CN110960499A - 一种泊沙康唑胃漂浮片及其制备方法 - Google Patents
一种泊沙康唑胃漂浮片及其制备方法 Download PDFInfo
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- RAGOYPUPXAKGKH-XAKZXMRKSA-N posaconazole Chemical compound O=C1N([C@H]([C@H](C)O)CC)N=CN1C1=CC=C(N2CCN(CC2)C=2C=CC(OC[C@H]3C[C@@](CN4N=CN=C4)(OC3)C=3C(=CC(F)=CC=3)F)=CC=2)C=C1 RAGOYPUPXAKGKH-XAKZXMRKSA-N 0.000 title claims abstract description 50
- 229960001589 posaconazole Drugs 0.000 title claims abstract description 47
- 230000002496 gastric effect Effects 0.000 title claims abstract description 6
- 238000002360 preparation method Methods 0.000 title abstract description 16
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 28
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims abstract description 23
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims abstract description 19
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims abstract description 19
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims abstract description 19
- 239000008101 lactose Substances 0.000 claims abstract description 19
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims abstract description 18
- 235000019359 magnesium stearate Nutrition 0.000 claims abstract description 14
- 229910000030 sodium bicarbonate Inorganic materials 0.000 claims abstract description 9
- 235000017557 sodium bicarbonate Nutrition 0.000 claims abstract description 9
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- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 14
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 10
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 claims description 10
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- UHPMCKVQTMMPCG-UHFFFAOYSA-N 5,8-dihydroxy-2-methoxy-6-methyl-7-(2-oxopropyl)naphthalene-1,4-dione Chemical compound CC1=C(CC(C)=O)C(O)=C2C(=O)C(OC)=CC(=O)C2=C1O UHPMCKVQTMMPCG-UHFFFAOYSA-N 0.000 description 1
- 201000002909 Aspergillosis Diseases 0.000 description 1
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- 201000008827 tuberculosis Diseases 0.000 description 1
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Abstract
