CN111150729B - 一种成膜组合物及其应用 - Google Patents
一种成膜组合物及其应用 Download PDFInfo
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- CN111150729B CN111150729B CN202010047883.7A CN202010047883A CN111150729B CN 111150729 B CN111150729 B CN 111150729B CN 202010047883 A CN202010047883 A CN 202010047883A CN 111150729 B CN111150729 B CN 111150729B
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Abstract
本发明涉及一种成膜组合物及其应用,具体地,所述成膜组合物包含大麻二酚和褪黑素以及乳化剂、成膜剂、增重剂、消泡剂等辅料。由本发明的成膜组合物制得的膜可速溶于水且不黏腻、耐牵拉,在制膜过程中不易起皱、不易断裂,产品质量高且产量高。
Description
技术领域
本发明属于制膜领域,具体地,本发明涉及一种包含大麻二酚和褪黑素的成膜组合物及其应用。
背景技术
大麻(Cannabis sativa L.),又称为火麻或线麻,是桑科、大麻属植物。大麻中含有的大麻二酚成分是目前在其它动植物中尚未分离出的酚类化合物。大麻二酚是非成瘾性成分,具有很高的药用价值。研究表明,若将大麻二酚合理地应用在医学上,则有抗癫痫、抗精神病,抗忧郁,止痛,减轻癌症因化疗而引起的恶心以及治疗哮喘等功能。大麻二酚还是一种强力抗氧化剂,具有阻断某些毒品人体神经的不利影响,并且具有阻断乳腺癌转移、抗类风湿性关节炎、抗失眠等一系列生理活性功能。
由于大麻二酚的药用价值,越来越多的大麻二酚制剂被开发出来。然而现有的大麻二酚制剂存在很多缺点,例如,大麻二酚口服给药不能总是快速起效。也有一些儿科和/或老年患者由于不能吞咽、恶心或其它胃肠问题导致难以服用口服制剂。另外,通常包含大麻提取物的薄膜或晶片是非常粘稠的,具有苦味的后味,会导致患者不依从;以及常规的薄膜或晶片通常无法包括高负载的活性成分。
因此,如何得到一种单位剂型含量准确、使用方便的以大麻二酚为活性成分的制剂是本领域一个重要的研究方向。
发明内容
本发明针对现有技术上的不足,本发明的目的是提供一种包含大麻二酚和褪黑素的成膜组合物,以用于制备不黏腻、单位剂型含量准确、使用方便、生产过程中损耗更少的膜剂。
第一方面,本发明提供了一种成膜组合物,所述成膜组合物包含活性成分和辅料;所述活性成分为大麻二酚和褪黑素;所述辅料包含乳化剂、成膜剂、增重剂、消泡剂、脱膜剂、矫味剂和唾液分泌促进剂。
在一优选例中,所述乳化剂选自下组:丙二醇、乙二醇、丙三醇、三醋精、柠檬酸三乙酰酯、聚丙二醇、聚乙二醇、矿物油、甘油单酸酯、甘油二酸酯、甘油三酸酯,及其组合。
在一优选例中,所述成膜剂选自下组:普鲁兰多糖、聚葡萄糖、壳聚糖、淀粉、羟丙基甲基纤维素、羟乙基纤维素、羟丙基纤维素、羧甲基纤维素、黄原胶、黄芪胶、阿拉伯胶、金合欢树胶、瓜尔胶、果胶、明胶、角叉菜胶、刺槐豆胶、右旋糖酐、吉兰糖胶、海藻酸盐、聚乙烯吡咯烷酮、聚环氧乙烷、聚乙烯醇、聚乙二醇、聚丙烯酸、甲基丙烯酸甲酯共聚物、羧乙烯基共聚物、乙基纤维素、羟丙基乙基纤维素、邻苯二甲酸醋酸纤维素、羟丙基甲基纤维素邻苯二甲酸酯、磷酸钙、滑石、硅酸钙、碳酸钙,及其组合。
