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比索洛尔口腔黏附片的研制与体外评价

Development and in vitro evaluation of buccoadhesive carvedilol tablets.

作者信息

Yamsani Vamshi Vishnu, Gannu Ramesh, Kolli Chandrasekhar, Rao M E Bhanoji, Yamsani Madhusudan Rao

机构信息

Centre for Biopharmaceutics and Pharmacokinetics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal-506 009, A.P. India.

出版信息

Acta Pharm. 2007 Jun;57(2):185-97. doi: 10.2478/v10007-007-0015-7.

Abstract

Buccoadhesive tablets of carvedilol were prepared using HPMC K4M, HPMC K15M and Carbopol 934 as mucoadhesive polymers. Fifteen formulations were developed with varying concentrations of polymers. Formulations of the BC or BD series were composed of HPMC K4M or HPMC K15M in ratios of 1:1 to 1:5 whereas in the BE series Carbopol 934 was used (1:0.25 to 1:1.50). The formulations were tested for in vitro drug release, in vitro bioadhesion, moisture absorption and in vitro drug permeation through porcine buccal mucosa. Formulation BC3 showed maximum release of the drug (88.7 +/- 0.4%) with the Higuchi model release profile and permeated 21.5 +/- 2.9% of the drug (flux 8.35 +/- 0.291 microg h(-1)cm(-2)) permeation coefficient 1.34 +/- 0.05 cm h(-1)) through porcine buccal membrane. BC3 formulation showed 1.62 +/- 0.15 N of peak detachment force and 0.24 +/- 0.11 mJ of work of adhesion. FTIR results showed no evidence of interaction between the drug and polymers. XRD study revealed that the drug is in crystalline form in the polymer matrix. The results indicate that suitable bioadhesive buccal tablets with desired permeability could be prepared.

摘要

使用羟丙甲纤维素K4M、羟丙甲纤维素K15M和卡波姆934作为粘膜粘附聚合物制备了卡维地洛口腔粘附片。开发了15种不同聚合物浓度的制剂。BC或BD系列制剂由比例为1:1至1:5的羟丙甲纤维素K4M或羟丙甲纤维素K15M组成,而BE系列使用卡波姆934(1:0.25至1:1.50)。对这些制剂进行了体外药物释放、体外生物粘附、吸湿以及药物通过猪口腔粘膜的体外渗透测试。制剂BC3显示出最大药物释放量(88.7 +/- 0.4%),符合Higuchi模型释放曲线,并且有21.5 +/- 2.9%的药物透过猪口腔膜(通量为8.35 +/- 0.291 μg h(-1)cm(-2)),渗透系数为1.34 +/- 0.05 cm h(-1))。BC3制剂显示出1.62 +/- 0.15 N的峰值分离力和0.24 +/- 0.11 mJ的粘附功。傅里叶变换红外光谱(FTIR)结果表明药物与聚合物之间没有相互作用的迹象。X射线衍射(XRD)研究表明药物在聚合物基质中呈结晶形式。结果表明,可以制备出具有所需渗透性的合适的生物粘附口腔片。

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