Department of Clinical Pharmaceutics, School of Pharmaceutical Sciences, University of Shizuoka.
Department of Pharmacy, Shizuoka Children Hospital.
Chem Pharm Bull (Tokyo). 2020;68(10):989-995. doi: 10.1248/cpb.c20-00521.
Dantrolene capsule, an effective therapeutic agent for the treatment of spasticity, is administered to children who cannot swallow the capsule after reformulation into a powder. The powdered drug can alter the specified dosage and it is also difficult to dispense the powdered formulation because of its bulky and sticky nature. To resolve these problems, we reformulated dantrolene capsules into granules using a centrifugal planetary mixer in the pharmacy. The granules containing lactose-cornstarch, D-mannitol, or microcrystalline cellulose as a diluent were examined to determine particle size distribution, flowability, drug content uniformity, and disintegration time. The granules with microcrystalline cellulose were superior to the other forms, owing to their smaller size, good drug content uniformity, and rapid disintegration. We further investigated the usability of the granules in the dispensing procedure (dividing and packing) and in the dosing process (retrieval from package) using the powders as controls. The deviation of the divided amount and loss on dosing were reduced relative to the powders. In addition, drug dissolution properties and storage stability for 12 months were the same as those of the powders. Therefore, we concluded that dantrolene granules are excellent alternatives as an extemporaneous preparation in pharmacies.
丹曲林胶囊是一种有效的痉挛治疗药物,对于不能吞服胶囊的儿童,可以将其重新配方制成粉末。粉末状药物会改变规定的剂量,而且由于其体积大和粘性大,难以分配粉末制剂。为了解决这些问题,我们在药剂科使用离心行星混合机将丹曲林胶囊重新制成颗粒。含有乳糖-玉米淀粉、D-甘露醇或微晶纤维素作为稀释剂的颗粒进行了粒径分布、流动性、药物含量均匀性和崩解时间的检查。含有微晶纤维素的颗粒由于其较小的粒径、良好的药物含量均匀性和快速崩解而优于其他形式。我们进一步研究了使用粉末作为对照在配药过程(分装和包装)和剂量过程(从包装中取出)中颗粒的可用性。与粉末相比,分装量的偏差和剂量损失减少。此外,药物溶解特性和 12 个月的储存稳定性与粉末相同。因此,我们得出结论,丹曲林颗粒是药剂科中一种优秀的临时制剂替代品。