在一优选例中,所述增重剂选自下组:乳糖、甘露醇、葡萄糖、蔗糖、右旋糖、山梨糖醇、木糖醇、赤藓糖醇、硫酸钙、碳酸钙、磷酸氢钙、硬脂酸、直链淀粉、支链淀粉、微晶纤维素,及其组合。
在一优选例中,所述消泡剂选自下组:二甲基硅油、二甲基硅氧烷、聚二甲基硅氧烷、脂肪醇、脂肪酸皂、脂肪酸酯,及其组合。
在一优选例中,所述脱膜剂选自下组:二氧化钛、碳酸钙、硫酸钡、二氧化硅,及其组合。
在一优选例中,所述矫味剂选自下组:三氯蔗糖、蔗糖、葡萄糖、糖精钠、果糖、木糖醇、甜菊糖、安赛蜜、麦芽糖、甘露醇、糖精、柠檬酸、甘草、果汁、阿斯巴甜、蜂蜜,及其组合;或所述矫味剂为来自下组一种或多种植物的有机油:姜、茴香、肉桂、薄荷、甜橙、薰衣草、橘子、樱桃、芒果、蓝莓、草莓。
在一优选例中,所述唾液分泌促进剂选自下组:薄荷油、柠檬酸、苹果酸、乳酸、酒石酸,及其组合。
本发明第二方面提供了一种成膜体系,所述成膜体系由活性成分、辅料和水组成;所述活性成分为大麻二酚和褪黑素;所述辅料包含乳化剂、成膜剂、增重剂、消泡剂、脱膜剂、矫味剂和唾液分泌促进剂。
本发明第三方面提供了第一方面所述的成膜组合物的用途,所述成膜组合物用于制备药物、食物或保健品;或所述成膜组合物用于制备口服制剂或外用制剂。
应理解,在本发明范围内中,本发明的上述各技术特征和在下文(如实施例)中具体描述的各技术特征之间都可以互相组合,从而构成新的或优选的技术方案。限于篇幅,在此不再一一累述。
具体实施方式
如文本使用,术语“室温”表示温度为15-30℃。
如文本使用,术语“丝”为0.1毫米。
如文本使用,“约”表示在限定范围的±10%以内;较佳地在±5%以内。
除非另外说明,否则本文所使用的千分比、百分比和份数按重量计算。
本发明的成膜组合物
本发明的成膜组合物包含活性成分和用于制备速溶膜剂的辅料。
本发明所用的活性成分之一为褪黑素(Melatonine,MT)是由脑松果体分泌的激素之一,属于吲哚杂环类化合物。其化学名为N-[2-(5-甲氧基-3-吲哚)乙基]乙酰胺,又称为松果体素、褪黑色素。主要功能为改善睡眠,有较强的调整时差功能;还可以调节中枢神经系统、免疫系统、心血管系统。
本发明所用的另一活性成分大麻二酚为固态的高纯度的大麻二酚。其可以是发明人根据已知的方法提取自大麻,也可以通过市售购得。
在另一优选例中,本发明所用的大麻二酚中,四氢大麻酚(THC)的含量低于0.3%或为0%。
在另一优选例中,本发明所用的大麻二酚中,大麻二酚的含量大于等于95%。
在另一优选例中,本发明所用的大麻二酚中,大麻二酚的含量大于等于98%。
在另一优选例中,本发明所用的大麻二酚中,大麻二酚的含量大于等于99%。
在另一优选例中,所述活性成分中,大麻二酚为所述成膜组合物总重量的3.37~27.82wt%。
在另一优选例中,所述活性成分中,大麻二酚为所述成膜组合物总重量的3.71~25.88wt%。
在另一优选例中,所述活性成分中,褪黑素为所述成膜组合物总重量的0.83~10.12wt%。
在另一优选例中,所述活性成分中,褪黑素为所述成膜组合物总重量的1.11~7.76wt%。
本发明的成膜组合物制得的膜剂可以通过口腔给药,在接触唾液时能够迅速溶解并释放活性成分。因此,选择合适的辅料对于需要制备的制剂具有关键的作用。另外,用于成膜组合物的辅料应与活性成分有很好的相容性,且对受试者无毒性。
本发明的成膜组合物包含一种或多种乳化剂。本发明所用的乳化剂可以使得活性成分与其他成分很好的相容。适合用于本发明的乳化剂包括,但不限于,丙二醇、乙二醇、丙三醇(或称为甘油)、三醋精、柠檬酸三乙酰酯、聚丙二醇、聚乙二醇、矿物油、甘油单酸酯(例如,癸酸甘油单酯、辛酸甘油单酯)、甘油二酸酯(例如,癸酸甘油二酯、辛酸甘油二酯)、甘油三酸酯,及其组合。
