CN111728954A - 一种盐酸倍他司汀软胶囊及其制备方法 - Google Patents
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Abstract
一种盐酸倍他司汀软胶囊及其制备方法,该软胶囊含有活性成分是盐酸倍他司汀,每粒软胶囊含盐酸倍他司汀4mg~8mg,该软胶囊包括原料药粉或药液及胶液两部分,所述药液由原料药粉和填充物组成。将明胶与甘油、蒸馏水溶解后配制胶液,涂于平坦的钢板表面,使厚薄均匀,然后加热使表面水分蒸发成软胶片;将盐酸倍他司汀原料药粉碎过80目筛,加入植物油搅拌均匀,制成药液,将药液置于两块胶片之间,用压丸模制成胶囊,开启模板取出胶丸,洗涤两次,干燥,得到盐酸倍他司汀软胶囊。优点是:属口服固体制剂,剂型为软胶囊,携带和使用方便,且可以有效防止药物吸潮。采用钢板模压制法和旋转模压制法制成,工艺简单,制作方便。
Description
技术领域
本发明涉及一种盐酸倍他司汀软胶囊及其制备方法。
背景技术
盐酸倍他司汀为双胺氧化酶抑制剂。对脑血管、心血管,特别是对椎底动脉***有较明显的扩张作用,显著增加心、脑及周围循环血流量,改善血循环,并降低全身血压,此外能增加耳蜗和前底血流量,从而消除内耳性眩晕、耳鸣和耳闭感,还能增加毛细血管通透性,促进细胞外液的吸收,消除淋巴内水肿,能对抗儿茶酚胺的缩血管作用及降低动脉压,并有抑制血浆凝固及ADP诱导的血小板凝集作用,能延长大白鼠体外血栓形成时间,还有轻微的利尿作用。临床上主要用于美尼尔氏综合症,血管性头痛及脑动脉硬化,并可用于治疗急性缺血性脑血管疾病,如脑血栓,脑栓塞,一过性脑供血不足等,高血压所致的直立性眩晕,耳鸣等亦有效。
盐酸倍他司汀上市以来,以其确切的疗效和较少的毒副反应而受到医务工作者和患者的重视和欢迎,但由于其较强的吸湿性,难于制成口服固体制剂,临床上常用的基本局限于口服溶液和注射剂(包括粉针剂、输液),由于其成本较高,且携带服用均不方便,尤其对老年患者更是如此,因此限制了盐酸倍他司汀的广泛应用。
发明内容
本发明要解决的技术问题是提供一种盐酸倍他司汀胶囊及其制备方法,属口服固体制剂,剂型为软胶囊,携带和使用方便,且可有效防止药物吸潮。
本发明的技术方案是:
一种盐酸倍他司汀软胶囊,其特殊之处在于:软胶囊含有活性成分是盐酸倍他司汀,每粒软胶囊含盐酸倍他司汀4mg~8mg,该软胶囊包括原料药粉或药液及胶液两部分,所述药液由原料药粉和填充物组成,原料药粉与胶液中的明胶的质量比为1:(31.25~37.5),所述填充物为植物油。
进一步的,所述胶液是由明胶、增塑剂和水组成,其中,明胶与增塑剂、水的质量比分别为1:(0.6~0.68)、1:(1~1.5),增塑剂为甘油。
进一步的,所述植物油为花生油或大豆油,所述植物油与原料药粉的质量比为(3~5):0.8。
进一步的,所述软胶囊包括原料药粉和胶液两部分时,在原料药粉中还加入助溶剂。
进一步的,所述助溶剂为对氨基苯甲酸。
进一步的,所述原料药粉与助溶剂的质量比为1:2.5。
进一步的,所述软胶囊外层还包覆一层肠溶衣,所述肠溶衣包衣剂由聚乙烯醇、增塑剂聚乙二醇和水组成,所述聚乙烯醇与聚乙二醇、水的质量比分别为6:1、1:20。
一种盐酸倍他司汀软胶囊的制备方法,其具体步骤如下:
将明胶与甘油、蒸馏水溶解后配制胶液,涂于平坦的钢板表面,使厚薄均匀,然后以70℃~95℃的温度加热使表面水分蒸发成软胶片;将盐酸倍他司汀原料药粉碎过80目筛,加入植物油搅拌均匀,制成药液,将药液置于两块胶片之间,用压丸模制成胶囊,开启模板取出胶丸,洗涤两次,干燥,得到盐酸倍他司汀软胶囊。
一种盐酸倍他司汀软胶囊的制备方法,其具体步骤如下:
将盐酸倍他司汀粉碎过80目筛,放入自动旋转压囊机的灌装槽内待用;取甘油和水混合均匀,加热至70℃~80℃,加入明胶搅拌,明胶全溶后,加入非离子表面活性剂对氨基苯甲酸,搅拌均匀,放入自动旋转压囊机的铺展箱内,开启自动旋转压囊机,制成盐酸倍他司汀软胶囊。
一种盐酸倍他司汀软胶囊的制备方法,其具体步骤如下:
(1)将明胶与甘油、蒸馏水溶解后配制胶液,涂于平坦的钢板表面,使厚薄均匀,然后以70℃~95℃的温度加热使表面水分蒸发成软胶片;
