Veterinary tiamulin suspension injection and preparation method thereof

Our pharmacokinetics department offers the clients a broad spectrum of high quality of services in the areas of in vitro ADME, in vivo pharmacokinetics studies and bioanalysis services, ranging from small molecules to large molecules, such as protein and antibody. The animal species involved in our services are non-human primate, canine, mice, rat, rabbit and hamster. Meanwhile, non-human primate experimental platform and isotope platform for protein/antibody are certified by the Shanghai Government.Email:marketing@medicilon.com.cn Web:www.medicilon.com

The invention relates to the technical field of medicine, and discloses a veterinary tiamulin suspension injection and preparation method thereof. The veterinary tiamulin suspension injection comprises the following compositions in percents by weight: 20% of tiamulin, 6-10% of a suspending agent Arabic gum, 0.2-1% of a suspending agent polyvinyl pyrrolidone, 0.1-0.3% of a surfactant, 0.3-0.9% of a flocculating agent, other auxiliary agent and the balance water. The veterinary tiamulin suspension injection of the invention is good in stability, rapid in absorption, high in bioavailability and substantial in effect, and helps to provide a new efficient dosage form for veterinary tiamulin.

Tiamulin (tiamulin / thiamutin / dynamutiIin), also known as Tai Miao Ling, Tai Miao neomycin, Mycoplasma net, Thai animal husbandry neomycin, sulfur Kremlin, is higher fungi Basidiomycetes Pleurotus Pleurotus mutilus fermentation obtained after Pleuromutilin then hydrogenated fumarate by chemical synthesis, is an antibiotic for livestock and poultry. The drug is bacteriostatic antibiotic, antibacterial mechanism of the Department of bacterial 50S ribosomal subunit and inhibit bacterial protein synthesis, a variety of Gram-positive bacteria, mycoplasma and certain spirochetes have good antibacterial activity, especially for mycoplasma special effects, and to maintain a high concentration in the respiratory tract mycoplasma breeding is by far Mycoplasma gallisepticum poultry is considered to be the most effective antibiotic, and recommend the drug of choice for the control of animal mycoplasma infection.

Currently, tiamulin application forms on our limited conventional soluble powders and premixes, traditional forms of application has allowed dose, the presence of first-pass effect, the bioavailability and low defects, and tiamulin streptozotocin itself animal respiratory irritant strong, as premixed spices administration can cause severe coughing animals, have significant side effects, dosage forms for veterinary applications Tiamulin has a decisive role.

development for clinical application tiamulin injectable formulation, well overcome the inherent disadvantages of conventional formulations, while rich forms veterinary clinical use of tiamulin, clinical medicine and veterinary development has a great significance.

The present embodiment, after the determination of the date of suspension of the sample is placed (4500 ± 500) at LX bright light conditions, in the first 10 days of sampling, was determined by HPLC, while observing the preparation color is white, no significant changes in sedimentation volume ratio of 90.6% weight dispersion and particle fineness good undetermined degradation

The product, pH value of 3.80. Experiments show that the use of bright light test and 6 months accelerated test for this case tiamulin injection suspensions stability studies implemented tiamulin content phase high performance liquid chromatography. The test results show that the relative content, Appearance, grain fineness and PH value and other indicators of the present embodiment embodiment of the samples showed no change, indicating that the light of the present embodiment example preparation, thermal stability, in line with the provisions of suspension of pharmacy requirements .

In the pharmacokinetic study, the selection of seven healthy pigs, three-period crossover design by intramuscular injection in the present embodiment example, a dose of lOmg ^ kg-1 bw, bioavailability was 83.23% ± 13.32% Table Alpha tiamulin in pigs rapidly absorbed, widely distributed, peak quickly and eliminate faster.

The present embodiment, after the determination of the date of suspension of the sample is placed (4500 ± 500) at LX bright light conditions, in the first 10 days of sampling, was determined by HPLC, while observing the preparation color is white, no significant changes in sedimentation volume ratio of 90.2%, weight dispersion and particle fineness good undetermined degradation

The product, pH value of 3.79. Experiments show that the use of bright light test and 6 months accelerated test for this case tiamulin injection suspensions stability studies implemented tiamulin content phase high performance liquid chromatography. The test results show that the relative content, Appearance, grain fineness and PH value and other indicators of the present embodiment embodiment of the samples showed no change, indicating that the light of the present embodiment example preparation, thermal stability, in line with the provisions of suspension of pharmacy requirements .

In the pharmacokinetic study, the selection of seven healthy pigs, three-period crossover design by intramuscular injection in the present embodiment example, a dose of lOmg ^ kg-1 bw, bioavailability was 82.53% ± 13.88% Table Alpha tiamulin in pigs rapidly absorbed, widely distributed, peak quickly and eliminate faster.