Maejima T, Kubo M, Osawa T, Nakajima K, Kobayashi M
Pharmaceutics Research Laboratory, Tanabe Seiyaku Co., Ltd., Osaka, Japan.
Chem Pharm Bull (Tokyo). 1998 Mar;46(3):534-6. doi: 10.1248/cpb.46.534.
The tumbling melt granulation (TMG) method was applied to prepare controlled-release fine granules of diltiazem hydrochloride (DH). The entire process, from the preparation of the cores by the adherence of DH to the sucrose crystal to the subsequent coating of the controlled-release layer, was performed without using any solvent. A mixture of meltable material, talc, and ethylcellulose was used for the controlled-release layer and controlled-release fine granules approximately 400 microns in diameter were obtained with excellent producibility. The dissolution rate of DH from these fine granules was similar to that of a once-a-day dosage form obtained in the market; further, the dependency of the dissolution profile on pH of the media was less. Thus, it was concluded that this TMG method was very useful for preparing not only controlled-release beads of granule size (usually 500 to 1400 microns) but also fine granules.
采用翻滚熔融制粒（TMG）法制备盐酸地尔硫䓬（DH）控释细颗粒。整个过程，从通过将DH附着于蔗糖晶体来制备核芯到随后的控释层包衣，均在不使用任何溶剂的情况下进行。将可熔融材料、滑石粉和乙基纤维素的混合物用于控释层，制得直径约400微米的控释细颗粒，生产性良好。这些细颗粒中DH的溶出速率与市售一日一次剂型的溶出速率相似；此外，溶出曲线对介质pH的依赖性较小。因此，可以得出结论，这种TMG方法不仅对于制备通常粒径为500至1400微米的控释微丸，而且对于制备细颗粒都非常有用。
