抛物线拟合法研究氮酮(Azone)促进左旋咪唑透皮吸收的最佳浓度

采用静态小室装置,以左旋咪唑(LMS)为模型药物,用离子对HPLC法测定LMS浓度.采用抛物线拟合法建立不同时间下氮酮(Azone)浓度对LMS透皮吸收率的数学模型.用此模型准确求得氮酮对LMS透皮吸收的最佳浓度是3.05±0.57%,同时证明氮酮对LMS有显著的透皮吸收作用.     

左旋咪唑擦剂对猪肺丝虫病的疗效观察

左旋咪唑擦剂对猪肺丝虫病有很好治疗效果,而且方法比较简便。对35头自然感染猪治疗结果表明,虫卵消失率和驱虫率达100％,同时对猪蛔虫和钩虫也有良妤驱虫效果,可作为猪场和养猪农户驱除猪肺内和胃肠道内线虫的理想药物。左旋眯唑擦剂对猪蛔虫、钩虫有良好驱虫效果,但对猪肺丝虫(后圆线虫)的驱虫效果尚不清楚。我国许多省区猪肺丝虫病流行十分严重,个别地区感染率高达70～80％以上,影响养猪业的发展。以往治疗本病主要通过灌服或注射驱虫药,给驱治工作带来困难。左旋咪唑擦剂只需在猪耳背部皮肤上涂抹适量药物即可奏效, 群众易于掌握使用。现将结果报道如下。     

复方痢菌净搽剂的制备及初步安全性稳定性考察

为了研制以痢菌净和左旋咪唑为主药的复方透皮制剂,试验采用正交设计法,以痢菌净和左旋咪唑为模型药物,通过离体鼠皮体外渗透试验,以透皮速率常数(J)为指标筛选处方组分.并通过验证试验,确定复方痢菌净透皮剂的处方组成主要为:4％痢菌净、7.5％盐酸左旋咪唑、2.5％氮酮、14％苯甲醇、10％丙二醇、40％乙醇.根据优化处方制备的复方痢菌净搽剂稳定性好,无皮肤刺激性,含量测定方法简便,质量控制方法可靠.     

呋喃妥因透皮吸收作用的研究

采用简单小室法，初步研究了呋喃妥因软膏体外透皮吸收情况。结果表明，０．５％的氨酮对呋喃肥因无透皮促进作用，含２％氮酮的呋喃肥因软膏在各时间下的透皮吸收量比不含氮酮者均提高１倍以上；含２％与１％呋喃妥因的软膏之间，含两种透皮促进剂与一种透皮促进剂的软膏之间，呋喃妥因的透皮吸收在数量统计学上无显著差异。     

磷酸左旋咪唑对猪颚口线虫的驱虫试验

本文用磷酸左旋咪唑对自然感染刚刺颚口线虫的猪进行了驱虫试验．结果表明：按每kg体重4～6mg剂量一次颈侧肌注5％的磷酸左旋咪唑注射液，驱虫率和驱净率均达100％，效果显著，并对猪体没有不良临床副反应．     

丙硫苯咪唑透皮剂对小鼠蛲虫的驱除效果

用丙硫苯咪唑透皮剂以不同剂量擦拭自然感染晓虫等肠道寄生虫的小鼠的耳部和尾部。结果２０ｍｇ／ｋｇ剂量组的驱虫效果与口服同样剂量的驱虫效果基本相同。用药３天驱虫率达到１００％，虫卵减少率达９０％以上。     

联合用药驱除山羊肝片吸虫、莫尼茨绦虫和捻转血矛线虫试验

应用两种药物驱除山羊自然感染肝片吸虫、莫尼茨绦虫和捻转血矛线虫的试验,结果表明：硫双二氯酚和左旋咪唑联合用药对肝片吸虫和捻转血矛线虫的粗计驱虫率和驱净率均为100％,对莫尼茨绦虫分别为94．2％和80％;硝氯酚和左旋咪唑联合用药对捻转血矛线虫的粗计驱虫率和驱净率均为100％,对肝片吸虫分别为81．0％和60．0％,对莫尼茨绦虫无效;吡喹酮和左旋咪唑联合用药对捻转血矛线虫的粗计驱虫率和驱净率均为100％,对莫尼茨绦虫分别为94．1％和80．0％,对肝片吸虫无效。建议在山羊生产中采用硫酸二氯酚和左旋咪唑联合用药驱除肝片吸虫、莫尼茨绦虫和捻转血矛线虫可获得最佳驱虫效果。     

