CN114848601B - 一种番石榴叶提取物泡腾片及其制备方法和应用 - Google Patents
一种番石榴叶提取物泡腾片及其制备方法和应用 Download PDFInfo
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- CN114848601B CN114848601B CN202210231927.0A CN202210231927A CN114848601B CN 114848601 B CN114848601 B CN 114848601B CN 202210231927 A CN202210231927 A CN 202210231927A CN 114848601 B CN114848601 B CN 114848601B
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- leaf extract
- guava leaf
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Abstract
本发明公开了一种番石榴叶提取物泡腾片及其制备方法和应用，所述番石榴叶提取物泡腾片包括如下重量含量原料：番石榴叶提取物环糊精包合物30％‑40％、酒石酸27.2％‑33.2％、碳酸氢钠27.2％‑33.2％、聚乙二醇0.5％‑2.5％、硬脂酸镁0.1％‑1.0％、聚乙烯吡咯烷酮0.5％‑1.5％，所述番石榴叶提取物环糊精包合物由番石榴叶提取物与羟丙基‑β‑环糊精制得。通过复配特定比例的番石榴叶提取物环糊精包合物、酒石酸、碳酸氢钠、聚乙二醇、硬脂酸镁和聚乙烯吡咯烷酮，制得一种可快速崩解、溶解性好、口感佳好，且具有降血糖作用的番石榴叶提取物泡腾片。
Description
技术领域
本发明属于功能性组合物领域，尤其涉及一种番石榴叶提取物泡腾片及其制备方法和应用。
背景技术
糖尿病是一种慢性疾病，以长期高血糖为特征。糖尿病是全球的公共卫生危机，目前全世界有超过3.82亿人患有糖尿病，预计到2035年这一数字将增加到5.92亿。其中，2型糖尿病约占糖尿病病例的90％，并且以胰岛素抵抗为特征。目前用于治疗2型糖尿病的西药通常较剧烈且伴有多种不良反应，包括体重增加、低血糖、肠胃气胀、心衰和尿道感染。因此，使用作用温和、副作用小的天然植物草药防治糖尿病具有庞大的市场前景。
番石榴叶是桃金娘科番石榴属植物的叶子，该植物广泛分布于我国南方地区，番石榴叶中富含黄酮和酚酸等有利于降低血糖的活性成分，民间用于糖尿病的辅助治疗。目前通常将番石榴叶泡茶的形式服用，该方式有以下缺点：(1)番石榴叶茶口感苦涩，难以被年轻人接受；(2)该方式难以将活性成分充分浸出，效果差且造成浪费；(3)长期直接服用过多番石榴叶会导致肠道蠕动受抑制，导致便秘不良反应。
番石榴叶提取物泡腾片通常崩解困难、溶解度差等缺点，在水中不能充分溶解，不仅溶液中存在浑浊影响观感的现象，且还存在口服利用度不高的问题，因此市面上较少将番石榴叶提取物制成泡腾片。
发明内容
