CN101332177A - 包含布洛芬、氨甲环酸及硅酸钙的固形制剂 - Google Patents
包含布洛芬、氨甲环酸及硅酸钙的固形制剂 Download PDFInfo
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- CN101332177A CN101332177A CNA2008101265216A CN200810126521A CN101332177A CN 101332177 A CN101332177 A CN 101332177A CN A2008101265216 A CNA2008101265216 A CN A2008101265216A CN 200810126521 A CN200810126521 A CN 200810126521A CN 101332177 A CN101332177 A CN 101332177A
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- ibuprofen
- tranexamic acid
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
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- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
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- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Inorganic Chemistry (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
本发明提供一种在高温保存条件下膨胀得到抑制的、包含布洛芬和氨甲环酸的固形制剂。一种包含布洛芬和氨甲环酸的固形制剂，其特征在于所述固形制剂包含硅酸钙。
Description
技术领域
[0001]本发明涉及在高温保存条件下膨胀得到抑制的、包含布洛芬和氨甲环酸(tranexamic acid)的固形制剂。
背景技术
[0002]布洛芬作为非类固醇类抗炎症药(NSAID)是被广泛使用的药物，对慢性关节风湿病、关节痛及关节炎、神经痛及神经炎、腰脊痛等疾病、症状的消炎和镇痛有效，此外对感冒综合症、急性支气管炎、慢性支气管炎的急性恶化期的消炎和解热等也有效。但是，因为布洛芬有胃肠障碍等副作用，并且镇痛效果较小，所以研究了与各种药物的配合制剂。
[0003]例如已经报道了布洛芬与布西丁等苯胺衍生物类解热镇痛剂配合的解热镇痛剂(参照专利文献1)、布洛芬与咖啡因配合的制剂(参照专利文献2)、布洛芬与可待因配合的镇痛组合物(参照专利文献3和4)、布洛芬与对乙酰氨基酚配合的解热镇痛剂(参照专利文献5和6)、布洛芬与对乙酰氨基酚和烯丙基异丙基乙酰脲或溴代戊酰脲配合的解热镇痛剂(参照专利文献7)、布洛芬与氯化溶菌酶配合的感冒药(参照专利文献8)、包含布洛芬和氨甲环酸的解热镇痛剂(参照专利文献9)等。特别是氨甲环酸作为具有抗胞浆素作用、抗过敏作用、抗炎症作用等的药物得到广泛使用，开发了许多将布洛芬与氨甲环酸组合的配合制剂。例如已经报道了在布洛芬与氨甲环酸中进一步配合咖啡因的解热镇痛剂(参照专利文献10)、配合抗坏血酸的解热镇痛组合物(参照专利文献11)、组合对乙酰氨基酚等非吡唑啉酮类解热镇痛药的医药制剂(参照专利文献12)、配合假麻黄碱及/或脱羟肾上腺素的鼻炎用医药组合物(参照专利文献13)、进一步配合去甲麻黄碱或假麻黄碱等α-受体刺激剂以及类黄酮构成的感冒用医药组合物(参照专利文献14)、配合氯马斯汀及/或溴己胺的医药组合物(参照专利文献15)等。
