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目的制备新型盐酸倍他洛尔/蒙脱石微球滴眼剂并研究其初步刺激性。方法以蒙脱石为离子交换载体材料,用2种处方以O_1/O_2溶剂挥发法制备盐酸倍他洛尔缓释微球;对比微球的载药量和包封率等物化性能以得到最优处方,并将最优处方制备的微球制成滴眼剂以研究其初步刺激性。结果最优处方为丙烯酸树脂300mg(RS∶RL=1∶3),柠檬酸三乙酯60mg,甘油30mg,乳化剂400mg(吐温-80∶司盘-80=1∶2),盐酸倍他洛尔30mg,蒙脱石50mg,内外相体积比为1∶6。最优处方制得的微球载药量和包封率分别为14.31%和94.35%,初步刺激性实验显示微球滴眼剂对眼部组织无明显刺激性。结论微球制备方法简便易行,重复性好;制备的微球滴眼剂无明显刺激性,具有广阔的应用前景。
Objective To prepare a new type of betaxolol / montmorillonite microsphere eye drop and study its preliminary irritation. Methods Montmorillonite was used as ion exchange carrier material, and the two kinds of prescriptions were used to prepare betaxolol hydrochloride sustained-release microspheres by the O_1 / O_2 solvent evaporation method. The drug loading and entrapment efficiency of the microspheres were compared to obtain the most Excellent prescription, and the best prescription prepared microspheres eye drops to study its initial irritation. The results showed that the best prescription was 300mg of acrylic resin (RS: RL = 1: 3), 60mg of triethyl citrate, 30mg of glycerol and 400mg of emulsifier (Tween-80: Span-80 = Lol 30mg, montmorillonite 50mg, internal and external volume ratio of 1: 6. The optimum prescription of microspheres drug loading and entrapment efficiency were 14.31% and 94.35%, preliminary irritation experiments showed that microspheres eye drops no obvious irritation to the eye tissue. Conclusion The microspheres preparation method is simple and easy to operate with good repeatability. The prepared microspheres eye drops have no obvious irritation and have broad application prospects.