RESUMEN
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.
Asunto(s)
Dantroleno/química , Dantroleno/farmacología , Cápsulas/química , Celulosa/química , Composición de Medicamentos , Estabilidad de Medicamentos , Excipientes/química , Lactosa/química , Manitol/química , Tamaño de la Partícula , Polvos/química , Solubilidad , Almidón/químicaRESUMEN
Eight new caffeic acid oligomers, clinopodic acids J-Q (1-8), were isolated from whole plants of Clinopodium gracile, together with nine known caffeic acid oligomers. The caffeic acid oligomers with two to four dihydrobenzofuran rings were isolated as natural products for the first time. Clinopodic acid M (4) showed the strongest hyaluronidase inhibitory activity, IC(50) (19 µM) among the 22 compounds isolated from this plant.
Asunto(s)
Ácidos Cafeicos/química , Inhibidores Enzimáticos/química , Hialuronoglucosaminidasa/antagonistas & inhibidores , Lamiaceae/química , Ácidos Cafeicos/aislamiento & purificación , Inhibidores Enzimáticos/aislamiento & purificación , Hialuronoglucosaminidasa/metabolismo , Espectroscopía de Resonancia Magnética , Conformación MolecularRESUMEN
From the aerial parts of Clinopodium chinense var. parviflorum, nine new phenylpropanoids, clinopodic acids A-I (2-10), were isolated together with a known phenylpropanoid, rosmarinic acid (1). The structures of these new compounds were elucidated on the basis of spectroscopic analysis. Clinopodic acid C (4) showed MMP-2 inhibitory activity (IC(50) 3.26 microM).
