Rohera Bhagwan D, Parikh Nilesh H
College of Pharmacy and Allied Health Professions, St. John's University, 8000 Utopia Parkway, Jamaica, NY 11439, USA.
Pharm Dev Technol. 2002 Nov;7(4):407-20. doi: 10.1081/pdt-120015043.
Two commercially available formulations of aqueous ethylcellulose dispersion differing in their plasticizer, i.e., Surelease/E-7-7050 containing dibutyl sebacate (DBS) and Surelease/E-7-7060 containing glyceryl tricaprylate/caprate (GTC), were evaluated and compared for their film properties as a function of polymeric coat level. Ibuprofen tablets were coated at 1, 2, 3, and 5% w/w levels using each Surelease formulation, and the coated tablets were evaluated for their drug release characteristics, coat reflectivity (gloss), surface texture, Brinell hardness, and elastic modulus. The drug release was dependent on the coat level and followed Hixson-Crowell cube-root model at 1% coat level. However, at > or = 2% coat levels, the release from tablets coated with GTC plasticized formulation appeared to be best described by non-Fickian release mechanism and that from tablets coated with DBS plasticized formulation appeared to follow apparent zero-order release mechanism. At equal coat levels, tablets coated with GTC plasticized Surelease yielded lower drug release rates, higher reflectivity (gloss), lower surface roughness, higher Brinell hardness, and lower elastic modulus than those coated with DBS plasticized formulation. A good correlation was observed between the drug release rates and the reflectivity and surface texture of the coated tablets. The film-coats of GTC plasticized formulation were harder and more elastic than those of DBS plasticized formulation indicating better mechanical integrity.
对两种市售的水性乙基纤维素分散体配方进行了评估和比较，这两种配方的增塑剂不同，即含有癸二酸二丁酯（DBS）的Surelease/E - 7 - 7050和含有三辛酸甘油酯/癸酸甘油酯（GTC）的Surelease/E - 7 - 7060，研究了它们作为聚合物包衣水平函数的薄膜性能。使用每种Surelease配方以1%、2%、3%和5%（w/w）的水平对布洛芬片剂进行包衣，并对包衣片剂的药物释放特性、包衣反射率（光泽度）、表面质地、布氏硬度和弹性模量进行了评估。药物释放取决于包衣水平，在1%包衣水平时遵循希克森 - 克劳威尔立方根模型。然而，在包衣水平≥2%时，用GTC增塑配方包衣的片剂的释放似乎最好用非菲克释放机制来描述，而用DBS增塑配方包衣的片剂的释放似乎遵循表观零级释放机制。在相同包衣水平下，用GTC增塑的Surelease包衣的片剂比用DBS增塑配方包衣的片剂具有更低的药物释放速率、更高的反射率（光泽度）、更低的表面粗糙度、更高的布氏硬度和更低的弹性模量。观察到药物释放速率与包衣片剂的反射率和表面质地之间存在良好的相关性。GTC增塑配方的薄膜包衣比DBS增塑配方的薄膜包衣更硬且更有弹性，表明其机械完整性更好。
