CN102106818B - Isoliquiritigenin micro-emulsion composition - Google Patents
Isoliquiritigenin micro-emulsion composition Download PDFInfo
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Abstract
本发明公开了一种含有异甘草素的微乳剂组合物，其包括异甘草素、乳化剂、助乳化剂、油和水。该组合物可以大大提高异甘草素的溶解度。The invention discloses a microemulsion composition containing isoliquiritigenin, which comprises isoliquiritigenin, emulsifier, co-emulsifier, oil and water. The composition can greatly improve the solubility of isoliquiritigenin.
Description
技术领域 technical field
本发明涉及一种能显著增加异甘草素溶解度的异甘草素微乳剂组合物。The invention relates to an isoliquiritigenin microemulsion composition capable of significantly increasing the solubility of isoliquiritigenin.
背景技术 Background technique
异甘草素是从豆科甘草属(Glycyrrhiza)植物的根及根茎中提取的一个重要的查尔酮化合物，具有抗肿瘤、抗病毒、抗自由基、抑制脂质过氧化、抑制免疫缺陷病毒HIV等生物活性，此外还可治疗肠痉挛，糖尿病，抑郁性精神病等。其中抗肿瘤作用是近年来国内外的研究热点。异甘草素属于弱酸类药物，难溶于水，易溶于甲醇、乙醇、乙酸乙酯，在石油醚中不溶。异甘草素水溶差的性质限制了其制剂的有效开发利用。Isoliquiritigenin is an important chalcone compound extracted from the roots and rhizomes of Glycyrrhiza plants of the leguminous family. It has anti-tumor, anti-virus, anti-free radical, inhibits lipid peroxidation, and inhibits immunodeficiency virus HIV and other biological activities, in addition, it can also treat intestinal spasms, diabetes, depressive psychosis, etc. Among them, the antitumor effect is a research hotspot at home and abroad in recent years. Isoliquiritigenin is a weak acid drug, insoluble in water, easily soluble in methanol, ethanol, ethyl acetate, insoluble in petroleum ether. The poor water solubility of isoliquiritigenin limits the effective development and utilization of its formulations.
中国专利公告号为CN 101648883A公开了异甘草素衍生物的合成方法，该方法虽然通过合成异甘草素衍生物的方法增加了异甘草素的溶解度，但采用的是化学衍生化的药物化学手段，而不是采用能够增加药物溶解度的药剂学手段增加异甘草素的溶解度。Chinese patent notification number CN 101648883A discloses a synthetic method of isoliquiritigenin derivatives. Although the method increases the solubility of isoliquiritigenin by synthesizing isoliquiritigenin derivatives, it uses chemical derivatization medicinal chemistry means. Instead of using pharmaceutical means that can increase drug solubility to increase the solubility of isoliquiritigenin.
发明内容 Contents of the invention
本发明的目的在于提供一种能显著提供异甘草素溶解度的微乳剂组合物。The object of the present invention is to provide a microemulsion composition which can significantly improve the solubility of isoliquiritigenin.
本发明的目的是这样实现的：The purpose of the present invention is achieved like this:
异甘草素微乳剂组合物由异甘草素和辅料组成。The isoliquiritigenin microemulsion composition consists of isoliquiritigenin and auxiliary materials.
异甘草素微乳剂组合物的辅料由乳化剂、助乳化剂、油相和水相组成。微乳剂辅料中的乳化剂包括聚氧乙烯蓖麻油、聚氧乙烯氢化蓖麻油、卵磷脂、吐温-80的至少一种；助乳化剂包括异丙醇、丙二醇、乙醇、甘油的至少一种；油相包括油酸乙酯、油酸、辛酸癸酸甘油酯、肉豆蔻酸异丙酯、棕榈酸异丙酯的至少一种；微乳剂辅料重量份组成为乳化剂1～25份，助乳化剂2～50份，油相5～20份，水相为5-80份。The auxiliary material of the isoliquiritigenin microemulsion composition consists of emulsifier, co-emulsifier, oil phase and water phase. The emulsifier in the microemulsion auxiliary material includes at least one of polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil, lecithin, Tween-80; the co-emulsifier includes at least one of isopropanol, propylene glycol, ethanol, glycerin The oil phase includes at least one of ethyl oleate, oleic acid, caprylic capric glyceride, isopropyl myristate, and isopropyl palmitate; the microemulsion auxiliary material is composed of 1 to 25 parts by weight of an emulsifier, which helps 2-50 parts of emulsifier, 5-20 parts of oil phase and 5-80 parts of water phase.
