Dissolution Kinetics of Griseofulvin in Mixed Micellar Solutions

Smidt, Jan H. de; Grit, Mustafa; Crommelin, Daan J.A.

doi:10.1002/jps.2600830904

Cited by 18 publications

(8 citation statements)

References 12 publications

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“…The intrinsic dissolution rate was plotted against the square root of rotational speed, apparent diffusion coefficients (Dapp) were calculated from the slopes of these plots using the Levich equation, 16 and kinematic viscosities of the solutions were derived from literature data. 17,18 StatisticssPaired Student's t-tests of the pharmacokinetic data and linear regression of the Levich plots were conducted using a standard statistical package (SigmaStat, Jandel Scientific, San Rafael, CA).…”

Section: Methodsmentioning

confidence: 99%

“…The data in Figure 6 are linear, indicating that dissolution of Hf‚HCl in NaTC and NaTC/lecithin solutions was convection-diffusion controlled, consistent with reports for other poorly water soluble drugs such as griseofulvin. 18,24 However, dissolution of Hf‚HCl cannot be completely accounted for by the convection-diffusion model as the intercepts of both plots were significantly greater than zero. Similar observations of a nonzero intercept have been reported for indomethacin 25 and phenylbutazone 26 where natural convection (which may occur at low rotational speeds) was suggested as an additional mechanism contributing to the dissolution process, although the basis for the non-zero intercept was not addressed.…”

Section: Intrinsic Dissolution Studiessthementioning

confidence: 97%

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A physicochemical Basis for the Effect of Food on the Absolute Oral Bioavailability of Halofantrine

Humberstone

Porter

Charman

1996

Journal of Pharmaceutical Sciences

122

134

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Halofantrine hydrochloride (Hf.HCl) is a highly lipophilic phenanthrenemethanol antimalarial. The poor and erratic absorption of Hf after oral administration has been implicated in some treatment failures. Food increases the oral bioavailability of Hf in humans approximately 3-5-fold, although neither the absolute bioavailability nor the basis for the food effect has been fully defined. In this study, the mean (+/-SD, n = 3) absolute oral bioavailability of 250 mg Hf.HCl tablets in beagles was 8.6 +/- 5.3% in the fasted state, which increased approximately 12-fold when administered postprandially. These data indicate that Hf.HCl is efficiently absorbed from the postprandial intestinal environment. The solubility and intrinsic dissolution rate of Hf.HCl were investigated as a function of bile salt concentration (sodium taurocholate, NaTC, 0-30 mM) and micellar composition (4:1 NaTC:lecithin). At premicellar (fasted) concentrations of NaTC (< 5 mM), the solubility and intrinsic dissolution rate were very low (< 15 micrograms/mL; < 0.01 microgram s-1 cm-2). At NaTC concentrations typical of the postprandial state, the solubility and dissolution rate improved dramatically. For example, solubility in 30 mM NaTC increased approximately 1000-fold relative to buffer control, with even greater enhancement (3000-fold) associated with mixed micellar systems. These data suggest that the improved absorption of Hf.HCl in the fed state is most likely due to the increased solubilization and dissolution of the drug in the presence of bile salt mixed micelles.

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Section: Methodsmentioning

confidence: 99%

Section: Intrinsic Dissolution Studiessthementioning

confidence: 97%

A physicochemical Basis for the Effect of Food on the Absolute Oral Bioavailability of Halofantrine

Humberstone

Porter

Charman

1996

Journal of Pharmaceutical Sciences

122

134

View full text Add to dashboard Cite

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“…Singh et al 6 investigated the influence of micelle-drug solubilization on the dissolution rate for the benzocainepolysorbate 80 system under different hydrodynamic models. De Smidt et al [7][8][9] reported the effect of sodium lauryl sulfate on the dissolution of griseofulvin, a poorly soluble drug. On the other hand, Mooney et al 10,11 investigated the effect of pH on the solubility and dissolution of ionizable drugs based on a film model with total component material balances for reactive species, proposed by Olander.…”

Section: Introductionmentioning

confidence: 99%

Dissolution of Ionizable Water‐Insoluble Drugs: The Combined Effect of pH and Surfactant

