Preparation And Antibacterial Effects Of Valnemulin Hydrochloride Formulations

In this article we have prepared VA ointment, suppository and glycerogelatin granules, and antibacterial effects were studied. In foreign countries VA has been used for the prevention and treatment of gram-positive bacteria and mycoplasma caused by various animal diseases in veterinary clinic, and VA has many characteristics including broad spectrum antimicrobial, antibacterial activity is relatively strong, half-life is very short, first-pass effect is significant, and the plasma concentration was affect by administration methods. We prepared ointments, glycero gelatin bolts and granules of VA, and studied its antibacterial effect.1. Preparation of glycerogelatin suppository and study on the effect of treatment for bacterial vaginosis1.1Preparation of glycerogelatin suppositoryWith PEG and glycerogelatin water-soluble matrix, oleaginous matrix is mainly semi-synthetic fatty glyceride matrix. Use the dissolution rate, melt time of suppositories as select standards to select the type and amount of suppositories. The results showed that the stability of the glycerogelatin suppository is very good.1.2Control the quality of Valnemulin hydrochloride vaginal suppositoryRefer to "Chinese Veterinary Pharmacopoeia" inspect suppositories appearance, weight differences, melt time and the dissolution test, and the result shows that the suppositories are in line with "Chinese Veterinary Pharmacopoeia" requirements, and have potent stability.1.3Study on the treatment of Valnemulin hydrochloride vaginal suppository against g S.aureusAdministering in rats with the way of single and multiple vaginal and conducteing irritation test, using Staphylococcus aureus infection of the vagina of rats,and then use valnemulin hydrochloride suppository to treatment and to evaluate its efficacy. The results show that there is no irritant for the rats; The cure ration of low,medium and high (50,100,150mg/Kg) dose of valnemulin hydrochloride vaginal suppository were60%,100%,100%, compareing with ornidazole (100mg/Kg), with fairly low doses, there was no significant difference (P>0.05), but the dose-effect relationship is obvious.2. Study on the prepartion and antibacterial effect of Valnemulin hydrochloride OintmentsTwo kinds of Valnemulin hydrochloride ointment, W/O and O/W, was prepared by emulsification method, then, the percutaneous permeability ration was determined by HPLC. Result shows that percutaneous penetration rate of W/O ointment was30%±0.42%after10hours, while O/W ointment was18.45%±0.69%after10hours. We can see that the percutaneous penetration rate of W/O ointment is better than O/W ointment, therefore, it had potent antibacterial activity, and two kinds of ointment showed good stability.3. Preparation and antibacterial effect of Valnemulin hydrochloride granules3.1Study on the preparation of VA granulesVA granules was prepared using wet granulation granules, use formability, moisture absorption and melting of the particles as index, screening type and amount of accessories. The results showed that the quality of prescription granules in compliance "Chinese Veterinary Pharmacopoeia" requirement and the process optimal prescription is reasonable and feasible.3.2Control the quality of VA granules VA granules was prepared using wet granulation granules and using UV spectrophotometry determination the content of VA granules, the results showed that determination VA granules with UV, the method is simple, reliable, and reproducible. Appearance, granularity, dry agravity and nature of dissolve were fitting to the request.3.3Study on the treatment of VA granules against the E.coli model of diarrhea miceChoose mice as experimental animals, with pathogenic E. coli infection in mice by intraperitoneal injection to establish diarrhea model,4h after administration of different doses of VA granules gavage treatment. After3days treatment, the results showed thatVA granules could be used to cure diarrhea diseases caused by Escherichia coli.