CN108379457A - 一种安神助眠药物及其无水制备方法 - Google Patents
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Abstract
本发明公开了一种安神助眠药物及无水制备方法，按重量份数计，所述安神助眠药物的原料组成为：γ‑氨基丁酸1‑3份，铁皮石斛干粉5‑15份，唾液酸1‑2份，黄原胶5‑10份，乙基纤维素15‑30份，羟丙基纤维素50‑80份。本发明将γ‑氨基丁酸与铁皮石斛、唾液酸联合使用，能够有效增强γ‑氨基丁酸的功能活性，安神助眠效果更好，安全性高。此外，本发明的整个挤出过程持续时间很短且无须加入水或有机溶剂，不需加热干燥，因此不易发生水解问题，完美解决了传统制药工艺存在的诸多问题。
Description
技术领域
本发明涉及一种安神助眠药物及无水制备方法，属于生物技术领域。
背景技术
γ-氨基丁酸，英文名：γ-aminobutyric acid (GABA)，化学名称：4-氨基丁酸，别名： γ-氨基丁酸，氨酪酸，哌啶酸；分子式：C4H9NO2；分子量：103.1。GABA是目前研究较为深入的一种重要的抑制性神经递质，它参与多种代谢活动，具有很高的生理活性。具有镇静、抗应激、促进食欲、调节内分泌等多种生物学功能。2009年9月27日，卫生部批准γ-氨基丁酸等六种物质为新资源食品，充分说明了γ-氨基丁酸极高的生物安全性。将γ-氨基丁酸应用于安神助眠是一个热门且意义重大的研究课题。本发明发现将γ-氨基丁酸与铁皮石斛、唾液酸联合使用，能够有效增强其功能活性。
而熔融挤压法创造性的将加工技术和药学结合起来，将高分子材料在玻璃化转变温度之上对其进行处理，促使热塑性粘合剂或聚合物、药物活性成分达到分子水平的有效混合。热熔挤出技术结合了固体分散体技术和机械制备的诸多优势，实现了无粉尘、连续化操作、良好的重现性、极高的生产效率和在线监测。不仅可以促进难溶性活性成分溶解从而提高其生物利用度，还可用于制备缓控释、肠溶制剂；此外，这一技术还能用于制备掩味微丸或者其它特殊形状的制剂，如膜剂、棒剂和空心圆柱剂型等。由于整个挤出过程持续时间很短且无须加入水或有机溶剂，不需加热干燥，因此不易发生水解问题。自从首次被应用于药物制剂领域开始，其完美解决传统制药工艺存在的诸多问题，已经成为国内外研究的热点技术。
发明内容
本发明的目的在于针对现有技术不足，提供一种安神助眠药物及无水制备方法。
为实现上述目的，本发明采用如下技术方案：
一种安神助眠药物，按重量份数计，所述安神助眠药物的原料组成为：γ-氨基丁酸1-3份，铁皮石斛干粉5-15份，唾液酸1-2份，黄原胶5-10份，乙基纤维素15-30份，羟丙基纤维素50-80份。
所述铁皮石斛干粉是将铁皮石斛烘干粉碎至80目。
如上所述的安神助眠药物的制备方法为：将各组分原料混合后送入热熔挤出机，在热熔挤出机内进行加热熔融、挤出；热熔挤出机各区的温度设定为：喂料温度25-40℃，传输区温度35-60℃，混合区一段温度50-90℃，混合区二段温度80-140℃，混合区三段温度70-130℃，脱气区温度70-130℃，挤出区温度70-130℃，压片制成600mg片剂。
本发明的有益效果在于：
1）本发明将γ-氨基丁酸与铁皮石斛、唾液酸联合使用，能够有效增强γ-氨基丁酸的功能活性，安神助眠效果更好，安全性高；
2）由于本发明的整个挤出过程持续时间很短且无须加入水或有机溶剂，不需加热干燥，因此不易发生水解问题，完美解决了传统制药工艺存在的诸多问题。
具体实施方式
以下结合具体实施例对本发明做进一步说明，但本发明不仅仅限于这些实施例。
一种安神助眠药物，按重量份数计，所述安神助眠药物的原料组成为：γ-氨基丁酸1-3份，铁皮石斛干粉5-15份，唾液酸1-2份，黄原胶5-10份，乙基纤维素15-30份，羟丙基纤维素50-80份；所述铁皮石斛干粉是将铁皮石斛烘干粉碎至80目。
