El-Banna H M, Eshra A G, Hammouda Y
Pharmazie. 1977 Aug-Sep;32(8-9):511-5.
A trial was made to study the possibility of preparing high-quality therapeutic tablets by direct compression of the solidified drugcarrier melt via solid dispersion technique. Paracetamol-mannitol, amylobarbitone-urea and caffeine-nicotinamide systems were investigated. Phase diagrams of the first two systems were found to be of the simple eutectic type, while that of the third system was a peritectic type. Solubility studies were also carried out. Dissolution rate studies showed that the fused mannitol/paracetamol (80:20), urea/amylobarbitone (80:20) and nicotinamide/caffeine (50:50 and 70:30) solid dispersions exhibited better rates of dissolution than those of the pure drugs. Comparative studies were carried on with tablets prepared by direct compression of the drug-carrier solidified melt exhibiting the highest dissolution rate and by slugging the pure drug and the drug-carrier physical mixture of corresponding composition. The physical properties and dissolution rate data showed the superiority of the tablets prepared by the solid dispersion technique. The drug release from these tablets was 4.5, 7.6 and 3.7 times greater than that from tablets prepared from pure paracetamol, amylobarbitone and caffeine respectively.
进行了一项试验，以研究通过固体分散技术直接压制固化的药物载体熔体来制备高质量治疗片剂的可能性。对扑热息痛-甘露醇、异戊巴比妥-尿素和咖啡因-烟酰胺体系进行了研究。发现前两个体系的相图为简单低共熔型，而第三个体系的相图为包晶型。还进行了溶解度研究。溶出速率研究表明，熔融的甘露醇/扑热息痛（80:20）、尿素/异戊巴比妥（80:20）和烟酰胺/咖啡因（50:50和70:30）固体分散体的溶出速率比纯药物的溶出速率更好。对通过直接压制具有最高溶出速率的药物载体固化熔体以及将纯药物和相应组成的药物载体物理混合物制粒所制备的片剂进行了比较研究。物理性质和溶出速率数据表明了通过固体分散技术制备的片剂的优越性。这些片剂的药物释放量分别比由纯扑热息痛、异戊巴比妥和咖啡因制备的片剂大4.5倍、7.6倍和3.7倍。