针对上述现有技术中的不足，本发明的目的在于提供一种番石榴叶提取物泡腾片。通过复配特定比例的番石榴叶提取物环糊精包合物、酒石酸、碳酸氢钠、聚乙二醇、硬脂酸镁和聚乙烯吡咯烷酮，制得一种可快速崩解、溶解性好、口感佳好，且具有降血糖作用的番石榴叶提取物泡腾片。
一种番石榴叶提取物泡腾片，包括如下重量含量原料：番石榴叶提取物环糊精包合物30％-40％、酒石酸27.2％-33.2％、碳酸氢钠27.2％-33.2％、聚乙二醇0.5％-2.5％、硬脂酸镁0.1％-1％、聚乙烯吡咯烷酮0.5％-1.5％，所述番石榴叶提取物环糊精包合物由番石榴叶提取物与羟丙基-β-环糊精制得。
本方案所选用的番石榴叶提取物富含黄酮类化合物和酚酸类化合物，具有降低餐后血糖的功效。
本方案所选用的羟丙基-β-环糊精具有内腔疏水、外部亲水的特性，使其可依据范德华力、疏水相互作用力、主客体分子间的匹配作用等与番石榴叶提取物形成包合物，掩盖番石榴叶提取物的苦涩味，提高番石榴叶提取物泡腾片的水溶性。
本方案选用酒石酸和碳酸氢钠作为酸源和碱源，酒石酸中含有羟基和羧基，与番石榴叶提取物、环糊精、聚乙二醇、硬脂酸镁、聚乙烯吡咯烷酮中的羟基、羧基或酰胺键存在氢键和静电作用，增强各物质间的相互作用，提高番石榴叶提取物泡腾片的崩解度和溶解度，增强番石榴叶提取物泡腾片的降血糖等功效。
发明人在实验过程中发现将聚乙二醇或硬脂酸镁作为润滑剂用于制备番石榴叶提取物泡腾片，番石榴叶提取物泡腾片存在水溶性不佳的问题，即番石榴叶提取物泡腾片在水中不能充分溶解，不仅溶液中存在浑浊影响观感的现象，且还存在口服利用度不高的问题。而发明人发现特定比例的聚乙二醇、硬脂酸镁的复配可有效的提高番石榴叶提取物泡腾片的水溶性，解决番石榴叶提取物泡腾片在压片过程中出现粘冲现象。
硬脂酸镁为非水溶性的润滑剂，泡腾片在水中溶解时水表面容易形成一层薄膜，且有混浊，影响了溶液的澄清度。虽然聚乙二醇是水溶性润滑剂，但将其作为润滑剂应用于制备番石榴叶提取物泡腾片，同样出现番石榴叶提取物泡腾片溶解性不佳的问题。但发明人在实验中发现特定比例的聚乙二醇、硬脂酸镁的复配不仅能有效的提高番石榴叶提取物泡腾片的水溶性，且能更有效的使番石榴叶提取物泡腾片快速崩解，提高番石榴叶提取物泡腾片的利用度，增强番石榴叶提取物泡腾片的降血糖功效。
优选地，所述番石榴叶提取物泡腾片包括如下重量含量原料：番石榴叶提取物环糊精包合物37.5％、酒石酸29.3％、碳酸氢钠29.3％、聚乙二醇1.0％、硬脂酸镁0.5％、聚乙烯吡咯烷酮1.0％，所述番石榴叶提取物环糊精包合物由番石榴叶提取物与羟丙基-β-环糊精制得。
优选地，所述番石榴叶提取物包括重量含量为不超过1.5％的黄酮类化合物和不超过2.3％的酚酸类化合物。
优选地，所述黄酮类化合物为芦丁、桑色素、槲皮素、山奈酚的混合物；所述酚酸类化合物为绿原酸、没食子酸、阿魏酸、咖啡酸的混合物。
优选地，所述番石榴叶提取物与羟丙基-β-环糊精的重量比为1:1。
优选地，所述聚乙二醇的相对分子量为4000。
优选地，所述番石榴叶提取物泡腾片还包括重量含量为0.2％-0.8％的甜菊糖苷、0.5％-1.5％的三氯蔗糖。
优选地，所述番石榴叶提取物泡腾片还包括重量含量为0.5％的甜菊糖苷、0.9％的三氯蔗糖。
