Evaluation of Dantrolene Granules Extemporaneously Reformulated from Capsules in a Pharmacy

Abstract

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.

Extemporaneous preparation of rifampicin granules from capsules to improve usability

“…We previously reported the reconstitution of dantrolene 5% granules from capsules using a compounding mixer. 6 We intended to manufacture dantrolene granules for preparing for special needs before accepting medical prescriptions. Therefore, at 10 g in a 58 mL vessel, the batch size was larger than that of this study.…”

“…We considered the amount of medicine taken out of the sachet as the amount of dosing. 6 Therefore, weight loss on dosing was calculated using equation 3.…”

“…It enables small-scale and rapid production-for example, 10 g in a 58 mL vessel in less than 1 min. 6 In this study, we used rifampicin capsules as a model medicine. Rifampicin is a bactericidal antibiotic drug of the rifamycin group 7 and is an essential drug for the treatment of tuberculosis.…”

Development of Ethylcellulose Microparticles for Taste Masking of Fexofenadine

“…Powders and granules are applicable dosage forms for children and older people. 2,3) However, unpleasant taste such as bitterness due to the elution of drugs into the oral cavity may cause refusal to take medication. The taste of medicines is very important because human taste is highly subjective and children are more sensitive to bitter substances than adults.…”