兽医寄生虫药物 制剂研究进展

从经皮给药制剂，缓、控释给药制剂和靶向给药制剂三个方面综述了兽医寄生虫药物制剂的研究进展     

经络穴位给药系统在兽医临床上的应用

经络穴位给药系统以中医经络理论为基础,具有经穴效应和药物效应的双重治疗特性,已广泛应用于兽医临床.目前,兽医临床上常用穴位给药方式是穴位埋植和穴位注射,而常用穴位主要是后海穴、百会穴、肺龠穴.随着经络穴位给药系统的广泛应用,新型经络穴位给药制剂和经络穴位给药作用机理已成为经络穴位给药系统研究的重点.     

硫酸庆大霉素药剂学研究进展

本文以“庆大霉素”“制剂”“药物动力学”“Gentamycin”“preparation”“pharmacokinetics”为关键词,组合查询1988-2018年在中国知网、万方、维普、中国专利信息网、PubMed、Web of Science等国内外数据库中收录的相关文献,归纳、总结硫酸庆大霉素制剂学及药物动力学方面的研究进展。结果表明:共检索到相关文献261篇,其中有效文献44篇。硫酸庆大霉素作为常用的氨基糖苷类药物之一,具有广泛的临床应用价值。目前,以硫酸庆大霉素作为单一主药上市的庆大霉素制剂多为注射途径给药制剂与普通口服制剂。缓控迟释制剂、经皮给药制剂等近年来发展迅速,逐步成为硫酸庆大霉素制剂研发的重点,为硫酸庆大霉素制剂研发开辟了新的思路。     

凝胶剂研究进展

凝胶剂具有载药量大、使用方便、皮肤的生物相容性好等诸多优点,成为一种极具市场潜力的经皮给药制剂,被广泛应用于医药以及化妆品相关领域。本文对凝胶剂的分类、制备工艺、释药机制、临床应用等多个方面进行综述,凝胶剂有多种分类方式,按基质类型可以分为亲水性凝胶、亲脂性凝胶与乳剂型凝胶;根据所受外界刺激的不同可以分为温度敏感型凝胶、pH敏感型凝胶和离子敏感型凝胶等。目前,凝胶剂的制备工艺仍采用“冷法”为主,即准确称取处方量的凝胶基质,加入适量蒸馏水与相关辅料,搅拌均匀,置于4℃冰箱内至完全溶解,充分溶胀后即得;凝胶剂的释药机制主要遵循Higuchi方程、零级释药方程和一级动力学方程等。     

中药透皮吸收研究进展

经皮给药系统,又称经皮治疗系统,系指皮肤贴敷方式用药,药物以一定的速率通过皮肤经毛细血管吸收进入体循环产生药效的一种给药方式。作者对经皮给药系统的发展历史、吸收机制、影响因素,透皮吸收的作用途径、促进方法等作一综述。     

低频超声透皮给药的作用机制和影响因素

低频率超声可以提高药许多药物的透皮传输,其机制有多种解释,但最被普遍认可的是超声的空化作用,多数研究人员认为超声是通过改变皮肤角质层角化细胞的排列结构来促进药物的透皮吸收。低频超声透皮给药在离体和动物活体实验研究上得到广泛的应用,不论是小分子药物的透皮吸收还是大分子药物的透皮吸收都取得了不错的成果。然而临床上应用低频超声介导药物进行治疗的相关报道不多。若低频超声给药的安全性得到证实,低频超声透皮给药必将成为一种安全、快速、可控、有效、经济的新型给药方式。     

靶向给药系统的研究进展

靶向给药系统是药剂学研究的一个热点,是一类能使药物浓集定位于病变组织、器官、细胞或细胞内结构的新型给药系统,使药物能够可控性地分布,并于靶区持续缓慢地释放药物,有效降低其对正常组织的毒副作用,从而提高疗效,降低治疗费用。靶向给药制剂应用     