本发明的另一目的在于提供一种番石榴叶提取物泡腾片的制备方法，包括如下步骤：
步骤S1.取番石榴叶，粉碎，过20～40目筛，加水，加热回流浸提，趁热抽滤，滤液浓缩至浓稠，冷冻、真空干燥，得番石榴叶提取物干粉。
步骤S2.取番石榴叶提取物干粉溶于水，加入羟丙基-β-环糊精水溶液中，搅拌，冷冻，真空干燥，得番石榴叶提取物环糊精包合物。
步骤S3.将番石榴叶提取物环糊精包合物、酒石酸、碳酸氢钠、聚乙二醇、硬脂酸镁、聚乙烯吡咯烷酮分别粉碎，过60～100目筛。
步骤S4.将步骤S3得到的番石榴叶提取物环糊精包合物、酒石酸、碳酸氢钠、聚乙二醇、硬脂酸镁、聚乙烯吡咯烷酮混合均匀，压片，得番石榴叶提取物泡腾片。
本方案在步骤S1中通过加热回流浸提，趁热抽滤的操作，提高了番石榴叶提取物泡腾片的有效活性成分，提高了番石榴叶提取物泡腾片的水溶性，增强番石榴叶提取物泡腾片的降血糖功效。
本发明再一目的在于提供一种所述的番石榴叶提取物泡腾片在降血糖中的应用。
具体实施方式
为了使本技术领域的人员更好地理解本发明中的技术方案，下面将结合本发明实施例对本发明的技术方案进行清楚、完整地描述，显然，所描述的实施例仅仅是本发明一部分实施例，而不是全部的实施例。基于本发明中的实施例，本领域普通技术人员在没有做出创造性劳动前提下所获得的所有其他实施例，都应当属于本发明保护的范围。
实施例1：番石榴叶提取物泡腾片的制备。
步骤S1.取番石榴叶，粉碎，过20～40目筛，在200g的番石榴叶粉末加2000mL的水，加热回流浸提3h，趁热抽滤，滤液浓缩至浓稠，-20℃冷冻、70pa以下真空干燥24h，得番石榴叶提取物干粉。
步骤S2.取番石榴叶提取物溶于70℃蒸馏水(番石榴叶提取物与蒸馏水的重量比为50:1)，加入羟丙基-β-环糊精(番石榴叶提取物与羟丙基-β-环糊精质量比1:1)水溶液中，70℃下搅拌1h，-20℃冷冻，70pa以下真空干燥24h，得番石榴叶提取物环糊精包合物。
步骤S3.将番石榴叶提取物环糊精包合物、酒石酸、碳酸氢钠、聚乙二醇、硬脂酸镁、甜菊糖苷分别粉碎，过60～100目筛。
步骤S4.将步骤S3得到的番石榴叶提取物环糊精包合物30％、酒石酸33.2％、碳酸氢钠33.0％、聚乙二醇0.5％、硬脂酸镁0.1％、甜菊糖苷0.2％、聚乙烯吡咯烷酮1.5％、三氯蔗糖1.5％混合均匀，压片，得番石榴叶提取物泡腾片。
所述聚乙二醇的相对分子量为4000；所述黄酮类化合物的重量含量为1.5％；所述酚酸类化合物的重量含量为2.3％。
实施例2：番石榴叶提取物泡腾片的制备。
步骤S1.取番石榴叶，粉碎，过20～40目筛，在200g的番石榴叶粉末加2000mL的水，加热回流浸提3h，趁热抽滤，滤液浓缩至浓稠，-20℃冷冻、70pa以下真空干燥24h，得番石榴叶提取物干粉。
步骤S2.取番石榴叶提取物溶于70℃蒸馏水(番石榴叶提取物与蒸馏水的重量比为50:1)，加入羟丙基-β-环糊精(番石榴叶提取物与羟丙基-β-环糊精质量比1:1)水溶液中，70℃下搅拌1h，-20℃冷冻，70pa以下真空干燥24h，得番石榴叶提取物环糊精包合物。
步骤S3.将番石榴叶提取物环糊精包合物、酒石酸、碳酸氢钠、聚乙二醇、硬脂酸镁、甜菊糖苷分别粉碎，过60～100目筛。
