纳米混悬剂的特征及其在兽医上的应用前景

<正>纳米混悬剂是以表面活性剂为助悬剂,将药物颗粒分散在水中,通过粉碎或者控制析晶技术形成的稳定的纳米胶态分散体。不论是难溶于水的药物还是既难溶于水又难溶于油的药物,均可以通过纳米技术制备得到相应的纳米混悬剂。作为一种中间剂型,可利用纳米混悬剂进一步制备适合口服、注射或其他给药途径的药物剂型,以提高药物的吸收和生物利用度。与传统意义上的基质骨架型纳米体系不同,纳     

我国对纳米混悬剂优势和应用的研究进展

纳米混悬剂（Nanosuspensions）是以表面活性剂为助悬剂将药物颗粒分散在水中，通过粉碎或者控制析晶技术形成的稳定的纳米胶态分散体，与传统意义上的基质骨架型纳米体系不同，纳米混悬剂无需载体材料，它可通过表面活性剂的稳定作用，将纳米尺度的药物粒子分散在水中形成稳定的体系。由于纳米混悬剂的特性，其在各种给药途径中都体现出了独特的优势。国外从20世纪末开始就已经展开了对纳米混悬剂的研究，国内有关研究近几年也相继增多，现将国内对纳米混悬剂优势和应用的研究情况介绍如下。     

穿心莲内酯纳米混悬剂的制备与评价

为优选穿心莲内酯纳米混悬剂的制备工艺并进行初步评价,试验以二甲基亚砜为溶剂、水为反溶剂,采用反溶剂法制备穿心莲内酯纳米混悬剂(ANDRO-NS),以得率为指标,通过单因素试验和正交试验优化了ANDRO-NS的制备工艺,并进行验证试验,采用透射电镜、激光粒径仪对所制备的纳米混悬剂进行表征。结果显示:1%吐温-80混和0.05%泊洛沙姆为稳定剂,药物浓度为40 mg/mL,反溶剂和溶剂的体积比为20,搅拌速率为1400 r/min,搅拌时间为80 min,制得的ANDRO-NS平均粒径为568.51±13.74 nm,粒径合适,稳定性良好。试验表明,采用反溶剂沉淀法制备的ANDRO-NS工艺简单,值得进一步研究。     

蒲公英多糖纳米乳对蛋鸡生产性能及雏鸡免疫机能影响研究

蒲公英为菊科蒲公英属（Taraxacum mongolicum Hand-Mazz.）多年生草本植物perennial herb的带根全草,具有清热解毒、消肿散结、利尿通淋等功效。蒲公英中含有丰富的糖类,而多糖是生物体内普遍存在的一类生物大分子,具有许多重要的生物活性,也是多种内源性生物活性分子的组成成分,具有提高机体免疫力、抗菌、抗病毒、抗寄生虫、抗肿瘤、延缓衰老等一系列作用。本项研究旨在探讨蒲公英多糖纳米乳对蛋鸡生产性能和雏鸡免疫力的影响,寻找一种能够有效提高蛋鸡生产性能和免疫性能的新型制剂。纳米乳剂（Nanoemulsion,NE）是指乳滴的直径大小处在纳米尺度的一种特殊的乳剂,具有其他药物载体不可比拟的优点：物理稳定性好,可提高难溶性药物的溶解度、促进大分子水溶性药物在体内的吸收、提高药物生物利用度等。     

恩诺沙星注射混悬剂在猪体内的药物动力学用生物利用度

本试验是探讨恩诺沙星注射混悬剂肌注给药的药物动力学特征,同时进行恩诺沙星普通注射剂静注和肌注给药的药物动力学试验,目的在于比较注射混悬剂和普通注射剂的药动学特征,并考察混悬剂的生物利用度,对恩诺沙星注射混悬剂作出药物动力学评价,以了解混悬剂能否达到长效的作用,为临床应用制剂提供理论依据.     

地克珠利可溶性粉的工艺研究

提高难溶性药物溶解度的方法很多,降低药物粒径和采用环糊精包合是比较常用的方法,有操作简便、适用于大生产等优点。主要采用这两种技术提高了难溶性药物地克珠利的溶解度。     

药物几种制剂的生产

1液体制剂内服或外用液体制剂是指将固体或液体药物在一定条件下溶解或分散在水、醇、脂肪油或甘油中,有时加入添加剂以增加药物的溶解度、分散度,增加产品的稳定性或改进其不良气味。对于这类液体制剂的一般要求是,溶液应澄明,乳剂或混悬剂应保证其分散相小而均匀,有效成分的浓度应准确、稳定,     

紫苏油纳米乳中α-亚麻酸在家兔体内的药动学研究

<正>紫苏油是传统中药,近年来发现其在治疗心血管疾病、抗肿瘤方面亦有显著功效。由于紫苏油难溶于水,吸收差,生物利用度低,大大限制了其在临床上的应用和药效的发挥。生物利用度低主要由肝脏代谢及在水中的溶解度低引起,而纳米乳可提高难溶性药物的溶解度,从而提高生物利用度。本试验采用气相色谱法测定药物在体内的含量,研究紫苏油纳米乳在家兔体内的药动学,现将结果报道如下。1材料1.1试验动物     

