CN108392467A - 一种替米考星注射液及其制备方法 - Google Patents
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Abstract
本发明公开了一种替米考星注射液,包括1000ml的如下重量组分,替米考星300g、有机溶剂100‑500g、增稠剂250g、抗氧剂2‑10g、乳化剂100g,其制备方法包括以下步骤:A.取有机溶剂,加入增稠剂加热至增稠剂溶解;B.加入抗氧剂,待抗氧剂溶解后加入替米考星;C.待替米考星溶解后,加入乳化剂,混合均匀后再加入有机溶剂定容;D.过滤灌封,在100摄氏度下灭菌30分钟,本发明使替米考星被平稳缓慢吸收,一小时浓度是现有技术的近十分之一,故一般剂量不会引起中毒,用量在原来基础上可以增加而不增加用药中毒的风险,解决了替米考星注射液在猪上应用易中毒的难题。
Description
技术领域
本发明涉及兽药领域,特别涉及一种替米考星注射液及其制备方法。
背景技术
替米考星是由泰乐菌素的一种水解产物半合成的畜禽专用抗生素,是20世纪80年代开发的半合成大环内酯类畜禽专用抗生素,主要用于防治家畜肺炎(由胸膜肺炎放线杆菌、巴氏杆菌、支原体感染引起),禽支原体病及泌乳动物的乳腺炎。
参照2015版中国兽药典第一部中“替米考星注射液”标准,替米考星注射液为替米考星与丙二醇等制成的灭菌溶液,其制备方法是,取600ml丙二醇加入300克替米考星,缓慢加入磷酸使替米考星溶解,调PH值到5.5-6.5.用丙二醇定容到1000ml,然后过滤、灭菌、灌封。其适用范围和用量及不良反应如下:
【用法与用量】皮下注射:牛,每1kg体重0.033ml。仅注射1次。
【不良反应】本品对动物的毒性作用主要是心血管系统,可引起心动过速和收缩力减弱。牛一次静脉注射5mg/kg即致死。猪、灵长类动物和马静脉注射也有致死性危险。牛皮下注射50mg/kg可引起心肌毒性,150mg/kg可致死。
现有技术的替米考星注射液对心脏毒性较大,特别是在猪上应用,经应用结论得出,采用肌肉注射10mg/kg体重,即出现呼吸紧促、呕吐和惊厥等中毒症状,但不至于引起死亡,采用15mg/kg体重,危急病例很快死亡,对一般病例采用30mg/kg体重,15分钟内可造成死亡,死亡率高达80%。牛一次静脉注射5mg/kg即致死。牛皮下注射50mg/kg可引起心肌毒性,150mg/kg可致死,猪、灵长类动物和马静脉注射也有致死性危险。
因此,在保证替米考星注射液药效的基础上降低其致死性危险,是极具价值的。
发明内容
为了克服上述现有技术的不足,本发明提供了一种替米考星注射液,吸收缓慢平稳,大大降低了对于动物心血管系统的毒性。
为达到上述目的,本发明解决其技术问题所采用的技术方案是:一种替米考星注射液,包括1000ml的如下重量组分,替米考星300g、有机溶剂100-500g、增稠剂250g、抗氧剂2-10g、乳化剂100g。
作为优选,所述有机溶剂为甘油缩甲醛、二甲基亚砜、丙二醇中一种或几种的组合。
作为优选,所述增稠剂为聚维酮类。
作为优选,所述抗氧化剂是BHT。
作为优选,乳化剂是磷脂类、司盘80中一种或两种的组合。
本发明同时提供了该替米考星注射液的制备方法,包括以下步骤:
A.取有机溶剂,加入增稠剂加热至增稠剂溶解;
B.加入抗氧剂,待抗氧剂溶解后加入替米考星;
C.待替米考星溶解后,加入乳化剂,混合均匀后再加入有机溶剂定容;
D.过滤灌封,在100摄氏度下灭菌30分钟。
由于上述技术方案的运用,本发明与现有技术相比具有下列有益效果:
现有技术的替米考星注射液皮下注射吸收迅速,一小时可达到血药峰浓度,而本发明采用一种缓释技术,使替米考星被平稳缓慢吸收,一小时浓度是现有技术的近十分之一,故一般剂量不会引起中毒,用量在原来基础上可以增加而不增加用药中毒的风险,解决了替米考星注射液在猪上应用易中毒的难题。
具体实施方式
下面结合具体实施例,对本发明的内容做进一步的详细说明:
实施例一:取甘油缩甲醛300ml、二甲基亚砜100ml加入BHT10g,溶解后加入250g聚维酮K90加热使之溶解,然后加入300g替米考星,溶解后加入卵磷脂100g。加入丙二醇至1000ml,检验合格后过滤灌封,100摄氏度30分钟灭菌即得。
实施例二:取甘油缩甲醛300ml、丙二醇100ml加入BHT10g,溶解后加入250g聚维酮K90加热使之溶解,然后加入300g替米考星,溶解后加入卵磷脂100g。加入丙二醇至1000ml,检验合格后过滤灌封,100摄氏度30分钟灭菌即得。
经使用结果得出本发明的适用范围、用法用量及不良反应:
【用法与用量】皮下注射:牛,每1kg体重0.05ml。猪每公斤体重0.06ml仅注射1次。
【不良反应】本品对动物的毒性作用主要是心血管系统,可引起心动过速和收缩力减弱。牛一次静脉注射5mg/kg即致死。猪、灵长类动物和马静脉注射也有致死性危险。牛皮下注射100mg/kg可引起心肌毒性,200mg/kg可致死。猪皮下注射100mg/kg可引起心肌毒性,200mg/kg可致死。
故相对于现有技术,本发明吸收缓慢平稳,大大降低了对于动物心血管系统的毒性,尤其是解决替米考星注射液在猪上应用易中毒的难题。
上述实施例只为说明本发明的技术构思及特点,其目的在于让熟悉此项技术的人士能够了解本发明的内容并加以实施,并不能以此限制本发明的保护范围,凡根据本发明精神实质所作的等效变化或修饰,都应涵盖在本发明的保护范围内。
Claims (6)
1.一种替米考星注射液,其特征在于:包括1000ml的如下重量组分,替米考星300g、有机溶剂100-500g、增稠剂250g、抗氧剂2-10g、乳化剂100g。
2.根据权利要求1所述的一种替米考星注射液,其特征在于:所述有机溶剂为甘油缩甲醛、二甲基亚砜、丙二醇中一种或几种的组合。
3.根据权利要求1所述的一种替米考星注射液,其特征在于:所述增稠剂为聚维酮类。
4.根据权利要求1所述的一种替米考星注射液,其特征在于:所述抗氧化剂是BHT。
5.根据权利要求1所述的一种替米考星注射液,其特征在于:所述乳化剂是磷脂类、司盘80中一种或两种的组合。
6.基于权利要求1~5所述的一种替米考星注射液,本发明还研制了一种制备方法,其特征在于,所述制备方法包括以下步骤:
A.取有机溶剂,加入增稠剂加热至增稠剂溶解;
B.加入抗氧剂,待抗氧剂溶解后加入替米考星;
C.待替米考星溶解后,加入乳化剂,混合均匀后再加入有机溶剂定容;
D.过滤灌封,在100摄氏度下灭菌30分钟。
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CN109077999A (zh) * | 2018-08-31 | 2018-12-25 | 田红卫 | 一种长效缓释替米考星注射液及其制备方法 |
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CN109077999A (zh) * | 2018-08-31 | 2018-12-25 | 田红卫 | 一种长效缓释替米考星注射液及其制备方法 |
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