步骤S4.将步骤S3得到的番石榴叶提取物环糊精包合物40％、酒石酸27.4％、碳酸氢钠27.3％、聚乙二醇2.5％、硬脂酸镁1.0％、甜菊糖苷0.8％、聚乙烯吡咯烷酮0.5％、三氯蔗糖0.5％混合均匀，压片，得番石榴叶提取物泡腾片。
所述聚乙二醇的相对分子量为4000；所述黄酮类化合物的重量含量为1.5％；所述酚酸类化合物的重量含量为2.3％。
实施例3：番石榴叶提取物泡腾片的制备。
步骤S1.取番石榴叶，粉碎，过20～40目筛，在200g的番石榴叶粉末加2000mL的水，加热回流浸提3h，趁热抽滤，滤液浓缩至浓稠，-20℃冷冻、70pa以下真空干燥24h，得番石榴叶提取物干粉。
步骤S2.取番石榴叶提取物溶于70℃蒸馏水(番石榴叶提取物与蒸馏水的重量比为50:1)，加入羟丙基-β-环糊精(番石榴叶提取物与羟丙基-β-环糊精质量比1:1)水溶液中，70℃下搅拌1h，-20℃冷冻，70pa以下真空干燥24h，得番石榴叶提取物环糊精包合物。
步骤S3.将番石榴叶提取物环糊精包合物、酒石酸、碳酸氢钠、聚乙二醇、硬脂酸镁、甜菊糖苷分别粉碎，过60～100目筛。
步骤S4.将步骤S3得到的番石榴叶提取物环糊精包合物37.5％、酒石酸29.3％、碳酸氢钠29.3％、聚乙二醇1.0％、硬脂酸镁0.5％、甜菊糖苷0.5％、聚乙烯吡咯烷酮1.0％、三氯蔗糖0.9％混合均匀，压片，得番石榴叶提取物泡腾片。
所述聚乙二醇的相对分子量为4000；所述黄酮类化合物的重量含量为1.5％；所述酚酸类化合物的重量含量为2.3％。
对比例1：番石榴叶提取物泡腾片的制备。
将实施例3中的聚乙二醇1.0％、硬脂酸镁0.5％替换成聚乙二醇1.5％，其余步骤不变。
对比例2：番石榴叶提取物泡腾片的制备。
将实施例3中的聚乙二醇1.0％、硬脂酸镁0.5％替换成硬脂酸镁1.5％，其余步骤不变。
对比例3：番石榴叶提取物泡腾片的制备。
将实施例3中的步骤S1的加热回流浸提3h，趁热抽滤，滤液浓缩至浓稠替换成加热回流浸提3h，滤液浓缩至浓稠，其余步骤不变。
对比例4：番石榴叶提取物泡腾片的制备。
将实施例3中的所述聚乙二醇的相对分子量为4000替换成所述聚乙二醇的相对分子量为6000。
对比例5：番石榴叶提取物泡腾片的制备。
将实施例3中的所述聚乙二醇的相对分子量为4000替换成所述聚乙二醇的相对分子量为2000。
α-葡萄糖苷酶抑制实验(pNPG法)：
(1)实验材料：α-葡萄糖苷酶(α-GC)来源于嗜热脂肪芽胞杆菌(Sigma，G3651)、阿卡波糖(Acarbose)、实施例1-3、对比例1-5制得的番石榴叶提取物泡腾片、4-硝基苯-α-D-吡喃葡萄糖苷(4-N-trophenyl-α-D-glucopyranoside，pNPG)、PBS缓冲液、碳酸钠。
(2)试剂配置：PBS(0.1M，PH＝6.8)、α-葡萄糖苷酶(1U/ml)、4-硝基苯基-α-D-吡喃葡萄糖苷(PNPG，5mM)、碳酸钠(1M)、以实施例1-3、对比例1-5制得番石榴叶提取物泡腾片作为样品和阿卡波糖作为阳性对照组。
(3)番石榴叶提取物泡腾片的α-葡萄糖苷酶抑制活性和半数抑制浓度IC50的测试：
