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Physicochemical characterization and in vivo evaluation of flurbiprofen-loaded solid dispersion without crystalline change.
Drug Deliv. 2011 Jan; 18(1):46-53.DD

Abstract

To develop a novel flurbiprofen-loaded solid dispersion without crystalline change, various flurbiprofen-loaded solid dispersions were prepared with water, sodium carboxylmethyl cellulose (Na-CMC), and Tween 80. The effect of Na-CMC and Tween 80 on aqueous solubility of flurbiprofen was investigated. The physicochemical properties of solid dispersions were investigated using SEM, DSC, and X-ray diffraction. The dissolution and bioavailability in rats were evaluated compared to commercial product. Unlike conventional solid dispersion systems, the flurbiprofen-loaded solid dispersion gave a relatively rough surface and changed no crystalline form of drug. These solid dispersions were formed by attaching hydrophilic carriers to the surface of drug without crystal change, resulting in changing the hydrophobic drug to hydrophilic form. Furthermore, the flurbiprofen-loaded solid dispersion at the weight ratio of flurbiprofen/Na-CMC/Tween 80 of 6/2.5/0.5 improved ~60-fold drug solubility. It gave higher AUC, T(max), and C(max) compared to commercial product. The solid dispersion improved almost 1.5-fold bioavailability of drug compared to commercial product in rats. Thus, the flurbiprofen-loaded solid dispersion would be useful to deliver poorly water-soluble flurbiprofen with enhanced bioavailability without crystalline change.

Authors+Show Affiliations

College of Pharmacy, Yeungnam University, 214-1 Dae-Dong, Gyongsan 712-749, South Korea.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

20726805

Citation

Oh, Dong Hoon, et al. "Physicochemical Characterization and in Vivo Evaluation of Flurbiprofen-loaded Solid Dispersion Without Crystalline Change." Drug Delivery, vol. 18, no. 1, 2011, pp. 46-53.
Oh DH, Park YJ, Kang JH, et al. Physicochemical characterization and in vivo evaluation of flurbiprofen-loaded solid dispersion without crystalline change. Drug Deliv. 2011;18(1):46-53.
Oh, D. H., Park, Y. J., Kang, J. H., Yong, C. S., & Choi, H. G. (2011). Physicochemical characterization and in vivo evaluation of flurbiprofen-loaded solid dispersion without crystalline change. Drug Delivery, 18(1), 46-53. https://doi.org/10.3109/10717544.2010.509365
Oh DH, et al. Physicochemical Characterization and in Vivo Evaluation of Flurbiprofen-loaded Solid Dispersion Without Crystalline Change. Drug Deliv. 2011;18(1):46-53. PubMed PMID: 20726805.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Physicochemical characterization and in vivo evaluation of flurbiprofen-loaded solid dispersion without crystalline change. AU - Oh,Dong Hoon, AU - Park,Young-Joon, AU - Kang,Jun Heok, AU - Yong,Chul Soon, AU - Choi,Han-Gon, Y1 - 2010/08/21/ PY - 2010/8/24/entrez PY - 2010/8/24/pubmed PY - 2011/3/18/medline SP - 46 EP - 53 JF - Drug delivery JO - Drug Deliv VL - 18 IS - 1 N2 - To develop a novel flurbiprofen-loaded solid dispersion without crystalline change, various flurbiprofen-loaded solid dispersions were prepared with water, sodium carboxylmethyl cellulose (Na-CMC), and Tween 80. The effect of Na-CMC and Tween 80 on aqueous solubility of flurbiprofen was investigated. The physicochemical properties of solid dispersions were investigated using SEM, DSC, and X-ray diffraction. The dissolution and bioavailability in rats were evaluated compared to commercial product. Unlike conventional solid dispersion systems, the flurbiprofen-loaded solid dispersion gave a relatively rough surface and changed no crystalline form of drug. These solid dispersions were formed by attaching hydrophilic carriers to the surface of drug without crystal change, resulting in changing the hydrophobic drug to hydrophilic form. Furthermore, the flurbiprofen-loaded solid dispersion at the weight ratio of flurbiprofen/Na-CMC/Tween 80 of 6/2.5/0.5 improved ~60-fold drug solubility. It gave higher AUC, T(max), and C(max) compared to commercial product. The solid dispersion improved almost 1.5-fold bioavailability of drug compared to commercial product in rats. Thus, the flurbiprofen-loaded solid dispersion would be useful to deliver poorly water-soluble flurbiprofen with enhanced bioavailability without crystalline change. SN - 1521-0464 UR - https://www.unboundmedicine.com/medline/citation/20726805/Physicochemical_characterization_and_in_vivo_evaluation_of_flurbiprofen_loaded_solid_dispersion_without_crystalline_change_ L2 - https://www.tandfonline.com/doi/full/10.3109/10717544.2010.509365 DB - PRIME DP - Unbound Medicine ER -