CN1739513A - 一种氯雷他定口腔崩解片剂及其制备方法 - Google Patents
一种氯雷他定口腔崩解片剂及其制备方法 Download PDFInfo
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Abstract
本发明属医药领域，具体涉及一种治疗过敏性疾病的氯雷他定口腔崩解片及其制备方法，氯雷他定口腔崩解片剂，包括药物活性成分氯雷他定和赋形剂的混合物，其特征在于所述的赋形剂包括崩解剂、填充剂、可溶性多元醇和渗透剂；该片剂中各组分的重量比为：氯雷他定20％～50％、崩解剂5％～15％、填充剂10％～30％、可溶性多元醇30％～60％、渗透剂1％～5％。本发明与普通口服制剂相比，因胃肠道粘膜被速崩后的药物广泛覆盖，起效迅速。而且药物可以通过口腔粘膜吸收，免去了首过效应，提高了生物利用度，减少了对胃肠道的刺激。由于口腔崩解片在口内不需水即可服下，为饮水不便的人们口服用药提供了方便。
Description
技术领域
本发明属医药领域，具体涉及一种治疗过敏性疾病的氯雷他定口腔崩解片及其制备方法。
背景技术
过敏反应是一种急性的、全身性的、严重到甚至危及生命的变态反应，是在患者以前被某种变应原致敏后再次接触同一变应原时发生的。过敏反应的症状可在接触变应原后立即或2小时内出现。患者感觉不适、烦躁、心悸、颤抖、皮肤潮红发痒、耳鸣、咳嗽、打喷嚏、荨麻疹、水肿或因哮喘及气管阻塞引起呼吸困难，可在不出现呼吸系统症状的情况下发生心血管系统衰竭。通常在发生过敏反应时可能出现心血管或呼吸系统的症状，但两种系统的症状不同时出现，多次发生过敏反应的人，每次发作时的症状常常类似。过敏反应的过程非常快，可很快导致虚脱、抽搐、小便失禁、意识丧失，1～2分钟内出现中风。除非立即进行紧急治疗，否则过敏反应常常导致死亡。
过敏反应可由各种变应原引起。第一次接触变应原时不会发生过敏反应，而再次接触则可能发生。但大多数人并不知道何时第一次接触过某种变应原。
氯雷他定是一种长效、无镇静作用、无抗胆碱能作用的新一代长效三环抗组胺药，具有选择性对抗外周H1-受体的作用。在治疗剂量范围内，无嗜睡作用，适用于流泪、打喷嚏、过敏性鼻炎、急性或慢性荨麻疹症及其它过敏性皮肤病。对酒精无强化作用。作用迅速，服药后30分钟内开始起效，不会通过血脑屏障。
氯雷他定为白色或类白色结晶性粉末；几乎无臭，无味。在水或乙醇中极微溶，在乙醚或氯仿中不溶；在碱性溶液中溶解。目前的氯雷他定一般都是口服的胃溶制剂，药物不能被迅速吸收，起效较慢，而且服用不方便，尤其对于因过敏性疾病而吞咽功能不好的患者。
发明内容
本发明的目的在于克服背景技术中存在的缺陷，提供一种起效快、生物利用度高、服用方便的氯雷他定口腔崩解片剂。
本发明一种氯雷他定口腔崩解片剂，包括药物活性成分氯雷他定和赋形剂的混合物，所述的赋形剂包括崩解剂、填充剂、可溶性多元醇和渗透剂；该片剂中各组分的重量比为：氯雷他定20％～50％、崩解剂5％～15％、填充剂10％～30％、 可溶性多元醇30％～60％、渗透剂1％～5％。
还可以包括0.5％～3％的香精、0.5％～3％的甜味剂和0.5％～1.5％的润滑剂中的一种或多种。
其中所述的崩解剂为交聚维酮，交联羧甲基纤维素钠、低取代羟丙基纤维素、羧甲基淀粉钠中的一种或多种混合。
所述的填充剂为预胶化淀粉、可压性淀粉、乳糖、蔗糖及葡萄糖、纤维素及微晶纤维素、明胶中的一种或多种混合。
所述的可溶性多元醇为甘露醇、木糖醇、山梨糖醇和麦芽糖醇中的一种或多种混合。
所述的渗透剂对水有高亲和性的二氧化硅、麦芽糖糊精中的一种或多种混合。
本发明还提供了一种氯雷他定口腔崩解片剂的制备方法，其特征在于按组分配方混合，用粉末压片法或冷冻干燥法制备得到片剂。
本发明的口腔崩解片，与普通口服制剂相比，因胃肠道粘膜被速崩后的药物广泛覆盖，起效迅速。而且药物可以通过口腔粘膜吸收，免去了首过效应，提高了生物利用度，减少了对胃肠道的刺激。为过敏性疾病患者提供了一种新的方便剂型。由于口腔崩解片在口内不需水即可服下，为饮水不便的人们口服用药提供了方便。
此片剂是在口腔中与唾液接触时产生崩解，一般在小于40秒内崩解，或甚至在小于30秒内崩解。本发明中提供的口腔崩解片具有较好硬度，既可便于包装和运输，又便于工业化生产。
具体实施方式
我们从下列实施例进一步详细举例说明本发明，但应理解本发明的范围决不限于此。
