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用于治疗口腔扁平苔藓的倍他米松微粒/片的物理化学性质及体外黏膜黏附特性

Physicochemical and in vitro mucoadhesive properties of microparticles/discs of betamethasone for the management of oral lichen planus.

作者信息

Monajjemzadeh Farnaz, Gholizadeh Narges, Yousefzadeh Mobaraki Nahid, Jelvehgari Mitra

机构信息

a Department of Pharmaceutical and Food Analysis , Tabriz University of Medical Sciences , Tabriz , Islamic Republic of Iran.

b Department of Oral Medicine , Tehran University of Medical Sciences , Tehran , Islamic Republic of Iran.

出版信息

Pharm Dev Technol. 2016 Dec;21(8):996-1005. doi: 10.3109/10837450.2015.1089895. Epub 2015 Sep 28.

Abstract

This study involved the preparation and evaluation of buccal-mucoadhesive microparticles/discs of bethamethasone disodium phosphate (BDSP). The microparticles were prepared using the emulsion solvent diffusion method. Microparticles were prepared and characterized by encapsulation efficiency particle size, Fourier Transform Infra Red (FTIR) spectrums, Differential Scanning Calorimetric (DSC) thermograms and mucoadhesive properties. FTIR studies reported that BDSP was changed to bethamethasone base molecule inside the intact microparticles. The best drug to polymers ratio in microparticles was F containing 50 mg drug, 50 mg HPMC (as non-ionic and hydrophilic polymer) and 50 mg carbomer 934p (an anionic mucoadhesive polymer). The production yield of F1 microparticles was calculated as 78.60% with loading efficiency of about 65.14% and the mean particle size was also measured as 281.84 μm. It was proposed that during the microparticle preparation procedure, water soluble salt of the drug may be converted to the base which could be more effective in the buccal mucosa due to its higher partition coefficient and lipophilicity. The highest and lowest releases resulted from the discs prepared from F and F, respectively, compared with the commercial tablet and untreated drug powder (p < 0.05). The data revealed that the discs exhibited good percentage of mucoadhesion (F, 326 g/cm). It may be concluded that drug loaded buccal-mucoadhesive microparticles are a suitable delivery system for BDSP, and may be used in the effective management of lichen planus.

摘要

本研究涉及磷酸倍他米松二钠(BDSP)口腔黏膜黏附微粒/片的制备与评价。微粒采用乳化溶剂扩散法制备。通过包封率、粒径、傅里叶变换红外光谱(FTIR)、差示扫描量热法(DSC)热谱图和黏膜黏附性能对微粒进行了制备和表征。FTIR研究表明,完整微粒内部的BDSP转变为倍他米松碱分子。微粒中最佳的药物与聚合物比例为配方F,含50mg药物、50mg羟丙甲纤维素(作为非离子亲水性聚合物)和50mg卡波姆934p(一种阴离子黏膜黏附聚合物)。F1微粒的产率计算为78.60%,载药效率约为65.14%,平均粒径也测定为281.84μm。有人提出,在微粒制备过程中,药物的水溶性盐可能转化为碱,由于其较高的分配系数和亲脂性,在口腔黏膜中可能更有效。与市售片剂和未处理的药粉相比,分别由配方F和配方F制备的片的释放率最高和最低(p<0.05)。数据显示,该片剂表现出良好的黏膜黏附百分比(配方F,326g/cm)。可以得出结论,载药口腔黏膜黏附微粒是BDSP的一种合适给药系统,可用于扁平苔藓的有效治疗。

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