[专利文献1]特公昭64-8602号公报
[专利文献2]特公平1-24131号公报
[专利文献3]特开平3-7218号公报
[专利文献4]特开平5-194227号公报
[专利文献5]特开平5-148139号公报
[专利文献6]特开平11-158066号公报
[专利文献7]特开平5-246845号公报
[专利文献8]特开平7-188004号公报
[专利文献9]特开平9-48728号公报
[专利文献10]特许第3667381号公报
[专利文献11]特开2006-1920号公报
[专利文献12]特开2005-187328号公报
[专利文献13]特开2005-232128号公报
[专利文献14]特开2005-194269号公报
[专利文献15]特开2006-124380号公报
发明内容
[0004]本发明人等致力于对包含布洛芬和氨甲环酸的固形制剂进行研究开发。当对包含布洛芬和氨甲环酸的固形制剂的保存性和稳定性进行研究时，发现如果在1～25℃下保存，这些固形制剂可以持续长期地稳定保存，但在高温保存条件下会发生膨胀，在制剂上发生裂纹等。
[0005]于是，为了解决包含布洛芬和氨甲环酸的固形制剂在高温保存条件下膨胀的问题，本发明人等探讨了该原因(膨胀机理)。包含布洛芬和氨甲环酸的固形制剂在高温保存条件下的膨胀不是由于成分分解等造成，也不是由于吸湿造成，根据以往的知识假定的任何膨胀机理都不能理解该膨胀，充分阐明该原因(膨胀机理)非常困难。
[0006]本发明人等已经发现，作为膨胀现象的再现条件，高温保存条件下的膨胀仅仅在同时配合布洛芬和氨甲环酸时发生，把布洛芬和氨甲环酸分别作为单一成分时不发生膨胀。因此，例如可以初步考虑把两种成分作成分开的多层片或包芯片以减少布洛芬与氨甲环酸接触的解决方法。但是，多层片或包芯片的制造繁杂，通过该制造不仅使成本增加、生产效率降低，还遗留有在各层的界面膨胀的问题，所以不能说是好的解决方法。
[0007]另一方面，作为与机理阐明相分离的直接的解决方法，本发明人等尝试了用糖衣或涂膜等进行包衣以抑制制剂的膨胀。但是，固形制剂膨胀的程度大，仅用糖衣或涂膜来防止是困难的。
[0008]此外，像以往进行的那样，可以通过把包含布洛芬和氨甲环酸的固形制剂始终保持在1～25℃以抑制膨胀，但在流通上、保管上以及进一步使用上带来大的不便。
[0009]因此，本发明把提供一种在高温保存条件下膨胀得到抑制的、包含布洛芬和氨甲环酸的固形制剂作为课题。
[0010]本发明人等发现对于制造包含布洛芬和氨甲环酸的固形制剂，通过添加使用硅酸钙，可以得到在高温条件下不产生急剧膨胀问题的稳定的固形制剂，完成了本发明。
[0011]即，本发明涉及一种包含布洛芬和氨甲环酸的固形制剂，所述固形制剂包含硅酸钙。
[0012]因此，本发明涉及下面的[1]～[3]。
[1]一种包含布洛芬和氨甲环酸的固形制剂，其特征在于所述固形制剂包含硅酸钙。
[2]一种包含布洛芬和氨甲环酸的固形制剂，其特征在于所述固形制剂包含作为膨胀抑制成分的硅酸钙。
[3]一种包含硅酸钙的、用于包含布洛芬和氨甲环酸的固形制剂的膨胀抑制剂。
[0013]此外，本发明也涉及下面的[4]～[9]。
[4]一种包含布洛芬和氨甲环酸的固形制剂的制造方法，其特征在于所述制造方法包含添加硅酸钙的步骤。
[5]一种包含布洛芬和氨甲环酸的固形制剂的制造方法，其特征在于所述制造方法包含添加作为膨胀抑制成分的硅酸钙的步骤。
[6]一种硅酸钙的应用，其用于制造包含布洛芬和氨甲环酸的固形制剂。
[7]一种硅酸钙的应用，其用于制造膨胀得到抑制的、包含布洛芬和氨甲环酸的固形制剂。
[8]一种硅酸钙的应用，其用于抑制包含布洛芬和氨甲环酸的固形制剂的膨胀。
[9]一种抑制固形制剂膨胀的方法，所述方法通过添加硅酸钙抑制包含布洛芬和氨甲环酸的固形制剂的膨胀。
