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Titolo:
Improved dissolution behavior of fenbufen by spherical crystallization
Autore:
Di Martino, P; Barthelemy, C; Piva, F; Joiris, E; Palmieri, GF; Martelli, S;
Indirizzi:
Univ Camerino, Dipartimento Sci Chim, I-62032 Camerino, Italy Univ Camerino Camerino Italy I-62032 o Sci Chim, I-62032 Camerino, Italy Univ Lille 2, F-59006 Lille, France Univ Lille 2 Lille France F-59006Univ Lille 2, F-59006 Lille, France
Titolo Testata:
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
fascicolo: 10, volume: 25, anno: 1999,
pagine: 1073 - 1081
SICI:
0363-9045(1999)25:10<1073:IDBOFB>2.0.ZU;2-0
Fonte:
ISI
Lingua:
ENG
Soggetto:
AGGLOMERATION; CRYSTALS; COMPRESSION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
13
Recensione:
Indirizzi per estratti:
Indirizzo: Barthelemy, C Univ Camerino, Dipartimento Sci Chim, Via S Agostino 1, I-62032 Camerino, Italy Univ Camerino Via S Agostino 1 Camerino Italy I-62032 Italy
Citazione:
P. Di Martino et al., "Improved dissolution behavior of fenbufen by spherical crystallization", DRUG DEV IN, 25(10), 1999, pp. 1073-1081

Abstract

Fenbufen is an analgesic, antipyretic and anti-inflammatory drug that is characterized by poor water solubility, a defect increased by very low wettability. Poor water solubility, particularly at low pH, could decrease absorption in the upper part of the gastrointestinal tract, which would be inconvenient for good bioavailability. Different spherical crystallization processes have been considered as methods to improve fenbufen dissolution behavior. A two-solvent system, in the presence of a bridging liquid, is the onlymethod capable of producing spherical fenbufen crystals. In a first step, fenbufen solubility was considered in different solvents. The drug crystalsformed were typically needle shaped. This characteristic was considered asa favorable parameter to obtain spherical crystals. After the selection ofthe best fenbufen solvent, several ratios of solvent (S)-nonsolvent (NS) (tetrahydrofuran [THF]-demineralized water) were studied. The addition of a bridging liquid (isopropyl acetate) improved spherical crystallization. Theresults from this method were reproducible batch to batch. The spherical crystals obtained showed a clear improvement in dissolution capacity, probably due to better wettability. Dissolution studies were then carried out on these spherical crystals stored for 1 month at different relative humidities (RHs). The dissolution profiles remained unchanged.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 18/01/20 alle ore 01:47:08