CN1528326A - 主治痤疮的复方外用药物 - Google Patents
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Abstract
本发明涉及一种主治痤疮的复方外用药物。其特征在于：复方外用药物的基质载体中含有下列有效活性成分(重量百分比)：阿达帕林0.01～2％，抗菌药0.25～5％。本发明的优点在于：本发明是以复方制剂形式包含维A酸类及抗菌类两类治疗痤疮的主成分，以同时发挥3种(及以上)的疗效作用(溶解角栓、调节角化、抗微生物、抗炎症、减轻皮脂分泌的继发因素等)在药理学上发挥了互补及协同作用，使治疗作用更全面、深入，疗效更满意。
Description
技术领域：
本发明涉及一种治疗痤疮的外用药物，尤其是一种主治痤疮的复方外用药物。
背景技术：
痤疮是皮脂腺慢性疾病，可分为炎性及非炎性痤疮两类，是皮肤科第二大常见病，发病率约占皮肤病7～10％，患病年龄覆盖11～30岁间，男女皆可罹患。
现已知下述四种发病因素及环节在痤疮发生、发展及转归中起关键作用：1、毛囊及皮脂腺单位中的微生物作用，首先是厌氧的丙酸痤疮杆菌，次为需氧的表皮及金黄色葡萄球菌等优势化脓菌，有认为酵母菌属亦参与发病；2、雄激素及皮脂腺功能亢进，前者包括雄激素一受体亲和力增高和/或5a-还原酶活性增强，使高活性的2H-睾酮增多；后者主要指雄激素依赖性的皮脂腺增生和皮脂分泌增多；3、毛囊皮脂腺导管角化异常，最终导致毛囊口粉刺形成及角质栓塞，并诱发及加剧炎症；4、炎症的启动及毛囊-皮脂腺的炎症的毁坏。
药物是治疗座疮的主要手段，抗痤疮的药物是国内外皮肤科药物研究的热点，其作用原理主要围绕和针对上述发病环节。药物抗痤疮分系统及局部两种途径，局部治疗主要针对轻度痤疮及参与中度痤疮的治疗，重度痤疮在综合疗法的前提下也需要局部治疗加以配合。对于炎性痤疮主要治则是抗菌、消炎；对于非炎性痤疮主要治则是溶解粉刺。
现有治疗痤疮的药物多为单方，作用比较单一。例如主要针对炎性痤疮的药物多为抗生素，包括红霉素、克林霉素(包括磷酸盐及盐酸盐)、氯霉素，主要起抗菌作用，兼有抗炎作用；而主要针对非炎性痤疮的药物有维A酸类，过氧化苯甲酰、水杨酸、乳酸等，其中过氧化苯甲酰同时有很强的抗菌作用。
单方治疗存在的主要问题是作用单一，最多只能针对1～2个发病环节(如抗菌加抗炎，或抗菌加抗角栓)。此外，上述粉刺溶角药物多有局部刺激和/或过敏作用，过氧化苯甲酰有强氧化作用，如组成复方制剂，质量不易稳定，使配伍药物浓度，疗效波动，保存条件、保质期和使用方便性等方面都受到较大影响。
发明内容：
本发明的目的在于：针对治疗痤疮的单方制剂使用中存在的问题，提供一种新的主治痤疮的复方外用药物。
本发明的目的是这样实现的：一种主治痤疮的复方外用药物，其特征在于：复方外用药物的基质载体中含有下列有效活性成分(重量百分比)：阿达帕林0.01～2％，抗菌药0.25～5％。
阿达帕林是第三代维A酸类药物，维A酸类药物局部治疗痤疮的化合物，主要包括第一代的全反式维A和十三顺以及酸维A酸第三代的阿达帕林和他扎罗汀。阿达帕林的相对优点是维A酸类药物中较新的化合物，即具有维A酸类的药物的生物活性，又具有其独特的化学稳定性，光稳定性及高选择性。在治疗作用上，阿达帕林具有与维A酸结合蛋白和维A酸受体RARβ和γ作用的选择性，因而在获得相同疗效的同时，不良反应较第一代维A酸显著减轻。此外，阿达帕林的毛囊穿透性和亲脂性也有利其发挥局部治疗作用。
维A酸类药物局部治疗痤疮的原理在于改善上皮细胞分化，减轻角栓形成和促进角质栓(黑头粉刺)溶解，使毛囊-皮脂腺炎症得以引流，不利于厌氧菌生长，使抗菌药物易于透入毛囊皮脂腺内以增强抑、杀菌作用。
本复方中选用的抗菌药物的共同特点是：这些药物对痤疮发病相关的主要病原菌如厌氧丙酸痤疮杆菌及需氧皮肤化脓菌(金黄色葡萄球菌，表皮葡萄球菌，链球菌等)都有抑制作用，从而减轻和消除发病的感染环节。
此外，本研究组已发现所选用的抗菌药物在抗菌的同时，还具有抑制白细胞趋化活性，这对抑制炎症介质的释放，减轻组织破坏，减少刺激皮脂分泌诱因，阻断痤疮炎症环节的启动及发展，缓解痤疮临床炎症症状起到重要作用。
由此可见，本发明的优点在于：本发明是以第三代维A酸类产品阿达帕林的复方制剂形式，它包含维A酸类及抗菌类两类治疗痤疮的主成分，以同时发挥3种(及以上)的疗效作用(溶解角栓、调节角化、抗微生物、抗炎症、减轻皮脂分泌的继发因素等)在药理学上发挥了互补及协同作用，使治疗作用更全面、深入，疗效更满意。
具体实施方式：
下面非限制性的例举了本发明涉及的部分实施例。
实施例1：
本实施例的有效活性成分采用阿达帕林0.1％(重量百分比，下同)和盐酸(或磷酸)克林霉素1％，基质载体采用十六醇、凡士林、液体石蜡、单硬脂酸甘油酯、甘油、增溶剂、乳化剂、羟苯乙酯和蒸馏水。
