Abstract. The purpose of this study was to investigate the nasal absorption of progesterone from carbopol-based nasal gels in rabbits. Progesterone nasal gels were prepared by dispersing carbopol 974 (1%, 1.5%, and 2%) in distilled water followed by addition of progesterone/progesterone-β cyclodextrin complex dissolved in propylene glycol then neutralization. The potential use of β cyclodextrin (CD) as nasal absorption enhancer by simple addition, as a physical mixture and as a complex with progesterone was investigated. The absolute bioavailability of progesterone from nasal gels in rabbits was studied by estimating the serum progesterone level by competitive solid-phase enzyme immunoassay in comparison to intravenous injection. The carbopol gel formulations produced a significant increase in bioavailability. CD complex promotes the nasal absorption of progesterone from carbopol gels as compared with gels where the CD is added by simple addition and gels which do not contain CD. This method of addition of CD as an inclusion complex in the gels could be considered as a preferred platform in nasal drug administration.
This study investigates the preparation of colon specific drug delivery of diclofenac sodium (DS) using maltiparticulate system with chitosan phthalate (CP). Technique adopted to prepare sphere shaped multiparticulate system was extrusion and spheronization. The prepared pellets resulted with good spherical geometry with 1.1 ± 0.20 mm diameter. DS loaded system shows a maximum delivery pH of 7.4 and the same depressed at pH 1.2. The developed system significantly (p < .05) increase in the peak plasma concentration (C max ) of DS pellets when compared to that of pure DS. As expected the novel formulation showed a significant increase in oral bioavailability of DS for about three times. Additionally, the CP pellets of DS showed a momentous improvement in anti-inflammatory activity and reduced/ inhibited ulcer index.
K E Y W O R D Schitosan phthalate, in vivo, pH dependent, sustained release
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