实施例1：本实施例制备1000片氯雷他定口腔崩解片(规格：0.25g)，使用下述成分：
物料名称 投料量
氯雷他定 250g
甘露醇 420g
微晶纤维素 150g
交聚维酮 70g
阿司帕坦 20g
薄荷香精 10g
二氧化硅 20g
硬脂酸镁 5g
工艺步骤：原料、辅料颗粒，加入阿司帕坦、薄荷香精及二氧化硅、硬脂酸镁，混合均匀，压片，包装。
对上述处方的样品进行口感、口腔崩解时间、崩解时限、脆碎度测定。
检测项目
口感 好
口腔崩解时限 28秒
崩解时限 19秒
脆碎度 0.5％
实施例2：本实施例制备1000片氯雷他定口腔崩解片(规格：0.25g)，使用下述成分：
物料名称 投料量
氯雷他定 250g
山梨醇 400g
葡萄糖 80
蔗糖 70g
交联羧甲基纤维素钠 60g
甜叶菊苷 25g
甜橙香精 10g
二氧化硅 20g
十八烷基富马酸钠 5g
工艺步骤：原料、辅料颗粒，加入甜叶菊苷、甜橙香精及二氧化硅、十八烷基富马酸钠，混合均匀，压片，包装。
对上述处方的样品进行口感、口腔崩解时间、崩解时限、脆碎度测定。
检测项目
口感 好
口腔崩解时限 25秒
崩解时限 16秒
脆碎度 0.6％
实施例3：本实施例制备1000片氯雷他定口腔崩解片(规格：0.25g)，使用下述成分：
物料名称 投料量
氯雷他定 250g
甘露醇 200g
蔗糖 220g
明胶 50g
羟乙基纤维素 40g
薄荷香精 10g
工艺步骤：原料、辅料用水溶解，充分混匀，加入到模具中放置于冻干机中低温冻结，抽真空至物料干燥，密封包装。
对上述处方的样品进行口感、口腔崩解时间、崩解时限测定。
检测项目
口感 好
口腔崩解时限 19秒
崩解时限 14秒
Claims (10)
1、一种氯雷他定口腔崩解片剂，包括药物活性成分氯雷他定和赋形剂的混合物，其特征在于所述的赋形剂混合物包括崩解剂、填充剂、可溶性多元醇和渗透剂；该片剂中各组分的重量比为：氯雷他定20％～50％、崩解剂5％～15％、填充剂10％～30％、可溶性多元醇30％～60％、渗透剂1％～5％。
2、根据权利要求1所述的一种氯雷他定口腔崩解片剂，其特征在于还包括0.5％～3％的香精、0.5％～3％的甜味剂和0.5％～1.5％的润滑剂中的一种或多种。
3、根据权利要求1所述的一种氯雷他定口腔崩解片剂，其特征在于所述的崩解剂为交聚维酮，交联羧甲基纤维素钠、低取代羟丙基纤维素、羧甲基淀粉钠中的一种或多种混合。
4、根据权利要求1所述的一种氯雷他定口腔崩解片剂，其特征在于所述的填充剂为预胶化淀粉、可压性淀粉、乳糖、蔗糖及葡萄糖、纤维素及微晶纤维素、明胶中的一种或多种混合。
5、根据权利要求1所述的一种氯雷他定口腔崩解片剂，其特征在于所述的可溶性多元醇为甘露醇、木糖醇、山梨糖醇和麦芽糖醇中的一种或多种混合。
6、根据权利要求1所述的一种氯雷他定口腔崩解片剂，其特征在于所述的渗透剂对水有高亲和性的二氧化硅、麦芽糖糊精中的一种或多种混合。
7、根据权利要求2所述的一种氯雷他定口腔崩解片剂，其特征在于制备1000片片剂时使用氯雷他定250g、甘露醇420g、微晶纤维素150g、交聚维酮70g及适量的香精、甜味剂和润滑剂。
8、根据权利要求2所述的一种氯雷他定口腔崩解片剂，其特征在于制备1000片片剂时使用氯雷他定250g、山梨醇400g、葡萄糖80g、蔗糖70g、交联羧甲基纤维素钠60g、二氧化硅20g及适量的香精、甜味剂和润滑剂。
9、根据权利要求2所述的一种氯雷他定口腔崩解片剂，其特征在于制备1000片片剂时使用氯雷他定250g、甘露醇200g、蔗糖220g、明胶50g、羟乙基纤维素40g及适量香精。
10、根据权利要求1～9任何一项所述的一种氯雷他定口腔崩解片剂的制备方法，其特征在于按组分配方混合，用粉末压片法或冷冻干燥法制备得到片剂。
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| CN100463674C (zh) * | 2006-12-22 | 2009-02-25 | 江苏奥赛康药业有限公司 | 一种氯雷他定口腔速溶膜及其制备方法 |
| CN102048682B (zh) * | 2009-10-31 | 2012-09-12 | 鲁南制药集团股份有限公司 | 一种氯雷他定的乳膏剂及其应用 |
