Camargo Pharmaceutical Services , Cincinnati, OH , USA and.
Pharm Dev Technol. 2014 Feb;19(1):91-102. doi: 10.3109/10837450.2012.757783. Epub 2013 Jan 17.
Twelve hydrophobic coating agents were assessed for their effects on drug release after coating sugar cores by a flexible hot-melt coating method using direct blending. Drug-containing pellets were also produced and used as cores. The cores were coated with single or double wax layers containing acetaminophen (APAP). The harder the wax, the slower the resultant drug releases from single-coated beads. Wax coating can be deposited on cores up to 28% of the beads final weight and reaching 58% with wax and drug. Carnauba-coated beads dissolved in approximately 6 h releasing 80% of the loaded drug. Applying another wax layer extended drug release over 20 h, while still delivering 80% of the loaded drug. When drug-containing pellets (33-58% drug loading) were used as cores, double wax-coated pellets exhibited a near zero-order drug release for 16 h, releasing 80% of the loaded drug delivering 18 mg/h. The simple process of hot-melt coating by direct blending of pellet-containing drug-coated formulations provides excellent options for immediate and sustained release formulations when higher lipid coating or drug loading is warranted. Predicted plasma drug concentration time profiles using convolution and in vitro drug release properties of the beads were performed for optimal formulations.
十二种疏水性包衣剂通过直接混合的柔性热熔包衣法对糖芯进行包衣后对药物释放的影响进行了评估。还生产了载药丸芯并将其用作芯材。芯材用含有对乙酰氨基酚（APAP）的单层或双层蜡层进行包衣。蜡越硬，单层包衣珠的药物释放越慢。蜡涂层可沉积在丸芯上，达到丸芯最终重量的 28%，达到 58%的蜡和药物。涂有巴西棕榈蜡的丸芯在大约 6 小时内溶解，释放出 80%的载药。再涂一层蜡可将药物释放延长至 20 小时以上，同时仍可释放 80%的载药。当含有药物的丸芯（33-58%药物载量）用作芯材时，双层蜡包衣丸芯可在 16 小时内实现近零级药物释放，释放 80%的载药量，释放速率为 18mg/h。含药丸芯的直接混合热熔包衣的简单工艺为需要更高脂质包衣或药物载量的即时和持续释放制剂提供了极好的选择。使用卷积和珠体外药物释放特性对预测的血浆药物浓度时间曲线进行了优化制剂。