本发明公开了一种泊沙康唑胃漂浮片及其制备方法。该泊沙康唑胃漂浮片包括包括以下重量百分比成分:泊沙康唑20%‑45%;HPMC K4M 20%‑50%;卡波姆934 5%‑20%;碳酸氢钠;1%‑10%;乳糖5%‑25%;十二烷基硫酸钠1%‑5%;PEG3%‑10%;硬脂酸镁0.5%‑5%。本发明具有具有生产工艺简单,生产设备通用,成本低,适合企业规模化生产,患者携带和吞服方便,顺应性强,提高了药物的稳定性,降低了药物的个体差异且与现有剂型具有一样的疗效的效果。
Description
技术领域
本发明涉及药物制剂领域,特别涉及一种泊沙康唑胃漂浮片及其制备方法。
背景技术
泊沙康唑是由伊曲康唑衍生而来,是一种广谱的三唑类抗真菌药,用于难治性疾病或其他药物耐药所引起的真菌感染(如曲霉菌病、结核菌病和镰刀菌病等),该药由美国Schering-Plough公司研制上市,是一种新的化学分子实体,是第一个被FDA批准的用于预防由侵袭性曲霉菌引起病变的抗菌药物。
泊沙康唑为弱碱性药物,其在在胃酸性环境中溶解度较高,溶解度约为0.8mg/mL,在pH5-7的缓冲盐溶液中溶解度<0.001mg/mL,其表明泊沙康唑到达肠道时,溶解后的泊沙康唑会沉淀,而泊沙康唑的主要吸收部位位于小肠,这就泊沙康唑生物利用率低的主要原因。由于市售肠溶片(Noxafil)采用了固体分散体技术,设备成本较高,设备目前相对通用性低;而市售另一种剂型为口服混悬液,该剂型携带和服用不方便,且有文献报道个体差异较大。因此,需要研制一种新的泊沙康唑制剂来解决该药物目前存在的弊端。
发明内容
根据本发明的一个方面,提供了一种泊沙康唑胃漂浮片,包括以下重量百分比成分:泊沙康唑20%-45%;HPMC K4M 20%-50%;卡波姆9345%-20%;碳酸氢钠;1%-10%;乳糖5%-25%;十二烷基硫酸钠1%-5%;PEG3%-10%;硬脂酸镁0.5%-5%。
在一些实施方式中,优选泊沙康唑胃漂浮片包括以下重量百分比成分:泊沙康唑29%;HPMC K4M 40.5%;卡波姆9345.8%;碳酸氢钠2.9%;乳糖13.9%;十二烷基硫酸钠1.5%;PEG 5.8%;硬脂酸镁0.6%。
根据本发明的另一个方面,提供了的泊沙康唑胃漂浮片的制备方法,制备步骤如下:
S1:将泊沙康唑、羟丙基甲基纤维素,卡波姆934,碳酸氢钠,乳糖,十二烷基硫酸钠,PEG分别过80目筛;
S2:上述物料加入混合机中混合均匀;
S3:将步骤2中物料转移至流化床中,制粒;
S4:将所得颗粒与硬脂酸镁混合后压片。
在一些实施方式中,其中的S3的步骤中,流化床制粒时不加入液体物料。
在一些实施方式中,其中的S3的步骤中,流化床制粒进风温度为40-80℃。
在一些实施方式中,其中的S3的步骤中,设定物料温度为60摄氏度,风机频率设置为15HZ;出风温度设置为40℃,制粒完成。
在一些实施方式中,其中的S3的步骤中,制粒完成后,关闭加热,设定风机频率,冷却,当物料温后收集。
在一些实施方式中,其中的S4的步骤中,压片后制得的泊沙康唑胃漂浮片的硬度为3-5KN
本品较市售肠溶片的优点在于:
1)制备工艺简单,设备普及度高,适合企业规模化生产,极具市场开发前景
2)利用药物本身的溶解特点,达到肠溶片一样的疗效。
本品较市售混悬液的优点在于:
1)患者服用方便,顺应性强
2)提高了药物的稳定性
降低了药物的个体差异
具体实施方式
下面结合实施例对本发明作进一步详细的说明。
实施例一
处方:(制备1000片)
处方组成 | 用量 |
泊沙康唑 | 100g |
羟丙基甲基纤维素K4M | 140g |
卡波姆934 | 20g |
碳酸氢钠 | 10g |
十二烷基硫酸钠 | 5g |
乳糖 | 48g |
PEG4000 | 20g |
硬脂酸镁 | 2g |
制备方法:
将泊沙康唑、羟丙基甲基纤维素,卡波姆934,碳酸氢钠,乳糖,十二烷基硫酸钠,PEG 4000分别过80目筛;
称取处方量泊沙康唑,十二烷基硫酸钠,羟丙基甲基纤维素,卡波姆934,碳酸氢钠,乳糖,十二烷基硫酸钠,PEG 4000于混合机中混合10min;
将步骤2中物料转移至流化床中,制粒,设定物料温度为60摄氏度,风机频率设置为15HZ;出风温度设置为40℃;制粒完成后,关闭加热,设定风机频率18Hz,冷却,当物料温度降至30℃时,收集物料。
将步骤3中所得物料与硬脂酸镁混合后压片,片剂硬度为3-5KN。
实施例二
处方:(制备1000片)
处方组成 | 用量 |
泊沙康唑 | 100g |
羟丙基甲基纤维素K4M | 120g |
卡波姆934 | 40g |
碳酸氢钠 | 10g |
十二烷基硫酸钠 | 5g |
乳糖 | 48g |
PEG4000 | 20g |
硬脂酸镁 | 2g |
制备方法:
将泊沙康唑、羟丙基甲基纤维素,卡波姆934,碳酸氢钠,乳糖,十二烷基硫酸钠,PEG4000分别过80目筛;
称取处方量泊沙康唑,十二烷基硫酸钠,羟丙基甲基纤维素,卡波姆934,碳酸氢钠,乳糖,十二烷基硫酸钠,PEG4000于混合机中混合10min;
将步骤2中物料转移至流化床中,制粒,设定物料温度为60摄氏度,风机频率设置为15HZ;出风温度设置为40℃;制粒完成后,关闭加热,设定风机频率18Hz,冷却,当物料温度降至30℃时,收集物料。
