CN100512817C - 复方噻拉嗪注射液及制备工艺 - Google Patents

复方噻拉嗪注射液及制备工艺 Download PDF

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CN100512817C
CN100512817C CNB2006101316238A CN200610131623A CN100512817C CN 100512817 C CN100512817 C CN 100512817C CN B2006101316238 A CNB2006101316238 A CN B2006101316238A CN 200610131623 A CN200610131623 A CN 200610131623A CN 100512817 C CN100512817 C CN 100512817C
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xylazine
ethylenediaminetetraacetic acid
compound injection
dihydroetorphine
hydrochlorate
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CN1957918A (zh
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闫章年
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Abstract

本发明提供一种复方噻拉嗪注射液及制备工艺，将噻拉嗪100g、乙二胺四乙酸61～66g放入重蒸馏水中，在60～90温度下溶解，按5000～2500∶1的比例取盐酸二氢埃托啡进行溶液混匀，制成每ml含噻拉嗪100mg、乙二胺四乙酸61～66mg、盐酸二氢埃托啡10～20μg的混合溶液，灌封于安瓿，灭菌制得。本发明是为野生动物的麻醉、制动提供一种强效制动药物，可用于工业化生产，促进人工养殖业和野生动物保护工作。

Description

复方噻拉嗪注射液及制备工艺
技术领域：
本发明制剂一种动物用麻醉药物，进一步讲是提供了一种复方噻拉嗪注射液及制备工艺，属于兽药制备技术领域。
技术背景：
本发明涉及的噻拉嗪(化学名2-(2，6-二甲苯氨基)-4-H-5，6-二氢-1，3噻嗪)是兽医用于止痛、催眠、肌肉松弛的药，为非麻醉性镇痛、镇静剂，用于麻醉动物，通常为单方制剂，其麻醉速度较慢，在实际使用时为了快速麻醉动物，往往麻醉药量用的非常大，因此，也给被麻醉动物带来很多副作用。
盐酸二氢埃托啡(化学名7a-[1-(R)-羟基-1-甲基丁基]6，14-内乙四氢东罂粟碱的盐酸盐)是一种高效麻醉性镇痛药，对小鼠、大鼠、兔、狗或猴，皮下或肌内注射的有效镇痛剂量在0.1～0.5μg/Kg体重之间，注射用药或舌下用药产生作用较快，口服用药效果差。盐酸二氢埃托啡作用于阿片受体，有效镇痛剂量为盐酸吗啡的数千至上万分之一，但有效维持时间短于盐酸吗啡；呼吸抑制作用相对轻于盐酸吗啡。盐酸二氢埃托啡的治疗指数，小鼠为174468，大鼠为13340，兔为109，最小致死量与最小镇痛有效量之比，狗为4000，猴为50。盐酸吗啡的治疗指数，小鼠为148，大鼠为59，兔为108，最小致死量与最小镇痛有效量之比，狗为201。盐酸二氢埃托啡对豚鼠和兔总胆管括约肌有直接松驰作用；与中枢神经抑制药有相互协同作用；猴的亚急性毒性试验未见蓄积作用，无致畸胎和致突变作用；对猴的成瘾性(身体依赖性)小于盐酸吗啡。
在实际使用过程中，盐酸二氢埃托啡与噻拉嗪单独作为麻醉剂使用时，存在着注射计量过大，毒副作用较大，具有相当的危险性的缺欠。
经检索未见盐酸二氢埃托啡与噻拉嗪作为复方制剂用于动物麻醉的文献报道。
发明内容：
本发明提供一种复方噻拉嗪注射液及制备工艺，是为野生动物的麻醉、制动提供一种强效制动药物，可用于工业化生产，促进人工养殖业和野生动物保护工作。
本发明复方噻拉嗪注射液是由以下物质按重量份数比制成的：
将噻拉嗪100g、乙二胺四乙酸61～66g放入重蒸馏水中，在60～90温度下溶解，按5000～2500：1的比例取盐酸二氢埃托啡进行溶液混匀，制成每ml含噻拉嗪100mg、乙二胺四乙酸61～66mg、盐酸二氢埃托啡10～20μg的混合溶液，灌封于安瓿，灭菌制得。
以下试验证明了本发明的麻醉效果：
药效验证：临床药理研究证明，此药物成份较单独应用时，处方中的含量较单方应用时剂量减少了80％以上，药效作用却显著增强，可以确保100％麻醉、制动多种动物。
用法及体内过程：本品肌注给药，吸收迅速，2.5min后即可从被给药动物体的血中检出，达峰时间为药后28～32min，排泄较快，48小时体内清除率达88％以上，无蓄积残留。
用量：鹿科动物1.0～1.5ml/100kg体重，熊2.0～3.0ml/100kg体重，狮、虎2.5～3.0ml/100kg体重，象0.03～0.05ml/100kg体重，犬科动物0.03～0.04/kg体重。
适用范围：野生动物的手术麻醉、运输、助产、串笼、人工授精、输精等凡需要对野生动物进行药物制动的均可应用。
本发明的积极效果在于：将噻拉嗪与盐酸二氢埃托啡制成复合制剂，经国内多个野生动物保护中心、动物园系统、人工养殖单位、养熊场等大面积推广应用(逾100万例)证明，对多种野生动物具有理想的麻醉制动效果，安全可靠、使用简便、成本低廉，。
具体实施方式
通过以下实施例进一步举例描述本发明，并不以任何方式限制本发明，在不背离本发明的技术解决方案的前提下，对本发明所作的本领域普通技术人员容易实现的任何改动或改变都将落入本发明的权利要求范围之内。
实施例1
将噻拉嗪100g、乙二胺四乙酸61g放入重蒸馏水中，在60～70温度下溶解，按2500：1的比例取盐酸二氢埃托啡进行溶液混匀，制成每ml含噻拉嗪100mg、乙二胺四乙酸61mg、盐酸二氢埃托啡20μg的混合溶液，灌封于安瓿，灭菌制得。
实施例2
将噻拉嗪100g、乙二胺四乙酸66g放入重蒸馏水中，在70～90温度下溶解，按5000：1的比例取盐酸二氢埃托啡进行溶液混匀，制成每ml含噻拉嗪100mg、乙二胺四乙酸66mg、盐酸二氢埃托啡20μg的混合溶液，灌封于安瓿，灭菌制得。
实施例3
将噻拉嗪100g、乙二胺四乙酸64g放入重蒸馏水中，在65～80温度下溶解，按4500：1的比例取盐酸二氢埃托啡进行溶液混匀，制成每ml含噻拉嗪100mg、乙二胺四乙酸64mg、盐酸二氢埃托啡15μg的混合溶液，灌封于安瓿，灭菌制得。