[0014]根据本发明，即使在高温保存条件下，也可以得到使包含布洛芬和氨甲环酸的固形制剂的膨胀得到抑制的稳定的固形制剂。
[0015]使用本发明的包含布洛芬和氨甲环酸的固形制剂，即使在运送及保管时经受高温保存条件，也不会发生急剧的膨胀，不会在制剂上产生裂纹等。因此，即使在各种各样的流通和保管条件下都可以维持固形制剂的作为产品的价值，并且也成为方便使用的固形制剂。
具体实施方式
[0016]本发明涉及一种包含布洛芬和氨甲环酸的固形制剂，所述固形制剂包含硅酸钙。
[0017]包含在本发明的固形制剂中的布洛芬，不仅可以使用布洛芬，也可以使用药学上可接受的布洛芬的盐，其可以使用市售的产品。包含在本发明固形制剂中的布洛芬的比例，相对于固形制剂整体而言，布洛芬优选为1～70质量％，更优选为5～60质量％，特别优选为7～50质量％。
[0018]包含在本发明的固形制剂中的氨甲环酸，不仅可以使用氨甲环酸，也可以使用药学上可接受的氨甲环酸的盐，其可以使用市售的产品。包含在本发明固形制剂中的氨甲环酸的比例，相对于固形制剂整体而言，氨甲环酸优选为1～70质量％，更优选为5～60质量％，特别优选为7～50质量％。
[0019]本发明硅酸钙的比例，相对于固形制剂整体，优选为0.01～50质量％，更优选为0.1～30质量％，特别优选为1～15质量％。
[0020]本发明的固形制剂可以包含布洛芬和氨甲环酸以外的一种或两种以上的药物，例如可选自解热镇痛剂、抗组胺剂、镇咳剂、那可丁类、支气管扩张剂、去痰剂、催眠镇静剂、维生素类、抗炎症剂、胃粘膜保护剂、生药类、中医处方、咖啡因类等。
[0021]作为解热镇痛剂可以举出例如乙酰水杨酸、乙酰水杨酸铝、对乙酰氨基酚、乙水杨胺、水杨酰水杨酸、水杨酰胺、乳酰氨基苯乙醚、水杨酸钠等。
[0022]作为抗组胺剂可以举出例如盐酸氮
斯汀、盐酸异西喷地、富马酸氯马斯汀、富马酸酮替芬、盐酸二苯拉林、盐酸苯海拉明、盐酸二苯特罗、盐酸曲普利啶、盐酸曲吡那敏、盐酸松齐拉敏、盐酸芬乙嗪、盐酸甲地嗪、水杨酸苯海拉明、二苯基双磺酸卡比沙明(carbinoxaminediphenyldisulfonic acid)、酒石酸阿利马嗪、丹宁酸苯海拉明、茶氯酸二苯拉林、美海屈林萘二磺酸盐、亚甲基双水杨酸异丙嗪(promethazinemethylenedisalicylate)、马来酸卡比沙明、dl-马来酸氯苯那敏、d-马来酸氯苯那敏、美喹他嗪、磷酸二苯特罗。
[0023]作为镇咳剂可以举出例如盐酸阿洛拉胺、盐酸氯哌斯汀、枸橼酸喷托维林、柠檬酸替培啶、地布酸钠、氢溴酸右美沙芬、右美沙芬·酚酞啉盐(dextromethorphan phenolphthalin salt)、海苯酸替培啶、芬地柞酸氯哌斯汀、磷酸可待因、磷酸双氢可待因。
[0024]作为那可丁类可以举出例如盐酸那可丁、那可丁等。
[0025]作为支气管扩张剂可以举出例如dl-盐酸甲基麻黄碱、dl-甲基麻黄碱糖精盐(methylephedrine saccharin salt)等。
[0026]作为去痰剂可以举出例如愈创木酚磺酸钾、愈创甘油醚、盐酸溴己胺、盐酸氨溴索、羧甲司坦等。
[0027]作为催眠镇静剂可以举出溴代戊酰脲、烯丙基异丙基乙酰脲等。
[0028]作为维生素类可以举出维生素B1、维生素B2、维生素C、橙皮苷和其衍生物，以及它们的盐类等。
[0029]作为抗炎症剂可以举出氯化溶菌酶、舍雷肽酶、甘草酸及其类似物等。
[0030]作为胃粘膜保护剂可以举出氨基乙酸、硅酸镁、合成硅酸铝、合成水滑石、氧化镁、二羟基甘氨酸铝(甘羟铝)、氢氧化铝凝胶、氢氧化铝\碳酸镁混合干燥凝胶、氢氧化铝/碳酸氢钠共沉淀物、氢氧化铝/碳酸钙/碳酸镁共沉淀物、氢氧化镁/硫酸铝钾共沉淀物、碳酸镁、硅酸铝镁等。