洛美沙星（Lomefloxacin）透皮吸收搽剂中氮酮的最佳浓度

应用洛美沙星搽剂作为模型药物，采用离体鼠皮，研究了氮酮（Azone)在0%，1%，3%，5%，7%浓度时对洛美沙星透皮吸收的影响。试验结果表明，氮酮在洛美沙星透皮吸收搽剂中最佳浓度为4.01%。     

诺氟沙星软膏的透皮吸收试验

不同浓度氮酮（Ａｚｏｎｅ）及不同浓度Ｎ－甲基－２－砒咯烷酮（ＮＰ）对诺氟沙星（Ｎｏｒ）体外透皮吸收试验结果表明，１％－５％（质量分数）的Ａｚｏｎｅ对Ｎｏｒ透皮吸收均有一定促进作用，但在统计学上无显著差异，Ｎｏｒ累积透皮释药量与时间呈良好的线性关系，符合零级动力学过程；ＮＰ对Ｎｏｒ无透皮促渗透作用。     

松萝酸体外透皮试验研究

采用简化体外透皮释放测定装置 ,初步研究了松萝酸在透皮促渗剂作用下的透皮吸收作用。结果表明单一的透皮促进剂氮酮 ( Azone)及以氮酮为主的复合透皮促进剂 ( 2 % Azone 2 0 %丙二醇 ,2 % Azone 2 0 %二甲基亚砜 ,2 % Azone 2 0 %尿素 )对松萝酸的透皮吸收均无促进作用     

中药软膏剂体外透皮效果研究

为评价复方中药软膏剂中不同浓度的透皮剂药物氮酮对马属动物的透皮效果,首先利用中药复方水提醇沉浓缩液制备中药软膏剂,然后在软膏剂中分别加入2%、4%、5.5%、7%的透皮剂药物氮酮,以软膏剂中的淫羊藿苷成分作为标记物,利用酶标仪法测定经智能药物透皮仪处理后的马皮肤透过液中的标记物含量。结果表明,在中药软膏剂中加入5.5%的氮酮作为促渗剂,所获得的药物渗透效果最佳。该研究为马属动物中药软膏剂中透皮剂药物的选择提供了理论依据,也为复方中药透皮给药系统的研究提供了更为安全、有效、稳定的给药途径。     

薄荷醇和氮酮对甲硝唑在犬中体外透皮吸收的影响

研究不同的溶液载体（PBS,5％薄荷醇和5％氮酮）和不同部位的皮肤对甲硝唑在犬中体外透皮吸收和皮内摄取的影响。取下北京犬颈部、胸部以及腹部皮肤,-20℃保存。使用时,皮肤解冻固定在改良Franz透皮扩散仪上,保持恒速（200±1）r／min,恒温（35±0．5）℃。在扩散池中的皮肤角质层上加入2mL溶液载体（含甲硝唑58．4μmol）,以20％乙醇为溶剂溶解薄荷醇和氮酮,在预定时间点取样1mL,采用HPLC方法测定各接受液中的药物量和皮肤中摄取的药物量。结果显示,与PBS相比,薄荷醇和氮酮能增加所有部位甲硝唑的透皮吸收量和皮内摄取量（P〈0．05）。同一溶液载体在不同部位的渗透性存在差异,腹部〉颈部〉胸部,不同部位的皮内摄取量也存在差异,颈部〉胸部〉腹部。说明甲硝唑在不同溶液载体和不同部位皮肤的渗透性存在差异。     

Dermal necrosis caused by Pasteurella multocida infection in turkeys

Severe dermal necrosis caused by Pasteurella multocida Serotype 1 was diagnosed in three dressed turkey carcasses and two live turkeys from a commercial flock. The dressed carcasses were among several condemned at a processing plant. The isolate, P. multocida Serotype 1, produced progressive dermal necrosis when experimentally inoculated into injured skin of turkeys. The organism was reisolated from the dermal lesions. The turkey houses were found to be infested by mice; the skin injury and infection with P. multocida probably originated from mouse bites.     

