CN112717034A - 一种藤茶提取物在制备治疗畜禽消化道疾病药物中的应用 - Google Patents
一种藤茶提取物在制备治疗畜禽消化道疾病药物中的应用 Download PDFInfo
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Abstract
本发明属于畜牧养殖药剂制备技术领域,具体涉及一种藤茶提取物在制备治疗畜禽消化道疾病药物中的应用;通过对藤茶中的二氢杨梅素进行提取,再与辅料、粘合剂混合进行颗粒剂的制备,所用的辅料种类少、价格低廉、易获取,采用两次包衣法进行颗粒剂的制备,确保颗粒剂在动物肠道中溶解,靶向释放,使得疗效快,减少药剂的使用,提高牲畜免疫力。
Description
技术领域
本发明属于畜牧养殖药剂制备技术领域,具体涉及一种藤茶提取物在制备治疗畜禽消化道疾病药物中的应用。
背景技术
在畜牧养殖生产过程中,畜禽常受到一些病原微生物的影响,导致畜禽发病,尤其是呼吸道、消化道疾病大量发生,使畜禽的免疫力和生产性能下降,给养殖业造成了巨大损失。近年来化学药物耐药性日益严重,化学药物的治疗效果常常不理想。因此,针对这些疾病问题,亟待需要寻求一种安全有效的药物。
藤茶学名为显齿蛇葡萄,亦称莓茶、长寿藤、灵芝草、观音草、藤婆茶、龙须茶等。其主要成分是二氢黄酮醇类黄酮化合物二氢杨梅素(DIHYDROMYRICETIN,DMY或DIM)。研究表明,藤茶茎叶中DMY含量可以高达30%以上,易于提取,藤茶二氢杨梅素在畜禽生长、肉质改善以及防病、提高免疫力等方面均具有一定功效,尤其是在动物抗菌、抗氧化和增强免疫力方面的作用显著。因此,将藤茶二氢杨梅素应用于养殖业生产中对呕吐、腹泻、咳喘等常见的消化道和呼吸道疾病进行防范和治疗,开发成适应于临床用药的颗粒剂,在缓解化学药物的耐药性和提高养殖业的效益方面具有深入意义。
申请号为CN200310110467.3的专利文件公开了二氢杨梅素在制备治疗口腔溃疡的药物中的用途,其公开了可将二氢杨梅素与合适的辅料和/或其他成分一同制成颗粒剂。但此专利是应用于口腔溃疡的治疗。
发明内容
本发明为解决上述问题,提供了一种藤茶提取物在制备治疗畜禽消化道疾病药物中的应用方法。
具体是通过以下技术方案来实现的:
1、一种肠溶颗粒剂,是以藤茶提取物为主药,加入辅料和粘合剂后经两次包衣制成。
进一步,所述的辅料,包括但不限于淀粉、蔗糖和木糖醇。
进一步,所述的粘合剂为浓度75-80%的乙醇。
进一步,所述的辅料和粘合剂与主药的质量比为2-4:1-3:1。
2、所述的肠溶颗粒剂的制备方法,包括以下步骤:
(1)制粒:藤茶经水煎、过滤、烘干、粉碎后得到藤茶粗提物,将藤茶粗提物溶解于60倍的热水中,加热45min后趁热过滤,冷却后置于0~4℃冰箱中冷藏过夜,析出结晶,反复操作3-4次,得到二氢杨梅素纯品(含量≥90%),再将其与辅料混合,以粘合剂润湿混合物后过14目筛制粒得到粗粒药剂;
(2)制微丸:将步骤(1)中制得的粗粒药剂进行冻干处理,再将其进行超微粉碎至平均粒径为1mm,得到微丸;
(3)包衣:将步骤(2)中制得的微丸以丙烯酸树脂Ⅰ号为原料,采用底喷包衣法进行包衣;
(4)矫味:在步骤(3)的包衣过程进行至80-90%时,在包衣液中加入糖和香精,继续包衣,得到肠溶颗粒剂。
进一步,所述的步骤(4)中所用的糖,是由蔗糖与香精以1:0.2-0.5的质量比混合而成。
3、所述的肠溶颗粒剂,用于治疗畜禽消化道疾病。
综上所述,本发明的有益效果在于:本发明通过对藤茶中的二氢杨梅素进行提取,再与辅料、粘合剂混合进行颗粒剂的制备,所用的辅料种类少、价格低廉、易获取,采用两次包衣法进行颗粒剂的制备,确保颗粒剂大部分在动物肠道中溶解,靶向释放,使得疗效快,减少药剂的使用,提高牲畜免疫力。