实施例2：
本实施例的有效活性成分采阿达帕林0.05％和红霉素2％，基质载体采用十六醇、凡士林、液体石蜡、单硬脂酸甘油酯、甘油、增溶剂、乳化剂、羟苯乙酯和蒸馏水。
实施例3：
先将实施例1或实施例2中的两种有效活性成分及总量0.1％的羟苯乙酯溶于增溶剂中；再将总量8～12％的十六醇、总量5～10％的凡士林、总量8～12％的液体石蜡、总量5～10％的单硬脂酸甘油酯及适量的乳化剂混合加热至80～85℃；将总量0.5～5％的甘油与适量的蒸馏水混合加热至80～85℃，并将其与上述十六醇、凡士林、液体石蜡、单硬脂酸甘油酯及乳化剂的混合物混合乳化；将乳化后的混合物离开热源，搅拌冷却至65℃时，加入溶有两种有效活性成分和羟苯乙酯的增溶剂，搅拌均匀形成乳膏。
实施例4：
本实施例的有效活性成分采用阿达帕林0.1％和氯霉素1％，基质载体采用卡波姆、乙醇、丙二醇、EDTA-2Na、羟苯乙酯、中和剂和蒸馏水。
实施例5：
本实施例的有效活性成分采用阿达帕林0.05％和四环素2％，基质载体采用卡波姆、乙醇、丙二醇、EDTA-2Na、羟苯乙酯、中和剂和蒸馏水。
实施例6：
先将实施例4或实施例5中的两种有效活性成分溶于总量5～20％的乙醇中，总量0.1％的羟苯乙酯溶于总量5～20％的丙二醇中；用适量的蒸馏水加总量0.05～2％的EDTA-2Na溶解，加入总量0.1～2％的卡波姆溶胀成胶；将上述的溶液加入溶胶中搅拌均匀，用适量的中和剂将PH值调至5～7，搅拌均匀形成凝胶。
实施例7：
本实施例的有效活性成分采用阿达帕林0.15％和甲硝唑0.75％，基质载体采用甘油、助溶剂、氮酮、抗氧剂和乙醇。
实施例8：
本实施例的有效活性成分采用阿达帕林0.1％和替硝唑1％，基质载体采用甘油、助溶剂、氮酮、抗氧剂和乙醇。
实施例9：
本实施例的有效活性成分采用阿达帕林0.1％和塞克硝唑5％，基质载体采用甘油、助溶剂、氮酮、抗氧剂和乙醇。
实施例10：
先将实施例7或实施例8或实施例9中的两种有效活性成分溶于适量的助溶剂中，并将总量10～15％的甘油、适量的氮酮、抗氧剂溶于适量的乙醇中，待所有成分溶解后，再加入适量的乙醇直至药物制剂的总重量，搅拌均匀形成搽剂。
实施例11：
本实施例的有效活性成分采用阿达帕林0.1％和氧氟沙星0.5％，基质载体采用增溶剂、甘油、成膜剂和蒸馏水。
实施例12：
本实施例的有效活性成分采用阿达帕林0.1％和环丙沙星0.5％，基质载体采用增溶剂、甘油、成膜剂和蒸馏水。
实施例13：
先将实施例11或实施例12中的两种有效活性成分溶于增溶剂中；用适量的蒸馏水将成膜剂溶胀成胶状后加入总量5～30％的甘油混匀，将溶有两种有效活性成分增溶剂加入溶胀的胶状物中，再加入适量的蒸馏水直至药物制剂的总重量，搅拌均匀形成涂膜剂。
Claims (3)
1、一种主治痤疮的复方外用药物，其特征在于：复方外用药物的基质载体中含有下列有效活性成分(重量百分比)：阿达帕林0.01～2％，抗菌药0.25～5％。
2、根据权利要求1所述的主治痤疮的复方外用药物，其特征在于：所述的基质载体中含有的有效活性成分中的抗菌药及其含量为盐酸克林霉素0.5～2％，或磷酸克林霉素0.5～2％，或红霉素0.5～5％，或氯霉素0.25～2％，或四环素0.25～2.5％，或甲硝唑0.5～5％，或替硝唑0.5～5％，或塞克硝唑0.5～5％，或氧氟沙星0.2～2％，或环丙沙星0.2～2％。
3、根据权利要求1所述的主治痤疮的复方外用药物，其特征在于：所述的复方外用药物含有的有效活性成分与基质载体混合后，形成乳膏或凝胶或搽剂或涂膜剂。
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Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100446773C (zh) * | 2006-04-29 | 2008-12-31 | 王菊荣 | 复方痤疮微乳膏及制备方法 |
| CN101884642A (zh) * | 2010-07-30 | 2010-11-17 | 哈尔滨乐泰药业有限公司 | 一种治疗痤疮的复方乳膏及其制备方法 |
| WO2019082090A1 (en) * | 2017-10-24 | 2019-05-02 | Glenmark Pharmaceuticals Limited | TOPICAL PHARMACEUTICAL COMPOSITION OF ADAPALENE AND MINOCYCLIN |
