共查询到17条相似文献，搜索用时 265 毫秒
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替米考星微丸肠溶包衣的处方筛选 总被引：2，自引：1，他引：1
采用挤出滚圆方法制备替米考星载药丸芯,以丙烯酸树脂Ⅱ和Ⅲ为材料利用离心造粒包衣设备对丸芯进行包衣。结果显示,所制备的替米考星肠溶微丸在pH=1盐酸溶液中2 h内累积释放度小于10%,用0.2 mol/L的磷酸钠溶液将溶出介质pH调至6.8,继续运转45 min后累积释放度达80%以上,符合《中国药典》对肠溶制剂的要求。 相似文献
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为改善替米考星的水溶性，提高其生物利用度，试验选用聚乙二醇6000和泊洛沙姆188作为载体，采用熔融法制备替米考星固体分散体。以体外累积溶出度为评价指标，通过正交试验筛选最佳制备工艺，选用X-射线衍射法、傅里叶红外光谱法、扫描电镜法进行物相鉴定。结果显示，替米考星固体分散体最佳制备工艺为联合载体PEG6000：P188=20:1、药载比1:3、搅拌时间1 h、固化时间12 h；物相鉴定表明，替米考星为非晶态，固体分散体为晶体结构，替米考星以无定形态分散于载体中；替米考星固体分散体在2 min时溶出度达到71.8%，15 min时完全溶解，显著提高了替米考星的溶出速率。该制备工艺简单，选用联合载体制备替米考星固体分散体，能够有效避免单一载体制备替米考星固体分散体出现的缺陷，有效提高溶出度，方便临床饮水用药。 相似文献
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通过考察3种替米考星颗粒制剂在酸性溶液和缓冲液中的释放情况，为新制剂的进一步研发和临床应用提供理论依据。采用高效液相色谱法对3种不同制剂中替米考星的含量及其体外溶出度进行测定。色谱柱选择Hypersil ODS-2 C18(4.6 mm×250 mm, 5μm),以水∶乙腈∶四氢呋喃∶磷酸二丁胺(790∶130∶55∶25)为流动相，流速1.0 mL/min,检测波长290 nm,柱温30℃。分别以盐酸溶液和磷酸盐缓冲液为溶出介质，测定3种新研制的替米考星不同制剂体外溶出曲线，溶出方法选用浆法，转速为75 r/min,温度为37℃±0.5℃。在所建立的方法学基础上，替米考星在10μg/mL～1000μg/mL范围内与峰面积呈良好的线性关系，在90 min时3种新研制的替米考星不同制剂在酸性溶液中的溶出度分别为100%、5.73%和8.29%,供试品1与供试品2、供试品3及对照品之间差异显著(P<0.05),供试品2、供试品3与对照品之间无明显差异；120 min时3种新研制的替米考星不同制剂在磷酸盐缓冲液中的累积溶出度分别为100%、97.53%和93.60%,3种供试品与对照品... 相似文献
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为了提高替米考星水溶性、适口性和临床使用疗效,试验采用固体分散体技术,通过喷雾熔融载体包被药物的工艺制备了替米考星固体分散体,并对该制剂水溶性、溶出度、稳定性及临床使用进行了考察。结果表明:本试验制备的替米考星固体分散体水溶性高于市售普通替米考星粉剂,溶水后8 min溶出度达到90%以上,制剂常温干燥放置90 d后溶出度依然达到95%以上;临床应用结果显示该制剂适口性和治疗效果优于市售普通制剂。说明采用固体分散体技术制备的替米考星制剂具有较好的水溶性、溶出度和稳定性,在临床应用中表现出良好的适口性和疗效。 相似文献
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为了客观评价替米考星肠溶颗粒临床应用于猪的安全性,选取40头25日龄健康三元杂交猪,随机将其分成4组,每组10头,分别以1倍、3倍、5倍推荐剂量的替米考星肠溶颗粒拌料给药45 d,试验期内对受试猪进行血常规、血凝、血生化、尿常规、增重、料重比、脏器系数等指标的测定及病理学检查。结果显示,替米考星肠溶颗粒对受试猪的血液学指标、尿液指标、主要生产性能等方面未造成明显影响,说明替米考星肠溶颗粒以5倍推荐剂量(2000 g/1000 kg)临床应用于猪是安全的。 相似文献
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Jincheng Xiong Qianqian Zhu Yaxin Zhao Shuaike Yang Jiyue Cao Yinsheng Qiu 《Journal of veterinary pharmacology and therapeutics》2019,42(3):336-345
The purpose of this study was to compare the pharmacokinetics and relative bioavailability of tilmicosin enteric granules and premix after oral administration at a dose of 40 mg/kg in pigs. Three kinds of different respiratory pathogens were selected for determination of minimal inhibitory concentration (MIC) to tilmicosin. Eight healthy pigs were assigned to a two‐period, randomized crossover design. A modified rapid, sensitive HPLC method was used for determining the concentrations of tilmicosin in plasma. Pharmacokinetic parameters were calculated by using WinNonlin 5.2 software. The MIC90 of tilmicosin against Haemophilus parasuis, Actinbacillus pleuropneumoniae, and Pasteurella multocida were all 8 μg/ml. These results indicated that these common pig respiratory bacteria are sensitive to tilmicosin. The main parameters of time to reach maximum plasma concentration (Tmax), elimination half‐life (t1/2β), mean residence time (MRT), and apparent volume of distribution (VF) were 2.03 ± 0.37 hr, 