(2)将盐酸倍他司汀原料药粉碎过80目筛,加入植物油搅拌均匀,制成药液,将药液置于两块胶片之间,用压丸模制成胶囊,开启模板取出胶丸,洗涤两次,干燥,得到盐酸倍他司汀软胶囊;
(3)包肠溶衣
取聚乙烯醇酞酸酯和聚乙二醇,加水使其溶解,配成肠溶衣液;将盐酸倍他司汀软胶囊加入包衣机,开动包衣机,将肠溶衣液均匀喷于盐酸倍他司汀上,干燥,得到盐酸倍他司汀肠溶软胶囊。
本发明提供将盐酸倍他司汀原料药和植物油类制成药物溶液,或将盐酸倍他司汀原料药份按照规定比例制成软胶囊,使用甘油作为增塑剂具有较强吸湿能力,从而保证药物有较好的稳定性,并无任何气味,促其成为透明或半透明的软胶囊,其外观,溶出度,含量符合中国药典各项规定。盐酸倍他司汀软胶囊剂型为软胶囊,属口服固体制剂,携带和使用方便,且可有效防止药物吸潮。采用钢板模压制法和旋转模压制法制成,工艺简单,制作方便。
具体实施方式
下面的实施例仅限于解释本发明,而不针对实施本发明有所限制。
实施例1
处方
制备工艺(压制法)
(1)明胶与甘油、蒸馏水溶解后配成胶夜,涂于平坦的钢板表面,使厚薄均匀,然后以70℃~95℃的温度加热使表面水分蒸发,制成软胶片;
(2)将盐酸倍他司汀原料药粉碎过80目筛,加入花生油搅拌均匀,制成药液,将药液置于两块胶片之间,用压丸模制成胶囊,开启模板取出胶丸,洗涤两次,干燥,得到成品盐酸倍他司汀软胶囊200粒,每粒含盐酸倍他司汀4mg。
按照溶出度测定法(中国药典二部附录),取六粒盐酸倍他司汀软胶囊样品,分别测定溶出度,六组检测结果如表1所示:
表1六组盐酸倍他司汀软胶囊溶出度测定结果(批号:190301)
1# | 2# | 3# | 4# | 5# | 6# |
95.6% | 97.3% | 96.5% | 95.5% | 98.1% | 100.2% |
按照溶出度测定法(中国药典二部附录),取盐酸倍他司汀软胶囊样品,以不同的时间测定溶产品出度,结果如表2所示:
表2不同时间盐酸倍他司汀软胶囊溶出度测定结果(批号:190301)
时间 | 10天 | 20天 | 30天 | 40天 | 50天 | 60天 |
含量 | 90% | 89% | 92% | 85% | 91% | 92% |
按照溶出度测定法(中国药典二部附录),取盐酸倍他司汀软胶囊样品,测定10组含量均匀度,结果如表3所示
表3盐酸倍他司汀软胶囊含量均匀度测定结果(批号:190301)
第1组 | 第2组 | 第3组 | 第4组 | 第5组 | 第6组 | 第7组 | 第8组 | 第9组 | 第10组 |
90.3% | 95.1% | 96.2% | 91.1% | 97.8% | 99.1% | 92.3% | 93.4% | 96.1% | 98.1% |
实施例2
处方
将盐酸倍他司汀粉碎过80目筛,放入自动旋转压囊机的灌装槽内待用;取甘油和水混合均匀,加热至70℃~80℃,加入明胶搅拌,明胶全溶后,加入非离子表面活性剂对氨基苯甲酸,搅拌均匀,放入自动旋转压囊机的铺展箱内,开启自动旋转压囊机,制成成品盐酸倍他司汀软胶囊100粒,每粒含盐酸倍他司汀8mg。
按照溶出度测定法(中国药典二部附录),取六粒盐酸倍他司汀软胶囊样品,分别测定溶出度,六组检测结果如表4所示:
表4六组盐酸倍他司汀软胶囊溶出度测定结果(批号:190302)
1# | 2# | 3# | 4# | 5# | 6# |
92.1% | 95.3% | 94.5% | 98.2% | 99.3% | 95.6% |
按照溶出度测定法(中国药典二部附录),取盐酸倍他司汀软胶囊样品,以不同的时间测定产品溶出度,结果如表5所示:
表5不同时间盐酸倍他司汀软胶囊溶出度测定结果(批号:190302)
时间 | 10天 | 20天 | 30天 | 40天 | 50天 | 60天 |
含量 | 88% | 90% | 86% | 90% | 93% | 95% |
按照溶出度测定法(中国药典二部附录),取盐酸倍他司汀软胶囊样品,测定10组含量均匀度,结果如表6所示
表6盐酸倍他司汀软胶囊含量均匀度测定结果(批号:190302)
第1组 | 第2组 | 第3组 | 第4组 | 第5组 | 第6组 | 第7组 | 第8组 | 第9组 | 第10组 |
