Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, PR China.
Pharm Dev Technol. 2011 Jun;16(3):269-77. doi: 10.3109/10837451003664081. Epub 2010 Mar 10.
The aim of this paper was to study the comparative stability of venlafaxine hydrochloride (VEN) sustained-release pellets prepared by double-polymer coatings and hot-melt subcoating combined Eudragit(®) NE30D outercoating. The uncoated VEN pellets, containing 45% (w/w) VEN, 45% (w/w) MCC (PH101), 10% (w/w) stearic acid and 0.5% (w/w) Carbopol974, were prepared by extrusion-spheronization. Satisfactory release profiles were obtained when VEN pellets were prepared by 4% EC subcoating combined with 4% Eudragit(®) NE30D outercoating and 8% hot-melt subcoating combined with 6% Eudragit(®) NE30D outercoating, respectively. The storage stability was monitored by measuring the drug release over six months storage at 40°C/75% RH and at room temperature (25 ± 2°C/60% RH). The release of pellets with double-polymer coatings increased markedly, while drug release of pellets prepared by hot-melt subcoating combined with polymer coating gradually decreased. Basically, the former may be attributed to the main role of drug migration into the EC subcoating, and the latter may be caused by the fusion and resolidification of stearic acid particles and the further aging of the Eudragit(®) NE30D outercoating. In summary, regardless of the change in release, drug dissolution met the standard requirement and the stability was acceptable during the storage period.
本文旨在研究盐酸文拉法辛（VEN）双层聚合物包衣和热熔挤出 Eudragit（®） NE30D 肠溶包衣联合控释微丸的稳定性。未包衣的 VEN 微丸，含 45%（w/w）VEN、45%（w/w）MCC（PH101）、10%（w/w）硬脂酸和 0.5%（w/w）Carbopol974，由挤出滚圆法制备。当 4%乙基纤维素（EC）包衣联合 4%Eudragit（®） NE30D 肠溶包衣，以及 8%热熔挤出包衣联合 6%Eudragit（®） NE30D 肠溶包衣时，可得到满意的释放曲线。分别在 40°C/75%RH 和室温（25 ± 2°C/60%RH）下储存 6 个月后，监测药物释放情况，评估其稳定性。双层聚合物包衣微丸的释放明显增加，而热熔挤出包衣联合聚合物包衣微丸的药物释放逐渐减少。前者可能主要归因于药物向 EC 包衣层的迁移，后者可能是由于硬脂酸颗粒的融合和再结晶以及 Eudragit（®） NE30D 肠溶包衣的进一步老化。总之，无论释放情况如何变化，药物溶出度均符合标准要求，在储存期间稳定性可接受。
