CN109908354A - 盐酸舍曲林口服浓缩液及其制备工艺 - Google Patents
盐酸舍曲林口服浓缩液及其制备工艺 Download PDFInfo
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
本申请涉及药品领域,具体为盐酸舍曲林口服浓缩液及其制备工艺。该口服液处方由盐酸舍曲林、甘油、乙醇、抗氧剂、甜味剂、香精组成。与常规固体制剂如片剂、胶囊相比,口服液分散度大,吸收快,生物利用度高。同时,口服液可以提高了患者的顺应性,方便具有吞咽口服固体制剂困难的患者使用,保证给药剂量的准确性。此外,本发明采用抗氧剂叔丁基羟基茴香醚(BHA),可减少有关物质,使制剂性质更稳定。
Description
技术领域
本发明属于医药技术领域,具体涉及一种盐酸舍曲林口服浓缩液及其制备工艺。
背景技术
舍曲林是选择性5-羟色胺再回收抑制剂中最新的一种,能帮助提高机体的能力,有效地减轻病人的抑郁症状,包括烦躁情绪,并能减轻持续性的疲劳症状以及焦虑状态,具有长效、对肝细胞毒性低、体内清除快等特点,在国际上已广泛用以治疗抑郁性及强迫性精神障碍。美国辉瑞制药公司将其开发为盐酸舍曲林口服浓缩液及片剂,商品名为ZOLOFT(左洛复)目前已在多个国家上市。
与常规固体制剂如片剂、胶囊相比,口服液分散度大,吸收快,生物利用度高。同时,口服液可以提高了患者的顺应性,方便具有吞咽口服固体制剂困难的患者使用,保证给药剂量的准确性。此外,本专利采用抗氧剂叔丁基羟基茴香醚(BHA),可减少有关物质,使制剂性质更稳定。
发明内容
本申请的目的在于在于提供一种盐酸舍曲林口服浓缩液及其制备工艺,本申请的目的是通过如下方案解决的:
所述的盐酸舍曲林口服浓缩液,含有盐酸舍曲林、甘油、乙醇、抗氧剂、甜味剂、香精及纯水。
所述的盐酸舍曲林口服浓缩液,抗氧剂为叔丁基羟基茴香醚(BHA)、2,6-二叔丁基羟基甲苯(BHT)、维生素E、抗坏血酸棕榈酸酯的一种或两者以上的混合物,优选叔丁基羟基茴香醚(BHA)。
所述的盐酸舍曲林口服浓缩液,甜味剂为山梨糖醇、甘露醇、果糖、蔗糖、麦芽糖、乳糖、葡萄糖、木糖醇、糖精钠、阿司帕坦、甜菊苷中的一种或两者以上的混合物,优选阿司帕坦。
所述的盐酸舍曲林口服浓缩液,香精为苹果、水蜜桃、樱桃、橙味、草莓,哈密瓜中的一种或两者以上的混合物。
所述的盐酸舍曲林口服浓缩液,包含如下比例的成分:
所述的盐酸舍曲林口服浓缩液,将抗氧剂、甜味剂、香精加入到处方量的乙醇中磁力搅拌溶解,倒入容量瓶中,加入一定量的甘油定容。倒入烧杯中,磁力搅拌混合均匀,加入处方量的原料药进行磁力搅拌溶解,溶解后进行超声15min除气泡,既得样品。
具体实施方式
本申请涉及盐酸舍曲林口服浓缩液及其制备工艺,本领域技术人员可以借鉴本文内容,适当改进工艺参数实现。特别需要指出的是,所有类似的替换和改动对本领域技术人员来说是显而易见的,它们都被视为包括在本发明。本申请的方法及应用已经通过较佳实施例进行了描述,相关人员明显能在不脱离本申请内容、精神和范围内对本文所述的方法和应用进行改动或适当变更与组合,来实现和应用本发明技术。
实施例1:
制备工艺:
将抗氧剂、甜味剂、香精加入到处方量的乙醇中磁力搅拌溶解,倒入容量瓶中,加入一定量的甘油定容。倒入烧杯中,磁力搅拌混合均匀,加入处方量的原料药进行磁力搅拌溶解,溶解后进行超声15min除气泡,既得样品。
实施例2:
制备工艺:
将抗氧剂、甜味剂、香精加入到处方量的乙醇中磁力搅拌溶解,倒入容量瓶中,加入一定量的甘油定容。倒入烧杯中,磁力搅拌混合均匀,加入处方量的原料药进行磁力搅拌溶解,溶解后进行超声15min除气泡,既得样品。
实施例3:
制备工艺:
将抗氧剂、甜味剂、香精加入到处方量的乙醇中磁力搅拌溶解,倒入容量瓶中,加入一定量的甘油定容。倒入烧杯中,磁力搅拌混合均匀,加入处方量的原料药进行磁力搅拌溶解,溶解后进行超声15min除气泡,既得样品。
实施例4:
制备工艺:
将抗氧剂、甜味剂、香精加入到处方量的乙醇中磁力搅拌溶解,倒入容量瓶中,加入一定量的甘油定容。倒入烧杯中,磁力搅拌混合均匀,加入处方量的原料药进行磁力搅拌溶解,溶解后进行超声15min除气泡,既得样品。
实施例5:
制备工艺:
