CN116159030A - 一种乙酰半胱氨酸咀嚼片及其制备方法 - Google Patents
一种乙酰半胱氨酸咀嚼片及其制备方法 Download PDFInfo
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Abstract
本发明公开了一种乙酰半胱氨酸咀嚼片及其制备方法，属于药物剂型技术领域。该乙酰半胱氨酸咀嚼片包括以下按重量份计的组分：乙酰半胱氨酸20份、乳糖16‑22份、甘露醇4‑8份、木糖醇3‑7份、苹果粉6‑12份、薄荷脑0.2‑0.6份、矫味剂0.03‑0.05份、润滑剂0.3‑0.5份。其制备方法包括原料粉碎过筛、称量混合、制粒、干燥、整粒、混合及压片等步骤。本发明的乙酰半胱氨酸咀嚼片能够很好地掩盖药物本身气味，大大提高服用顺应性，且方便服用。
Description
技术领域
本发明涉及药物剂型技术领域，具体涉及一种乙酰半胱氨酸咀嚼片及其制备方法。
背景技术
乙酰半胱氨酸为还原型谷胱甘肽(GSH)的前体，属体内氧自由基清除剂，其化学名为N-乙酰基-L-半胱氨酸，分子式为C5H9NO3S，相对分子质量为163.20,外观为白色结晶粉末，熔点为109～111℃，易溶于水和乙醇；有类似蒜的臭气，味酸，有吸湿性。乙酰半胱氨酸具有较强的粘痰溶解作用，其分子中所含的巯基能使痰液中糖蛋白多肽链中的二硫键断裂，从而降低痰液的粘滞性，并使痰液化而易咳出。乙酰半胱氨酸还能使脓性痰液中的DNA纤维断裂，因此不仅能溶解白色黏痰，也能溶解脓性痰，因此一般作为粘液溶解剂使用。其后又发现乙酰半胱氨酸具有肝脏细胞的保护作用而用于治疗醋氨酚中毒所致的肝脏毒性损伤，现在已是治疗醋氨酚中毒的重要药物。最近大量的研究发现乙酰半胱氨酸在如艾滋病、癌症、药物及重金属中毒、心脏病，帕金森病以及吸烟损害等方面具有广泛的作用。经国内外的多年研究证实，口服乙酰半胱氨酸在临床应用上具有极大的价值，随着研究的深入会有更多新的发现，乙酰半胱氨酸将会更引人注目。目前，国内上市的口服乙酰半胱氨酸已有片剂、喷雾剂、颗粒剂、粉剂等剂型。其中，喷雾剂局部作用于气管，吸入时有一定刺激性，使支气管有烧灼感，可引起咳呛、恶心、呕吐、口臭等。虽然片剂、颗粒剂、粉剂的刺激性比喷雾剂要轻微一些，但是片剂、颗粒剂、粉剂对冲服的水温有要求(低于40度)，这给一般患者增加了难度，另外由乙酰半胱氨酸分子中存在的硫基带来的不良味道和气味依然会引起儿童和过敏体质人群的排斥。因此，目前市面上几乎没有乙酰半胱氨酸咀嚼片。但随着人们对常用口释药品服用要求的不断提高，传统的片剂、喷雾剂、颗粒剂、粉剂已经不能满足人们对方便快捷的需求。因此，十分有必要研发一种方便服用、能够很好掩盖药物本身气味、提高服用顺应性的乙酰半胱氨酸咀嚼片及其制备方法。
发明内容
为了克服现有技术的不足，本发明的目的在于提供一种乙酰半胱氨酸咀嚼片，该乙酰半胱氨酸咀嚼片能够很好地掩盖药物本身气味，大大提高服用顺应性，且方便服用。
为解决上述问题，本发明所采用的技术方案如下：
一种乙酰半胱氨酸咀嚼片，其包括以下按重量份计的组分：乙酰半胱氨酸20份、乳糖16-22份、甘露醇4-8份、木糖醇3-7份、苹果粉6-12份、薄荷脑0.2-0.6份、矫味剂0.03-0.05份、润滑剂0.3-0.5份。
在上述配方中，乳糖的粘合性好，将乳糖作为咀嚼片的辅料，不易吸潮，可压性好，片剂表面光滑美观，且有着很好的化学稳定性。
甘露醇作在本发明的片剂用赋形剂，具有良好的制粒性，而且具有爽口、化学稳定性好、有甜味、对口腔有舒服感的优点，特别适用于本发明的赋形剂。