| US11033491B2 (en) | 2002-10-25 | 2021-06-15 | Vyne Therapeutics Inc. | Dicarboxylic acid foamable vehicle and pharmaceutical compositions thereof |
| US11219631B2 (en) | 2009-07-29 | 2022-01-11 | Vyne Pharmaceuticals Inc. | Foamable compositions, breakable foams and their uses |
| US11324691B2 (en) | 2016-09-08 | 2022-05-10 | Journey Medical Corporation | Compositions and methods for treating rosacea and acne |
| US11421207B2 (en) | 2017-11-28 | 2022-08-23 | C-Lecta Gmbh | Method for producing trehalose employing a trehalose phosphorylase variant |
| US11433025B2 (en) | 2007-12-07 | 2022-09-06 | Vyne Therapeutics Inc. | Oil foamable carriers and formulations |
| US12138311B2 (en) | 2009-10-02 | 2024-11-12 | Journey Medical Corporation | Topical tetracycline compositions |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11033491B2 (en) | 2002-10-25 | 2021-06-15 | Vyne Therapeutics Inc. | Dicarboxylic acid foamable vehicle and pharmaceutical compositions thereof |
| CN100446773C (zh) * | 2006-04-29 | 2008-12-31 | 王菊荣 | 复方痤疮微乳膏及制备方法 |
| US11433025B2 (en) | 2007-12-07 | 2022-09-06 | Vyne Therapeutics Inc. | Oil foamable carriers and formulations |
| US11219631B2 (en) | 2009-07-29 | 2022-01-11 | Vyne Pharmaceuticals Inc. | Foamable compositions, breakable foams and their uses |
| US12138311B2 (en) | 2009-10-02 | 2024-11-12 | Journey Medical Corporation | Topical tetracycline compositions |
| CN101884642A (zh) * | 2010-07-30 | 2010-11-17 | 哈尔滨乐泰药业有限公司 | 一种治疗痤疮的复方乳膏及其制备方法 |
| US11324691B2 (en) | 2016-09-08 | 2022-05-10 | Journey Medical Corporation | Compositions and methods for treating rosacea and acne |
| WO2019082090A1 (en) * | 2017-10-24 | 2019-05-02 | Glenmark Pharmaceuticals Limited | TOPICAL PHARMACEUTICAL COMPOSITION OF ADAPALENE AND MINOCYCLIN |
| CN111343969A (zh) * | 2017-10-24 | 2020-06-26 | 格兰马克药品有限公司 | 阿达帕林和米诺环素的局部药物组合物 |
| US11421207B2 (en) | 2017-11-28 | 2022-08-23 | C-Lecta Gmbh | Method for producing trehalose employing a trehalose phosphorylase variant |
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