纳米乳药物载体应用的研究进展

药物载体是指能够改变药物进入体内的方式和在体内的分布,控制药物的释放速率,并将药物输送到靶器官的物质。纳米乳作为新型药物载体,具有不可比拟的优点。纳米乳为各向同性的透明液体,热力学稳定,可过滤灭菌,易于保存;可作为油溶性药物和水难溶性药物的载体,使不溶或难溶性药物的溶解度显著提高,从而提高药物的生物利用度及机体的吸收速度;能够促进大分子水溶性药物在机体内的吸收,提高易酸败、易水解和易挥发药物的稳定性,也可作为缓释给药系统或靶向给药系统可使药物浓集在靶向器官,增强药物的疗效;乳滴粒径小且均匀,能提高包封药物的分散度,     

纳米混悬制剂在兽药中的研究进展

部分兽药原料药由于水溶性较差或渗透性较低，导致生物利用度低，不能发挥良好的疗效。将药物制成纳米混悬制剂，能够减小药物粒度，改善药物溶解度，增加药物溶出度，并改变药物在生物体内的药代动力学特征，有效提高生物利用度。另外，纳米混悬制剂具备制造方法简单、条件温和等优势，满足理想的兽药开发条件。本文就纳米混悬制剂的制备方法，及其在兽药应用领域给药途径进行了综述，为纳米混悬制剂在兽药领域的研制提供参考及借鉴。     

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。     

Drinking water as a medium for drugs

If drug treatment is necessary in large herd sizes, the administration with feed or drinking water is preferred. The use of the drinking water as a vehicle for drugs may be accompanied by several problems. An important condition for a successful medication is a good water solubility of the administered compound. The solubility is influenced by the quality of the used drinking water. The stability of the dissolved drug and incompatibilities with other water ingredients are additional limiting factors. The success of the treatment is influenced also by the taste of the medicated water which may cause a reduced water consumption. The use of tap water instead of spring water may be helpful to improve the efficacy of drug treatment via drinking water.     

包合技术增强抗菌药物抗菌疗效研究进展

细菌性疾病严重危害动物机体健康,影响畜牧养殖业经济利润。抗菌药物已诱导多种细菌产生耐药性,这在一定程度上降低了其治疗效果。然而,通过提高抗菌药物使用剂量以加强疗效不仅容易引起毒副作用,还易导致药物残留。因此,寻找新方案来提升传统抗菌药物的抗菌活性成为药物研究者工作重点。以传统抗菌药物作为客体分子,利用包合技术将其同价格低廉的环糊精等主体分子制成包合物,可改善药物理化性质及抗菌活性,显示出良好发展前景。包合物不仅能改善药物溶解性、稳定性,还兼具备缓释效果,可有效提高抗菌药物生物利用度。同时,其还能与细菌膜结合,协助抗菌药物穿越膜结构,最终提高药物抗菌效果并降低抗菌药物使用剂量。本文将从包合技术的发展历史、增强抗菌药物活性应用现状以及提高抗菌药物药效学机制三个方面进行总结,以期为兽药研究者提供有效的借鉴。     

Research Process on Design of Liposomes as Drug Delivery System and Its Application in the Field of Veterinary Medicine

As an excellent pharmaceutical carrier,liposomes exhibit characteristics of wide drug loading range,high efficiency and low toxicity.Besides increasing stability and solubility of loading drugs,liposomes can ascribe targeting and sustained release features to loading drugs.Meanwhile,it can improve bioavailability of loading drugs.Based on the above characteristics,liposomes is becoming hot spot of research and application.This article reviewed construction methods of liposomes based on structure,particle design and chosen of preparation method.Combined with application and demands of veterinary medicine,research progress on application of liposome in the field of veterinary medicine was submitted.It is expected that this article will provide reference for the development of new drug delivery systems used in the field of veterinary medicine.     

脂质体递药系统设计思路及其兽药应用研究进展

脂质体作为一种优良的药物载体,具有载药范围广、高效、低毒等特点,能增加包载药物的稳定性和溶解度,赋予药物靶向和缓释的递药特性,并能有效提高药物的生物利用度,是近年来多领域研究和应用的热点。作者从脂质体的结构、粒径设计及制备方法筛选层面总结脂质体的构建思路,结合兽药应用特点和用药需求归纳脂质体递药系统在兽药领域的研究进展,以期为新型递药系统在兽药领域的研发应用提供参考。     