| RU2566270C2 (ru) * | 2010-03-29 | 2015-10-20 | Ферринг Б.В. | Быстрорастворимая фармацевтическая композиция |
| RU2566269C2 (ru) * | 2010-03-29 | 2015-10-20 | Ферринг Б.В. | Быстрорастворимая фармацевтическая композиция |
| CN107648191A (zh) * | 2017-09-27 | 2018-02-02 | 扬子江药业集团上海海尼药业有限公司 | 一种氯雷他定片及其制备工艺 |
| US9974826B2 (en) | 2008-05-21 | 2018-05-22 | Ferring B.V. | Methods comprising desmopressin |
| US10137167B2 (en) | 2008-05-21 | 2018-11-27 | Ferring B.V. | Methods comprising desmopressin |
| CN111249239A (zh) * | 2020-01-17 | 2020-06-09 | 中国药科大学 | 一种氯雷他定纳米晶体及其制备方法 |
| US11963995B2 (en) | 2008-05-21 | 2024-04-23 | Ferring B.V. | Methods comprising desmopressin |
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| CN100463674C (zh) * | 2006-12-22 | 2009-02-25 | 江苏奥赛康药业有限公司 | 一种氯雷他定口腔速溶膜及其制备方法 |
| US9974826B2 (en) | 2008-05-21 | 2018-05-22 | Ferring B.V. | Methods comprising desmopressin |
| US10137167B2 (en) | 2008-05-21 | 2018-11-27 | Ferring B.V. | Methods comprising desmopressin |
| US11020448B2 (en) | 2008-05-21 | 2021-06-01 | Ferring B.V. | Methods comprising desmopressin |
| US11963995B2 (en) | 2008-05-21 | 2024-04-23 | Ferring B.V. | Methods comprising desmopressin |
| CN102048682B (zh) * | 2009-10-31 | 2012-09-12 | 鲁南制药集团股份有限公司 | 一种氯雷他定的乳膏剂及其应用 |
| RU2566270C2 (ru) * | 2010-03-29 | 2015-10-20 | Ферринг Б.В. | Быстрорастворимая фармацевтическая композиция |
| RU2566269C2 (ru) * | 2010-03-29 | 2015-10-20 | Ферринг Б.В. | Быстрорастворимая фармацевтическая композиция |
| CN107648191A (zh) * | 2017-09-27 | 2018-02-02 | 扬子江药业集团上海海尼药业有限公司 | 一种氯雷他定片及其制备工艺 |
| CN107648191B (zh) * | 2017-09-27 | 2018-08-17 | 扬子江药业集团上海海尼药业有限公司 | 一种氯雷他定片及其制备工艺 |
| CN111249239A (zh) * | 2020-01-17 | 2020-06-09 | 中国药科大学 | 一种氯雷他定纳米晶体及其制备方法 |
| CN111249239B (zh) * | 2020-01-17 | 2022-02-11 | 中国药科大学 | 一种氯雷他定纳米晶体及其制备方法 |
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