公司 | 稳定的迈华替尼药物组合物及其制备方法 |
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| US11214541B2 (en) | 2016-02-15 | 2022-01-04 | Sanofi | Substituted 6,7-dihydro-5H-benzo[7]annulene compounds, processes for their preparation and therapeutic uses thereof |
| US11713296B2 (en) | 2018-09-07 | 2023-08-01 | Sanofi | Salts of methyl 6-(2,4-dichlorophenyl)-5-[4-[(3S)-l-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylate and preparation process thereof |
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2015
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| TWI768087B (zh) * | 2017-07-24 | 2022-06-21 | 法商賽諾菲公司 | 包含帕博西尼(palbociclib)及6-(2,4-二氯苯基)-5-[4-[(3s)-1-(3-氟丙基)吡咯啶-3-基]氧基苯基]-8,9-二氫-7h-苯并[7]輪烯-2-甲酸的組合 |
| JP2020526572A (ja) * | 2017-07-24 | 2020-08-31 | サノフイＳａｎｏｆｉ | パルボシクリブ及び６−（２，４−ジクロロフェニル）−５−［４−［（３ｓ）−１−（３−フルオロプロピル）ピロリジン−３−イル］オキシフェニル］−８，９−ジヒドロ−７ｈ−ベンゾ［７］アヌレン−２−カルボン酸を含む組み合わせ並びに癌の処置のためのその使用 |
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| US12528768B2 (en) | 2019-12-09 | 2026-01-20 | Sanofi | Crystalline form of a 7H-benzo[7]annulene-2-carboxylic acid derivative |
| US12427142B2 (en) | 2020-02-27 | 2025-09-30 | Sanofi | Combination comprising alpelisib and 6-(2,4-dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl[oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid |
| US12595230B2 (en) | 2020-10-19 | 2026-04-07 | Sanofi | Substituted 6,7-dihydro-5H-benzo[7]annulene compounds and their derivatives, processes for their preparation and therapeutic uses thereof |
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