其中,药理作用如下:藤茶,味苦、微涩,性凉,具有清热利湿,平肝降压,活血通络的功效,主治:用于痢疾,泄泻,小便淋痛,高血压,头昏目胀,跌打损伤。对藤茶中的二氢杨梅素进行提取,添加辅料并非是为了更容易制备颗粒剂,辅料为淀粉时药物溶出效果最好,实际可吸收的药物也更多。在制微丸的时候进行冻干处理,可最大限度的保证二氢杨梅素的活性,避免了采用烘干的方法进行干燥容易造成药物失活或活性降低的情况出现。采用包衣法制备颗粒剂,先采用丙烯酸树脂Ⅰ号对颗粒剂进行包衣,再加入糖和香精进行包衣,糖可以起到诱食、矫味的作用,可避免颗粒剂外层的糖溶解后包衣出现孔洞,避免二氢杨梅素在胃中就释放,使其仅在肠道中溶解释放二氢杨梅素,使药物能有效地在肠道被吸收,提高药物的利用率。并且在应用过程中,我们发现,此肠溶颗粒剂并不止是针对于动物的消化道疾病有效,还可以用于治疗呼吸道疾病,增强动物免疫力。
具体实施方式
下面对本发明的具体实施方式作进一步详细的说明,但本发明并不局限于这些实施方式,任何在本实施例基本精神上的改进或代替,仍属于本发明权利要求所要求保护的范围。
实施例1
1、一种肠溶颗粒剂,是以藤茶提取物为主药,加入淀粉和粘合剂后经两次包衣制成。
进一步,所述的粘合剂为浓度75%的乙醇。
进一步,所述的淀粉和粘合剂与主药的质量比为3:2:1。
2、所述的肠溶颗粒剂的制备方法,包括以下步骤:
(1)制粒:藤茶经水煎、过滤、烘干、粉碎后得到藤茶粗提物,将藤茶粗提物溶解于60倍的热水中,加热45min后趁热过滤,冷却后置于4℃冰箱中冷藏过夜,析出结晶,反复操作4次,得到二氢杨梅素纯品(经检测,含量为96%),再将其与淀粉混合,以粘合剂润湿混合物后过14目筛制粒得到粗粒药剂;
(2)制微丸:将步骤(1)中制得的粗粒药剂进行冻干处理,再将其进行超微粉碎至平均粒径为1mm,得到微丸;
(3)包衣:将步骤(2)中制得的微丸以丙烯酸树脂Ⅰ号为原料,采用底喷包衣法进行包衣;
(4)矫味:在步骤(3)的包衣过程进行至90%时,在包衣液中加入糖和香精,继续包衣,得到肠溶颗粒剂。
进一步,所述的步骤(4)中所用的糖,是由蔗糖与香精以1:0.4的质量比混合而成。
实施例2
1、一种肠溶颗粒剂,是以藤茶提取物为主药,加入蔗糖和粘合剂后经两次包衣制成。
进一步,所述的粘合剂为浓度80%的乙醇。
进一步,所述的蔗糖和粘合剂与主药的质量比为2:3:1。
2、所述的肠溶颗粒剂的制备方法,包括以下步骤:
(1)制粒:藤茶经水煎、过滤、烘干、粉碎后得到藤茶粗提物,将藤茶粗提物溶解于60倍的热水中,加热45min后趁热过滤,冷却后置于0℃冰箱中冷藏过夜,析出结晶,反复操作3次,得到二氢杨梅素纯品(经检测,含量为90%),再将其与蔗糖混合,以粘合剂润湿混合物后过14目筛制粒得到粗粒药剂;
(2)制微丸:将步骤(1)中制得的粗粒药剂进行冻干处理,再将其进行超微粉碎至平均粒径为1mm,得到微丸;
(3)包衣:将步骤(2)中制得的微丸以丙烯酸树脂Ⅰ号为原料,采用底喷包衣法进行包衣;
(4)矫味:在步骤(3)的包衣过程进行至80%时,在包衣液中加入糖和香精,继续包衣,得到肠溶颗粒剂。
进一步,所述的步骤(4)中所用的糖,是由蔗糖与香精以1:0.2的质量比混合而成。
实施例3
1、一种肠溶颗粒剂,是以藤茶提取物为主药,加入木糖醇和粘合剂后经两次包衣制成。
进一步,所述的粘合剂为浓度75%的乙醇。
进一步,所述的木糖醇和粘合剂与主药的质量比为4:3:1。
2、所述的肠溶颗粒剂的制备方法,包括以下步骤:
(1)制粒:藤茶经水煎、过滤、烘干、粉碎后得到藤茶粗提物,将藤茶粗提物溶解于60倍的热水中,加热45min后趁热过滤,冷却后置于2℃冰箱中冷藏过夜,析出结晶,反复操作4次,得到二氢杨梅素纯品(经检测,含量为93%),再将其与木糖醇混合,以粘合剂润湿混合物后过14目筛制粒得到粗粒药剂;
(2)制微丸:将步骤(1)中制得的粗粒药剂进行冻干处理,再将其进行超微粉碎至平均粒径为1mm,得到微丸;