药物透皮吸收常用实验方法概述

治疗畜禽疾病的传统给药方式主要是采用注射、口服或将药物投入饮水或饲料中。随着制剂技术的不断发展 ,透皮制剂在兽医临床上的应用日趋广泛。透皮制剂与其他给药方式相比较 ,主要具有可产生持久、恒定及可控的血药浓度 ;避免肝脏对药物首过代谢的降解作用 ;给药方法简单、可减轻副作用、在发生问题时能及时停止给药 ;可减少给药次数和剂量等优点。鉴于此 ,透皮制剂在兽医临床领域倍受关注。近年来 ,兽医科技工作者通过不懈努力 ,已有许多兽用透皮制剂相继问世 ,使用最多的是杀虫剂。透皮实验法是研究透皮吸收药物必不可少的实验手段 ,笔者…     

应用盐酸环丙沙星不同给药方法治疗牛胃肠炎的效果

为探究应用盐酸环丙沙星不同给药方法治疗牛肠胃炎的不同的治疗效果,于2016年1月—2018年3月收治了210头患胃肠炎的病牛,应用盐酸环丙沙星药进行治疗,该文运用了3组给药方法,通过对比得出3组不同给药方式的效果。3组给药方式为口服、瓣胃注射、肌肉注射。瓣胃注射给药的病牛治愈率是95.71%,口服给药方式的病牛治愈率为61.42%,肌肉注射治疗病牛的给药方式治愈率为72.85%,首次运用瓣胃注射方式的治愈率明显高于其他给药方式(P<0.05)。运用瓣胃注射方式治疗患肠胃病的病牛,具有显著的效果,可直接医治病牛肠胃内纤毛虫的生长,具有显著的抗菌效果,可改善患肠胃炎的病牛,易被兽医应用和借鉴。     

中药治疗奶牛乳房炎的研究进展

本文主要对中药治疗奶牛乳房炎的临床应用、给药方式进行了综述．对中草药防治奶牛乳房炎的前景进行了展望。希望对中药治疗奶牛乳房炎的临床用药提供参考。     

Comparison of pharmacokinetics of fentanyl after intravenous and transdermal administration in cats

OBJECTIVE: To compare pharmacokinetic and pharmacodynamic characteristics of fentanyl citrate after IV or transdermal administration in cats. ANIMALS: 6 healthy adult cats with a mean weight of 3.78 kg. PROCEDURE: Each cat was given fentanyl IV (25 mg/cat; mean +/- SD dosage, 7.19 +/- 1.17 mg/kg of body weight) and via a transdermal patch (25 microg of fentanyl/h). Plasma concentrations of fentanyl were measured by use of radioimmunoassay. Pharmacokinetic analyses of plasma drug concentrations were conducted, using an automated curve-stripping process followed by nonlinear, least-squares regression. Transdermal delivery of drug was calculated by use of IV pharmacokinetic data. RESULTS: Plasma concentrations of fentanyl given IV decreased rapidly (mean elimination half-life, 2.35 +/- 0.57 hours). Mean +/- SEM calculated rate of transdermal delivery of fentanyl was 8.48 +/- 1.7 mg/h (< 36% of the theoretical 25 mg/h). Median steady-state concentration of fentanyl 12 to 100 hours after application of the transdermal patch was 1.58 ng/ml. Plasma concentrations of fentanyl < 1.0 ng/ml were detected in 4 of 6 cats 12 hours after patch application, 5 of 6 cats 18 and 24 hours after application, and 6 of 6 cats 36 hours after application. CONCLUSIONS AND CLINICAL RELEVANCE: In cats, transdermal administration provides sustained plasma concentrations of fentanyl citrate throughout a 5-day period. Variation of plasma drug concentrations with transdermal absorption for each cat was pronounced. Transdermal administration of fentanyl has potential for use in cats for long-term control of pain after surgery or chronic pain associated with cancer.     

