盐酸沃尼妙林肠溶微丸的制备及质量评价

采用挤出滚圆法制备盐酸沃尼妙林微丸,将含不同比例丙烯酸树脂Ⅱ和Ⅲ及不同包衣增重的几种微丸进行体外释放度试验,选择合适的丙烯酸树脂Ⅱ和Ⅲ比例及包衣增重,同时对制剂的稳定性进行考察,以对自行研制的盐酸沃尼妙林质量进行初步评价.结果显示:丙烯酸树脂Ⅱ和丙烯酸树脂Ⅲ的比例为2∶1、包衣增重为15%时,包衣样品具有典型的肠溶特征,在模拟胃部环境中前2h累积释放量均小于标示量10%,进入肠道内45min的累积释放量大于70%,具有明显的定位释放功能.稳定性试验结果表明,在模拟市售包装的条件下,本品外观、含量等指标均保持稳定,说明微丸具有良好的稳定性、制备工艺可靠.     

盐酸沃尼妙林预混剂的研制及其对猪增生性肠的炎疗效观察

以盐酸沃尼妙林为原料,利用流化床制粒包衣技术成功制备微丸型盐酸沃尼妙林预混剂,用HPLC测定制剂中主药含量。结果表明,制得的产品粒度均匀、流动性良好、含量稳定。选用猪增生性肠炎的自然发病猪为试验对象,以延胡索酸泰妙菌素疗效为对照。结果显示,试验组的高中低不同剂量组(中剂量为推荐剂量)与对照组对猪增生性肠炎治愈率分别为91.0%、82.0%、66.7%和75.3%,有效率分别为96.7%、88.7%、76.7%和83.6%,相同推荐剂量的微丸型盐酸沃尼妙林预混剂组的治愈率和有效率均高于泰妙菌素预混剂组(P<0.05)。     

盐酸沃尼妙林包衣颗粒预混剂的制备及评价

为了改善盐酸沃尼妙林的适口性、降低刺激性以及提高稳定性,采用流化床制粒、包衣技术制备盐酸沃尼妙林包衣颗粒预混剂,正交试验法进行工艺参数的筛选,通过包衣效果试验和稳定性试验进行考察,筛选出最佳生产工艺。在此优化工艺条件下制得的盐酸沃尼妙林包衣颗粒预混剂临床适口性好、质量稳定。本品处方合理,制备工艺简单,为大规模生产提供了依据。     

盐酸沃尼妙林预混剂的制备及评价

采用流化床制粒、包衣技术制备盐酸沃尼妙林预混剂,正交试验法进行工艺参数的筛选,通过包衣效果试验和稳定性试验进行考察,筛选出最佳生产工艺。在此优化工艺条件下制得的盐酸沃尼妙林预混剂临床适口性好、质量稳定。本品处方合理,制备工艺简单,为大规模生产提供了依据。     

酒石酸沃尼妙林的制备和评价

制备了一种新型有机酸盐酒石酸沃尼妙林。通过扫描电子显微镜和X-衍射对其物理化学性质进行研究。结果表明:酒石酸沃尼妙林具结晶性,盐酸沃尼妙林是无定形的。稳定性试验表明:光照60 d,酒石酸沃尼妙林含量减少3.5%,而盐酸沃尼妙林降幅为18.2%;酒石酸沃尼妙林表现出比盐酸沃尼妙林更优的抗湿性,在65%和78%的湿度条件下放置2 d,酒石酸沃尼妙林和盐酸沃尼妙林的吸水量分别为1.30%,1.40%和4.50%,9.71%。体外抗菌敏感性试验表明上述2种盐的抗菌效果相同。酒石酸沃尼妙林对光照和湿度的稳定性将有利于其有效应用在兽医临床领域。     

盐酸沃尼妙林预混剂对猪气喘病的临床疗效试验

进行了盐酸沃尼妙林预混剂对猪气喘病的疗效试验。结果显示:以盐酸沃尼妙林预混剂300 mg/kg和400 mg/kg两种剂量混饲给药,对猪气喘病均有显著效果。盐酸沃尼妙林预混剂可有效控制猪体内的肺炎支原体病原,促进肺炎支原体所致肺组织病变的好转,甚至临床治愈,从而改善气喘病猪的症状。     

盐酸沃尼妙林预混剂对猪痢疾的临床疗效

分析探讨盐酸沃尼妙林预混剂对猪痢疾的临床疗效。方法:将2015年养猪场4~5月龄110头确诊为痢疾病猪作为研究对象,将110头病猪随机分为5组,各22头,进行隔离饲养,饲养条件均相同,A组给予100mg/kg盐酸沃尼妙林预混剂治疗,B组给予75mg/kg盐酸沃尼妙林预混剂治疗,C组给予50mg/kg盐酸沃尼妙林预混剂治疗,D组给予100mg/kg延胡索酸泰妙菌素预混剂治疗,E组正常饲喂,不给予任何抗菌药物,对比观察各组疗效。治疗10d后,沃尼妙林在平均日增重、死亡率方面均明显优于延胡索酸泰妙菌素(P0.05);推荐剂量为75mg/kg。盐酸沃尼妙林预混剂治疗猪痢疾疗效显著,可使猪痢疾减轻至消失,体重明显增加。     

