盐酸倍他洛尔-蒙脱石离子交换微球混悬剂的制备及质量评价

发布时间：2018-03-20 13:25

本文选题：蒙脱石　切入点：盐酸倍他洛尔　出处：《中国实验方剂学杂志》2015年19期 　论文类型：期刊论文

【摘要】：目的:将盐酸倍他洛尔-蒙脱石离子交换微球制备成眼用混悬剂,为新型微球混悬剂的眼部给药提供参考。方法:筛选盐酸倍他洛尔-蒙脱石离子交换微球混悬剂的辅料并进行制剂学评价,通过刺激性与离体角膜透过性试验考查混悬剂的生物学性质。结果:以0.15%卡波姆934P为助悬剂,0.01%聚山梨酯-80为润湿剂,制备的制剂稳定性良好,p H(7.0),渗透压(302 m Osm·kg-1),黏度(4.1 m Pa·s)和刺激性均符合眼用制剂要求。刺激性试验显示微球混悬剂对眼部组织无明显刺激性,贝特舒组结膜出现部分淋巴细胞浸润。角膜透过性试验中微球混悬剂表观渗透参数1.78×10-5cm·s-1,约为盐酸倍他洛尔溶液(3.57×10-5cm·s-1)的1/2倍和市售贝特舒(0.85×10-5cm·s-1)2倍。结论:离子交换微球可在一定程度上减缓药物的角膜透过性,虽然缓释性不及贝特舒,但刺激性显著低于贝特舒,具备一定的缓释性与低毒副作用。
[Abstract]:Objective: to prepare betalol hydrochloride montmorillonite ion-exchange microspheres into eye suspension. Methods: the adjuvant of betaloprolol hydrochloride and montmorillonite ion-exchange microsphere suspension was screened and evaluated. The biological properties of suspension were investigated by experiments of irritability and corneal permeability in vitro. Results: 0.15% Carbomer 934P was used as suspension aid and 0.01% polysorbate -80 as wetting agent. The prepared preparation has good stability, osmotic pressure 302m Osm 路kg-1C, viscosity of 4.1mPa 路s) and irritability. The irritation test showed that the microsphere suspension had no obvious irritation to ocular tissue. In the corneal penetration test, the apparent osmotic parameters of microsphere suspension were 1.78 脳 10 ~ (-5) cm 路s ~ (-1), about 1/2 times as much as betalol hydrochloride (3.57 脳 10 ~ (-5) cm 路s ~ (-1)) and 0.85 脳 10 ~ (-5) cm 路s ~ (-12) times of betaprolol hydrochloride. Conclusion: ion exchange microspheres can be obtained. To some extent, to slow down the corneal permeability of the drug, Although the slow-release ability was not as good as that of betaol, the irritability was significantly lower than that of Betellol, and had certain slow-release and low toxic side effects.
【作者单位】：广东药学院药科学院;中国药科大学药学院;
【基金】：国家自然科学基金项目(51102052)
【分类号】：R943

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