新型药物递送系统在兽药制剂领域的研究进展

新型药物递送系统在新药研发中的应用近年来在国内外受到了广泛的重视。兽用新型载药系统的研究,解决了兽用药物在动物体内半衰期短、靶向性差、药物利用率低以及药物溶解性特定要求等问题,可开发出新型、高效、安全的生物药物剂型。兽药新型递药系统已在兽药领域展现出广阔的前景,并成为兽药研发的新方向之一。本文就目前主要递药系统(如缓控释递药系统、纳米递药系统、靶向给药系统、透皮给药系统、生物粘附给药系统、植入控释给药系统以及自乳化给药系统等)在兽药制剂领域的研究进展进行综述,并分析和探讨了新型递药系统在兽医领域应用瓶颈、现有研究面临的挑战及未来的发展趋势,以期为新型递药系统在兽药领域的应用提供参考。     

Systemic absorption of amitriptyline and buspirone after oral and transdermal administration to healthy cats

A prospective study was performed to determine the relative availability of buspirone and amitriptyline after oral and transdermal routes of administration in 6 adult cats. For topical administration, drugs were compounded in a transdermal organogel containing pluronic and lecithin (PLO). Using a crossover design, each cat received a single dose of amitriptyline (5 mg) and buspirone (2.5 mg) by the transdermal and oral route of administration with at least a 2-week washout interval between drug treatments. Blood samples were obtained at 0, 0.5, 1, 2, 4, 6, 8, 10, and 12 hours after drug administration for determination of plasma drug concentrations. Plasma concentrations of immunoreactive amitriptyline and buspirone were determined using commercial enzyme-linked immunosorbent assay (ELISA) tests. Systemic absorption of amitriptyline and buspirone administered by the transdermal route was poor compared with the oral route of administration. Until supporting pharmacokinetic data are available, veterinarians and cat owners should not rely on the transdermal route of administration for treating cats with amitriptyline or buspirone.     

Evaluation of transdermal morphine and fentanyl pluronic lecithin organogel administration in dogs

Transdermal administration of morphine and fentanyl using a pluronic lecithin organogel was evaluated in dogs. IV administration of morphine and fentanyl resulted in therapeutic serum drug concentrations. Following transdermal administration, however, median serum drug concentrations were never above the limit of quantitation for morphine or fentanyl. These findings indicate that use ofa pluronic lecithin organogel for transdermal administration of morphine or fentanyl cannot be justified.     

Pharmacokinetics of fentanyl following intravenous and transdermal administration in horses

REASONS FOR PERFORMING STUDY: Although fentanyl has been reported to cause CNS excitation in horses, a transdermal therapeutic system (TTS) containing this mu agonist has recently been used empirically in equine medicine to treat moderate to severe pain. A better understanding of the disposition of fentanyl following transdermal administration would facilitate the clinical use of TTS fentanyl to obtain analgesia in horses. OBJECTIVES: To determine the pharmacokinetics of fentanyl following i.v. and TTS patch administration in healthy, mature horses and to evaluate the tolerance of horses to TTS fentanyl administration. METHODS: The pharmacokinetics of fentanyl in serum were assessed following a single i.v. dose, a single TTS dose, and multiple TTS doses in 6 healthy horses. Physical examinations, haematology and serum biochemistry analyses during transdermal fentanyl application were then performed to determine tolerance of continuous fentanyl administration. RESULTS: Fentanyl was very rapidly and completely absorbed following a single TTS dose. Mean serum fentanyl concentrations consistent with analgesia in other species were reached by 1 h and maintained until 32 h after patch application. Similar steady state serum concentrations were obtained when multiple doses of TTS fentanyl were administered every 48 or 72 h over 8 or 9 days, with less fluctuation in serum concentrations during the 48 h dosing interval. Three horses exhibited brief (< 12 h) episodes of increased body temperature; however, transdermal fentanyl administrations were not associated with other significant changes in haematology and biochemistry panels or physical examination findings. CONCLUSIONS AND POTENTIAL RELEVANCE: Although the pharmacodynamics of fentanyl have not been investigated fully in horses, transdermally-administered fentanyl exhibited a favourable pharmacokinetic profile without clinically relevant side effects and may be a useful analgesic in equine patients.     