木糖醇作为低糖甜味剂、口感清凉，在本发明配方中与其它辅料协同作为营养补充剂和辅助治疗剂，适合糖尿病患者服用。
苹果其味道酸甜适口，营养丰富。苹果的香气对人的心理影响最大，配方中加入苹果能协助遮掩主药的气味，且富含鞣酸、果胶、膳食纤维既有通便又有止泻的双重功效与作用，非常适合老人和病人服用。
薄荷脑，作为赋香剂用于本制剂中，使咀嚼片产生清凉的、新鲜的、愉快的薄荷特征香气，提升服用过程的舒适感。
阿斯巴甜和三氯蔗糖为甜味素，安全性高，甜味纯正，具有和蔗糖极其近似的清爽甜味，在本发明中作为必要矫味剂，且有明显的增甜、增香效果，能有效掩盖乙酰半胱氨酸的气味，且香味持久。
作为本发明优选的方案，本发明的乙酰半胱氨酸咀嚼片包括以下按重量份计的组分：乙酰半胱氨酸20份、乳糖16份、甘露醇4份、木糖醇6份、苹果粉4份、薄荷脑0.4份、矫味剂0.05份、润滑剂0.5份。
作为本发明优选的方案，所述矫味剂为阿斯巴甜和/或三氯蔗糖。
作为本发明优选的方案，所述润滑剂为硬脂酸镁或微粉硅胶。
本发明还提供了如上所述的乙酰半胱氨酸咀嚼片的制备方法，其包括以下步骤：
S1、将乙酰半胱氨酸及辅料粉碎后分别过60～80目筛，按配方量准确称量各组分，备用；
S2、将除润滑剂外的组分充分混合，得到总混合粉；向总混合粉中加入体积浓度为60％～70％的乙醇制软材，用16～20目筛制颗粒，在40～60℃下减压干燥4～8h，使颗粒水分为3％～4％；
S3、将步骤S2干燥好的物料过20～30目筛整粒，加入润滑剂并充分混合；
S4、压片，并控制片重为490～510mg，包装，即得。
作为本发明优选的方案，所述步骤S2的混合时间为20～30min。
作为本发明优选的方案，所述步骤S3的混合时间为10～20min。
相比现有技术，本发明的有益效果在于：
本发明以乙酰半胱氨酸、乳糖、甘露醇、苹果粉、薄荷脑等原料并以科学合理的配比制备了乙酰半胱氨酸咀嚼片，得到的乙酰半胱氨酸咀嚼片能够很好地掩盖药物本身气味，口感良好、易被患者接受，大大提高服用顺应性，且方便服用。
本发明提供的乙酰半胱氨酸咀嚼片的制备方法包括粉碎的原料经过混合、预制软材、制粒、干燥、压片等工序，制成表面光滑、酸甜适口的乙酰半胱氨酸咀嚼片。
附图说明
图1为本发明所述的乙酰半胱氨酸咀嚼片的制备方法的工艺流程图；
图2为本发明实施例1所制得的乙酰半胱氨酸咀嚼片的实物图。
具体实施方式
下面结合附图和具体实施方式对本发明作进一步详细说明。
实施例1
一种乙酰半胱氨酸咀嚼片，其包括以下按重量份计的组分：乙酰半胱氨酸20份、乳糖16份、甘露醇4份、木糖醇6份、苹果粉4份、薄荷脑0.4份、阿斯巴甜0.05份、润滑剂0.5份。
如图1所示，其制备方法括如下步骤：
S1、将乙酰半胱氨酸及辅料粉碎后分别过60目筛，按配方量准确称量各组分，备用；
S2、将除润滑剂外的组分充分混合30min，得到总混合粉；向总混合粉中加入体积浓度为60％的乙醇制软材，用16目筛制颗粒，在60℃下减压干燥，使颗粒水分为3％～4％；
S3、将步骤S2干燥好的物料过20目筛整粒，加入配方量的润滑剂并充分混合10min；
S4、压片，并控制片重为0.5g/片，包装，即得。
实施例2
一种乙酰半胱氨酸咀嚼片，其包括以下按重量份计的组分：乙酰半胱氨酸20份、乳糖16份、甘露醇4份、木糖醇5份、苹果粉5份、薄荷脑0.4份、阿斯巴甜0.05份、润滑剂0.5份。
其制备方法包括如下步骤：
S1、将乙酰半胱氨酸及辅料粉碎后分别过60目筛，按配方量准确称量各组分，备用；
