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Evaluation of Dantrolene Granules Extemporaneously Reformulated from Capsules in a Pharmacy
Chemical & Pharmaceutical Bulletin ( IF 1.5 ) Pub Date : 2020-10-01 , DOI: 10.1248/cpb.c20-00521
Yasunori Miyazaki 1 , Ayaka Tsuboi 2 , Saori Maruyama 2 , Hiroaki Aoshima 2 , Tomonobu Uchino 1 , Yoshiyuki Kagawa 1
Affiliation  

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.

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中文翻译:

从药房中的胶囊重新配制的丹特罗颗粒的评价

丹特罗胶囊是治疗痉挛的有效治疗剂,适用于在将其重新制成粉末后不能吞咽胶囊的儿童。粉末状药物可以改变指定的剂量,并且由于其体积大且粘性大,因此也难以分配粉末状制剂。为了解决这些问题,我们在药房中使用离心式行星混合器将丹特罗胶囊重新制成颗粒剂。检查含有乳糖-玉米淀粉,D-甘露糖醇或微晶纤维素作为稀释剂的颗粒,以确定粒度分布,流动性,药物含量均匀性和崩解时间。具有微晶纤维素的颗粒由于其较小的尺寸,良好的药物含量均匀性和快速崩解而优于其他形式。我们进一步研究了这些粉末在分配过程(分装和包装)和配料过程(从包装中取出)中的有效性,使用粉末作为对照。相对于粉末,减小了分配量的偏差和计量损失。另外,药物溶解特性和12个月的储存稳定性与粉末相同。因此,我们得出的结论是,在药房中,丹特罗颗粒是一种即兴制剂,是极好的替代品。12个月的药物溶解特性和储存稳定性与粉末相同。因此,我们得出的结论是,在药房中,丹特罗颗粒是一种即兴制剂,是极好的替代品。12个月的药物溶解特性和储存稳定性与粉末相同。因此,我们得出的结论是,在药房中,丹特罗颗粒是一种即兴制剂,是极好的替代品。

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更新日期:2020-10-28
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