新开元(兽药新产品)上市发布会召开

新开元为10%的盐酸沃尼妙林预混剂,主要用于预防与治疗猪痢疾、猪地方性肺炎、猪结肠螺旋体病(结肠炎)和猪增生性肠病(回肠炎)。长期以来,该药完全依赖于进口。回盛在2008年开始开展此药的合成研究,2009年合成成功,     

盐酸沃尼妙林与猪鸡兔血浆蛋白结合率的检测和比较

本试验采用超滤法结合高效液相色谱-串联质谱法(HPLC-MS/MS)测定沃尼妙林与猪、鸡和兔血浆蛋白结合率,并对血浆中不同浓度沃尼妙林的蛋白结合率进行比较。结果表明,建立的液相色谱-串联质谱联用法用于沃尼妙林生物样品的测定具有简便、灵敏与选择性高的特点。沃尼妙林具有较强的血浆蛋白结合率,其在猪、鸡和兔血浆中的平均蛋白结合率分别为84.4%±1.07%,87.5%±1.83%和86.6%±1.96%。沃尼妙林的血浆蛋白结合率在0.1~10μg/m L的考察浓度范围内无显著性差异,蛋白结合呈现非浓度依赖的特性。     

替米考星微丸肠溶包衣的处方筛选

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。     

替米考星肠溶微丸的制备及其评价

采用挤出滚圆法制备含药微丸,药物以固体分散体的形式存在微丸中,流化床进行肠溶包衣,制得替米考星肠溶微丸。通过不同的工艺处方筛选,考察其理化性质及体外释放特性。分别采用紫外分光光度计测定替米考星的含量,电子显微镜、红外分光光度法和差示扫描量热法确证微丸的特性。结果显示,微晶纤维素在一定程度上对微丸骨架的成型有影响,而包衣的厚度影响微丸的体外释放行为。释放度实验表明替米考星肠溶微丸能达到肠溶制剂的效果。     

替米考星肠溶微丸的质量评价

采用高效液相色谱法和体外溶出度试验测定替米考星肠溶微丸的载药量和溶出度,对自行研制的替米考星肠溶微丸进行初步质量评价。结果显示,制剂含量平均在20%,在人工胃液中不溶出,在人工肠液中溶出度达90%以上,达到了肠溶效果。     

Influences of different Fe sources on Fe bioavailability and homeostasis in SD rats

The purpose of this study was to determine whether the enteric coating process affects growth performance, Fe bioavailability, and gene expression levels that maintain iron balance in the body. The test was divided into the control group, ferrous sulfate group, ferrous fumarate group, ferrous glycine chelate(1:1) (Fe‐Gly(1:1)) group, ferrous glycine chelate(2:1) (Fe‐Gly(2:1)) group, enteric‐coated Fe‐Gly(1:1) group, and enteric‐coated Fe‐Gly(2:1) group. The results showed that the growth performance of the rats in each iron supplement group was no significant difference among them. The results of serum biochemical indicators showed that the antioxidant capacity of the rats in the iron supplement group after enteric coating increased. The iron supplementation effect of Fe‐Gly(1:1) and Fe‐Gly(2:1) was better than that of ferrous sulfate, and the effect of Fe‐Gly(1:1) after enteric coating was enhanced. The expression levels of IRP1 and IRP2 in the genes of enteric‐coated Fe‐Gly(1:1) and enteric‐coated Fe‐Gly(2:1) were significantly higher than those of ferrous sulfate. The expression levels of IRP1 and IRP2 in the protein of enteric‐coated Fe‐Gly(1:1) group were significantly higher than those in the Fe‐Gly(1:1) group. The above results show that Fe‐Gly can improve the bioavailability and antioxidant capacity of iron and reduce the iron output of feces after enteric coating.     

