Choulis N H, Abellana-Intaphan L, Narang P K
Pharmazie. 1978 May;33(5):289-91.
Studies conducted in this laboratory have indicated the feasibility of producing long-acting methadone tablets. In examining further, methadone hydrochloride suspensions were developed using spermaceti or eudragit retard-1 for particle coating. These procedures involved the addition of the active compound (methandone hydrochloride) to: a) melted spermaceti which was dried, and the dried mixture was pulverized and added to a methyl cellulose water solution; afterwards wild cherry syrup was added to the suspension, and b) Eudragit retard-1 crystals which were pulverized, dissolved in acetone/isopropanol (1:1) solvent system, dried, and to this product again the suspending agent methyl cellulose was added followed by wild cherry syrup to produce suspensions containing 10, 20, and 30 mg/ml methadone. These formulations were further used for in vivo studies, in male albino rats of Wistar strain. The pain threshold method was utilized in order to determine the duration of methadone. Over 75 h resistance to pain was recorded. Using the same technique, suspensions of methadone-naloxone combinations and the salts methadone-alpha-naphthalenesulfonate and methadone-o-benzoylbenzoate were prepared and examine similarly.
本实验室进行的研究表明了生产长效美沙酮片剂的可行性。进一步研究发现，使用鲸蜡醇或丙烯酸树脂缓释型1对颗粒进行包衣，开发出了盐酸美沙酮混悬液。这些步骤包括将活性化合物（盐酸美沙酮）添加到：a）融化后干燥的鲸蜡醇中，干燥后的混合物被粉碎并添加到甲基纤维素水溶液中；之后向混悬液中添加野樱桃糖浆，以及b）将丙烯酸树脂缓释型1晶体粉碎，溶解在丙酮/异丙醇（1:1）溶剂体系中，干燥，再向该产品中添加悬浮剂甲基纤维素，随后添加野樱桃糖浆，以制备含10、20和30mg/ml美沙酮的混悬液。这些制剂进一步用于对雄性Wistar品系白化大鼠的体内研究。采用疼痛阈值法来测定美沙酮的持续时间。记录到超过75小时的抗疼痛能力。使用相同技术，制备了美沙酮-纳洛酮组合以及美沙酮-α-萘磺酸盐和美沙酮-邻苯甲酰苯甲酸酯盐的混悬液，并进行了类似的研究。
