恩诺沙星缓释注射液的制备及其缓释性能评价

Preparation of enrofloxacin sustained-release injection and evaluation of its sustained-release properties

[目的]制备恩诺沙星缓释注射液,并对其缓释性能进行评价。[方法]采用分散法制备恩诺沙星缓释注射液,考察制剂的沉降体积比,重新分散性,通针性,pH值和渗透压等各项质量指标,通过体外释放试验和家兔体内药动学实验评价制剂的缓释性能。[结果]制备的恩诺沙星缓释注射液稳定,具有良好的通针性,pH约为7.04,渗透压约为0.267osml/kg。体外试验中,恩诺沙星缓释注射液在0.5h的累积释放率仅为20%,直至12h累积释放率才达到80.2%。恩诺沙星缓释注射液主要的药物动力学参数是:清除率CL为1081.561±267.35 ml!h-1,Tmax为4h,体内平均滞留时间MRT为34.271±9.316 h。[结论]制备的恩诺沙星缓释注射液符合注射剂的要求,体内外试验均表明制剂具有一定的缓释效果。

[Objectiv]To prepare enrofloxacin sustained-release injection, then evaluate its sustained-release properties.[Method]The enrofloxacin sustained-release injection is prepared by grinding. The quality of the preparation is evaluated from the following aspects： the sedimentation rate, the redispersion, the ability the preparation through the needle, the pH value, and the osmotic pressure. The sustained-release properties of the preparation is investigated by in vitro release test and in v/vo pharmacokinetic behavior.[Result]The enrofloxacin sustained-release injection was stable and had good ability through the needle, the pH was 7.04, the osmotic pressure was 0.267 osml/kg. In the in vitro test, enrofloxacin sustained--release injection in the 0.5h release only 20%, and reach 80.2% up to 12h, The pharmacokinetic parameters of enrofioxacin sustained--release injection were showed as follows; The CL Was 1081.561±267.35 ml h-l, The Tmax was 4h, MPT was 54.271±9.516 h.[Conclusion] The quality of enrofloxacin sustained-release injection consistent with requirements of injections. And the preparation had obvious sustained-release effect.