Production And Research Of Berberine Hydrochloride Sustainde Release Injection

Berberine treatment is widely used in animal husbandry gastroenteritis, bacillary dysentery and other diseases of the broad-spectrum antimicrobial agents. Due to good solvency in water, its oral bioavailability is comparatively low. As ordinary injection, its obvious disadvantage was rapid drug metabolism. In order to improve the bioavailability, to maintain stable plasma concentration and to reduce the injection times, berberine hydrochlorid was made into sustained-release injections with liposomes as drug carriers.In this research, taking the particle size and particle size distribution of blank liposomes as standards for the evaluation of thin-film dispersion method, ultrasonic dispersion method, injection method, and reverse evaporation method, some common methods of preparation for liposomes were studied and assessed ,and injection method was regarded as the best excellent one;Taking liposome encapsulation efficiency of berberine hydrochloride as standards for the evaluation , parameters which could affect the quality of the preparation process were optimized with a orthogonal method. The best preparation process: the concentration of berberine hydrochloride solution was 3.0mg / ml, incubation temperature of water bath was 65℃, and incubation time was 30minutes; The quality standards of berberine hydrochloride sustained-release injection was established, multi-batch injection of berberine hydrochloride sustained-release quality were inspected, and its average particle size liposomes was in the 250nm , encapsulation efficiency was 83% ~ 85%, the leakage rate was about 1% after two weeks, the dissolutions in vitro after 2h, 6h and 12h dissolved were respectively 27.4%, 59.9% and 78.7%, with sustained-release effect; The acceleration test and long-term experiments were taken to inspect the sustained-release injection, results showed that berberine hydrochloride sustained-release injections were able to be preserved for one year in 4℃±2℃under the light, with the appearance of characters, PH , drug content and the average particle size of liposomes was basically unchanged; By the rabbit experiments on injection of berberine hydrochloride sustained-release to study the pharmacokinetics preliminarily, the results were that the peak time of the berberine hydrochloride injection and berberine sustained-release injection were 0.395h and 3.06h, and the latter could maintain a more stable blood concentration in 2 to 10 hours with a clear sustained-release effect .In this experiment, the berberine hydrochloride sustained-release injections were prepared by injection method of liposomes , and the preparation method for the injection was optimized with a orthogonal method, the stability of the injections was studied , the storage conditions were determined and the quality standards were established. Most of all, the preliminary study on the injection of berberine hydrochloride sustained-release pharmacokinetics provided a reliable theoretical basis.