酒石酸沃尼妙林的制备和评价

Preparation, characterization, and evaluation of valnemulin hydrogen tartrate

关键词:  酒石酸沃尼妙林  结晶  稳定性  抗菌活性  应用

Key words:  valnemulin hydrogen tartrate  crystalline  stability  antibacterial activity  application

摘要:

盐酸沃尼妙林是一种治疗猪细菌感染疾病的抗生素，由于刺激性强和不稳定等缺陷限制了在兽医临床的应用。本研究制备了一种新型有机酸盐：酒石酸沃尼妙林。通过红外光谱、扫描电子显微镜和X-衍射对其物理化学性质进行研究。结果表明：酒石酸沃尼妙林具高结晶性，盐酸沃尼妙林是无定形的。稳定性试验表明：光照60天，酒石酸沃尼妙林含量减少3.5%，而盐酸沃尼妙林降幅较大为18.2%；酒石酸沃尼妙林表现出比盐酸沃尼妙林更优的抗湿性，在65%和78%的湿度条件下放置2天，酒石酸沃尼妙林和盐酸沃尼妙林的吸水量分别为1.30%，1.40%和4.50%，9.71%。体外抗菌敏感性试验表明上述2种盐的抗菌效果相同。酒石酸沃尼妙林对光照和湿度的稳定性将有利于其有效应用在兽医临床领域。

Abstract:

Valnemulin hydrochloride is an antibiotic for the treatment of swine infections in; however the irritating odor and unstable properties limits its application in veterinary clinics. In this study, a novel organic acid salt: valnemulin hydrogen tartrate was prepared. Its physicochemical properties were studied by comparing with valnemulin hydrochloride by infrared (IR) spectroscopy, scanning electron microscopy (SEM) and powder X-ray difffractometry (XRD). The results indicated that valnemulin hydrogen tartrate was highly crystalline whereas valnemulin hydrochloride was amorphous pattern. The stability studies showed that after sunlight irradiation for 60 days, the content of valnemulin hydrogen tartrate decreased only 3.5%, whereas valnemulin hydrochloride decreased dramatically 18.2%. Meanwhile, valnemulin hydrogen tartrate showed better anti-relative humidity (RH) ability than valnemulin hydrochloride. Under conditions of 65% and 78% RH for 2 days, the water absorption values of valnemulin hydrogen tartrate were 1.3% and 1.4%, whereas those of valnemulin hydrochloride were 4.50% and 9.71%, respectively. Finally, antimicrobial susceptibility test manifested that the above two salts of valnemulin exhibited similar antibacterial activity. The decreased hygroscopicity and improved photostability of valnemulin hydrogen tartrate will be more beneficial for its effective application as a veterinary drug than valnemulin hydrochloride.