将实施例1-3和对比例1-5制得的番石榴叶提取物泡腾片分别配制成番石榴叶提取物如下浓度：10μg/mL、20μg/mL、40μg/mL、80μg/mL、160μg/mL、320μg/mL，阿卡波糖配制成如下浓度：10μg/mL、20μg/mL、40μg/mL、80μg/mL、160μg/mL、320μg/mL，分别加入表1中，用于计算α-葡萄糖苷酶抑制率和半数抑制浓度IC50。
表1.α-葡萄糖苷酶抑制率的测试物质组成及孵育。
按表1的添加量分别将番石榴叶提取物泡腾片、阿卡波糖、PBS(0.1M，PH＝6.8)和α-葡萄糖苷酶(1U/ml)混合，37℃孵育10分钟，加入pNPG(5mM)，37℃孵育20分钟，再加入碳酸钠(1M)，用酶标仪在96孔板中测定405nm波长下的吸光度值。番石榴叶提取物泡腾片的α-葡萄糖苷酶抑制率的计算公式为：(总反应产物-抑制后反应产物)/总反应产物*100％，即[(阴性对照组-空白对照组)-(样品组-样品空白组)]/(阴性对照组-空白对照组)*100％。阿卡波糖的α-葡萄糖苷酶抑制率的计算公式为：(总反应产物-抑制后反应产物)/总反应产物*100％，即[(阴性对照组-空白对照组)-(阳性对照组-阳性空白组)]/(阴性对照组-空白对照组)*100％。并由α-葡萄糖苷酶抑制率计算α-葡萄糖苷酶半数抑制浓度IC50，结果见表2。
表2.α-葡萄糖苷酶的抑制率、半数抑制浓度IC50。
由表2可以看出，本发明实施例1-3制备得到的番石榴叶提取物泡腾片对α-葡萄糖苷酶具有良好的抑制作用。
便秘实验：
(1).实验材料：实施例1-3和对比例1-5制得的番石榴叶提取物泡腾片、番石榴叶提取物颗粒、番石榴叶提取物胶囊、SD大鼠100只(排便正常、大便形状圆润)，体重(200±20)g，雌雄各半。本批实验动物在实验室温度25±3℃，湿度55％±10％，持续12小时明暗交替饲养。
(2).实验方法：将SD大鼠100只，体重(200±20)g，雌雄各半，适应性喂养一周。根据实验目的将动物随机分为10组，即实施例1组、实施例2组、实施例3组、对比例1组、对比例2组、对比例3组、对比例4组、对比例5组、番石榴叶提取物颗粒组、番石榴叶提取物胶囊组。各组分别对应食用实施例1-3、对比例1-5的番石榴叶提取物泡腾片、番石榴叶提取物颗粒、番石榴叶提取物胶囊，每天食用0.5g，食用前采用40℃水溶解，实验期间大鼠按组别分笼，给予标准饲料和饮用水常规饲养，7天后进行效果评价。评价结果如表3所示。
表3.缓解便秘实验测试结果。
从表3可知，食用本发明实施例1-3制备的番石榴叶提取物泡腾片基本不会使大鼠出现便秘现象；对比例1-5所制备的番石榴叶提取物泡腾片的水溶性差，口服利用度低，少量大鼠出现便秘现象；而食用其他制剂的番石榴叶提取物(如颗粒型、胶囊型)则有过半的大鼠会出现便秘现象。
溶解性测试：
将实施例1-3、对比例1-5制得的番石榴叶提取物泡腾片5g(内含1.5g-20g番石榴叶提取物)和实施例2中的步骤S1制得的番石榴叶提取物干粉1.875g分别溶于200g、20℃水中，搅拌30min，观察是否有浑浊现象，过滤，得到滤渣，烘干，水溶性以产品在滤液中的重量百分比表示，即滤液的重量百分比＝(番石榴叶提取物泡腾片总重量-滤渣重量)/番石榴叶提取物泡腾片总重量×100％。结果见表4。
