| Meloxicam is a enol amides new nonsteroidal anti-inflammatory drugs,with antipyretic,analgesic and anti-inflammatory effect,and has a high selectivity and has a long half-time and low side effects.At present,meloxicam tablets,injections and other forms have been reported,but meloxicam soluble powder has not yet been reported at home and abroad.This subject mainly explores the preparation of meloxicam soluble powder,its stability and pharmacokinetics in broilers to provide the basis for the application of this preparation in the prevention and treatment of chicken diseases.1.Preparation of meloxicam soluble powder: meloxicam content was determined at suitable wavelength(362 nm)by UV spectrophotometric rapid scanning and standard curve was drawed(A=0.0278C+0.0593,R2=0.982).Best formulation composition was as follows: meloxicam 0.4g,organic complex solubilizer A 1%,inorganic complex solubilizer 4%,polymer complex solubilizer 5%,adding lactose to 100 g.by crushing,sieving,mixing,dosage,packaging and quality inspection processes,meloxicam soluble powder was prepared successfully.2.HPLC method was used to determine meloxicam concentration in soluble powder and to prepare standard curve.The results showed that meloxicam has a good linear relationship in the concentration range from 0 to 101.7μg/ml.RSD of within-day precision test was 0.08%.Recovery rates were above 95%,the content of meloxicam was from 103% to 106%,RSD 0.067%.This method has good repeatability and high recovery rate.Samples were measured at room temperature for several times during 24 h,the RSD was 0.067%,which suggesting that the samples was quite stable in 24 h and the loss of meloxicam content was less than 2% within the 6months accelerated test(high temperature(30±2)℃and high humidity RH(65±5)%).Therefore,Meloxicam soluble powder has good stability under high temperature and high humidity conditions,and meloxicam is not easy to be degraded during the storage process.3.The pharmacokinetic experiment of meloxicam in chickens:healthy and uniform weight broilers at 43 days-age were randomly divided into three groups.The first and second group were orally administrated with a Meloxicam soluble powder at the dose of 0.5 and 1mg/kg body wight,respectively.The Third group was intravenously injected of a Meloxicam soluble powder at the dose of 1mg/kg body wight.The blood samples were obtained from the wing vein at different time points in 96 h.After treating blood sample,the drug content in the blood was detected by HPLC to calculate the pharmacokinetic parameters.The test results of the first and second group showed: pharmacokinetic parameters of AUC is 5.25 h·μg/ml and 10.96 h·μg/ml.Cmax is 1.81mg/L and 0.47 mg/L.thus,Cmax and AUC were dose-dependent.With the increase of dose,Cmax,AUC value also increased,the higher the dose,the more the body’s absorption of drugs.Tmax of the two groups is 1.2 h and 2.1 h.T1/2 is 7.33 h and 4.66 h.The test results of the second and third group showed: the elimination half-life was 7.33 h and 4.66 h,which showing the slow elimination.AUC is 10.96 h·μg/ml and 17.36 h·μg/ml,so oral bioavailability was 63.13%. |
PDF Full Text Request