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61.
The aim of this study was to determine the pharmacokinetics and prostaglandin E2 (PGE2) synthesis inhibiting effects of intravenous (IV) and transdermal (TD) flunixin meglumine in eight adult female Boer goats. A dose of 2.2 mg/kg was administered intravenously (IV) and 3.3 mg/kg administered TD using a cross‐over design. Plasma flunixin concentrations were measured by LC‐MS/MS. Prostaglandin E2 concentrations were determined using a commercially available ELISA. Pharmacokinetic (PK) analysis was performed using noncompartmental methods. Plasma PGE2 concentrations decreased after flunixin meglumine for both routes of administration. Mean λz‐HL after IV administration was 6.032 hr (range 4.735–9.244 hr) resulting from a mean Vz of 584.1 ml/kg (range, 357.1–1,092 ml/kg) and plasma clearance of 67.11 ml kg?1 hr?1 (range, 45.57–82.35 ml kg?1 hr?1). The mean Cmax, Tmax, and λz‐HL for flunixin following TD administration was 0.134 μg/ml (range, 0.050–0.188 μg/ml), 11.41 hr (range, 6.00–36.00 hr), and 43.12 hr (15.98–62.49 hr), respectively. The mean bioavailability for TD flunixin was calculated as 24.76%. The mean 80% inhibitory concentration (IC80) of PGE2 by flunixin meglumine was 0.28 μg/ml (range, 0.08–0.69 μg/ml) and was only achieved with IV formulation of flunixin in this study. The PK results support clinical studies to examine the efficacy of TD flunixin in goats. Determining the systemic effects of flunixin‐mediated PGE2 suppression in goats is also warranted.  相似文献   
62.
63.

Objective

To describe adverse reactions and measure plasma fentanyl concentrations in calves following administration of a fentanyl transdermal patch (FTP).

Study design

Prospective, experimental clinical study.

Animals

Six female Holstein calves and one male Angus calf. Four calves were healthy experimental animals and three calves were clinical patients.

Methods

Plasma fentanyl concentrations were measured in blood collected from a jugular vein. FTP 2 μg kg–1 hour–1 and 1 μg kg–1 hour–1 was applied to four and three calves, respectively. Heart rate, respiratory rate, temperature and ataxia were recorded at the same times as blood collection (0, 2, 4, 6, 12, 24, 36, 48, 60, 72, 84 and 96 hours). Substance P concentrations were determined via radioimmunoassay for two calves.

Results

After the FTP (2 μg kg–1 hour–1) application, two calves developed tachycardia, hyperthermia, excitement and ataxia within 6 hours; no adverse effect was observed in the other two calves. The three calves administered FTP (1 μg kg–1 hour–1) exhibited tachycardia and excitement, and the FTP were removed at 4 hours. Naloxone was administered to two calves before the adverse clinical signs ceased, while adverse events in the other three calves resolved within 2 hours of FTP removal. Variables returned to previous baseline values by 2–4 hours after FTP removal. Maximum plasma fentanyl concentrations were variable among calves (0.726–6.923 ng mL–1). Substance P concentrations measured in two calves were not consistently depressed during FTP application. Fentanyl concentrations at 4 and 6 hours were significantly associated with the appearance of adverse effects.

Conclusions and clinical relevance

FTP (1–2 μg kg–1 hour–1) administered to calves may result in adverse behavioral and cardiovascular effects. Patch removal and treatment with an opioid antagonist may resolve these adverse effects. Additional research is needed to determine optimal FTP dosing for cattle.  相似文献   
64.
将恩诺沙星与皮肤渗透促进剂氮酮按药剂学方法配制的透皮吸收搽剂 ,经皮给药防治哺乳仔猪肠型大肠杆菌病 ,收到了与恩诺沙星注射剂、口服剂同样的效果 .表明透皮吸收制剂在兽医临床上具有广阔的应用前景 .  相似文献   
65.
洛美沙星(Lomefloxacin)透皮吸收搽剂中氮酮的最佳浓度   总被引:4,自引:0,他引:4  
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%。  相似文献   
66.
The topical administration of the compound Chinese herbal medicine transdermal preparation has been widely used in treating the mastitis of cows. In order to understand the metabolic process, four cows suffering from clinical mastitis were selected for the pharmacokinetic study. The transdermal preparation was applied to the diseased part of breast. Then the plasma and milk samples were collected respectively at 0, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, and 36 h, The concentrations of baicalin and phillyrin in plasma and milk were determined by HPLC and the data of time-concentrations were analyzed by the pharmacokinetic software. The results showed that two ingredients in the plasma were not detectable, but they in the milk had linear relationship with the time. The peak concentration of baicalin [(2.84 ±0.15)μg mL^-1] appeared at (4.93 ± 0.35) h, AUC0.1OQ was (27.32 ± 7.91) mg L^-1 h^-1, and the mean retention time was (28.31 ±0.49) h. The peak concentration of phillyrin [(0.49 ± 0.41) μg mL^-1] achieved at (3.68 ± 3.14) h, AUC0-LOQ was (4.10± 0.31) mg L^-1 h^-1, and the mean retention time was (14.52 ± 0.02) h. These suggested that two ingredients had slow absorbing speed and high absorbing degree. They could not be eliminated in a short time, thus exerted the topical curative effect.  相似文献   
67.
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.  相似文献   
68.
The objective of this study was to measure and compare the serum concentrations of dexamethasone after oral and transdermal administration using pluronic lecithin organogel in six healthy cats. The study was designed as a crossover, in which the cats were randomly assigned to two groups. The cats received a single dose (0.05 mg kg(-1)) of dexamethasone either orally or transdermally on the inner pinna. Blood samples were taken at 0, 5, 15, 30, 60, 90 and 120 min, and 3, 4, 6, 8, 12 and 24, 48 and 72 h post dexamethasone administration. A mean peak serum concentration of 30.1 ng mL(-1) was detected 15 min after oral administration. Serum concentrations were below detection limits by 24 h. In contrast, there was no significant increase in serum concentrations of dexamethasone after transdermal administration. In cats, transdermal administration of a single dose of dexamethasone did not result in significant serum concentrations compared to oral administration.  相似文献   
69.
70.
OBJECTIVE: To measure concentrations of lidocaine serum after application of two 5% patches on horses. STUDY DESIGN: Prospective experimental trial ANIMALS: Six client-owned, systemically healthy horses. METHODS: The hair was clipped on the medial aspect above the carpus of both fore limbs and 2 patches of 5% lidocaine were applied within 30 minutes of jugular catheter placement and the area was then bandaged. Venous blood was drawn from a jugular vein catheter that was inserted using lidocaine as a local block. Samples were drawn immediately before and at 2, 4, 6, 8, and 12 hours after patch application. The presence of lidocaine in serum was determined using an ELISA test. RESULTS: Lidocaine was detected in the serum of three horses at 0 hours immediately following the local block for catheter placement. Lidocaine was not detected at any other time from 2 to 12 hours. There was mild erythema at the site of patch placement at 12 hours in one horse but this resolved within 1 hour of patch removal. There were no other apparent adverse effects from the patches on any other horse. CONCLUSION: Five percent lidocaine patches applied proximally to the carpus did not result in detectable systemic concentrations of lidocaine. CLINICAL RELEVANCE: Any analgesic effects that might be produced by application of 5% lidocaine patches on horses will not be due to systemic absorption of the drug.  相似文献   
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