在另一优选例中,所述乳化剂选自下组:丙二醇、乙二醇、丙三醇(或称为甘油)、聚丙二醇、聚乙二醇,及其组合。
在另一优选例中,所述乳化剂为丙三醇和聚乙二醇的组合。
在另一优选例中,所述乳化剂为所述成膜组合物总重量的20.18~28.95wt%。
在另一优选例中,所述乳化剂为丙三醇和聚乙二醇的组合;其中,丙三醇为所述成膜组合物总重量的8.54~12.25wt%;聚乙二醇为所述成膜组合物总重量的11.64~16.70wt%。
本发明的成膜组合物还包含一种或多种成膜剂。本发明所用的成膜剂与活性成分有很好的相容性。适合用于本发明的成膜剂包括,但不限于,普鲁兰多糖、聚葡萄糖、壳聚糖、淀粉、羟丙基甲基纤维素、羟乙基纤维素、羟丙基纤维素、羧甲基纤维素、黄原胶、黄芪胶、阿拉伯胶、金合欢树胶、瓜尔胶、果胶、明胶、角叉菜胶、刺槐豆胶、右旋糖酐、吉兰糖胶、海藻酸盐(例如,海藻酸钠)、聚乙烯吡咯烷酮、聚环氧乙烷、聚乙烯醇、聚乙二醇、聚丙烯酸、甲基丙烯酸甲酯共聚物、羧乙烯基共聚物、乙基纤维素、羟丙基乙基纤维素、邻苯二甲酸醋酸纤维素、羟丙基甲基纤维素邻苯二甲酸酯、磷酸钙、滑石、硅酸钙、碳酸钙,及其组合。
在另一优选例中,所述成膜剂选自下组:羟丙基甲基纤维素、羟乙基纤维素、羟丙基纤维素、羧甲基纤维素、聚乙烯吡咯烷酮、聚环氧乙烷、聚乙烯醇、聚乙二醇、聚丙烯酸、甲基丙烯酸甲酯共聚物、羧乙烯基共聚物、乙基纤维素、羟丙基乙基纤维素、邻苯二甲酸醋酸纤维素、羟丙基甲基纤维素邻苯二甲酸酯,及其组合。
在另一优选例中,所述成膜剂为羟丙基甲基纤维素和聚乙烯醇的组合。
在另一优选例中,所述成膜剂为所述成膜组合物总重量的17.21~24.68wt%。
在另一优选例中,所述成膜剂为羟丙基甲基纤维素和聚乙烯醇的组合;羟丙基甲基纤维素为所述成膜组合物总重量的0.39~0.56wt%;聚乙烯醇为所述成膜组合物总重量的16.82~24.12wt%。
本发明的成膜组合物还包含一种或多种增重剂。本发明所用的增重剂可以提高各个成分的粘附性。适合用于本发明的增重剂包括,但不限于,乳糖、甘露醇、葡萄糖、蔗糖、右旋糖、山梨糖醇、木糖醇、赤藓糖醇、硫酸钙、碳酸钙、磷酸氢钙、硬脂酸、直链淀粉、支链淀粉、微晶纤维素,及其组合。
在另一优选例中,所述增重剂为直链淀粉。
在另一优选例中,所述增重剂为所述成膜组合物总重量的23.29~33.40wt%。
本发明的成膜组合物还包含一种或多种消泡剂。本发明所用的消泡剂可以减少成膜体系的气泡产生、改善膜剂产品的质量。适合用于本发明的消泡剂包括,但不限于,二甲基硅油、二甲基硅氧烷、聚二甲基硅氧烷、脂肪醇、脂肪酸皂、脂肪酸酯,及其组合。
在另一优选例中,所述消泡剂为二甲基硅油。
在另一优选例中,所述消泡剂为所述成膜组合物总重量的3.88~5.57wt%。
本发明的成膜组合物还包含一种或多种脱膜剂。本发明所用的脱膜剂可以降低膜剂与基底膜的粘附性。适合用于本发明的脱膜剂包括,但不限于,二氧化钛、碳酸钙、硫酸钡、二氧化硅,及其组合。
在另一优选例中,所述脱膜剂为二氧化钛。
在另一优选例中,所述脱膜剂为所述成膜组合物总重量的0.04~0.06wt%。
本发明的成膜组合物还包含一种或多种矫味剂。本发明所用的矫味剂可以改善膜剂的口味,提高患者的依从性。适合用于本发明的矫味剂包括,但不限于,三氯蔗糖、蔗糖、葡萄糖、糖精钠、果糖、木糖醇、甜菊糖、安赛蜜、麦芽糖、甘露醇、糖精、柠檬酸、甘草、果汁、阿斯巴甜、蜂蜜,及其组合。