S2、将除润滑剂外的组分充分混合30min，得到总混合粉；向总混合粉中加入体积浓度为70％的乙醇制软材，用16目筛制颗粒，在50℃下减压干燥，使颗粒水分为3％～4％；
S3、将步骤S2干燥好的物料过20目筛整粒，加入配方量的润滑剂并充分混合10min；
S4、压片，并控制片重为0.5g/片，包装，即得。
实施例3
一种乙酰半胱氨酸咀嚼片，其包括以下按重量份计的组分：酰半胱氨酸20份、乳糖16份、甘露醇4份、木糖醇4份、苹果粉6份、薄荷脑0.4份、三氯蔗糖0.05份、润滑剂0.5份。
其制备方法包括如下步骤：
S1、将乙酰半胱氨酸及辅料粉碎后分别过80目筛，按配方量准确称量各组分，备用；
S2、将除润滑剂外的组分充分混合30min，得到总混合粉；向总混合粉中加入体积浓度为70％的乙醇制软材，用20目筛制颗粒，在50℃下减压干燥，使颗粒水分为3％～4％；
S3、将步骤S2干燥好的物料过20目筛整粒，加入配方量的润滑剂并充分混合10min；
S4、压片，并控制片重为0.5g/片，包装，即得。
一、乙酰半胱氨酸咀嚼片性状考察实验
为了鉴定乙酰半胱氨酸咀嚼片的性能，排除主药成分对主成分含量的影响，以咀嚼片的硬度、外观、口感以及乙酰半胱氨酸的含量回收值为指标，分别对以上实施例的咀嚼片进行评分，其中乙酰半胱氨酸的含量回收值的测定条件包括如下步骤：
(1)色谱条件:色谱柱:C18(250mmx4.6mm)，流动相:0.01mol/L磷酸盐缓冲液(磷酸二氢钠2.4g，加水溶解后磷酸调PH至2.15，加水至2000mL)L甲醇(95:5)；检测波长:210nm；柱温：30℃，流速:1mL/min，进样量:20uL。
(2)乙酰半胱氨酸对照品溶液的制备，精密称取乙酰半胱氨酸对照品25mg，置于25mL量瓶中，加0.025mol/L磷酸盐缓冲液制成每1mL中含有乙酰半胱氨酸1mg的溶液，摇匀。
(3)供试品溶液的制备，取乙酰半胱氨酸咀嚼片10片，研磨后精密称取适量，加0.025mol/L磷酸盐缓冲液，制成每1ml中含乙酰半胱氨酸1mg的溶液。
实验结果如表1和图2所示。
表1实施例1～3的乙酰半胱氨酸咀嚼片性状考察结果
| 项目 | 外观 | 口感 | 硬度(Kg/cm2) | 含量回收值 |
| 实施例1 | 表面完整，光洁 | 爽口、酸甜、清凉可口 | 4.8 | 99.2％ |
| 实施例2 | 表面完整，光洁 | 爽口、酸甜、清凉可口 | 4.7 | 99.0％ |
| 实施例3 | 表面完整，光洁 | 爽口、酸甜、清凉可口 | 5.2 | 100.3％ |
由图2可知，本发明所制得的乙酰半胱氨酸咀嚼片表面光滑，证明本发明的配方具有较佳的压片效果。表1的结果显示，实施例1～3所制得的咀嚼片，表面完整光滑、口感爽口、酸甜、清凉可口，硬度合适，且制备方法不影响主成分的含量水平，说明采用本发明的制备方法制得的咀嚼片性能较好，适合于工业化大生产。
上述实施方式仅为本发明的优选实施方式，不能以此来限定本发明保护的范围，本领域的技术人员在本发明的基础上所做的任何非实质性的变化及替换均属于本发明所要求保护的范围。
Claims (7)
1.一种乙酰半胱氨酸咀嚼片，其特征在于：包括以下按重量份计的组分：乙酰半胱氨酸20份、乳糖16-22份、甘露醇4-8份、木糖醇3-7份、苹果粉6-12份、薄荷脑0.2-0.6份、矫味剂0.03-0.05份、润滑剂0.3-0.5份。
2.根据权利要求1所述的乙酰半胱氨酸咀嚼片，其特征在于：包括以下按重量份计的组分：乙酰半胱氨酸20份、乳糖16份、甘露醇4份、木糖醇6份、苹果粉4份、薄荷脑0.4份、矫味剂0.05份、润滑剂0.5份。