异甘草素微乳剂中异甘草素重量份组成为0.05～1份。The weight part of isoliquiritigenin in the isoliquiritigenin microemulsion is 0.05-1 part.
本发明与现有技术相比，异甘草素微乳剂组合物是采用药剂学手段，以微乳为载体显著增加异甘草素溶解度法的方法，异甘草素在微乳中的溶解度为水中的900～1200倍，该方法没有改变异甘草素的物理化学性质，具有制备方法简单的特点，为异甘草素制剂研究奠定了基础。，Compared with the prior art, the isoliquiritigenin microemulsion composition of the present invention is a method of significantly increasing the solubility of isoliquiritigenin by using the microemulsion as a carrier by means of pharmacy. The solubility of isoliquiritigenin in the microemulsion is 900% of that in water. ~1200 times, this method does not change the physical and chemical properties of isoliquiritigenin, has the characteristics of simple preparation method, and lays the foundation for the research of isoliquiritigenin preparations. ,
具体实施方式 Detailed ways
实施例1Example 1
异甘草素：0.1份、聚氧乙烯蓖麻油：5份、乙醇：10份、肉豆寇酸异丙酯：10份、水：30份Isoliquiritigenin: 0.1 parts, polyoxyethylene castor oil: 5 parts, ethanol: 10 parts, isopropyl myristate: 10 parts, water: 30 parts
实施例2Example 2
异甘草素：0.3份、卵磷脂：9份、乙醇：9份、棕榈酸异丙酯：10份、水：20份Isoliquiritigenin: 0.3 parts, lecithin: 9 parts, ethanol: 9 parts, isopropyl palmitate: 10 parts, water: 20 parts
实施例3Example 3
异甘草素：0.4份、吐温-80：10份、丙二醇：5份、油酸乙酯：10份、水：35份Isoliquiritigenin: 0.4 parts, Tween-80: 10 parts, Propylene Glycol: 5 parts, Ethyl Oleate: 10 parts, Water: 35 parts
实施例4Example 4
异甘草素：0.5份、吐温-80：20份、异丙醇：10份、油酸：10份、水：60份Isoliquiritigenin: 0.5 parts, Tween-80: 20 parts, Isopropanol: 10 parts, Oleic acid: 10 parts, Water: 60 parts
实施例5Example 5
异甘草素：0.6份、聚氧乙烯氢化烯蓖麻油：10份、乙醇：20份、油酸乙酯：15份、水相：50份Isoliquiritigenin: 0.6 parts, polyoxyethylene hydrogenated ethylene castor oil: 10 parts, ethanol: 20 parts, ethyl oleate: 15 parts, aqueous phase: 50 parts
实施例6Example 6
异甘草素：0.2份、聚氧乙烯蓖麻油：20份、甘油：10份、肉豆寇酸异丙酯：20份、水：40份Isoliquiritigenin: 0.2 parts, polyoxyethylene castor oil: 20 parts, glycerin: 10 parts, isopropyl myristate: 20 parts, water: 40 parts
实施例7Example 7
异甘草素：0.06份、聚氧乙烯蓖麻油：20份、乙醇：20份、棕榈酸异丙酯：15份、水：45份Isoliquiritigenin: 0.06 parts, polyoxyethylene castor oil: 20 parts, ethanol: 20 parts, isopropyl palmitate: 15 parts, water: 45 parts
实施例8Example 8
异甘草素：0.2份、聚氧乙烯氢化烯蓖麻油：20份、乙醇：20份、辛酸癸酸甘油酯：10份、水相：75份Isoliquiritigenin: 0.2 parts, polyoxyethylene hydrogenated ethylene castor oil: 20 parts, ethanol: 20 parts, caprylic capric glyceride: 10 parts, water phase: 75 parts
实施例9Example 9
异甘草素：0.4份、聚氧乙烯氢化蓖麻油10份、甘油7.5份、油酸：15份，水相25份Isoliquiritigenin: 0.4 parts, polyoxyethylene hydrogenated castor oil 10 parts, glycerin 7.5 parts, oleic acid: 15 parts, water phase 25 parts