在另一优选例中,所述矫味剂为来自下组一种或多种植物的有机油:姜、茴香、肉桂、薄荷、甜橙、薰衣草,橘子,樱桃、草莓、芒果、蓝莓、草莓。
在另一优选例中,所述矫味剂选自下组:三氯蔗糖、蔗糖、果糖、木糖醇,及其组合。
在另一优选例中,所述矫味剂为三氯蔗糖。
在另一优选例中,所述矫味剂为蔗糖。
在另一优选例中,所述矫味剂为果糖。
在另一优选例中,所述矫味剂为所述成膜组合物总重量的1.29~1.86wt%。
本发明的成膜组合物还包含一种或多种唾液分泌促进剂。本发明所用的唾液分泌促进剂可以促进受试者的唾液分泌、加速膜剂在口腔中的溶解。适合用于本发明的唾液分泌促进剂包括,但不限于,薄荷油、柠檬酸、苹果酸、乳酸、酒石酸,及其组合。
在另一优选例中,所述唾液分泌促进剂为薄荷油。
在另一优选例中,所述唾液分泌促进剂为所述成膜组合物总重量的0.47~0.67wt%。
本发明的成膜组合物的应用
本发明成膜组合物可以用于制备膜剂。所述膜剂可以通过本领域技术人员熟知的方法制得,例如,溶剂浇铸法、热熔挤压法、固体分散挤压法、碾压法、涂布法等方法。
所述膜剂也可以通过如下描述的方法来制备。所述方法包括以下步骤:
(1)提供一种成膜体系;将活性成分、辅料与水混合;
(2)将步骤(1)的成膜体系消泡;
(3)将步骤(2)得到的混合物在制膜机上涂布、牵引、烘干,制得膜剂。
步骤(1)中的成膜体系由活性成分、辅料和水组成;所述活性成分为大麻二酚和褪黑素;所述辅料包含乳化剂、成膜剂、增重剂、消泡剂、脱膜剂、矫味剂和唾液分泌促进剂。
步骤(1)中所使用的水可以是以下的任何一种水:纯水、超纯水、RO水、蒸馏水、双蒸水、去离子水。
步骤(1)的成膜体系由活性成分、辅料和水混合而成。所述混合步骤可以在同一温度下进行,也可以在不同温度下进行。例如该混合步骤在室温至90℃下进行。在一优选例中,该混合步骤在室温至50℃下进行。在一优选例中,该混合步骤在80至90℃下进行。又例如该混合步骤可以先在较低温度(例如室温至50℃)下进行混合,然后在较高温度(例如80至90℃)下进行混合。又例如该混合步骤可以先在较高温度(例如80至90℃)下进行混合,然后在较低温度(例如室温至50℃)下进行混合。
步骤(2)的消泡时间为1-24小时;优选地,可在6-12小时。步骤(2)的消泡可以在真空环境下进行,也可以在常压环境下进行。步骤(2)的消泡还可以在超声波下进行。
本发明可以制备多种厚度的膜剂。在一优选例中,本发明的成膜组合物的厚度为2.5丝~20丝。例如5丝~12.5丝或12.5丝~20丝。
该方法还可以包括以下步骤:将制得的膜剂切割成适宜服用的尺寸或形状;然后进行包装。膜剂的单位剂型的尺寸可以为(1~5)cm x(1~5)cm。例如2.5cm x 3cm。膜剂的形状可以为正方形、长方形或条状。
本发明具有诸多优点:
本发明的成膜组合物制得的膜剂不黏腻、耐牵拉。在涂布烘干成膜时有很好的耐牵拉能力,薄膜既不会因为弹性过大而容易起皱、也不会因为弹性过小而容易脆裂。
本发明的成膜组合物制得的膜剂外观均匀完整、厚度均匀、色泽均匀、无气泡。本发明的成膜组合物制得的膜剂中活性成分分布均匀,每单位剂型中活性成分的含量精确。本发明的单位剂型的中活性成分的含量为2.5mg~50mg。例如5mg~20mg或20mg~50mg。
本发明的成膜组合物制得的膜剂具有很好的水溶性。在人体温度下可在5秒内完全溶解于水中;甚至可以在3秒内完全溶解。
