A Partially Organic Dissolution Medium for Griseofulvin Dosage Forms

Walkling, W. Douglas; Nayak, R. K.; Plostnieks, Janis; Cressman, William A.

doi:10.3109/03639047909055659

Cited by 8 publications

(2 citation statements)

References 6 publications

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“…The addition of glycerol, propylene glycol and ethanol as co‐solvents were tested and while all three increased solubility, ethanol was the most effective [40] . However, the addition of such solvents has no physiological relevance to the environment in which the drug dissolves, [42] while an increase in dissolution variability may be observed as a result of an interaction between some of the tablet components and the co‐solvents within the dissolution medium [43] …”

Section: Methods For Maintaining Dissolution Sink Conditionsmentioning

confidence: 99%

Overcoming sink limitations in dissolution testing: a review of traditional methods and the potential utility of biphasic systems

Phillips

Pygall²,

Cooper³

et al. 2012

Journal of Pharmacy and Pharmacology

169

109

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Objectives The conventional dissolution test, particularly the USP apparatus I and II, remains an important tool in the armory of the pharmaceutical development scientist. For realistic dissolution characterization, sink conditions, where saturation solubility of a drug in the dissolution medium is at least three times more than the drug concentration, are critical. These conditions can be problematic to maintain with formulations containing poorly-soluble actives. This review summarizes the role of the dissolution test in the pharmaceutical industry, together with some traditional techniques/additives used to enhance solubility and facilitate the achievement of sink conditions. The biphasic dissolution system, an innovative model for the treatment of poorly-soluble species, will also be discussed. Key findings The biphasic dissolution model utilizes media comprising immiscible aqueous and organic layers whereby the drug, following initial aqueous dissolution, partitions into the organic layer. This step, which acts to remove all dissolved species from the aqueous layer, enables further aqueous dissolution to occur and hence the dissolution-partition cycle continues. Crucially, the aqueous layer does not saturate allowing sink conditions to be maintained and hence the experiment will, in theory, yield complete dissolution. Summary This review highlights important concepts regarding solubility/sink limitation and intends to provoke debate among analytical and formulation scientists as to the potential advantages, long-term development and widespread implementation of a biphasic dissolution system in drug development.

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Section: Methods For Maintaining Dissolution Sink Conditionsmentioning

confidence: 99%

Overcoming sink limitations in dissolution testing: a review of traditional methods and the potential utility of biphasic systems

Phillips

Pygall²,

Cooper³

et al. 2012

Journal of Pharmacy and Pharmacology

169

109

View full text Add to dashboard Cite

show abstract

“…Equally, hydrophobic cosolvents are useful at improving solubility though they provide no physiological relevance (31). Such solvents also carry the risk of an increase in dissolution variability as a result of an interaction between some of the tablet components and the medium cosolvents (32).…”

Section: Introductionmentioning

confidence: 99%

Toward Biorelevant Dissolution: Application of a Biphasic Dissolution Model as a Discriminating Tool for HPMC Matrices Containing a Model BCS Class II Drug

Phillips¹,

Pygall²,

Cooper³

et al. 2012

Dissolution Technol.

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The potential of a biphasic dissolution system to assist with the analysis of controlled-release (CR), Biopharmaceutics Classification System (BCS) Class II pharmaceutical products has been investigated. Use of a biphasic dissolution medium (aqueous/octanol) provided sink conditions and afforded complete dissolution of nifedipine formulated in a CR matrix tablet while maintaining the dosage form in an aqueous environment. This was not possible in a monophasic (aqueousonly) dissolution medium. Consequently, the biphasic model allowed the discrimination of three formulations containing different HPMC loadings while the monophasic medium did not. The performance of the formulations in conventional dissolution media incorporating the inorganic salt dibasic sodium phosphate, the surfactant sodium dodecyl sulfate (SDS), and ethanol as solubility modifiers was assessed. The addition of the salt and surfactant failed to produce complete discrimination in a predictive manner. The use of a hydroalcoholic medium comprising water and ethanol enabled the statistical discrimination of the three formulations but not as effectively as the biphasic medium.

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In vitro dissolution medium with supramicellar surfactant concentration and its relevance for in vivo absorption

Gander

Ventouras²,

Gurny

et al. 1985

International Journal of Pharmaceutics

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A Partially Organic Dissolution Medium for Griseofulvin Dosage Forms

Cited by 8 publications

References 6 publications

Overcoming sink limitations in dissolution testing: a review of traditional methods and the potential utility of biphasic systems

Overcoming sink limitations in dissolution testing: a review of traditional methods and the potential utility of biphasic systems

Toward Biorelevant Dissolution: Application of a Biphasic Dissolution Model as a Discriminating Tool for HPMC Matrices Containing a Model BCS Class II Drug

In vitro dissolution medium with supramicellar surfactant concentration and its relevance for in vivo absorption

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