Tags

Type your tag names separated by a space and hit enter

Enhancement of the dissolution rate and oral absorption of a poorly water soluble drug by formation of surfactant-containing microparticles.
Int J Pharm. 2006 Jul 06; 317(1):61-8.IJ

Abstract

The slow dissolution rate exhibited by poorly water-soluble drugs is a major challenge in the drug development process. Following oral administration, drugs with slow dissolution rates generally show erratic and incomplete absorption which may lead to therapeutic failure. The aim of this study was to improve the dissolution rate and subsequently the oral absorption and bioavailability of a model poorly water-soluble drug. Microparticles containing the model drug (griseofulvin) were produced by spray drying the drug in the absence/presence of a hydrophilic surfactant. Poloxamer 407 was chosen as the hydrophilic surfactant to improve the particle wetting and hence the dissolution rate. The spray dried particles were characterized and in vitro dissolution studies and in vivo absorption studies were carried out. The results obtained showed that the dissolution rate and absolute oral bioavailability of the spray dried griseofulvin/Poloxamer 407 particles were significantly increased compared to the control. Although spray drying griseofulvin alone increased the drug's in vitro dissolution rate, no significant improvement was seen in the absolute oral bioavailability when compared to the control. Therefore, it is believed that the better wetting characteristics conferred by the hydrophilic surfactant was responsible for the enhanced dissolution rate and absolute oral bioavailability of the model drug.

Authors+Show Affiliations

School of Pharmacy, University of London, 29/39 Brunswick Square, London WC1N 1AX, United Kingdom.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

16647232

Citation

Wong, S M., et al. "Enhancement of the Dissolution Rate and Oral Absorption of a Poorly Water Soluble Drug By Formation of Surfactant-containing Microparticles." International Journal of Pharmaceutics, vol. 317, no. 1, 2006, pp. 61-8.
Wong SM, Kellaway IW, Murdan S. Enhancement of the dissolution rate and oral absorption of a poorly water soluble drug by formation of surfactant-containing microparticles. Int J Pharm. 2006;317(1):61-8.
Wong, S. M., Kellaway, I. W., & Murdan, S. (2006). Enhancement of the dissolution rate and oral absorption of a poorly water soluble drug by formation of surfactant-containing microparticles. International Journal of Pharmaceutics, 317(1), 61-8.
Wong SM, Kellaway IW, Murdan S. Enhancement of the Dissolution Rate and Oral Absorption of a Poorly Water Soluble Drug By Formation of Surfactant-containing Microparticles. Int J Pharm. 2006 Jul 6;317(1):61-8. PubMed PMID: 16647232.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Enhancement of the dissolution rate and oral absorption of a poorly water soluble drug by formation of surfactant-containing microparticles. AU - Wong,S M, AU - Kellaway,I W, AU - Murdan,S, Y1 - 2006/05/02/ PY - 2005/12/15/received PY - 2006/03/02/revised PY - 2006/03/04/accepted PY - 2006/5/2/pubmed PY - 2006/12/13/medline PY - 2006/5/2/entrez SP - 61 EP - 8 JF - International journal of pharmaceutics JO - Int J Pharm VL - 317 IS - 1 N2 - The slow dissolution rate exhibited by poorly water-soluble drugs is a major challenge in the drug development process. Following oral administration, drugs with slow dissolution rates generally show erratic and incomplete absorption which may lead to therapeutic failure. The aim of this study was to improve the dissolution rate and subsequently the oral absorption and bioavailability of a model poorly water-soluble drug. Microparticles containing the model drug (griseofulvin) were produced by spray drying the drug in the absence/presence of a hydrophilic surfactant. Poloxamer 407 was chosen as the hydrophilic surfactant to improve the particle wetting and hence the dissolution rate. The spray dried particles were characterized and in vitro dissolution studies and in vivo absorption studies were carried out. The results obtained showed that the dissolution rate and absolute oral bioavailability of the spray dried griseofulvin/Poloxamer 407 particles were significantly increased compared to the control. Although spray drying griseofulvin alone increased the drug's in vitro dissolution rate, no significant improvement was seen in the absolute oral bioavailability when compared to the control. Therefore, it is believed that the better wetting characteristics conferred by the hydrophilic surfactant was responsible for the enhanced dissolution rate and absolute oral bioavailability of the model drug. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/16647232/Enhancement_of_the_dissolution_rate_and_oral_absorption_of_a_poorly_water_soluble_drug_by_formation_of_surfactant_containing_microparticles_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(06)00198-0 DB - PRIME DP - Unbound Medicine ER -