本发明的成膜组合物制得的膜剂使用方便,不会发生吞咽困难。本发明的成膜组合物制得的膜剂可通过皮肤外用给药、口腔黏膜给药或舌下给药。该膜剂进入口腔后可快速吸附于口腔黏膜并使得活性成分迅速被吸收,从而使得活性成分获得较高的生物利用度,也方便具有吞咽困难的患者来服用该类药物。该膜剂中的活性成分避开了消化系统,从而避免了药物呕吐影响药物生物利用度。该膜剂中的活性成分通过口腔黏膜在几秒内即可被吸收并进入到血液中发挥疗效。
本发明的成膜组合物制得的膜剂可适用于不同受试者。所述受试者可以是哺乳动物,例如人或宠物。因此,其可以用于制备人类用药或宠物(例如狗、猫等宠物)用药、食物或保健品。
下面结合具体实施例,进一步阐述本发明。应理解,这些实施例仅用于说明本发明而不用于限制本发明的范围。下列实施例中未注明具体条件的实验方法,通常按照常规条件,或按照制造厂商所建议的条件。下列实施例中未注明来源的试剂均市售可得。
如下实施例中采用的大麻二酚购自Pharmstrip;其纯度为99%。为白色粉末。
如下实施例中采用的制膜机购自平阳县瑞笙机械科技有限责任公司;型号:OZM-360。
如下实施例中采用的薄荷油的密度为0.90g/ml。
如下实施例中采用的试剂至少为分析纯。
实施例1
配方:
步骤:
(1)将甘油、聚乙二醇、直链淀粉、二甲基硅油、羟丙基甲基纤维素与水(80mL)混合均匀后;然后加入大麻二酚、聚乙烯醇、三氯蔗糖、二氧化钛、薄荷油;最后加入褪黑素;将混合物混合均匀;
(2)将步骤(1)得到的混合物在真空环境下室温静置消泡10小时;
(3)将步骤(2)得到的混合物在制膜机上均匀涂布、牵引(牵引速度为0.1-0.5米每分钟),45-80℃烘干,制得厚度为约5丝的膜。
该配方制得的膜不黏腻且耐牵引。在制膜工艺的牵引过程中该配方制得的膜可以保持平整,不易起皱、不易断裂、不粘连、不起泡;且易于切割以及剥离。
最终将该膜切割为2.5cm x 3cm的膜剂后。经测试,该膜剂中活性成分的含量为约5mg每剂。膜剂产品的含水量为3%-5%。
实施例2
配方:
成分名称 | 用量(g) | 百分比(wt%) | |
成膜剂 | 聚乙烯醇 | 65 | 16.82 |
乳化剂 | 聚乙二醇 | 45 | 11.64 |
乳化剂 | 甘油 | 33 | 8.54 |
增重剂 | 直链淀粉 | 90 | 23.29 |
消泡剂 | 二甲基硅油 | 15 | 3.88 |
成膜剂 | 羟丙基甲基纤维素 | 1.5 | 0.39 |
脱膜剂 | 二氧化钛 | 0.15 | 0.04 |
矫味剂 | 三氯蔗糖 | 5 | 1.29 |
唾液分泌促进剂 | 薄荷油 | 1.8 | 0.47 |
活性成分 | 大麻二酚粉末 | 100 | 25.88 |
褪黑素 | 30 | 7.76 | |
100% |
步骤:
(1)将甘油、聚乙二醇、直链淀粉、二甲基硅油、羟丙基甲基纤维素与水(80mL)混合均匀后;然后加入大麻二酚、聚乙烯醇、三氯蔗糖、二氧化钛、薄荷油;最后加入褪黑素;将混合物混合均匀;
(2)将步骤(1)得到的混合物在真空环境下室温静置消泡10小时;
(3)将步骤(2)得到的混合物在制膜机上均匀涂布、牵引(牵引速度为0.05-0.3米每分钟),45-80℃烘干,制得厚度为约20丝的膜。
该配方制得的膜不黏腻且耐牵引。在制膜工艺的牵引过程中该配方制得的膜可以保持平整,不易起皱、不易断裂;且易于切割。
最终将该膜切割为2.5cm x 3cm的膜剂后。经测试,本实施例制得的膜剂中活性成分的含量为约50mg每剂。膜剂产品的含水量为3%-5%。
实施例3
配方:
成分名称 | 用量(g) | 百分比(wt%) | |