3.根据权利要求1或2所述的乙酰半胱氨酸咀嚼片，其特征在于：所述矫味剂为阿斯巴甜和/或三氯蔗糖。
4.根据权利要求1或2所述的乙酰半胱氨酸咀嚼片，其特征在于：所述润滑剂为硬脂酸镁或微粉硅胶。
5.一种如权利要求1～4中任一项所述的乙酰半胱氨酸咀嚼片的制备方法，其特征在于：包括以下步骤：
S1、将乙酰半胱氨酸及辅料粉碎后分别过60～80目筛，按配方量准确称量各组分，备用；
S2、将除润滑剂外的组分充分混合，得到总混合粉；向总混合粉中加入体积浓度为60％～70％的乙醇制软材，用16～20目筛制颗粒，在40～60℃下减压干燥4～8h，使颗粒水分为3％～4％；
S3、将步骤S2干燥好的物料过20～30目筛整粒，加入润滑剂并充分混合；
S4、压片，并控制片重为490～510mg，包装，即得。
6.根据权利要求5所述的乙酰半光氨酸咀嚼片的制备方法，其特征在于：所述步骤S2的混合时间为20～30min。
7.根据权利要求5所述的乙酰半光氨酸咀嚼片的制备方法，其特征在于：所述步骤S3的混合时间为10～20min。
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102028657A (zh) * | 2010-12-02 | 2011-04-27 | 海南美兰史克制药有限公司 | 乙酰半胱氨酸脂质体固体制剂 |
| US20190350857A1 (en) * | 2018-05-17 | 2019-11-21 | Fertin Pharma A/S | Oral tablet for taste masking of active ingredients |
| CN112206209A (zh) * | 2019-09-05 | 2021-01-12 | 杭州百诚医药科技股份有限公司 | 一种乙酰半胱氨酸颗粒剂及其制备方法 |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102028657A (zh) * | 2010-12-02 | 2011-04-27 | 海南美兰史克制药有限公司 | 乙酰半胱氨酸脂质体固体制剂 |
| US20190350857A1 (en) * | 2018-05-17 | 2019-11-21 | Fertin Pharma A/S | Oral tablet for taste masking of active ingredients |
| CN112206209A (zh) * | 2019-09-05 | 2021-01-12 | 杭州百诚医药科技股份有限公司 | 一种乙酰半胱氨酸颗粒剂及其制备方法 |
Non-Patent Citations (3)
| Title |
|---|
| 曹苗苗 等: "补骨咀嚼片的制备及其处方工艺研究", 中药材, vol. 39, no. 10, 22 November 2016 (2016-11-22), pages 2300 - 2305 * |
| 牟婵 等: "复方淫羊藿咀嚼片成型工艺研究", 亚太传统医药, vol. 12, no. 06, 22 March 2016 (2016-03-22), pages 37 - 39 * |
| 程天贵: "乙酰半胱氨酸制剂与临床应用研究进展", 中国生化药物杂志, vol. 28, no. 06, 20 December 2007 (2007-12-20), pages 430 * |
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