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CN109077999A - 一种长效缓释替米考星注射液及其制备方法 - Google Patents

一种长效缓释替米考星注射液及其制备方法 Download PDF

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CN109077999A
CN109077999A CN201811012891.7A CN201811012891A CN109077999A CN 109077999 A CN109077999 A CN 109077999A CN 201811012891 A CN201811012891 A CN 201811012891A CN 109077999 A CN109077999 A CN 109077999A
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Abstract

本发明提供一种长效缓释替米考星注射液，包括替米考星300g、有机溶媒100‑500ml、注射油200‑500mlg、胆固醇0.1g、磷脂0.5g,所述有机溶媒包括丙酮、氯仿、四氯化碳，可与油脂相溶且能溶解替米考星的溶剂,所述注射油为注射剂大豆油、注射剂玉米油、氢化蓖麻油。本发明的有益效果是：现有技术在猪上有效剂量使用可造成中毒现象的发生，本发明采用一种长效缓释技术，可延长药物在血液中的滞留时间，延长药物的作用时间，使替米考星缓慢被吸收，不至于使得药物在短时间吸收而中毒。

Description

一种长效缓释替米考星注射液及其制备方法
技术领域
本发明涉及一种长效缓释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。
目前替米考星注射液对心脏毒性较大，特别是在猪上应用，替米考星对猪心脏毒性较大经应用结论得出，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。
发明内容
现有技术在猪上有效剂量使用可造成中毒现象的发生，本发明采用一种长效缓释技术，可延长药物在血液中的滞留时间，延长药物的作用时间，使替米考星缓慢被吸收，不至于使得药物在短时间吸收而中毒。
技术方案：一种长效缓释替米考星注射液，包括替米考星300g、有机溶媒100-500ml、注射油200-500mlg、胆固醇0.1g、磷脂0.5g, 所述有机溶媒包括丙酮、氯仿、四氯化碳，可与油脂相溶且能溶解替米考星的溶剂, 所述注射油为注射剂大豆油、注射剂玉米油、氢化蓖麻油。
进一步，所述的替米考星300g、有机溶媒100-500ml、注射油200-500mlg、胆固醇0.1g、磷脂0.5g，溶解后的总量为1000ml。
进一步，还包括甘油缩甲醛。
本发明还涉及一种长效缓释替米考星注射液的制备方法，脂质体技术应用于本发明中，用油性溶剂做载体，取有机溶剂，加入替米考星、磷脂、胆固醇使之溶解，加入注射用油定容。检测合格以后过滤灌封、灭菌100摄氏度30分钟。
本发明与现有技术相比具有以下优点：
现有技术的替米考星注射液的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。
本发明的适用范围、用法用量及不良反应（经使用结果得出）：
【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。
两者比较，本发明缓慢吸收的原理得以体现出来，用量在原来基础上可以增加而不增加用药中毒的风险，而且本发明在猪上应用也解决可易中毒的难题，可广泛应用。
具体实施方式
本发明替米考星注射液，它包括1000ml的如下组分，替米考星300g、有机溶媒100-500ml、注射油200-500mlg、胆固醇0.1g、磷脂0.5g。
本发明中所述有机溶媒包括丙酮、氯仿、四氯化碳等可与油脂相溶的又能溶解替米考星的溶剂。还可添加适量甘油缩甲醛提高溶解率。所述注射油为注射剂大豆油、注射剂玉米油、氢化蓖麻油等。
本发明的替米考星注射液的制备方法，脂质体技术应用于本发明中，用油性溶剂做载体，取有机溶剂适量，加入替米考星、磷脂、胆固醇使之溶解，加入注射用油定容。检测合格以后过滤灌封、灭菌100摄氏度30分钟，即得。
实施例1：
取氯仿500ml，加入替米考星300g、磷脂0.5g、胆固醇0.1g使之完全溶解，加入注射油至1000ml，检验合格后过滤灌封，100摄氏度30分钟灭菌即得。
实施例2：
取丙酮400ml、甘油缩甲醛100ml混合均匀后，加入替米考星300g、磷脂0.5g、胆固醇0.1g加热使之溶解，加入大豆油至1000ml，检验合格后过滤灌封，100摄氏度30分钟灭菌即得。
以上显示和描述了本发明的基本原理和主要特征以及本发明的优点。本行业的技术人员应该了解。本发明不受上述实例的限制，上述实例和说明书中只是说明本发明的原理，在不脱离本发明的精神和范围的前提下本发明还会有各种变化和改进，这些变化和改进都落入要求保护的本发明范围内，本发明要求保护范围由所附的 权利要求书及其等效物界定。

Claims (6)

1.一种长效缓释替米考星注射液，其特征在于：包括替米考星300g、有机溶剂100-500ml、注射油200-500mlg、胆固醇0.1g、磷脂0.5g, 所述有机溶剂包括丙酮、氯仿、四氯化碳，可与油脂相溶且能溶解替米考星的溶剂, 所述注射油为注射剂大豆油、注射剂玉米油、氢化蓖麻油。
2.根据权利要求1所述的一种长效缓释替米考星注射液，其特征在于：所述的替米考星300g、有机溶剂100-500ml、注射油200-500mlg、胆固醇0.1g、磷脂0.5g，溶解后的总量为1000ml。
3.根据权利要求1或2所述的一种长效缓释替米考星注射液，其特征在于，还包括甘油缩甲醛。
4.一种长效缓释替米考星注射液的制备方法，其特征在于：脂质体技术应用于本发明中，用油性溶剂做载体，取有机溶剂，加入替米考星300g、磷脂0.5g、胆固醇0.1g使之溶解，加入注射油定容，检测合格以后过滤灌封、灭菌100摄氏度30分钟。
5.根据权利要求4所述的一种长效缓释替米考星注射液的制备方法，其特征在于：所述的有机溶剂为氯仿500ml，加入替米考星300g、磷脂0.5g、胆固醇0.1g使之完全溶解，加入注射油溶解后至1000ml，检验合格后过滤灌封，100摄氏度30分钟灭菌即得。
6.根据权利要求4所述的一种长效缓释替米考星注射液的制备方法，其特征在于：所述的有机溶剂为丙酮400ml、甘油缩甲醛100ml的混合物，加入替米考星300g、磷脂0.5g、胆固醇0.1g加热使之溶解，加入注射油1000ml，所述的注射油为大豆油，检验合格后过滤灌封，100摄氏度30分钟灭菌即得。
CN201811012891.7A 2018-08-31 2018-08-31 一种长效缓释替米考星注射液及其制备方法 Pending CN109077999A (zh)

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Application publication date: 20181225