兽用抗寄生虫药物新剂型及其新技术的研究进展

兽用抗寄生虫药物由于使用频繁,其给药技术研究一直备受重视.目前,兽用抗寄生虫药物新剂型和新技术的研究主要集中在缓释控释制剂和脂质体制剂,其次是透皮给药系统、微囊、微球、环糊精包合物、固体分散体等.但这些新剂型和新技术大多还处于研究阶段,在处方设计或制剂工艺方面都还存在一些问题,今后应加强这些新剂型的工艺和技术研究,以真正发挥这些新剂型的优点.     

Pharmacokinetics of multiple doses of transdermal flunixin meglumine in adult Holstein dairy cows

A transdermal formulation of the nonsteroidal anti‐inflammatory drug, flunixin meglumine, has been approved in the United States and Canada for single‐dose administration. Transdermal flunixin meglumine was administered to 10 adult Holstein cows in their second or third lactation at the label dose of 3.33 mg/kg every 24 hr for three total treatments. Plasma flunixin concentrations were determined using high‐pressure liquid chromatography with mass spectroscopy (HPLC ‐MS ). Pharmacokinetic analysis was completed on each individual animal with noncompartmental methods using computer software. The time to maximum drug concentration (T max) was 2.81 hr, and the maximum drug concentration was 1.08 μg/ml. The mean terminal half‐life (T½) was determined to be 5.20 hr. Clearance per fraction absorbed (Cl/F) was calculated to be 0.294 L/hr kg^?1, and volume of distribution of fraction (V z/F ) absorbed was 2.20 L/kg. The mean accumulation factor was 1.10 after three doses. This indicates changes in dosing may not be required when giving multiple doses of flunixin transdermal. Further work is required to investigate the clinical efficacy of transdermal flunixin after multiple daily doses.     

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。     

Evaluation of transdermal application of glipizide in a pluronic lecithin gel to healthy cats

OBJECTIVE: To evaluate plasma glipizide concentration and its relationship to plasma glucose and serum insulin concentrations in healthy cats administered glipizide orally or transdermally. ANIMALS-15 healthy adult laboratory-raised cats. PROCEDURE: Cats were randomly assigned to 2 treatment groups (5 mg of glipizide, PO or transdermally) and a control group. Blood samples were collected 0, 10, 20, 30, 45, 60, 90, and 120 minutes and 4, 6, 10, 14, 18, and 24 hours after administration to determine concentrations of insulin, glucose, and glipizide. RESULTS: Glipizide was detected in all treated cats. Mean +/- SD transdermal absorption was 20 +/- 14% of oral absorption. Mean maximum glipizide concentration was reached 5.0 +/- 3.5 hours after oral and 16.0 +/- 4.5 hours after transdermal administration. Elimination half-life was variable (16.8 +/- 12 hours orally and 15.5 +/- 15.3 hours transdermally). Plasma glucose concentrations decreased in all treated cats, compared with concentrations in control cats. Plasma glucose concentrations were significantly lower 2 to 6 hours after oral administration, compared with after transdermal application; concentrations were similar between treatment groups and significantly lower than for control cats 10 to 24 hours after treatment. CONCLUSIONS AND CLINICAL RELEVANCE: Transdermal absorption of glipizide was low and inconsistent, but analysis of our results indicated that it did affect plasma glucose concentrations. Transdermal administration of glipizide is not equivalent to oral administration. Formulation, absorption, and stability studies are required before clinical analysis can be performed. Transdermal administration of glipizide cannot be recommended for clinical use at this time.