95.1% | 96.2% | 91.3% | 94.1% | 94.2% | 96.1% | 98.9% | 92.1% | 93.1% | 96.2% |
实施例3
处方
(1)明胶与甘油、25g蒸馏水溶解后配成胶液,涂于平坦的钢板表面,使厚薄均匀,在70℃~95℃温度下加热,使表面水分蒸发,制成半透明软胶片;
(2)将盐酸倍他司汀粉碎过80目筛,加入大豆油搅拌均匀,制成药液,将药液置于两块胶片之间,由压丸模制成胶丸,开启模板取出胶丸,洗涤两次,干燥,得到盐酸倍他司汀软胶囊;
(3)包肠溶衣
取聚乙烯醇酞酸酯3g,聚乙二醇400 0.5g,加60g蒸馏水水使溶解,配成肠溶衣液;将盐酸倍他司汀软胶囊加入包衣机,开动包衣机,将肠溶衣液均匀喷于软胶囊上,干燥,即得成品盐酸倍他司汀肠溶软胶囊200粒,每粒含盐酸倍他司汀4mg。
取上述样品在不同的时间测定耐酸力,结果如表7所示:
表7耐酸力测定结果(批号190303)
时间 | 10天 | 20天 | 30天 | 40天 | 50天 | 60天 |
含量 | 95% | 97% | 94% | 96% | 93% | 95% |
以上仅为本发明的具体实施例而已,并不用于限制本发明,对于本领域的技术人员来说,本发明可以有各种更改和变化。凡在本发明的精神和原则之内,所作的任何修改、等同替换、改进等,均应包含在本发明的保护范围之内。
Claims (10)
1.一种盐酸倍他司汀软胶囊,其特征是:软胶囊含有活性成分是盐酸倍他司汀,每粒软胶囊含盐酸倍他司汀4mg~8mg,该软胶囊包括原料药粉或药液及胶液两部分,所述药液由原料药粉和填充物组成,原料药粉与胶液中的明胶的质量比为1:(31.25~37.5),所述填充物为植物油。
2.根据权利要求1所述的盐酸倍他司汀软胶囊,其特征是:所述胶液是由明胶、增塑剂和水组成,其中,明胶与增塑剂、水的质量比分别为1:(0.6~0.68)、1:(1~1.5),增塑剂为甘油。
3.根据权利要求1所述的盐酸倍他司汀软胶囊,其特征是:所述植物油为花生油或大豆油,所述植物油与原料药粉的质量比为(3~5):0.8。
4.根据权利要求1所述的盐酸倍他司汀软胶囊,其特征是:所述软胶囊包括原料药粉和胶液两部分时,在原料药粉中还加入助溶剂。
5.根据权利要求4所述的盐酸倍他司汀软胶囊,其特征是:所述助溶剂为对氨基苯甲酸。
6.根据权利要求4所述的盐酸倍他司汀软胶囊,其特征是:所述原料药粉与助溶剂的质量比为1:2.5。
7.根据权利要求1所述的盐酸倍他司汀软胶囊,其特征是:所述软胶囊外层还包覆一层肠溶衣,所述肠溶衣包衣剂由聚乙烯醇、增塑剂聚乙二醇和水组成,所述聚乙烯醇与聚乙二醇、水的质量比分别为6:1、1:20。
8.一种如权利要求1所述的盐酸倍他司汀软胶囊的制备方法,其特征是:
将明胶与甘油、蒸馏水溶解后配制胶液,涂于平坦的钢板表面,使厚薄均匀,然后以70℃~95℃的温度加热使表面水分蒸发成软胶片;将盐酸倍他司汀原料药粉碎过80目筛,加入植物油搅拌均匀,制成药液,将药液置于两块胶片之间,用压丸模制成胶囊,开启模板取出胶丸,洗涤两次,干燥,得到盐酸倍他司汀软胶囊。
9.一种如权利要求1所述的盐酸倍他司汀软胶囊的制备方法,其特征是:
将盐酸倍他司汀粉碎过80目筛,放入自动旋转压囊机的灌装槽内待用;取甘油和水混合均匀,加热至70℃~80℃,加入明胶搅拌,明胶全溶后,加入非离子表面活性剂对氨基苯甲酸,搅拌均匀,放入自动旋转压囊机的铺展箱内,开启自动旋转压囊机,制成盐酸倍他司汀软胶囊。
10.一种如权利要求7所述的盐酸倍他司汀软胶囊的制备方法,其特征是:
(1)将明胶与甘油、蒸馏水溶解后配制胶液,涂于平坦的钢板表面,使厚薄均匀,然后以70℃~95℃的温度加热使表面水分蒸发成软胶片;
(2)将盐酸倍他司汀原料药粉碎过80目筛,加入植物油搅拌均匀,制成药液,将药液置于两块胶片之间,用压丸模制成胶囊,开启模板取出胶丸,洗涤两次,干燥,得到盐酸倍他司汀软胶囊;
(3)包肠溶衣
取聚乙烯醇酞酸酯和聚乙二醇,加水使其溶解,配成肠溶衣液;将盐酸倍他司汀软胶囊加入包衣机,开动包衣机,将肠溶衣液均匀喷于盐酸倍他司汀上,干燥,得到盐酸倍他司汀肠溶软胶囊。
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