Claims (2)

1、一种复方噻拉嗪注射液，其特征在于是由以下物质按重量份数比组成的：
噻拉嗪100份、乙二胺四乙酸61～66份、盐酸二氢埃托啡0.01～0.02份，余量为重蒸馏水。
2、根据权利要求1所述复方噻拉嗪注射液的制备方法，包括以下步骤：
称取噻拉嗪100g、乙二胺四乙酸61～66g放入重蒸馏水中，在60～90℃温度下溶解，并与盐酸二氢埃托啡进行溶液混匀，制成每m1含噻拉嗪100mg、乙二胺四乙酸61～66mg、盐酸二氢埃托啡10～20μg的混合溶液，灌封于安瓿，灭菌制得。
CNB2006101316238A 2006-11-15 2006-11-15 复方噻拉嗪注射液及制备工艺 Expired - Fee Related CN100512817C (zh)

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TWI630208B (zh) 2008-12-08 2018-07-21 歐陸斯迪公司 二氫羥戊甲嗎啡
GB201309654D0 (en) 2013-05-30 2013-07-17 Euro Celtique Sa Method
CN105496953A (zh) * 2016-01-25 2016-04-20 温州科技职业学院 一种犬用复方丙泊酚水性注射液及其制备方法与应用

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
xylazine+DHE对大鼠的麻醉作用及其对β-内啡肽含量的影响. 张立树，闫章年，李东郊，田慧英，马鹤雯，刘全，杨永胜.中国兽医学报，第20卷第4期. 2000
xylazine+DHE对大鼠的麻醉作用及其对β-内啡肽含量的影响. 张立树，闫章年，李东郊，田慧英，马鹤雯，刘全，杨永胜.中国兽医学报，第20卷第4期. 2000 *
常用药物辅料手册. 李捷玮等，382-383，第二军医大学出版社. 2000 药剂学. 毕殿洲等，247-253，人民卫生出版社. 2001
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药剂学. 毕殿洲等，247-253，人民卫生出版社. 2001 *

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