成膜剂 | 聚乙烯醇 | 65 | 23.55 |
乳化剂 | 聚乙二醇 | 45 | 16.31 |
乳化剂 | 甘油 | 33 | 11.96 |
增重剂 | 直链淀粉 | 90 | 32.61 |
消泡剂 | 二甲基硅油 | 15 | 5.44 |
成膜剂 | 羟丙基甲基纤维素 | 1.5 | 0.54 |
脱膜剂 | 二氧化钛 | 0.15 | 0.05 |
矫味剂 | 三氯蔗糖 | 5 | 1.81 |
唾液分泌促进剂 | 薄荷油 | 1.8 | 0.65 |
活性成分 | 大麻二酚粉末 | 15 | 5.44 |
褪黑素 | 4.5 | 1.63 | |
100% |
步骤:
(1)将甘油、聚乙二醇、直链淀粉、二甲基硅油、羟丙基甲基纤维素与水(80mL)混合均匀后;然后加入大麻二酚、聚乙烯醇、三氯蔗糖、二氧化钛、薄荷油;最后加入褪黑素;将混合物混合均匀;
(2)将步骤(1)得到的混合物在真空环境下室温静置消泡10小时;
(3)将步骤(2)得到的混合物在制膜机上均匀涂布、牵引(牵引速度为0.05-0.3米每分钟),45-80℃烘干,制得厚度为约12.5丝的膜。
该配方制得的膜不黏腻且耐牵引。在制膜工艺的牵引过程中该配方制得的膜可以保持平整,不易起皱、不易断裂;且易于切割。
最终将该膜切割为2.5cm x 3cm的膜剂后。经测试,本实施例制得的膜剂中活性成分的含量为约20mg每剂。膜剂产品的含水量为3%-5%。
对比例1
配方:
成分名称 | 用量(g) | 百分比(wt%) | |
成膜剂 | 聚乙烯醇 | 65 | 24.12 |
乳化剂 | 聚乙二醇 | 45 | 16.70 |
乳化剂 | 甘油 | 33 | 12.25 |
增重剂 | 直链淀粉 | 90 | 33.40 |
消泡剂 | 二甲基硅油 | 15 | 5.57 |
成膜剂 | 瓜尔豆胶 | 1.5 | 0.56 |
脱膜剂 | 二氧化钛 | 0.15 | 0.06 |
矫味剂 | 三氯蔗糖 | 5 | 1.86 |
唾液分泌促进剂 | 薄荷油 | 1.8 | 0.67 |
活性成分 | 大麻二酚粉末 | 10 | 3.71 |
褪黑素 | 3 | 1.11 | |
100% |
操作步骤同实施例1;对比例1与实施例1的区别在于,对比例1的配方中将羟丙基甲基纤维素更换为瓜尔豆胶。结果该配方制得的膜含水量上升,超过了5%;且成膜会被拉伸。
对比例2
配方:
成分名称 | 用量(g) | 百分比(wt%) | |
成膜剂 | 聚乙烯醇 | 65 | 23.83 |
乳化剂 | 聚乙二醇 | 45 | 16.50 |
乳化剂 | 甘油 | 36.6 | 13.31 |
增重剂 | 直链淀粉 | 90 | 33.00 |
消泡剂 | 二甲基硅油 | 15 | 5.50 |
成膜剂 | 羟丙基甲基纤维素 | 1.5 | 0.55 |
脱膜剂 | 二氧化钛 | 0.15 | 0.05 |
矫味剂 | 三氯蔗糖 | 5 | 1.83 |
唾液分泌促进剂 | 薄荷油 | 1.8 | 0.66 |
活性成分 | 大麻二酚粉末 | 10 | 3.67 |
褪黑素 | 3 | 1.10 | |
100% |
操作步骤同实施例1;对比例2与实施例1的区别在于,甘油的用量上升10%。结果该配方制得的膜起泡严重,膜上存在大量泡眼,甚至出现网筛状破洞,导致膜的厚薄很不均匀。
测试例1水中的溶解时间
取实施例1至实施例3制得2.5cm x 3cm的膜剂进行水中溶解时间的测试。
