CN1222347A - 乳剂型鼻喷剂 - Google Patents
乳剂型鼻喷剂 Download PDFInfo
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Abstract
本发明为一种含甾体激素类抗炎药物的乳浊液,使用时喷(滴)入鼻腔内治疗过敏性鼻炎的乳剂型鼻喷剂,甾体激素类抗炎药溶于与水混合成乳剂的脂溶性辅料中,制剂含有的甾体激素类药物主要指以醋酸曲安萘德为代表的一些局部应用的甾体激素类抗炎药,可使用醋酸曲安萘德、肤轻松、倍它米松,在乳剂中占组份总量的0.01—0.5%,乳剂中还含有其他一些药用辅料,包括:稳定剂、防腐剂以及增稠剂,乳剂有水包油型乳剂和油包水型乳剂型,由于甾体激素类药物溶解于油性辅料中,无固体微粒,药剂起效快、作用时间长、对鼻腔无刺激又不会从鼻腔中被清除,充分发挥药物治疗作用。
Description
本发明为一种含甾体激素类抗炎药物的乳浊液，使用时喷(滴)入鼻腔内治疗过敏性鼻炎的乳剂型鼻喷剂。
过敏性鼻炎属常见病，目前治疗该病最有效的药物就是甾体激素类抗炎药物，美国专利US4,767,612提出了一种用曲安萘德治疗过敏性鼻炎的药品，这种药将微粒化的曲安萘德悬浮于无水乙醇和氟利昂中，使用时喷射至鼻腔中治疗，其缺点是刺激鼻腔，感觉不适，有时部分病人还会过敏。世界专利WO98/00178也提供了用水为基质的曲安萘德鼻剂，也能达到一定的治疗作用，由于甾体激素类药物均难溶于水，因此制备时药剂中要加入一定的悬浮剂，将其制成水混悬液，药物也需要制成细微的固体颗粒，在使用时往往还需要振摇，以改变其物理性质，才能发挥一定的疗效。上述的两种制剂在使用时，固体颗粒药物进入鼻腔后，会加速鼻腔纤毛运动，作为异物在短时间被清除，不能起到应有的效果。
本发明目的提供用于治疗过敏性鼻炎，直接作用于鼻腔的含甾体激素类的药物，是一种药物溶液为乳剂型，不含固体颗粒，不会因为纤毛运动从鼻腔中被清除的乳剂型鼻喷剂。
本发明采用的乳剂型鼻喷剂，甾体激素类抗炎药溶于与水混合而成乳剂的脂溶性辅料中。
本发明采用的乳剂型鼻喷剂为乳剂包括水包油型乳剂和油包水型乳剂。
本发明采用的乳剂型鼻喷剂的组份为：
组份 Wt％
甾体激素 0.01～0.5
溶剂 20～40
乳化剂 1～20
增稠剂 0.1～1.5
尼泊金乙酯 0.01～1
乙二胺四乙酸二钠 0.01～0.5
水 加至％
本发明采用的溶剂为羊毛脂和液体石蜡，增稠剂为羧甲基纤维素钠或卡波姆，增稠剂为司盘40和吐温80。
本发明优点是制成水包油或油包水型乳剂后，甾体激素类药物可溶解于油性辅料中，药剂起效快、作用时间长、对鼻腔无刺激又不会从鼻腔中被清除，充分发挥了药物治疗作用。
本发明为一种含有甾体激素类抗炎药的乳浊制剂，使用时可直接喷入或滴入鼻腔治疗过敏性鼻炎。该制剂中含有的甾体激素类药物主要指以醋酸曲安萘德为代表的一些局部应用的甾体激素类抗炎药，可使用醋酸曲安萘德、肤轻松、倍它米松，在乳剂中占组份总量的0.01-0.5％。乳剂中还含有其他一些药用辅料，包括：稳定剂、防腐剂以及增稠剂。其中脂溶性药用辅料包括羊毛脂和液体石蜡，在制剂中用作甾体激素类药物的溶剂，在乳剂中占组份总量的20-40％；乳化剂为非离子表面活性剂，包括吐温类和司盘类，在乳剂中占组份总量的1-20％；稳定剂为乙二胺四乙酸二钠，在乳剂中占组份总量的0.01-0.5％；防腐剂为尼泊金乙酯，在乳剂中占组份总量的0.01-1％。此外，增稠剂为羧甲基纤维素纳或卡波姆，黏度为300-800厘泊，在乳剂中占组份总量的0.1-1.5％。加入增稠剂可以增加分散媒的粘度，并赋予该乳剂以流变学性质，的目的有二，其一，增加分散媒的比重，使乳剂不易分层；其二，当药物喷入鼻腔内时，产生流变学作用，黏度增大不易流出，作为乳剂，水溶性药用辅料是水，在制剂中作赋型剂，在乳剂中占组份总量的40-80％。
本发明乳剂(水包油)组份实例1：(Wt ％)
醋酸曲安萘德 0.07
羊毛脂 10
液体石蜡 15
司盘40 4
吐温80 6
羧甲基纤维素钠 0.2
尼泊金乙酯 0.05
乙二胺四乙酸二钠 0.1
蒸馏水 加至％
本发明乳剂组份(水包油)实例2：(Wt％)
肤轻松 0.1
羊毛脂 15
液体石蜡 15
司盘40 4
吐温80 6
卡波姆 0.5
尼泊金乙酯 0.05