将步骤3中所得物料与硬脂酸镁混合后压片,片剂硬度为3-5KN。
实施例三
处方:(制备1000片)
处方组成 | 用量 |
泊沙康唑 | 60g |
羟丙基甲基纤维素K4M | 120g |
卡波姆934 | 40g |
碳酸氢钠 | 10g |
十二烷基硫酸钠 | 5g |
乳糖 | 48g |
PEG4000 | 20g |
硬脂酸镁 | 2g |
制备方法:
将泊沙康唑、羟丙基甲基纤维素,卡波姆934,碳酸氢钠,乳糖,十二烷基硫酸钠,PEG4000分别过80目筛;
称取处方量泊沙康唑,十二烷基硫酸钠,羟丙基甲基纤维素,卡波姆934,碳酸氢钠,乳糖,十二烷基硫酸钠,PEG4000于混合机中混合10min;
将步骤2中物料转移至流化床中,制粒,设定物料温度为60摄氏度,风机频率设置为15HZ;出风温度设置为40℃;制粒完成后,关闭加热,设定风机频率18Hz,冷却,当物料温度降至30℃时,收集物料。
将步骤3中所得物料与硬脂酸镁混合后压片,片剂硬度为3-5KN。
实施例四
处方:(制备1000片)
处方组成 | 用量 |
泊沙康唑 | 160g |
羟丙基甲基纤维素K4M | 120g |
卡波姆934 | 40g |
碳酸氢钠 | 10g |
十二烷基硫酸钠 | 5g |
乳糖 | 48g |
PEG4000 | 20g |
硬脂酸镁 | 2g |
制备方法:
将泊沙康唑、羟丙基甲基纤维素,卡波姆934,碳酸氢钠,乳糖,十二烷基硫酸钠,PEG4000分别过80目筛;
称取处方量泊沙康唑,十二烷基硫酸钠,羟丙基甲基纤维素,卡波姆934,碳酸氢钠,乳糖,十二烷基硫酸钠,PEG4000于混合机中混合10min;
将步骤2中物料转移至流化床中,制粒,设定物料温度为60摄氏度,风机频率设置为15HZ;出风温度设置为40℃;制粒完成后,关闭加热,设定风机频率18Hz,冷却,当物料温度降至30℃时,收集物料。
将步骤3中所得物料与硬脂酸镁混合后压片,片剂硬度为3-5KN。
试验一体内药动学实验:
取实验家兔18只(体重范围1.5Kg-2.0Kg),随机分成3组,每组6只,分别灌服实施一例制得的泊沙康唑胃漂浮片、市售肠溶片(Noxafil)和市售混悬液(Noxafil),按65mg/Kg剂量进行给药,分别于给药15min,30min,45min,1h,2h,3h,4h,6h,8h,10h后于家兔股静脉取血1.0mL,加入甲醇超声20min,离心,取上清液20μL,HPLC检测含量,各制剂的药代动力学参数如下表示:
上表的结果表明,按照市售例一制备得到的泊沙康唑胃漂浮片,与市售制剂相比,可认为疗效一致。
本发明所揭示的泊沙康唑口服制剂具有生产工艺简单,生产设备通用,成本低,患者携带和吞服方便。与现有剂型具有一样的疗效
对于本领域技术人员而言,显然本发明不限于上述示范性实施例的细节,而且在不背离本发明精神或基本特征的情况下,能够以其他的具体形式实现本发明。因此,无论从哪一点来看,均应将实施例看做示范性的,而且是非限制性的,本发明的范围由所附权利要求而不是上述说明限定,因此旨在将落在权利要求的等同要件的含义和范围内的所有变化囊括在本发明内。
Claims (8)
1.一种泊沙康唑胃漂浮片,其特征在于,包括以下重量百分比成分:泊沙康唑20%-45%;HPMC K4M 20%-50%;卡波姆9345%-20%;碳酸氢钠;1%-10%;乳糖5%-25%;十二烷基硫酸钠1%-5%;PEG3%-10%;硬脂酸镁0.5%-5%。
2.根据权利要求1所述的泊沙康唑胃漂浮片,其特征在于,包括以下重量百分比成分:泊沙康唑29%;HPMC K4M 40.5%;卡波姆9345.8%;碳酸氢钠2.9%;乳糖13.9%;十二烷基硫酸钠1.5%;PEG 5.8%;硬脂酸镁0.6%。
3.权利要求1所述的泊沙康唑胃漂浮片的制备方法,其特征在于,制备步骤为:
S1:将泊沙康唑、羟丙基甲基纤维素,卡波姆934,碳酸氢钠,乳糖,十二烷基硫酸钠,PEG分别过80目筛;
S2:上述物料加入混合机中混合均匀;
S3:将步骤2中物料转移至流化床中,制粒;
S4:将所得颗粒与硬脂酸镁混合后压片。
4.根据权利要求3所述的泊沙康唑胃漂浮片的制备方法,其特征在于,所述S3的步骤中,流化床制粒时不加入液体物料。
5.根据权利要求3所述的泊沙康唑胃漂浮片的制备方法,其特征在于,所述S3的步骤中,流化床制粒进风温度为40-80℃。
6.根据权利要求4所述的泊沙康唑胃漂浮片的制备方法,其特征在于,所述S3的步骤中,设定物料温度为60摄氏度,风机频率设置为15HZ;出风温度设置为40℃,制粒完成。
7.根据权利要求4所述的泊沙康唑胃漂浮片的制备方法,其特征在于,所述S3的步骤中,制粒完成后,关闭加热,设定风机频率,冷却,当物料温后收集。
8.根据权利要求4所述的泊沙康唑胃漂浮片的制备方法,其特征在于,
所述S4的步骤中,压片后制得的泊沙康唑胃漂浮片的硬度为3-5KN。
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