Jinno

Crison³

et al. 2000

Journal of Pharmaceutical Sciences

151

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“…Surfactants act as an absorption enhancer and increase drug dissolution and permeability by promoting wetting and penetration of dissolution fluid into the drug molecules (De Smidt, Grit, Crommelin, 1994). Both ionic and cationic surfactants are effective but anionic surfactants such as sodium lauryl sulphate (SLS) have higher solubility than cationic ones.…”

Section: Introductionmentioning

confidence: 99%

“…SLS has been proven as the agent of choice because it is inexpensive and possesses good solubilizing capacity at relatively low concentration. Various studies are available in the open literature that has highlighted the role of SLS as a solubility enhancer (De Smidt, Grit, Crommelin, 1994;Sun, Larive, Southard, 2003).…”

Section: Introductionmentioning

confidence: 99%

Formulation design and evaluation of Cefuroxime axetil 125 mg immediate release tablets using different concentration of sodium lauryl sulphate as solubility enhancer

Israr

Mahmood

Farahbakhsh

et al. 2014

Braz. J. Pharm. Sci.

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Cefuroxime axetil immediate release tablets were formulated by direct compression method with different percentages of sodium lauryl sulphate (SLS) such as 0.5, 1.0, 1.5 and also without SLS. Resulting batches of tablets were evaluated by both pharmacopeial and non-pharmacopeial methods to ascertain the physico-mechanical properties. Dissolution test were carried out in different medium like 0.07 M HCl, distilled water, 0.1M HCl of pH 1.2 and phosphate buffers at pH 4.5 and 6.8 to observe the drug release against the respective concentration of SLS used. Later, test formulations were compared by f1 (dissimilarity) and f2 (similarity) factors using a reference brand of cefuroxime axetil. Significant differences (p<0.05) in dissolution rate were recorded with the change in concentration of SLS in different media. Test formulation T3 containing 1% SLS was found to be best optimized formulation based on assay, disintegration, dissolution and similarity and dissimilarity factors. Uniterms:Cefuroxime axetil/immediate release tablets/physico-mechanical properties. Direct compression. Sodium lauryl sulphate.Formularam-se comprimidos de liberação imediata à base de cefuroxima axetil, pelo método de compressão direta, com diferentes percentagens de lauril sulfato de sódio (LSS), tais como 0,5, 1,0, 1,5, e também sem SLS. Os lotes resultantes dos comprimidos foram avaliados por ambos os métodos da farmacopeia e não farmacopeicos para determinar as propriedades físico-mecânicas. O teste de dissolução foi realizado em meios diferentes, como HCl 0,07 M, água destilada, HCl 0,1 M com pH 1,2 e os tampões fosfato (pH 4,5 e 6,8) para observar a liberação do fármaco contra a correspondente concentração de LSS utilizado. Em seguida, as formulações de teste foram comparadas por fatores f1 (dissimilaridade) e f2 (similaridade), utilizando uma marca de referência de cefuroxima axetil. Diferenças significativas (p<0,05) na taxa de dissolução foram registradas com a mudança na concentração de LSS em diferentes meios de dissolução. A formulação T3 contendo LSS a 1% foi considerada a melhor formulação otimizada com base nos ensaios de desintegração, dissolução e fatores de semelhança e dissimilaridade.Unitermos: Cefuroxima axetil/comprimidos de liberação imediata/propriedades físico-mecânicas. Compressão direta. Lauril sulfato de sódio.

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Dissolution Kinetics of Griseofulvin in Mixed Micellar Solutions

Cited by 18 publications

References 12 publications

A physicochemical Basis for the Effect of Food on the Absolute Oral Bioavailability of Halofantrine

A physicochemical Basis for the Effect of Food on the Absolute Oral Bioavailability of Halofantrine

Dissolution of Ionizable Water‐Insoluble Drugs: The Combined Effect of pH and Surfactant

Formulation design and evaluation of Cefuroxime axetil 125 mg immediate release tablets using different concentration of sodium lauryl sulphate as solubility enhancer

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