[0031]作为生药类可以举出大蒜、麻黄、南天竹果实(南天実)、樱皮、远志、甘草、桔梗、车前子、车前草、石蒜、茅香、贝母、茴香、黄柏、黄连、莪术、洋甘菊、桂皮、龙胆、牛黄、兽胆(包括熊胆)、沙参、生姜、苍术、丁香、陈皮、白术、地龙、竹节参、人参等生药以其提取物(萃取物、酊剂、干燥萃取物等)等。
[0032]作为中医处方可以举出葛根汤、桂枝汤、香苏散、柴胡桂枝汤、小柴胡汤、小青龙汤、麦门冬汤、半夏厚朴汤、麻黄汤等。
[0033]作为咖啡因类可以举出，例如无水咖啡因、咖啡因、苯甲酸钠咖啡因等。
[0034]本发明的固形制剂还可以包含作为添加物的赋形剂、粘合剂、崩解剂、润滑剂等。
[0035]作为赋形剂可以举出乳糖、淀粉类、结晶纤维素、蔗糖、糖醇、轻质无水硅酸等。作为粘合剂可以举出羟丙基甲基纤维素、羟丙基纤维素、明胶、α化淀粉、聚乙烯吡咯烷酮、聚乙烯醇、支链淀粉等。作为崩解剂可以举出羧甲基纤维素、羧甲基纤维素钙、低取代羟丙基纤维素、交聚维酮、交联羧甲基纤维素钠等。作为润滑剂可以举出甘油脂肪酸酯、蔗糖脂肪酸酯、硬化油、硬脂酸、硬脂酸镁、硬脂酸钙、滑石等。
[0036]作为本发明的固形制剂的剂型可以举出例如胶囊剂、丸剂、颗粒剂、片剂、散剂等，优选片剂。固形制剂也可以用糖衣或涂膜等进行包衣。
[0037]按照通常的方法，使本发明的固形制剂包含布洛芬、氨甲环酸和硅酸钙，并使本发明的固形制剂包含所需的添加物，可以制造本发明的固形制剂。即，例如剂型是片剂时，使其包含布洛芬、氨甲环酸、硅酸钙、通常使用的各种添加物以及所需的各种药物，按照日本药典制剂总则等通常的方法混合或造粒，把所需的润滑剂混合到所得混合物或造粒物中后进行压片，可以制造本发明的固形制剂。用于压片的造粒物，可以把布洛芬和氨甲环酸分开造粒，例如使其包含布洛芬、氨甲环酸、通常使用的各种添加物以及所需的各种药物，按照日本药典制剂总则等通常的方法，把布洛芬和氨甲环酸分开造粒，把这些造粒物与所需的润滑剂混合后进行压片，可以制造本发明的固形制剂。当布洛芬和氨甲环酸分开造粒时，硅酸钙可以包含在任一造粒物中，也可以在压片时混合。具体而言，例如固形制剂是片剂时，通过使用布洛芬、氨甲环酸、硅酸钙及各种药物和通常用于片剂制造的各种添加物进行湿式造粒，把得到的颗粒与润滑剂混合后进行压片，可以制造本发明的固形制剂。此外，通过使用布洛芬、氨甲环酸、硅酸钙及各种药物和通常用于片剂制造的各种添加物，按照日本药典制剂总则等通常的方法进行颗粒化，把该颗粒与润滑剂混合后进行压片，也可以制造本发明的固形制剂。
[0038]实施例
以下使用实施例进一步具体说明本发明，但本发明不限于这些实施例。
实施例1
[0039]把布洛芬900g(米沢浜理制造：商品名日本药典布洛芬)、氨甲环酸1499.4g(第一三共プロフア一マ制造：商品名日本药典氨甲环酸)、硅酸钙549g(エ一ザイフ一ドケミカル制造：商品名フロ一ライトRE)、羟丙基纤维素106.2g、结晶纤维素1348.2g、交联羧甲基纤维素钠360g投进高速搅拌造粒机(深江工業制造：FS-10型)混合后，添加纯净水466g后揉制。把该造粒物投进流化床式干燥机(フロイント產業制造：FLO-5型)干燥后，用整粒机(岡田精工制造：ND-10型)进行整粒。把该整粒物4762.8g和硬脂酸镁97.2g投进混合机(コトブキ制造：PM50型)混合后，用安装有直径8.5mm冲头的压片机(
鉄工所制造：HT-AP18SS型)压片，得到片重为270mg的片剂18000片。
[0040]比较例1
不配合实施例1的硅酸钙，而是用追加549g的结晶纤维素来代替进行配合，其它与实施例1相同，得到片剂。
[0041]实施例1
膨胀的评价
把实施例1和比较例1制造的片剂各一片放入玻璃瓶(2K规格)，盖上密封塞后，在40℃的恒温容器中保存1～6个月，或在50℃的恒温容器中保存1周～1个月。根据数显千分尺(digital micrometer)测定刚制造的片剂厚度以及保存后的片剂厚度，计算出用下式(1)定义的膨胀率(％)。