(3)包衣:将步骤(2)中制得的微丸以丙烯酸树脂Ⅰ号为原料,采用底喷包衣法进行包衣;
(4)矫味:在步骤(3)的包衣过程进行至85%时,在包衣液中加入糖和香精,继续包衣,得到肠溶颗粒剂。
进一步,所述的步骤(4)中所用的糖,是由蔗糖与香精以1:0.5的质量比混合而成。
实施例4
1、一种肠溶颗粒剂,是以藤茶提取物为主药,加入糊精和粘合剂后经两次包衣制成。
进一步,所述的粘合剂为浓度77%的乙醇。
进一步,所述的糊精和粘合剂与主药的质量比为2:1:1。
2、所述的肠溶颗粒剂的制备方法,包括以下步骤:
(1)制粒:藤茶经水煎、过滤、烘干、粉碎后得到藤茶粗提物,将藤茶粗提物溶解于60倍的热水中,加热45min后趁热过滤,冷却后置于4℃冰箱中冷藏过夜,析出结晶,反复操作4次,得到二氢杨梅素纯品(经检测,含量为95%),再将其与糊精混合,以粘合剂润湿混合物后过14目筛制粒得到粗粒药剂;
(2)制微丸:将步骤(1)中制得的粗粒药剂进行冻干处理,再将其进行超微粉碎至平均粒径为1mm,得到微丸;
(3)包衣:将步骤(2)中制得的微丸以丙烯酸树脂Ⅰ号为原料,采用底喷包衣法进行包衣;
(4)矫味:在步骤(3)的包衣过程进行至90%时,在包衣液中加入糖和香精,继续包衣,得到肠溶颗粒剂。
进一步,所述的步骤(4)中所用的糖,是由蔗糖与香精以1:0.3的质量比混合而成。
上述实施例中的包衣过程,其参数、设备均为常用参数和设备。
一、辅料筛选实验
1.1实验材料及方法
按表1所设定的条件加入主药和辅料,混合均匀,以浓度为75%的乙醇溶液为粘合剂制备二氢杨梅素颗粒剂粗粒药剂,过14目筛制备颗粒,于55-60通风干燥1.5h,过14目筛整粒。以软材的性状、颗粒粒度(以能通过一号筛和不能通过五号的总量占投料总量的百分比计算)、成型性为考核指标,考察不同用量的糊精、蔗糖、淀粉、木糖醇对上述指标的影响,结果如表2所示。
表1
1.2实验结果
表2
由实验结果可知,蔗糖对二氢杨梅素湿法制粒软材、颗粒粒度、成形性结果较好。最佳的投料比为主药:蔗糖粉=1:3,所得的颗粒剂符合兽药典标准,而且成形性较好。
二、乙醇浓度筛选实验
2.1实验材料及方法
取藤茶提取物4份,每份30克,按实施例1的配方、实验1.1的方法制备二氢杨梅素颗粒剂粗粒药剂,区别在于使用的乙醇浓度分别为75%、80%、85%、90%,对制成的颗粒进行考察,结果如表3所示。
2.2实验结果
表3
由实验结果可知,乙醇浓度对颗粒剂粗粒药剂的成型度有一定影响,乙醇浓度低时,颗粒易粘连结块,难以过筛,乙醇浓度高时,颗粒过于松散,成型的颗粒大小不均。
三、肠溶颗粒剂的体外溶解度实验
3.1实验材料
采用实施例1的方法制备肠溶颗粒剂。
3.2实验方法
在0.1mol/L的盐酸溶液中加入1%的胃蛋白酶作为模拟胃液;在pH7.0的磷酸缓冲液中加入1%的胰蛋白酶作为模拟肠液;在模拟液中加入20克肠溶颗粒剂,每间隔1h以液相色谱法测定溶液中二氢杨梅素的浓度,记录累计溶解度百分比,测试颗粒剂在体外的溶解度,结果如表4所示。
3.3实验结果
表4
由实验结果可知,颗粒剂在模拟胃液中的4h后溶解度均未超过5%,在1h时无药物释放。在模拟肠液中2h时溶解度迅速上升,在3h内药物释放达到80%以上,靶向效果明显。
四、急性毒性实验
材料与方法
4.1动物:选取健康活泼的小鼠,雌雄各10只,分为两组,每组雌雄各5只,一组为实验组,另一组为对照组。
受试药物:以实施例1-3的方法制备的肠溶颗粒剂,取颗粒剂15g,溶于50ml水中,得到受试药液。
4.2实验方法
参照《中药新药研究指南》,在室温23℃的实验室中,反复预试小鼠灌服受试药液50ml/kg,观察一周小鼠毒性反应和死亡情况,未能测出半数致死量,故选用最大耐受量进行实验。