将装有50ml蒸馏水的烧杯置于温度为37±2℃的恒温槽中,边搅拌边加入实施例1至实施例3制得2.5cm x 3cm的膜剂,结果发现,实施例1至实施例3制得的膜剂均能在3秒内完全溶解于水中。
实施例1至实施例3制得的膜剂可用于口服。该膜剂进入口腔后可快速吸附于口腔黏膜并快速溶解,从而使得活性成分可以快速被吸收。
实施例1至实施例3制得的膜剂还可用于外用,例如膜剂直接贴于具有青春痘、伤口或色素的皮肤上,可有效减轻该部位的症状。
募集了50名青春痘患者,作为志愿者。其中,25名患者不使用实施例1至实施例5制得的膜剂;而另25名患者使用实施例1至实施例5制得的膜剂(将膜剂直接贴于青春痘处)。结果发现,使用本发明膜剂24小时后青春痘处红肿明显消退;而不使用本发明膜剂的患者青春痘处无缓解。
采用本发明配方制得的膜剂外观均匀完整、厚度均匀、色泽均匀、无气泡。
采用本发明配方制得的膜剂不黏腻、耐牵拉(牵引过程中保持平整、不起皱、不断裂),且易于切割(切割边缘不破碎、整齐)以及剥离。制膜过程中产品合格率极高(合格率超过99%);且该膜剂在水中速溶、有利于提高生物利用度。
在本发明提及的所有文献都在本申请中引用作为参考,就如同每一篇文献被单独引用作为参考那样。此外应理解,在阅读了本发明的上述讲授内容之后,本领域技术人员可以对本发明作各种改动或修改,这些等价形式同样落于本申请所附权利要求书所限定的范围。
Claims (10)
1.一种成膜组合物,其特征在于,所述成膜组合物包含活性成分和辅料;所述活性成分为大麻二酚和褪黑素;所述辅料包含乳化剂、成膜剂、增重剂、消泡剂、脱膜剂、矫味剂和唾液分泌促进剂;所述成膜剂为羟丙基甲基纤维素和聚乙烯醇的组合;所述乳化剂为丙三醇和聚乙二醇的组合。
2.如权利要求1所述的成膜组合物,其特征在于,所述乳化剂为所述成膜组合物总重量的20.18~28.95wt%。
3.如权利要求1所述的成膜组合物,其特征在于,所述成膜剂为所述成膜组合物总重量的17.21~24.68wt%。
4.如权利要求1所述的成膜组合物,其特征在于,所述增重剂选自下组:乳糖、甘露醇、葡萄糖、蔗糖、右旋糖、山梨糖醇、木糖醇、赤藓糖醇、硫酸钙、碳酸钙、磷酸氢钙、硬脂酸、直链淀粉、支链淀粉、微晶纤维素,及其组合。
5.如权利要求1所述的成膜组合物,其特征在于,所述消泡剂选自下组:二甲基硅油、二甲基硅氧烷、聚二甲基硅氧烷、脂肪醇、脂肪酸酯,及其组合。
6.如权利要求1所述的成膜组合物,其特征在于,所述脱膜剂选自下组:二氧化钛、碳酸钙、硫酸钡、二氧化硅,及其组合。
7.如权利要求1所述的成膜组合物,其特征在于,所述矫味剂选自下组:三氯蔗糖、蔗糖、葡萄糖、糖精钠、果糖、木糖醇、甜菊糖、安赛蜜、麦芽糖、甘露醇、糖精、柠檬酸、甘草、果汁、阿斯巴甜、蜂蜜,及其组合;或所述矫味剂为来自下组一种或多种植物的有机油:姜、茴香、肉桂、薄荷、甜橙、薰衣草、橘子、樱桃、芒果、蓝莓、草莓。
8.如权利要求1所述的成膜组合物,其特征在于,所述唾液分泌促进剂选自下组:薄荷油、柠檬酸、苹果酸、乳酸、酒石酸,及其组合。
9.一种成膜体系,其特征在于,所述成膜体系由活性成分、辅料和水组成;所述活性成分为大麻二酚和褪黑素;所述辅料包含乳化剂、成膜剂、增重剂、消泡剂、脱膜剂、矫味剂和唾液分泌促进剂;所述成膜剂为羟丙基甲基纤维素和聚乙烯醇的组合;所述乳化剂为丙三醇和聚乙二醇的组合。
10.如权利要求1所述的成膜组合物的用途,其特征在于,所述成膜组合物用于制备药物;或所述成膜组合物用于制备口服制剂或外用制剂。
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