[0042]膨胀率(％)＝(D-D0)/D0×100 (1)
式中，D是保存后的片剂厚度，D0是刚制造的片剂厚度。
[0043]实施例1和比较例1得到的每片片剂的配方以及试验结果表示在下表1中。
[0044]表1 (配合量mg)
| 实施例1 | 比较例1 | |
| 布洛芬氨甲环酸羟丙基纤维素交联羧甲基纤维素钠硬脂酸镁结晶纤维素硅酸钙合计 | 50.083.35.920.05.474.930.5270 | 50.083.35.920.05.4105.4-270 |
| 50℃保存1周后的膨胀率(％) | 3.9 | 11.6 |
| 50℃保存2周后的膨胀率(％) | 5.7 | 13.6 |
| 50℃保存1个月后的膨胀率(％) | 8.1 | 14.6 |
| 40℃保存1个月后的膨胀率(％) | 1.9 | 7.5 |
| 40℃保存2个月后的膨胀率(％) | 3.2 | 9.7 |
| 40℃保存3个月后的膨胀率(％) | 4.3 | 10.7 |
| 40℃保存4个月后的膨胀率(％) | 5.3 | 11.5 |
| 40℃保存6个月后的膨胀率(％) | 6.1 | 12.5 |
膨胀率＝(随时间推移后的值-初始值)÷初始值×100(％)
[0045]根据表1可清楚地看出，在不包含硅酸钙的制剂(比较例1)中，40℃保存1个月后的膨胀率(％)是7.5％，50℃保存1周后的膨胀率(％)是11.6％，证实了在高温保存条件下急剧的、高的膨胀率。另一方面，在包含布洛芬和氨甲环酸、且包含硅酸钙的本发明的固型制剂(实施例1)中，膨胀率显著地降低到40℃保存1个月后的膨胀率(％)是1.9％，50℃保存1周后的膨胀率(％)是3.9％。
此外，在不包含硅酸钙的制剂(比较例1)中，40℃保存6个月后的膨胀率(％)是12.5％，50℃保存1个月后的膨胀率(％)是14.6％，证实了在高温保存条件下高的膨胀率。另一方面，在包含布洛芬和氨甲环酸、且包含硅酸钙的本发明的固形制剂(实施例1)中，膨胀率显著地降低到40℃保存6个月后的膨胀率(％)是6.1％，50℃保存1个月后的膨胀率(％)是8.1％。经过40℃和50℃的整个期间，与不包含本发明涉及的硅酸钙的比较例1的固形制剂的膨胀率相比，本发明的固形制剂的膨胀率显著降低。
[0046]此外，因为比较例1的膨胀率高，所以发脆，容易发生片剂的破裂和缺损，而本发明的固形制剂(实施例1)即使在上述那样严酷的高温条件下保存后也没有发生片剂的破裂和缺损，是稳定的片剂。
[0047]本发明提供一种包含布洛芬和氨甲环酸的、即使在高温条件下保存也不发生急剧膨胀的稳定的固形制剂。已知包含布洛芬和氨甲环酸的制剂，不仅可以得到这些成分具有的药效，也可以得到增强药效、降低副作用的附加效果，本发明可以稳定地提供这样有用的医药制剂。使用本发明得到的固形制剂，可以在长期保存和高温条件下使用，在制药工业上极其有用。
Claims (2)
1.一种包含布洛芬和氨甲环酸的固形制剂，其特征在于所述固形制剂包含硅酸钙。
2.一种抑制固形制剂膨胀的方法，其特征在于所述方法通过添加硅酸钙抑制包含布洛芬和氨甲环酸的固形制剂的膨胀。
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| CN112206218A (zh) * | 2020-10-24 | 2021-01-12 | 迪沙药业集团有限公司 | 一种甲硝唑维生素b6组合物 |
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| CN112206218A (zh) * | 2020-10-24 | 2021-01-12 | 迪沙药业集团有限公司 | 一种甲硝唑维生素b6组合物 |
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