实施例10Example 10
异甘草素：0.09份、吐温-8025份、乙醇：15份、油酸：18份、水相：80份Isoliquiritigenin: 0.09 parts, Tween-8025 parts, ethanol: 15 parts, oleic acid: 18 parts, water phase: 80 parts
实施例11Example 11
异甘草素：1份、聚氧乙烯氢化蓖麻油：20份、异丙醇：30份、棕榈酸异丙酯：20份、水相：65份Isoliquiritigenin: 1 part, polyoxyethylene hydrogenated castor oil: 20 parts, isopropyl alcohol: 30 parts, isopropyl palmitate: 20 parts, water phase: 65 parts
实施例12Example 12
异甘草素：0.05份、卵磷脂20份、丙二醇：40份、油酸乙酯：10份、水相：55份Isoliquiritigenin: 0.05 parts, lecithin 20 parts, propylene glycol: 40 parts, ethyl oleate: 10 parts, water phase: 55 parts
实施例13Example 13
异甘草素：0.7份、吐温-80：20份、甘油：20份、肉豆蔻酸异丙酯：18份、水相：70份Isoliquiritigenin: 0.7 parts, Tween-80: 20 parts, glycerin: 20 parts, isopropyl myristate: 18 parts, water phase: 70 parts
实施例14Example 14
异甘草素：0.8份、聚氧乙烯氢化蓖麻油：20份、丙二醇：40份、油酸：10份、水相：45份Isoliquiritigenin: 0.8 parts, polyoxyethylene hydrogenated castor oil: 20 parts, propylene glycol: 40 parts, oleic acid: 10 parts, water phase: 45 parts
实施例15Example 15
异甘草素：0.9份、聚氧乙烯蓖麻油：20份、异丙醇：20份、油酸乙酯：10份、水相：55份Isoliquiritigenin: 0.9 parts, polyoxyethylene castor oil: 20 parts, isopropanol: 20 parts, ethyl oleate: 10 parts, water phase: 55 parts
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| CN102335131B (en) * | 2011-10-10 | 2013-04-17 | 山西仁源堂药业有限公司 | Osthole micro emulsion, osthole micro emulsion sustained-release patch and preparation method thereof |
| CN102860982B (en) * | 2012-10-09 | 2014-08-20 | 石河子大学医学院第一附属医院 | Tilianin microemulsion composition |
| CN103461360B (en) * | 2013-09-26 | 2015-10-28 | 卞佳林 | The preparation method of a kind of Avermectin and griseofulvin composite pesticidal nanoemulsion |
| CN103478144B (en) * | 2013-09-26 | 2015-09-09 | 卞佳林 | A kind of Avermectin and griseofulvin composite pesticidal nanoemulsion |
| CN103976892B (en) * | 2014-05-16 | 2016-08-31 | 吴江市英力达塑料包装有限公司 | A kind of glabridin microemulsion and preparation method thereof |
| CN105669543A (en) * | 2015-12-31 | 2016-06-15 | 中国药科大学 | Isoliquiritigenin nicotinamide eutectic crystal and preparation method thereof |
| CN105622497A (en) * | 2015-12-31 | 2016-06-01 | 中国药科大学 | Isoliquiritigenin pyrazinamide eutectic crystal and preparation method thereof |
| CN111135142A (en) * | 2020-01-16 | 2020-05-12 | 兰州大学 | A kind of isoliquiritigenin nanoemulsion and preparation method thereof |
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| Title |
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| 鲁莹等.新型药物载体：微乳.《国外医药-合成药 生化药 制剂分册》.1999,第20卷(第4期),第253-256,Ⅰ,Ⅱ页. * |
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