Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, University of Granada, Granada, Spain.
Drug Dev Ind Pharm. 2010 Aug;36(8):885-92. doi: 10.3109/03639040903578726.
Although tramadol has less analgesic power than morphine, it presents fewer side effects and consequently is currently considered as a drug of choice in the treatment of chronic pain. The objective of this work was to obtain a sustained-release liquid preparation for oral administration, using pseudolatex of ethylcellulose as a delivery vehicle of the active principle.
Once an appropriate microencapsulation had been achieved, different formulations with different viscosing agents were designed and subsequently subjected to in vitro release studies, using Franz-type diffusion cells.
The pseudolatex with tramadol showed an encapsulation efficiency of 82% but was found to be dependent on the quantity of the drug. The images obtained through scanning electron microscopy showed sphere-shaped particles with a porous surface and diameter sizes of 3.5 and 5.5 microm. Infrared spectrophotometry and calorimetric analysis revealed the formation of a drug-polymer complex. Of the formulations proposed, that with xanthan gum released 46% of the drug, whereas Carbopol, sodium carboxymethylcellulose, and Avicel gave 50% and 55%, respectively. All followed a release kinetic of cube root, with the release mechanism of the active principle occurring through anomalous transport.
In accordance with the studies performed, we can confirm a liquid pharmaceutical preparation for oral use, capable of providing a sustained release of tramadol.
曲马多的镇痛效力虽不及吗啡，但副作用较少，因此目前被认为是治疗慢性疼痛的首选药物。本研究旨在使用乙基纤维素假胶作为活性药物的传递载体，制备一种可口服的缓释液体制剂。
实现适当的微囊化后，设计了不同粘度赋形剂的不同配方，并随后使用 Franz 型扩散池进行体外释放研究。
曲马多假胶的包封效率为 82%，但发现其取决于药物的用量。扫描电子显微镜的图像显示，球形颗粒具有多孔表面，直径为 3.5 和 5.5 微米。红外光谱和热分析表明形成了药物-聚合物复合物。在所提出的配方中，黄原胶释放了 46%的药物，而 Carbopol、羧甲基纤维素钠和微晶纤维素分别释放了 50%和 55%。所有配方均遵循立方根释放动力学，药物的释放机制通过非定常传递发生。
根据所进行的研究，我们可以确认一种可口服的液体药物制剂，能够提供曲马多的持续释放。