将抗氧剂、甜味剂、香精加入到处方量的乙醇中磁力搅拌溶解,倒入容量瓶中,加入一定量的甘油定容。倒入烧杯中,磁力搅拌混合均匀,加入处方量的原料药进行磁力搅拌溶解,溶解后进行超声15min除气泡,既得样品。
对比实施例1:
制备工艺:
将抗氧剂、甜味剂、香精加入到处方量的乙醇中磁力搅拌溶解,倒入容量瓶中,加入一定量的甘油定容。倒入烧杯中,磁力搅拌混合均匀,加入处方量的原料药进行磁力搅拌溶解,溶解后进行超声15min除气泡,既得样品。
有关物质结果:
实施例1、2、3、4、5与对比实施例1相比,有关物质最大未知单杂、总杂均明显优于对比实施例,实施例1、4、5选用抗氧剂叔丁基羟基茴香醚(BHA),有关物质最大未知单杂、总杂均明显优于实施例2、3,抗氧剂优选叔丁基羟基茴香醚(BHA)。
与常规固体制剂如片剂、胶囊相比,口服液分散度大,吸收快,生物利用度高。同时,口服液可以提高了患者的顺应性,方便具有吞咽口服固体制剂困难的患者使用,保证给药剂量的准确性。此外,本专利采用抗氧剂叔丁基羟基茴香醚(BHA),可减少有关物质,使制剂性质更稳定。
Claims (7)
1.一种盐酸舍曲林口服浓缩液,含有盐酸舍曲林、甘油、乙醇、抗氧剂、甜味剂、香精及纯水。
2.根据权利要求1所述的盐酸舍曲林口服浓缩液,抗氧剂为叔丁基羟基茴香醚(BHA)、2,6-二叔丁基羟基甲苯(BHT)、维生素E、抗坏血酸棕榈酸酯的一种或两者以上的混合物,优选抗氧剂为叔丁基羟基茴香醚(BHA)。
3.根据权利要求2所述的盐酸舍曲林口服浓缩液,抗氧剂为叔丁基羟基茴香醚(BHA)的用量范围为0.1~1.5 %。
4.根据权利要求1所述的盐酸舍曲林口服浓缩液,甜味剂为山梨糖醇、甘露醇、果糖、蔗糖、麦芽糖、乳糖、葡萄糖、木糖醇、糖精钠、阿司帕坦、甜菊苷中的一种或两者以上的混合物,优选阿司帕坦。
5.根据权利要求1所述的盐酸舍曲林口服浓缩液,香精为苹果、水蜜桃、樱桃、橙味、草莓,哈密瓜中的一种或两者以上的混合物。
6.根据权利要求1所述的盐酸舍曲林口服浓缩液,包含如下比例成分
。
7.根据权利要求1-6所述的盐酸舍曲林口服浓缩液,制备方法为:将抗氧剂、甜味剂、香精加入到处方量的乙醇中磁力搅拌溶解,倒入容量瓶中,加入一定量的甘油定容;倒入烧杯中,磁力搅拌混合均匀,加入处方量的原料药进行磁力搅拌溶解,溶解后进行超声15min除气泡,既得样品。
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| CN1261794A (zh) * | 1997-07-01 | 2000-08-02 | 辉瑞产品公司 | 增溶的舍曲林组合物 |
| CN1323202A (zh) * | 1998-10-13 | 2001-11-21 | 辉瑞产品公司 | 口服舍曲林浓缩物 |
| US20030096868A1 (en) * | 1998-10-13 | 2003-05-22 | Nancy J. Harper | Sertraline oral concentrate |
| CN101623252A (zh) * | 2008-07-09 | 2010-01-13 | 北京德众万全药物技术开发有限公司 | 盐酸舍曲林的口服液及其制备方法 |
| CN101632632A (zh) * | 2008-07-21 | 2010-01-27 | 北京迈劲医药科技有限公司 | 舍曲林口服水溶液及其制备方法 |
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| CN1261794A (zh) * | 1997-07-01 | 2000-08-02 | 辉瑞产品公司 | 增溶的舍曲林组合物 |
| CN1323202A (zh) * | 1998-10-13 | 2001-11-21 | 辉瑞产品公司 | 口服舍曲林浓缩物 |
| US20030096868A1 (en) * | 1998-10-13 | 2003-05-22 | Nancy J. Harper | Sertraline oral concentrate |
| CN101623252A (zh) * | 2008-07-09 | 2010-01-13 | 北京德众万全药物技术开发有限公司 | 盐酸舍曲林的口服液及其制备方法 |
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