含双氯芬酸钠的口腔黏附微球的制剂与理化特性
Formulation and physicochemical characterization of buccoadhesive microspheres containing diclofenac sodium.
作者信息
Jelvehgari Mitra, Valizadeh Hadi, Jalali Motlagh Ramin, Montazam Hassan
机构信息
Drug Applied Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
Biotechnology Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
出版信息
Adv Pharm Bull. 2014;4(3):295-301. doi: 10.5681/apb.2014.043. Epub 2014 Feb 7.
PURPOSE
The present study involves preparation and evaluation of diclofenac buccal-mucoadhesive microparticles for prolongation of buccal residence time.
METHODS
The microparticles were prepared by modified double-emulsion dehydration method (O1/W/O2) using sodium carboxymethylcellulose (CMC-Na) as mucoadhesive polymer. Calcium chloride was used as a cross-linking agent. Buccal-mucoadhesive microparticles with different drug to polymers ratios were prepared and characterized by encapsulation efficiency, particle size, DSC (Differential Scanning Calormetric), flowability, degree of swelling, surface pH, mucoadhesive property and drug release studies.
RESULTS
The best drug to polymer ratio in microparticles was 1:5 (F3) with CMC-Na. F1 microparticles showed loading efficiency 51.43% and mean particle size 1013.92 μm. The DSC showed stable character of drug in microparticles and revealed amorphous form. Microparticles had slower release than the commercial tablet (p<o.o5). The results of mucoadhesion study showed better retention of diclofenac microparticles in mucosa (>50 min). Histopathological studies revealed no buccal mucosal damage.
CONCLUSION
It may be concluded that drug loaded buccal-mucoadhesive microparticles are a suitable delivery system for DS.
目的
本研究涉及双氯芬酸口腔黏膜黏附微粒的制备及评价，以延长其口腔滞留时间。
方法
采用改良复乳脱水法（O1/W/O2），以羧甲基纤维素钠（CMC-Na）作为黏膜黏附聚合物制备微粒。氯化钙用作交联剂。制备了不同药物与聚合物比例的口腔黏膜黏附微粒，并通过包封率、粒径、差示扫描量热法（DSC）、流动性、溶胀度、表面pH值、黏膜黏附性能及药物释放研究对其进行表征。
结果
含CMC-Na的微粒中最佳药物与聚合物比例为1:5（F3）。F1微粒的载药效率为51.43%，平均粒径为1013.92μm。DSC显示微粒中药物性质稳定，呈无定形状态。微粒的释放比市售片剂慢（p<0.05）。黏膜黏附研究结果表明双氯芬酸微粒在黏膜中的滞留效果更好（>50分钟）。组织病理学研究显示口腔黏膜无损伤。
结论
可以得出结论，载药口腔黏膜黏附微粒是双氯芬酸的一种合适给药系统。
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