多西环素肠溶微丸的释放度测定

采用紫外分光光度法测定多西环素肠溶微丸的释放度。制剂在酸性介质中释药量符合中国药典对肠溶制剂的要求,在缓冲液介质中快速释药满足多西环素主要在小肠上段吸收的生理特性。     

Clinical efficacy of chlortetracycline hydrochloride administered in milk replacer to calves

Two similar groups of 14 calves were housed and fed identically in individual pens on a calf-rearing farm. The groups were balanced for weight and immunological status as determined by zinc sulphate turbidity values. When an outbreak of enteric and respiratory disease occurred one group was treated with 20 mg chlortetracycline hydrochloride/kg bodyweight daily for seven consecutive days, by adding the active ingredient to the milk replacer, while the other group was left untreated. Both groups received additional therapy as required. The calves were examined daily during the period of treatment and the clinical observations were assessed and analysed statistically. There was a significant difference between the clinical scores of the two groups on the second day of treatment (P less than 0.05) and on all subsequent days (P less than 0.01) indicating that the calves receiving chlortetracycline hydrochloride were less affected by the disease outbreak. The abnormal enteric and respiratory signs were associated with several potential pathogens including bacteria, viruses and protozoa. The treatment was therefore effective against enteric and respiratory disease involving several organisms.     

口服肠溶制剂在兽药领域中的应用前景

介绍了肠溶制剂的制剂特点、肠溶制剂包衣原理、肠溶包衣材料和肠溶制剂类型等内容。结合规模化养殖场对药物饮水给药的需求,从兽用肠溶制剂的药物开发特点及近几年的国内外研究情况等两方面做以阐述,以期为兽用肠溶微丸、肠溶微囊制剂研发提供新的思路。     

Pharmacokinetics of intravenous,plain oral and enteric‐coated oral omeprazole in the horse

The objectives were to document the pharmacokinetics of intravenous, enteric‐coated oral and plain oral omeprazole in fasted horses and to investigate the impact of feeding on the bioavailability of an enteric‐coated omeprazole. Twelve horses received four treatments: intravenous omeprazole (0.5 mg/kg) in the fasted state (IV‐Fasted), enteric‐coated omeprazole (4 mg/kg) orally in the fasted state (ECO‐Fasted), enteric‐coated omeprazole (4 mg/kg) orally in the fed state (ECO‐Fed) and plain omeprazole (4 mg/kg) orally in the fasted state (PL‐Fasted). Plasma omeprazole concentrations were determined by UHPLC‐MS. Bioavailability was higher (P = 0.038) in the ECO‐Fasted group (21.5 [9.0–27.7]%) than the PL‐Fasted group (10.1 [7.7–13.3]%). Similarly, AUC_0‐∞ was higher in the ECO‐Fasted group than the PL‐Fasted group (P = 0.027). No significant differences were present between the ECO‐Fasted and ECO‐Fed groups with regards to bioavailability, C_max, T_max or AUC_0‐∞. When the half‐life data from the oral formulations was pooled, it was longer than that observed in the IV‐Fasted group (100 [73–118] min) and 35 [34‐39] min, respectively; P < 0.0001). Bioavailability of enteric‐coated omeprazole was higher than previously reported and feeding had minimal impact. Bioavailability of plain omeprazole was approximately half that of enteric‐coated omeprazole. The longer half‐life observed following oral administration was consistent with the flip‐flop effect and has not previously been described for omeprazole in the horse.     

包膜赖氨酸对稚鳖生长性能的影响及机理探讨

试验选择平均体重为18.40 g稚鳖180只,分为3组(每组6个重复,每重复10只),分别饲喂赖氨酸缺乏的(赖氨酸水平1.51%),添加晶体赖氨酸和包膜赖氨酸(赖氨酸水平均为2.62%)等能等氮半合成饵料,试验期60d。结果表明,赖氨酸缺乏组鳖晒背率、惊吓逃跑率、特定生长率、肝脏赖氨酸-α-酮戊二酸还原酶活性较低,腐斑率和饵料系数高。添加包膜赖氨酸显著提高了鳖生活力,特定生长率和蛋白质效率,且作用效果优于晶体赖氨酸。赖氨酸缺乏组和晶体赖氨酸组鳖摄食后6 h内血清游离赖氨酸在2 h左右达到高峰水平,而包膜赖氨酸组在4 h左右达到高峰水平。说明包膜赖氨酸可延缓血清游离赖氨酸达到高峰浓度的时间,促进氨基酸的有效利用和蛋白质的合成。     

The effect of feeding on the pharmacokinetic variables of two commercially available formulations of omeprazole

The objectives of this study were to investigate the impact of formulation (enteric coated and buffered) and feeding on pharmacokinetic variables associated with the oral administration of omeprazole in the horse. Six thoroughbred racehorses were studied in a crossover design. Each received 2 g of an enteric coated or buffered formulation in both the fed and fasted state. Plasma omeprazole concentrations were determined by UHPLC‐MS. The effects of feeding or formulation on AUC_{0‐inf_obs}, half‐life, T_max or C_max were not statistically significant. However, a wider‐than‐expected degree of variation was present and examination of the raw data suggests that an effect of feeding, wherein the bioavailability of omeprazole may be reduced in the fed animal, may be present. Further investigation in a larger population of animals to assess the factors that contribute to the wide degree of absorption observed is warranted.