所述的安神助眠药物的制备方法为：将各组分原料混合后送入热熔挤出机，在热熔挤出机内进行加热熔融、挤出；热熔挤出机各区的温度设定为：喂料温度25-40℃，传输区温度35-60℃，混合区一段温度50-90℃，混合区二段温度80-140℃，混合区三段
温度70-130℃，脱气区温度70-130℃，挤出区温度70-130℃，压片制成600mg片剂。
表1 实施例1~3的安神助眠药物的原料组成（重量份数）
表2 制备过程的工艺参数
实施例2为最优方案。选择大约20g左右昆明种小鼠为实验对象，分两组，每组10只小鼠。试验组每天喂食实施例2所述片剂2次，每次喂食量为0.4mg/10g小鼠体重，连续喂食5天。对照组喂食等量饲料。通过直接睡眠实验、延长戊巴比妥钠睡眠时间实验、戊巴比妥钠阈下剂量催眠实验、巴比妥钠睡眠潜伏期试验来测定小鼠直接睡眠时间、戊巴比妥钠诱导的睡眠时间及阈下剂量的睡眠发生率、巴比妥钠诱导的小鼠睡眠的潜伏时间。结果受试物可较显著延长戊巴比妥钠催眠的中、高剂量组小鼠的睡眠时间；可较显著缩短巴比妥钠催眠中、高剂量组小鼠的入睡潜伏期。证明实施例所述片剂具有改善小鼠睡眠作用。
以上所述仅为本发明的较佳实施例，凡依本发明申请专利范围所做的均等变化与修饰，皆应属本发明的涵盖范围。
Claims (3)
1.一种安神助眠药物，其特征在于：按重量份数计，所述安神助眠药物的原料组成为：γ-氨基丁酸1-3份，铁皮石斛干粉5-15份，唾液酸1-2份，黄原胶5-10份，乙基纤维素15-30份，羟丙基纤维素50-80份。
2.根据权利要求1所述的安神助眠药物，其特征在于：所述铁皮石斛干粉是将铁皮石斛烘干粉碎至80目。
3.一种制备如权利要求1所述的安神助眠药物的方法，其特征在于：将各组分原料混合后送入热熔挤出机，在热熔挤出机内进行加热熔融、挤出；热熔挤出机各区的温度设定为：喂料温度25-40℃，传输区温度35-60℃，混合区一段温度50-90℃，混合区二段温度80-140℃，混合区三段温度70-130℃，脱气区温度70-130℃，挤出区温度70-130℃，压片制成600mg片剂。
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| CN1695492A (zh) * | 2004-05-10 | 2005-11-16 | 沙大年 | 一种稳定、调节血压和改善睡眠的保健食品及其制备方法 |
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| CN1695492A (zh) * | 2004-05-10 | 2005-11-16 | 沙大年 | 一种稳定、调节血压和改善睡眠的保健食品及其制备方法 |
Non-Patent Citations (4)
| Title |
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| 小傅: "燕窝能有效改善失眠", 《HTTPS://M.SOHU.COM/A/78420770_247279/?PVID=000115_3W_A&FROM=SINGLEMESSAGE&ISAPPINSTALLED=0》 * |
| 杨志明: "《中国石斛图鉴》", 31 December 2015, 四川科学技术出版社 * |
| 杨胜远: "γ-氨基丁酸的生理功能和研究开发进展", 《食品科学》 * |
| 熊龙启: "熔融挤压法在工业药剂中的应用", 《中国医药工业杂志》 * |
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Application publication date: 20180810 |