兽用抗菌增效剂制剂的研究进展

抗菌增效剂属于人工合成的二氨基嘧啶类药物，此类药物与抗菌药物联合使用时会以特定的机制来增强抗菌药的药物活性。近年来，由于抗生素的广泛使用甚至滥用导致细菌耐药的问题日益显现，通过加入抗菌增效剂而研制出的新制剂可以提高抗菌药在动物体内的利用率、降低药物用量、增强药物疗效、降低兽药残留及减少细菌耐药性。文章分析了近年来甲氧苄啶、二甲氧苄啶和艾地普林与各类抗生素的联合使用制备的制剂产品，发现其对疾病的治疗效果普遍优于单独使用抗生素。同时，配合中药的使用对细菌耐药的问题有显著改善，为后期抗菌增效剂的研究打开新的局面。随着对兽药制剂的研究，其不再局限于简单的剂型，通过运用新技术、新材料研制出的制剂，针对不同的给药部位和给药途径可以对病患进行更精准的治疗，减少药物达到靶部位的时间，增加患病部位的药量，此思路可为后续的研发方向提供支持和参考。文章将对抗菌药-抗菌增效剂联用制剂的研发情况进行综述。     

Considerations for application of biopharmaceutics classification system in chicken: Exemplified by seven drugs classification

Biopharmaceutics Classification System (BCS) has gained broad acceptance in promoting the development of human drugs. To date, the applicability of existing human BCS criteria has not been evaluated in chickens. The objective of this study was to discuss the feasibility of BCS extrapolation between species and establish a preliminary chicken BCS by classifying seven veterinary commonly used drugs including metronidazole, amoxicillin, sulfamethoxazole, sulfadiazine, ciprofloxacin hydrochloride, doxycycline hydrochloride, and trimethoprim. Firstly, we finished the determination of physiological parameters affecting solubility in chickens, including body temperature, gastrointestinal pH, and the fluid volume in the gastrointestinal tract (GI), and the drug is considered highly soluble in chicken BCS when the highest dose strength is soluble in 20.40 ml (fed) or 6.73 ml (fasted) over the pH range of 1–8 at 41°C. Drug solubility classification was based on dose number calculation. Metronidazol and amoxicillin were classed differently under fed and fasted conditions. Secondly, we discussed the effect of ABC transporters (MDCK vs. MDCK-chAbcb1/Abcg2) and pH (5.5 vs. 7.4) on drug permeability and classification. The drug is classified as highly permeable when its permeability is equal to or greater than metoprolol tartrate. Though ABC transporters and pH significantly affected the permeability values of drugs (p < .05), the permeability classification of the drugs has not been changed except for sulfamethoxazole. This work highlights some of the significant challenges that would be encountered in order to develop a chicken BCS, this valuable information could serve as a helpful tool during chicken drugs development and to minimize the potential risks when developing formulations.     

Interaction of host physiology and efficacy of antiparasitic drugs

Antiparasitic drugs must be conducted to the parasite by the host and are therefore subject to physiological and biochemical processes in the host. Usually the efficacy of an antiparasitic drug will depend on a toxic concentration being presented to the parasite for sufficient time to lead to irreversible damage. Because many drugs are, in part, absorbed and transported to the site of the parasite by the circulatory system the area under the plasma concentration curve (AUC) may reflect availability of drug to the parasite and likely efficacy. A number of host physiological factors affect the AUC. Many anthelmintics are given orally as solids. Some absorption occurs in the rumen of ruminants, but many heterocyclic compounds such as the benzimidazoles require the low pH of the abomasum or gastric stomach to render them soluble. Certain disease states, including gastrointestinal parasitism, can cause the gastric pH to rise. This may in turn reduce solubility and absorption with resultant faster rate of excretion, particularly when accompanied by diarrhoea, and a reduced AUC. Once the anthelmintic has been absorbed, after oral or systemic administration, it is usually rapidly transported to the liver. The liver and adipose tissue may store the drug, releasing it over a period to produce a sustained effect as occurs with ivermectin, or it may rapidly metabolise it. A few anthelmintics, such as febantel, probably need to be metabolised in order to become active. However, more frequently the liver is involved in oxidation or reduction, followed by conjugation with sulfate, glucuronide or glutathione to render the drug more polar, to increase its molecular weight, inactivate it and facilitate its excretion. The rate of metabolism has been found to vary considerably between species and thus different dose rates and treatment are often required to achieve adequate antiparasite activity, with species such as deer, cattle and probably goats metabolising some anthelmintics faster than sheep. Some interesting possibilities for altering the absorption and metabolism of anthelmintics by the host may allow improved efficacy and reliability of antiparasite activity without necessarily increasing the dose rate of anthelmintic.     

动物抗寄生虫药物作用机理研究进展

动物抗寄生虫药物主要用于防制动物寄生虫病,是保障畜牧业健康发展和公共卫生安全的有效手段。抗寄生虫药物的药效建立在药物分子与寄生虫或动物机体不同靶组织、靶细胞间相互作用的基础上。由于抗寄生虫药物种类多样,抗寄生虫机理复杂。随着新抗寄生虫药物的开发和科学研究的深入,尤其是化学合成和生物制药技术的发展,抗寄生虫药物的品种和数量都在不断的增加,新的药物结构和作用靶标不断发现,作用机理研究也不断深入。作者主要对抗寄生虫药物的作用机理研究进展进行综述。