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Development of an itraconazole-loaded gelatin microcapsule with enhanced oral bioavailability: physicochemical characterization and in-vivo evaluation.
J Pharm Pharmacol. 2010 Apr; 62(4):448-55.JP

Abstract

OBJECTIVES

The aim of this study was to develop a novel itraconazole-loaded gelatin microcapsule without ethanol with enhanced oral bioavailability.

METHODS

Various gelatin microcapsules were prepared using a spray-drying technique. Their physicochemical properties, dissolution, characteristics and pharmacokinetics in rats were evaluated and compared with those of a commercial product.

KEY FINDINGS

The gelatin microcapsule at a weight ratio for itraconazole/gelatin/citric acid of 1 : 3 : 0.3 was spherical in shape with a smooth surface and inner hole, and gave a maximum drug solubility of about 700 microg/ml. The gelatin microcapsule dramatically increased the initial dissolution rate of itraconazole compared with a commercial product in simulated gastric fluids (pH 1.2). Moreover, at the same dose as the commercial product, it gave significantly higher initial plasma concentrations, C(max) and AUC of itraconazole in rats than did the commercial product, indicating that providing the drug in the gelatin microcapsule caused enhanced absorption in rats. At half dose, it gave similar AUC, C(max) and T(max) values to the commercial product, suggesting that it was bioequivalent to the commercial product in rats.

CONCLUSIONS

The itraconazole-loaded gelatin microcapsule without ethanol developed using a spray-drying technique at half the dose of the commercial product can deliver itraconazole in a pattern that allows fast absorption in the initial phase, making it bioequivalent to the commercial product.

Authors+Show Affiliations

College of Pharmacy, Yeungnam University, Dae-Dong, Gyongsan, South Korea.No affiliation info availableNo affiliation info availableNo affiliation info availableNo 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

20604833

Citation

Li, Dong Xun, et al. "Development of an Itraconazole-loaded Gelatin Microcapsule With Enhanced Oral Bioavailability: Physicochemical Characterization and In-vivo Evaluation." The Journal of Pharmacy and Pharmacology, vol. 62, no. 4, 2010, pp. 448-55.
Li DX, Park YJ, Oh DH, et al. Development of an itraconazole-loaded gelatin microcapsule with enhanced oral bioavailability: physicochemical characterization and in-vivo evaluation. J Pharm Pharmacol. 2010;62(4):448-55.
Li, D. X., Park, Y. J., Oh, D. H., Joe, K. H., Lee, J. H., Yeo, W. H., Yong, C. S., & Choi, H. G. (2010). Development of an itraconazole-loaded gelatin microcapsule with enhanced oral bioavailability: physicochemical characterization and in-vivo evaluation. The Journal of Pharmacy and Pharmacology, 62(4), 448-55. https://doi.org/10.1211/jpp.62.04.0006
Li DX, et al. Development of an Itraconazole-loaded Gelatin Microcapsule With Enhanced Oral Bioavailability: Physicochemical Characterization and In-vivo Evaluation. J Pharm Pharmacol. 2010;62(4):448-55. PubMed PMID: 20604833.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of an itraconazole-loaded gelatin microcapsule with enhanced oral bioavailability: physicochemical characterization and in-vivo evaluation. AU - Li,Dong Xun, AU - Park,Young-Joon, AU - Oh,Dong Hoon, AU - Joe,Kwan Hyung, AU - Lee,Jung Hoon, AU - Yeo,Woo Hyun, AU - Yong,Chul Soon, AU - Choi,Han-Gon, PY - 2010/7/8/entrez PY - 2010/7/8/pubmed PY - 2011/1/15/medline SP - 448 EP - 55 JF - The Journal of pharmacy and pharmacology JO - J Pharm Pharmacol VL - 62 IS - 4 N2 - OBJECTIVES: The aim of this study was to develop a novel itraconazole-loaded gelatin microcapsule without ethanol with enhanced oral bioavailability. METHODS: Various gelatin microcapsules were prepared using a spray-drying technique. Their physicochemical properties, dissolution, characteristics and pharmacokinetics in rats were evaluated and compared with those of a commercial product. KEY FINDINGS: The gelatin microcapsule at a weight ratio for itraconazole/gelatin/citric acid of 1 : 3 : 0.3 was spherical in shape with a smooth surface and inner hole, and gave a maximum drug solubility of about 700 microg/ml. The gelatin microcapsule dramatically increased the initial dissolution rate of itraconazole compared with a commercial product in simulated gastric fluids (pH 1.2). Moreover, at the same dose as the commercial product, it gave significantly higher initial plasma concentrations, C(max) and AUC of itraconazole in rats than did the commercial product, indicating that providing the drug in the gelatin microcapsule caused enhanced absorption in rats. At half dose, it gave similar AUC, C(max) and T(max) values to the commercial product, suggesting that it was bioequivalent to the commercial product in rats. CONCLUSIONS: The itraconazole-loaded gelatin microcapsule without ethanol developed using a spray-drying technique at half the dose of the commercial product can deliver itraconazole in a pattern that allows fast absorption in the initial phase, making it bioequivalent to the commercial product. SN - 2042-7158 UR - https://www.unboundmedicine.com/medline/citation/20604833/Development_of_an_itraconazole_loaded_gelatin_microcapsule_with_enhanced_oral_bioavailability:_physicochemical_characterization_and_in_vivo_evaluation_ L2 - https://doi.org/10.1211/jpp.62.04.0006 DB - PRIME DP - Unbound Medicine ER -