Physicochemical characterization and dissolution enhancement of aceclofenac-hydroxypropyl beta-cyclodextrin binary systems.
The aim of this study is to prepare and characterize binary systems of aceclofenac (AC) with hydroxypropyl beta-cyclodextrin (HPbetaCD) in equimolar ratio. Solid binary systems of aceclofenac with HPbetaCD were prepared using cogrinding, kneading, and coevaporating methods, and a physical mixture was prepared for comparison. The binary systems were characterized by differential scanning calorimetry, thermogravimetric analysis, mass spectroscopy, 1H nuclear magnetic resonance (NMR) spectroscopy, scanning electron microscopy, and in vitro dissolution studies. 1H NMR studies showed that AC partially fits into the HPbetaCD torus cavity with a preferential inclusion of the phenyl ring of the drug. All the binary systems showed superior dissolution and lower dose:solubility ratio (D:S ratio) as compared to pure AC, but the kneaded product exhibited the best dissolution, with complete drug release within 10 min and a D:S ratio of 5 mL. Hence, it was suggested that complexation of aceclofenac with HPbetaCD may be used as an approach to change the drug from Biopharmaceutics Classification System BCS Class II to BCS Class I without changing its intrinsic permeability.
Dahiya
Sunita
S
Department of Pharmaceutics, Rajiv Academy for Pharmacy, Mathura--281 001, India. sunitadahiya73@rediffmail.com
Pathak
Kamla
K
D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage*; D002152:Calorimetry, Differential Scanning; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D003363:Cost Control; D004008:Diclofenac / Q000008:administration & dosage / Q000031:analogs & derivatives*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008855:Microscopy, Electron, Scanning; D012995:Solubility; D012996:Solutions; D013056:Spectrophotometry, Ultraviolet; D013818:Thermogravimetry; D047392:beta-Cyclodextrins / Q000737:chemistry*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D012996:Solutions; D047392:beta-Cyclodextrins; D004008:Diclofenac; D000073738:2-Hydroxypropyl-beta-cyclodextrin; C056498:aceclofenac