以小鼠的体重为准,按0.1ml/g的剂量,每12h灌胃一次,连续喂服实验组的小鼠一个月;对照组不喂服药液,均自由饮水和觅食,在灌胃药液期间及停止灌胃两周后,期间观察小鼠的状态,并通过血液采集分析、脏器组织活检等项目判断小鼠的健康状况。
4.3实验结果
小鼠在喂服实施例1-3制得的药液一个月内无一例死亡,进食和饮水均无异常,脏器组织活检结果显示正常,小鼠精神状态良好。
五、颗粒剂肠溶靶向效果实验
5.1实验材料
样品1:采用邻苯二甲酸醋酸纤维素(CAP)为内层包衣液制备肠溶颗粒剂,将15克颗粒剂溶解于50ml水中;
样品2:在包衣时将糖和香精从最开始便加入包衣液中进行制备肠溶颗粒剂,将15克颗粒剂溶解于50ml水中;
样品3:采用实施例1的方法制备的肠溶颗粒剂,将15克颗粒剂溶解于50ml水中。
5.2实验方法
5.2.1采用实验三的方法对样品1-3进行溶解度测试,测试样品的体外溶解度,结果如表5所示。
5.2.2大鼠体内靶向实验
选取健康大鼠21只,禁食12h,自由饮水。平均分为3组,每组分别以样品1-3进行灌胃,灌胃剂量按大鼠体重以50mg/kg进行,灌胃后分别于1h、2h、3h、4h、10h时随机选取一只处死,取出胃和肠道的内容物及组织,测定各部分组织中二氢杨梅素的含量,结果如表6所示。
5.3实验结果
表5
由实验结果可知,采用CAP作为包衣液对颗粒剂进行包衣,其也具有靶向肠溶效果,且在模拟胃液中的溶解度较小,但与样品3相比,样品1在模拟肠液中的溶解速度较慢,导致药物释放量不足。样品2在模拟胃液中溶解速度较快,靶向性较差,会导致药物在胃中分解释放,而只有少量能到达肠道吸收。
表6
由实验结果可知,样品1在大鼠胃中的溶解度较小,肠溶颗粒剂的靶向效果较好,但与样品3进行比较,其在大鼠肠道部分的溶解速率较慢,吸收速度慢,治疗效果不好。样品2则是在胃部就开始释放二氢杨梅素,导致其在胃部被吸收溶解,能到达肠道部分的药物较少,肠溶靶向性差。样品3的药物在胃中的含量较少,在肠道内容物中含量剧增,并在3h-4h时药物含量变化不大,说明其在这段时间内释放速率稳定,并且有缓慢下降的趋势。
Claims (8)
1.一种藤茶提取物在制备治疗畜禽消化道疾病药物中的应用方法,其特征在于,是以藤茶提取物为主药,加入辅料和粘合剂后经两次包衣制成肠溶颗粒剂。
2.如权利要求1所述的一种藤茶提取物在制备治疗畜禽消化道疾病药物中的应用方法,其特征在于,所述的辅料,包括但不限于淀粉、蔗糖和木糖醇。
3.如权利要求1所述的一种藤茶提取物在制备治疗畜禽消化道疾病药物中的应用方法,其特征在于,所述的粘合剂为浓度75-80%的乙醇。
4.如权利要求1所述的一种藤茶提取物在制备治疗畜禽消化道疾病药物中的应用方法,其特征在于,所述的两次包衣,是先采用丙烯酸树脂进行内层包衣,再以糖进行外层包衣。
5.一种治疗畜禽消化道疾病的肠溶颗粒剂,其特征在于,主药为藤茶提取物,其中主要活性成分为二氢杨梅素,二氢杨梅素的含量在90%以上。
6.一种治疗畜禽消化道疾病的肠溶颗粒剂的制备方法,其特征在于,包括以下步骤:
(1)制粒:制备藤茶提取物,再将其与辅料混合,以粘合剂润湿混合物后制粒得到粗粒药剂;
(2)制微丸:将步骤(1)中制得的粗粒药剂进行冻干处理,再将其进行超微粉碎,得到微丸;
(3)包衣:将步骤(2)中制得的微丸以丙烯酸树脂Ⅰ号为原料,采用底喷包衣法进行包衣;
(4)矫味:在步骤(3)的包衣过程进行至80-90%时,在包衣液中加入糖和香精,继续包衣,得到肠溶颗粒剂。
7.如权利要求6所述的一种治疗畜禽消化道疾病的肠溶颗粒剂的制备方法,其特征在于,所述的微丸,其平均粒径为1mm。
8.如权利要求6所述的一种治疗畜禽消化道疾病的肠溶颗粒剂的制备方法其特征在于,所述的糖,是由蔗糖与香精以1:0.2-0.5的质量比混合而成。
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