表4.溶解性测试结果。
从表4可知，在相同用量的情况下，本发明实施例1-3制备的番石榴叶提取物泡腾片的水溶性比由聚乙二醇或硬脂酸镁制得的番石榴叶提取物泡腾片的水溶性效果好，说明将聚乙二醇或硬脂酸镁作为润滑剂用于制备番石榴叶提取物泡腾片，番石榴叶提取物泡腾片存在水溶性不佳的问题，即番石榴叶提取物泡腾片在水中不能充分溶解，不仅溶液中存在浑浊影响观感的现象，且还存在口服利用度不高的问题，而将特定比例的聚乙二醇、硬脂酸镁的复配可有效的提高番石榴叶提取物泡腾片的水溶性，解决番石榴叶提取物泡腾片在压片过程中出现粘冲现象。
最后应当说明的是，以上实施例仅用以说明本发明的技术方案而非对其限制，尽管对照上述实施例对本发明进行了详细的说明，所属领域的普通技术人员应当理解，技术人员阅读本申请说明书后依然可以对本发明的具体实施方式进行修改或者等同替换，但这些修改或变更均未脱离本发明申请待批权利要求保护范围之内。
Claims (5)
1.一种番石榴叶提取物泡腾片，其特征在于，所述番石榴叶提取物泡腾片包括如下重量含量原料：番石榴叶提取物环糊精包合物30％-40％、酒石酸27.2％-33.2％、碳酸氢钠27.2％-33.2％、聚乙二醇0.5％-2.5％、硬脂酸镁0.1％-1.0％、聚乙烯吡咯烷酮0.5％-1.5％，所述番石榴叶提取物环糊精包合物由番石榴叶提取物与羟丙基-β-环糊精制得；所述聚乙二醇的相对分子量为4000；
所述番石榴叶提取物泡腾片的制备方法包括如下步骤：
步骤S1.取番石榴叶，粉碎，过20～40目筛，加水，加热回流浸提，趁热抽滤，滤液浓缩至浓稠，冷冻、真空干燥，得番石榴叶提取物干粉；
步骤S2.取番石榴叶提取物干粉溶于水，加入羟丙基-β-环糊精水溶液中，搅拌，冷冻，真空干燥，得番石榴叶提取物环糊精包合物；
步骤S3.将番石榴叶提取物环糊精包合物、酒石酸、碳酸氢钠、聚乙二醇、硬脂酸镁、聚乙烯吡咯烷酮分别粉碎，过60～100目筛；
步骤S4.将步骤S3得到的番石榴叶提取物环糊精包合物、酒石酸、碳酸氢钠、聚乙二醇、硬脂酸镁、聚乙烯吡咯烷酮混合均匀，压片，得到番石榴叶提取物泡腾片。
2.如权利要求1所述的番石榴叶提取物泡腾片，其特征在于，所述番石榴叶提取物泡腾片包括如下重量含量原料：番石榴叶提取物环糊精包合物37.5％、酒石酸29.3％、碳酸氢钠29.3％、聚乙二醇1.0％、硬脂酸镁0.5％、聚乙烯吡咯烷酮1.0％，所述番石榴叶提取物环糊精包合物由番石榴叶提取物与羟丙基-β-环糊精制得。
3.如权利要求1或2所述的番石榴叶提取物泡腾片，其特征在于，所述番石榴叶提取物与羟丙基-β-环糊精的重量比为1:1。
4.如权利要求1或2所述的番石榴叶提取物泡腾片，其特征在于，所述番石榴叶提取物泡腾片还包括重量含量为0.2％-0.8％的甜菊糖苷、0.5％-1.5％的三氯蔗糖。
5.如权利要求1或2所述的番石榴叶提取物泡腾片，其特征在于，所述番石榴叶提取物泡腾片还包括重量含量为0.5％的甜菊糖苷、0.9％的三氯蔗糖。
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