不同药物对放牧山羊捻转血矛线虫驱虫效果比较试验

为了筛选山羊捻转血矛线虫的理想驱虫药物,对8组检出有捻转血矛线虫感染的山羊群分别采用不同剂量的阿苯达唑、盐酸左旋咪唑、伊维菌素以及阿苯达唑-伊维菌素预混剂进行驱虫效果对比试验。结果盐酸左旋咪唑、伊维菌素以及阿苯达唑-伊维菌素预混剂对山羊捻转血矛线虫驱虫后,虫卵减少率均达95%以上,而阿苯达唑驱虫后的虫卵减少率低于95%。表明左旋咪唑、伊维菌素以及阿苯达唑-伊维菌素预混剂对山羊捻转血矛线虫的驱虫效果较好,而阿苯达唑有一定的抗药性。     

促渗剂对鹿茸多肽透皮吸收的影响及鹿茸多肽免疫活性检测

通过探讨不同质量浓度促渗剂月桂氮卓酮和冰片对鹿茸多肽透皮吸收的影响,优化出鹿茸多肽的给药方式,即通过口腔黏膜服用,为鹿茸运用于创伤、烧伤和美容提供依据。通过脾细胞增殖试验,检测鹿茸多肽的免疫活性。结果表明：（1）SDS-PAGE显示鹿茸酸粗提取物中含有不等量的蛋白质和多肽等,且多为大分子量多肽,但醇提多肽多为10000左右的某些小分子量多肽。（2）含5％月桂氮卓酮的醇提鹿茸多肽和含0．12％冰片的醇提鹿茸多肽比只含醇提鹿茸多肽溶液的累积透皮透过量多,说明促渗剂月桂氮卓酮和冰片能明显的增加醇提鹿茸多肽的透皮扩散速度和扩散的总量,而且0．12％冰片的促渗效率比5％月桂氮卓酮的促渗效果要高。（3）鹿茸多肽具有促进脾细胞增殖的活性,并存在剂量依赖性：醇提鹿茸多肽质量浓度从10mg／L上升到40mg／L时,对促进脾细胞增殖呈上升趋势,当质量浓度超过40mg／L时,增殖率增加不显著。     

In vitro dermal disposition of abamectin (avermectin B(1)) in livestock

Many avermectins are approved for topical application in domestic animals. However, extralabel use may result in significant dermal absorption and consequently the potential for adverse effects or violative residues. The primary aim of this study was to assess dermal disposition of abamectin in vitro in bovine, caprine, ovine, and porcine skin dosed in 100% isopropanol, commercial alcohol-based (Ivomec), or oil-based (Eprinex) formulations. Skin sections were perfused in a flow-through diffusion cell system for 8 h, and the disposition of radiolabel abamectin was determined from perfusate and skin samples. Abamectin absorption ranged from 0.09% to 0.20% dose and there were no significant differences between formulations in each species. Isopropanol significantly increased skin deposition in all species when compared to the oil formulation. Absorption was significantly greater in bovine skin than in porcine skin for the isopropanol-containing formulations, but there were no significant species differences for the oil formulation. While significant levels (11.69-50.23% dose) remained on the skin surface, the highest levels deposited in viable skin were observed in caprine skin (28.09% dose) and the lowest levels were in porcine skin (1.50% dose) which could lead to systemic absorption. In summary, these 8-h experiments demonstrated that the alcohol-based formulations compared to oil-based formulations enhanced abamectin absorption and skin deposition in several animal species, and this effect is more likely to be observed in ruminant species than in porcine species.     

In vitro development and characterization of canine epidermis on a porcine acellular dermal matrix

The aim of this study was to develop and to characterize a canine skin epidermal model able to form a proper epidermis on a porcine acellular dermal matrix (PADM). In addition, the role of fibroblasts in skin barrier formation was studied by incorporating or omitting canine dermal fibroblasts in the PADM. Canine epidermal composites were developed by seeding keratinocytes onto the surface of PADM that were previously seeded or non-seeded with dermal fibroblasts. After 14days of culture under air-exposed conditions and in a special growth medium, skin composites were histologically processed and immunohistochemically characterized to determine the expression of cytokeratins and of vimentin and the presence of basement membrane. In all composites, keratinocytes underwent differentiation to a multilayer epidermis with 5-7 viable cell layers. The stratum basalis, stratum spinosum, stratum granulosum and stratum corneum were identified. The expression of cytokeratins was similar to that described in healthy canine epidermis. Laminin and collagen IV immunostaining revealed a homogeneous layer in the epidermal-dermal junction only when the matrix had been seeded by canine dermal fibroblasts. The model may become a simple, useful and cost-effective tool to investigate the biology and pathology of canine epidermis and could partially replace animal testing in several areas of dermatological research.     

