Preparation And Quality Research Of Tosufuloxacin Tosylate Eye Drops

Tosufuloxacin tosylate is a fluorinated quinolone antibacterials which has low toxicity, strong penetration ability, high efficiency and broad spectrum of antimicrobial, however, its poor solubility and instability is the bottleneck of developing its eye drop preparation.To solve these two problems, at first, its physical and chemical properties were studied, then Aluminum potassium sulfate was used as an auxiliary solvent. To prepare feasible prescription and controllable quality of eye drops, single test and orthogonal test at60℃were made to screen and optimize formulation and preparation. The best prescription:molar ratio of tosufloxacin tosylate and aluminum potassium sulfate was1:1, borax content was0.5mg per mL, adjusted to pH5.5. A0.3%tosufloxacin tosylate eye drops was successfully prepared. To control the quality of intermediates and final product, two methods(UV and HPLC)were established to detect the content of tosufloxacin tosylate. UV:the linear rang of tosufloxacin tosylate was21.7μg/mL～76.9μg/mL(r=1), the average recovery was99.54%(RSD=0.55%). HPLC:the linear rang of tosufloxacin tosylate was12.22μg/mL～195.52μg/mL(r=0.999), the average recovery was100.21%(RSD=0.85%). Two methods can be used for determination.According to the national general notice of ophthalmic preparation, a series of methods for quality control such as identification tests and inspection tests were established. The quality of three batches eye drops were evaluated and the results all meet the requirements. Impact factors test and acceclerated test of three batches sample were done. Result:at40℃±2℃、low temperature、light conditions and two months of accelerated testing (40℃±2℃),the quality of sample was stable.The results of quality assessment, impact factors and acceclerated test of three batches sample proved the following:the first, the prescription, processing and packing of tosufloxacin tosylate eye drops were reasonable; the second, the solution of eye drops is stable and its quality can be controlled. In a word, test dates provided the basis for validity and storage of eye drops.