Wong Tin Wui, Wahab Selasiah, Anthony Yolande
Particle Design Research Group, Non-Destructive Biomedical and Pharmaceutical Research Centre, Faculty of Pharmacy, Universiti Teknologi MARA, Shah Alam, Selangor, Malaysia.
Drug Dev Ind Pharm. 2007 Jul;33(7):737-46. doi: 10.1080/03639040601015513.
The drug release behavior of beads made of poly(methyl vinyl ether-co-maleic acid) was investigated with respect to the influence of microwave irradiation. The beads were prepared by an extrusion method with sodium diclofenac as a model water-soluble drug. The beads were subjected to microwave irradiation at 80 W for 5 and 20 min, and at 300 W for 1 min 20 s and 5 min 20 s. The profiles of drug dissolution, drug content, drug-polymer interaction, and polymer-polymer interaction were determined by using dissolution testing, drug content assay, differential scanning calorimetry, and Fourier transform infra-red spectroscopy. Keeping the level of supplied irradiation energy identical, treatment of beads by microwave at varying intensities of irradiation did not bring about similar drug release profiles. The extent and rate of drug released from beads were markedly enhanced through treating the samples by microwave at 80 W as a result of loss of polymer-polymer interaction via the (CH(2))(n) moiety, but decreased upon treating the beads by microwave at 300 W following polymer-polymer interaction via the O-H, COOH, and COO(-) moieties as well as drug-polymer interaction via the N-H, O-H, COO(-), and C-O moieties. The beads treated by microwave at 300 W exhibited a higher level of drug release retardation capacity than those that were treated by microwave at 80 W in spite of polymer-polymer interaction via the (CH(2))(n) moiety was similarly reduced in the matrix. The mechanism of drug release of both microwave-treated and untreated beads tended to follow zero order kinetics. The drug release was markedly governed by the state of polymer relaxation of the matrix and was in turn affected by the state of polymer-polymer and/or drug-polymer interaction in beads.
研究了聚(甲基乙烯基醚 - 共 - 马来酸)制成的微球在微波辐照影响下的药物释放行为。以双氯芬酸钠作为模型水溶性药物,通过挤出法制备微球。微球分别在80W下进行5分钟和20分钟的微波辐照,以及在300W下进行1分20秒和5分20秒的微波辐照。通过溶出度测试、药物含量测定、差示扫描量热法和傅里叶变换红外光谱法测定药物溶出曲线、药物含量、药物 - 聚合物相互作用和聚合物 - 聚合物相互作用。在提供的辐照能量水平相同的情况下,对微球进行不同强度的微波处理并未带来相似的药物释放曲线。由于通过(CH(2))(n)部分导致聚合物 - 聚合物相互作用丧失,在80W下用微波处理样品使得微球中药物释放的程度和速率显著提高,但在300W下用微波处理微球后,通过O - H、COOH和COO(-)部分的聚合物 - 聚合物相互作用以及通过N - H、O - H、COO(-)和C - O部分的药物 - 聚合物相互作用,药物释放减少。尽管基质中通过(CH(2))(n)部分的聚合物 - 聚合物相互作用同样降低,但300W微波处理的微球比80W微波处理的微球表现出更高水平的药物释放延迟能力。微波处理和未处理的微球的药物释放机制都倾向于遵循零级动力学。药物释放明显受基质聚合物松弛状态的控制,进而受微球中聚合物 - 聚合物和/或药物 - 聚合物相互作用状态的影响。