乙二胺四乙酸二钠 0.1
蒸馏水 加至％
本发明乳剂组份(油包水)实例3：(Wt％)
倍它米松 0.1
羊毛脂 15
液体石蜡 15
司盘40 6
吐温80 4
羧甲基纤维素钠 0.2
尼泊金乙酯 0.05
乙二胺四乙酸二钠 0.1
蒸馏水 加至％
乳剂制备：称取处方量的羊毛脂，液体石腊，尼泊金乙酯置于烧怀中，水浴加热，待全部融化后，加入醋酸曲安萘德搅拌使溶解并加热至70-75℃；量取适量的蒸馏水，加入乙二胺四乙酸二钠使溶解，加入吐温80，搅拌中加入规定量的1％羧甲基纤维素钠溶液，混合均匀，加热至70-75℃，将水相与油相混合，不断搅拌，冷却至室温，倾入胶体磨中研匀分装。
1％羧甲基纤维素钠溶液的制备：量取蒸馏水1000ml，将10克羧甲基纤维素钠撒布于液面上，待基溶胀直至完全溶解。
使用时喷入或滴入鼻腔，可直接使用滴瓶滴入腔或使用压力泵或予压力泵射入鼻腔。
Claims (6)
1．本发明为一种治疗过敏性鼻炎的乳剂型鼻喷剂，含有甾体激素类抗炎药，其特征在于甾体激素类抗炎药溶于与水混合成乳剂的脂溶性辅料中。
2．根据权利要求1所述的乳剂型鼻喷剂，其特征在于乳剂包括水包油型乳剂和油包水型乳剂。
3．根据权利要求1所述的乳剂型鼻喷剂，其特征在于乳剂的组份为：
组份 Wt％
甾体激素 0.07～0.5
溶剂 20～40
乳化剂 1～20
增稠剂 0.1～0.5
尼泊金乙酯 0.01～0.1
乙二胺四乙酸二钠 0.01～0.5
水 加至％
4．根据权利要求3所述的乳剂型鼻喷剂，其特征在于溶剂为羊毛脂和液体石蜡。
5．根据权利要求3所述的乳剂型鼻喷剂，其特征在于增稠剂为司盘40和吐温80。
6．根据权利要求3所述的乳剂型鼻喷剂，其特征在于增稠剂力羧甲基纤维素钠或卡波姆。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 98124406 CN1222347A (zh) | 1998-10-30 | 1998-10-30 | 乳剂型鼻喷剂 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 98124406 CN1222347A (zh) | 1998-10-30 | 1998-10-30 | 乳剂型鼻喷剂 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1222347A true CN1222347A (zh) | 1999-07-14 |
Family
ID=5228624
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 98124406 Pending CN1222347A (zh) | 1998-10-30 | 1998-10-30 | 乳剂型鼻喷剂 |
Country Status (1)
| Country | Link |
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| CN (1) | CN1222347A (zh) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR3039399A1 (fr) * | 2015-07-31 | 2017-02-03 | Int Drug Licensing | Creme pour l'admnistration de steroides et son procede de preparation |
-
1998
- 1998-10-30 CN CN 98124406 patent/CN1222347A/zh active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR3039399A1 (fr) * | 2015-07-31 | 2017-02-03 | Int Drug Licensing | Creme pour l'admnistration de steroides et son procede de preparation |
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