29.31 ± 5.56 hr, 25.22 ± 2.57 hr, 4.06 ± 1.04 L/kg, and 3.05 ± 0.08 hr, 17.06 ± 1.77 hr, 15.55 ± 1.37 hr, 2.95 ± 0.62 L/kg after the orally administrated tilmicosin enteric granules and premix. The relative bioavailability of tilmicosin enteric granules to premix was 114.97 ± 7.19%, according to the AUC0‐t values. These results demonstrated that tilmicosin enteric granules produced faster tilmicosin absorption, slower elimination, larger tissue distribution, and higher bioavailability compared to the tilmicosin premix. The present study results manifest that tilmicosin enteric granules can be used as a therapeutic alternative to premix in clinical treatment. 相似文献
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HPLC法测定复方替米考星颗粒中有效成份含量 总被引：1，自引：1，他引：0
采用HPLC法同时测定了复方替米考星颗粒中替米考星、磺胺二甲氧嘧啶及甲氧苄啶的含量。色谱柱为Eclipse XCB-C18(250 mm×4.6 mm,粒径5μm),流动相为磷酸二丁胺缓冲液-乙腈-四氢呋喃-水(25∶115∶55∶805),检测波长280 nm,流速1.0 mL/min。出峰顺序为甲氧苄啶、磺胺二甲氧嘧啶、替米考星反式结构、替米考星顺式结构,理论塔板数分别为7963、15714、3282、8701。两峰之间的分离度分别为24.29、3.92、2.91;拖尾因子分别为0.92、0.90、0.97、0.94。替米考星、磺胺二甲氧嘧啶、甲氧苄啶的浓度线性范围分别是6.25～125μg/mL(R2=0.996),3.125～62.5μg/mL(R2=0.996),0.625～12.5μg/mL(R2=0.999);平均回收率分别为99.17%、99.06%和99.39%;RSD分别为0.8%、0.9%和0.9%。该法快速、灵敏、准确,适用于同时测定复方替米考星颗粒中三种成份的含量。 相似文献
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采用高效液相色谱法对替米考星合成生产过程进行监控,对泰乐菌素原料A、B两种组分在合成替米考星反应过程中的变化进行了探讨,该项研究成功解决了替米考星合成过程中收率降低的问题。 相似文献
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在常规饲养条件下,以200 mg/kg替米考星剂量水平添加到饲料中饲喂4种黄羽肉鸡,连续饲喂5d,停药后6h,1、3、5、7、10、14 d每1品种肉鸡分别宰杀5只,采集每只鸡的肌肉和肝脏组织,用高效液相色谱-串联质谱法进行残留量测定.结果表明,替米考星主要残留于肉鸡的肝脏组织中;肌肉、肝脏中替米考星残留消除速率相似.停药14 d后,肌肉、肝脏中替米考星残留量均低于最高残留限量.建议替米考星在黄羽肉鸡临床休药期以20 d为宜. 相似文献
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Montesissa C Capolongo F Santi A Biancotto G Dacasto M 《Veterinary journal (London, England : 1997)》2004,167(1):87-94
We investigated tilmicosin (TIM) metabolism, at 25, 50 or 100 microM, in cultures of primary hepatocytes from rabbits bred commercially for food and in liver microsomes prepared from both untreated and rifampicin (RIF)-treated rabbits. RIF is a well-known cytochrome P4503A (CYP 3A) inducer in rabbits and most macrolides are known to be substrates of CYP 3A.No peaks in addition to those of the cis and trans forms of TIM were observed by high performance liquid chromatography (HPLC) in extracts of microsomes from untreated rabbits. When TIM was incubated with induced microsomes, at least two peaks were found by HPLC and an additional peak, eluting at shorter retention time was isolated from hepatocytes incubated for 24h with the macrolide.The structures of the metabolites were then estimated by liquid chromatography-mass spectrometry (LC-MS) in concentrated extracts from induced microsomes. Five metabolites were separated and putatively identified: cis and trans demethylated tilmicosin, tilmicosin N-oxide and cis and trans tilmicosin epoxide. The overall amount of metabolites produced in vitro using livers of untreated and RIF treated rabbits was very low, has also been observed in vivo and in vitro in cattle, chickens and pigs. 相似文献