Dissolution of ionizable water-insoluble drugs: The combined effect of pH and surfactant
dc.contributor.author | Jinno, Junichi | en_US |
dc.contributor.author | Oh, Doo-man | en_US |
dc.contributor.author | Crison, John R. | en_US |
dc.contributor.author | Amidon, Gordon L. | en_US |
dc.date.accessioned | 2006-04-19T13:37:10Z | |
dc.date.available | 2006-04-19T13:37:10Z | |
dc.date.issued | 2000-02 | en_US |
dc.identifier.citation | Jinno, Junichi; Oh, Doo-man; Crison, John R.; Amidon, Gordon L. (2000)."Dissolution of ionizable water-insoluble drugs: The combined effect of pH and surfactant." Journal of Pharmaceutical Sciences 89(2): 268-274. <http://hdl.handle.net/2027.42/34499> | en_US |
dc.identifier.issn | 0022-3549 | en_US |
dc.identifier.issn | 1520-6017 | en_US |
dc.identifier.uri | https://hdl.handle.net/2027.42/34499 | |
dc.identifier.uri | http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=retrieve&db=pubmed&list_uids=10688756&dopt=citation | en_US |
dc.description.abstract | This study reports the results of the combined effect of pH and surfactant on the dissolution of piroxicam (PX), an ionizable water-insoluble drug in physiological pH. The intrinsic dissolution rate ( J total ) of PX was measured in the pH range from 4.0 to 7.8 with 0%, 0.5%, and 2.0% sodium lauryl sulfate (SLS) using the rotating disk apparatus. Solubility ( c total ) was also measured in the same pH and SLS concentration ranges. A simple additive model including an ionization (PX ↔ H + + PX − ) and two micellar solubilization equilibria (PX + micelle ↔ [PX] micelle , PX − + micelle ↔ [PX − ] micelle ) were considered in the convective diffusion reaction model. J total and c total of PX increased with increasing pH and SLS concentration in an approximately additive manner. Nonlinear regression analysis showed that observed experimental data were well described with the proposed model ( r 2 = 0.86, P < 0.001 for J total and r 2 = 0.98, P < 0.001 for c total ). The p K a value of 5.63 ± 0.02 estimated from c total agreed well with the reported value. The micellar solubilization equilibrium coefficient for the unionized drug was estimated to be 348 ± 77 L/mol, while the value for the ionized drug was nearly equal to zero. The diffusion coefficients of the species PX, PX − , and [PX] micelle were estimated from the experimental results as (0.93 ± 0.35) × 10 −5 , (1.4 ± 0.30) × 10 −5 , and (0.59 ± 0.21) × 10 −5 cm 2 /s, respectively. The total flux enhancement is less than the total solubility enhancement due to the smaller diffusion coefficients of the micellar species. This model may be useful in predicting the dissolution of an ionizable water insoluble drug as a function of pH and surfactant and for establishing in vitro – in vivo correlations, IVIVC, for maintaining bioequivalence of drug products. © 2000 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 89: 268–274, 2000 | en_US |
dc.format.extent | 258869 bytes | |
dc.format.extent | 3118 bytes | |
dc.format.mimetype | application/pdf | |
dc.format.mimetype | text/plain | |
dc.language.iso | en_US | |
dc.publisher | John Wiley & Sons, Inc. | en_US |
dc.subject.other | Chemistry | en_US |
dc.subject.other | Food Science, Agricultural, Medicinal and Pharmaceutical Chemistry | en_US |
dc.title | Dissolution of ionizable water-insoluble drugs: The combined effect of pH and surfactant | en_US |
dc.type | Article | en_US |
dc.rights.robots | IndexNoFollow | en_US |
dc.subject.hlbsecondlevel | Pharmacy and Pharmacology | en_US |
dc.subject.hlbtoplevel | Health Sciences | en_US |
dc.description.peerreviewed | Peer Reviewed | en_US |
dc.contributor.affiliationum | College of Pharmacy, The University of Michigan, Ann Arbor, Michigan 48109-1065 | en_US |
dc.contributor.affiliationum | College of Pharmacy, The University of Michigan, Ann Arbor, Michigan 48109-1065 | en_US |
dc.contributor.affiliationum | College of Pharmacy, The University of Michigan, Ann Arbor, Michigan 48109-1065 ; College of Pharmacy, The University of Michigan, Ann Arbor, Michigan 48109-1065 | en_US |
dc.contributor.affiliationother | PORT Systems LLC, 540 Avis Drive, Ann Arbor, Michigan 48108 | en_US |
dc.identifier.pmid | 10688756 | en_US |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/34499/1/14_ftp.pdf | en_US |
dc.identifier.doi | http://dx.doi.org/10.1002/(SICI)1520-6017(200002)89:2<268::AID-JPS14>3.0.CO;2-F | en_US |
dc.identifier.source | Journal of Pharmaceutical Sciences | en_US |
dc.owningcollname | Interdisciplinary and Peer-Reviewed |
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