In vitro degradation of equine keratin by dermatophytes and other keratinophilic fungi

Keratinolytic properties of two dermatophytes (Microsporum gypseum, Trichophyton mentagrophytes) and three moulds (Scopulariopsis brevicaulis, Alternaria alternata, Geotrichum candidum) isolated from diseased equine hooves were examined to improve the understanding of pathogenic mechanisms leading to equine onychomycosis. Equine hoof horn material and skin, as well as hoof keratin and dermal keratin extracted from corresponding tissues, were used as sole carbon and nitrogen sources in five test tubes for each fungus. Within 18 days, supernatants of all tubes were repeatedly examined for keratinolytic activity by SDS-PAGE and Western blot analysis. In addition, fungal growth rates were determined to identify the preferred tissue of the individual fungi. Among the fungi examined, M. gypseum was the most keratinolytic species, followed by T. mentagrophytes and S. brevicaulis. In the concentration applied, the moulds A. alternata and G. candidum showed minimal keratinolytic activity. With respect to growth rates, M. gypseum favoured hoof horn material, S. brevicaulis and G. candidum preferred skin as a keratin source, whereas for the other two fungi no clear preference was detectable.     

Evaluation of the dermal effects of cast padding in coaptation casts on dogs.

Three configurations of cast padding and no cast padding were evaluated for their effects on skin in dogs. Padding was placed over bony prominences, between bony prominences, and over both areas for full-length padding under short-limb walking casts applied to 1 pelvic limb of Greyhounds. Evaluations were performed by pressure measurement over the calcaneal tuberosity, measurement of skin thromboxane B2 (TxB2) concentrations in skin over bony prominences, and measurement of plasma TxB2 concentrations. Pressure studies were performed to evaluate cutaneous pressures related to no cast padding and various configurations of cast padding. Concentrations of TxB2 in the skin were determined to evaluate the skin inflammatory effects of no padding and the padding configurations, and TxB2 concentrations in the plasma were analyzed to ascertain whether they could be used to predict impending dermal pressure lesions. Flexion of casted limbs revealed the greatest pressure over the calcaneal tuberosity with full-length cast padding. This was followed in decreasing order by no cast padding, padding over the prominences, and padding between the prominences. Compared with all other bony prominences and padding configurations, TxB2 skin concentrations were significantly higher over the calcaneal tuberosity when no padding was used and over the lateral base of metatarsal V when padding was placed between the prominences. Over the calcaneal tuberosity, this was attributed to the sharpness of the prominence and its potential for movement. This high TxB2 concentration corresponded to the high pressure found in the pressure studies. Over the lateral base of metatarsal V, the increase in TxB2 concentration was related to the mass of the prominence and the tendency for localized padding to settle around the area.(ABSTRACT TRUNCATED AT 250 WORDS)     

Pathogenesis of psoroptic scabies in Hereford heifer calves

Hereford heifer calves were experimentally infested with Psoroptes ovis. Histologic examination of skin specimens was conducted at weekly intervals before and after treatment with ivermectin on postinfestation week 7. Electron microscopy revealed numerous degranulating mast cells in the skin of infested but not in control calves. many active, as well as degenerate, neutrophils were in the scab on infested calves. Microscopic epidermal ulcers developed on infested calves when live mites were present but not after treatment. Numbers of dermal neutrophils and plasma cells decreased and numbers of circulating neutrophils increased 1 week after treatment. Numbers of dermal eosinophils and mast cells in calves with eosinophilia increased for several weeks after treatment. Statistical analysis indicated significant correlations (P less than 0.05) among numbers of dermal inflammatory cells, hemogram values, and changes in dermal thickness. Seemingly, mite-induced epidermal damage was the key pathogenic event in psoroptic scabies in calves. Mast cell degranulation contributed to the pathogenesis of the dermatitis, and neutropenia was caused by sustained, poorly compensated efflux of neutrophils into the scab through mite-induced breaks in the epidermis.