丹酚酸B原位眼用凝胶剂的制备及体外释放
Research on Preparation and in Vitro Release of pH Sensitive Gel for Eye Cornea of Salvianolic Acid B
-
摘要: 目的 筛选丹酚酸B原位眼用凝胶剂处方, 完成相关体外释放研究.方法 通过离体角膜透过实验、刺激性实验、角膜水化值测定、凝胶粘度、胶凝能力、流动性等评价方法, 筛选丹酚酸B药物浓度、促透剂、増粘剂等辅料的种类及用量.结果 确定该凝胶剂的成分组成为:0.5%丹酚酸B、0.14%卡波姆、0.05%氮酮、0.3%羟丙甲基纤维素、0.1%羟苯乙酯和0.2%维生素C.角膜水化值 (77.32±1.88) .该凝胶在15 min时释放率27.21%的药物, 6 h后累计释放率达到97.44%.经过240 min的角膜透过实验, 丹酚酸B凝胶的累积释放量大于生理盐溶液的释放量 (P<0.05) .结论 该原位凝胶剂处方设计合理, 制备简单, 无刺激性, 延长药物在角膜的滞留时间, 增加药物角膜透过释放量.
-
关键词:
- 丹酚酸B /
- pH敏感型原位眼用凝胶剂 /
- 离体角膜透过 /
- 体外释放度测定
Abstract: Objective To prepare pH sensitive gel for eye cornea of salvianolic acid B and accomplish in vitro release study. Me thods We used corneal permeability, eye irritation in rabbits, hydration of the cornea, viscosity, gel capacity, transparency, liquidity as index, to select pH sensitive gel matrix composition. Re s ults The gel composition was: 0.5% of salvianolic acid B, 0.14% Carbomer, 0.3% HPMC, 0.05% Azone, 0.1% ethylparaben and 0.2% Vc. The corneal hydration level was 77.32±1.88.The gel released 27.21% drug in 15 min, and released 97.44% drug in 6 h. By research of corneal permeability, the cumulative release of gel was bigger than the one of saline (P<0.05) . Conclus ions The selection of the gel matrix prescription is reasonable in design, simple in process, not harsh to eyes, and can prolong the retention time of drug in corneas and improve the corneal penetration. -
[1]李德馨, 王思玲, 苏德森.白内障的发病机制与药物治疗[J].沈阳药科大学学报, 2002, 19 (4) :300-306. [2]杨玲, 朱莉静, 宋波.66例白内障青光眼联合手术的临床观察[J].昆明医科大学学报, 2014, 35 (3) :136-138. [3]田影, 何克江, 朱靖博.丹酚酸B的体外抗氧化活性[J].大连工业大学学报, 2008, 27 (4) :3-7. [4]冷非.丹酚酸B滴眼剂对大鼠糖尿病性白内障的影响[J].哈尔滨医科大学学报, 2009, 43 (4) :249-253. [5]吴升辉, 王燕凤, 张晓琴.丹酚酸B对糖尿病大鼠角膜的保护作用及其机制[J].国际眼科杂志, 2016, 16 (9) :1629-1631. [6]赵先, 王婧雯, 陆杨.丹酚酸B药理作用的研究进展[J].西北药学杂志, 2015, 30 (1) :107-110. [7] [7]ROBISON JR ED.Ophthalmic Drug Delivery Systems[M].Washington DC:American Pharmaceutical Association, 1980:1. [8]刘玉生, 薛晓, 李实, 等.环孢素A眼用p H敏感型乳剂凝胶的角膜滞留性及药效学[J].中国新药杂志, 2015, 24 (2) :199-201. [9] [9]SAFRTONE MF, CHETONI P, CERBAI R, et a1.Evaluation of ocular permeation enhancers:in vitro effects on corneal transport of fourβ-blockers, and in vitro/in vivo toxic activity[J].Int J Pharm, 1996, 142 (1) :103-113. [10]吴纯洁.葛根素眼用新型给药系统的研究[D].成都:四川大学, 2005. [11]张治强, 张玮, 陈光, 等.p H敏感型盐酸左氧氟沙星眼用即型凝胶的制备及其体外释放考察[J].药学实践杂志, 2010, 28 (2) :122-125. [12]张婧, 李翔, 罗云, 等.姜黄素眼用脂质体的角膜透过性研究[J].江西中医药大学学报, 2015, 27 (2) :79-81. [13] 李英.甲砜霉素p H敏感眼用凝胶的研究[D].沈阳:沈阳药科大学硕士论文, 2006:26. [14]邓翔, 何文.司帕沙星眼用p H敏感原位凝胶的制备及体外角膜透过性考察[J].医药导报, 2012, 31 (6) :783-785. [15]赵雯, 刘睿, 孙璐, 等.3种环糊精对姜黄素角膜渗透性影响研究[J].中草药, 2015, 46 (2) :201-206. [16]卢召战, 朱靖博, 刘天赐.p H及添加剂对丹酚酸B水溶液稳定性的影响[J].大连工业大学学报, 2008, 27 (3) :209-211. [17]黄世超, 瞿海斌.丹酚酸B稳定性研究进展[J].中国现代应用药学, 2015, 32 (5) :644-648. [18]李英.甲砜霉素p H敏感眼用凝胶的研究[D].沈阳:沈阳药科大学 (硕士论文) , 2006:26. [19]徐亚静, 胡容峰.黄芩苷p H敏感眼用原位凝胶剂的制备与评价[J].辽宁中医药大学学报, 2015, 17 (12) :39-42. -
点击查看大图
计量
- 文章访问数: 1928
- HTML全文浏览量: 716
- PDF下载量: 174
- 被引次数: 0
下载:
