Photodegradation kinetic study and stability-indicating assay of danazol using high-performance liquid chromatography

Kariem, Elrasheed A. Gad; Abounassif, Mohammad A.; Hagga, M. E. M.; Al-Khamees, Hamad A.

doi:10.1016/s0731-7085(00)00315-0

Cited by 22 publications

(5 citation statements)

References 5 publications

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“…The apparent decline of solubility with danazol FeSSIF above 400 min is likely due to photodecomposition of the compound. 36 Only the early time points were therefore used to characterize the solubility reported. and the inclusion of taurocholic acid and lecithin in the FaSSIF and FeSSIF, allowed the powder material to be wetted.…”

Section: Discussionmentioning

confidence: 99%

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Dissolution Rate and Apparent Solubility of Poorly Soluble Drugs in Biorelevant Dissolution Media

et al. 2010

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A series of poorly soluble BCS class II compounds with "grease ball" characteristics were assessed for solubility and dissolution rate in biorelevant dissolution media (BDM) with the purpose of investigating which molecular structures gain most in solubility when dissolved under physiologically relevant conditions. The compounds were studied in four media (simulated intestinal fluid in fasted (FaSSIF pH 6.5) and fed state (FeSSIF pH 5.0), and their corresponding blank buffers (FaSSIF(blk) and FeSSIF(blk))) at a temperature of 37 °C. The experimental results were used to analyze which molecular characteristics are of importance for the solubility in BDM and for in silico modeling using multivariate data analysis. It was revealed that a majority of the compounds exhibited a higher dissolution rate and higher solubility in the FaSSIF and FeSSIF than in their corresponding blank buffers. Compounds which were neutral or carried a positive charge were more soluble in FeSSIF than FaSSIF. The acidic compounds displayed clear pH dependency, although the higher concentration of solubilizing agents in FeSSIF than FaSSIF also improved the solubility. Five of the ten compounds were upgraded to BCS class I when dissolved in FaSSIF or FeSSIF, i.e., the maximum dose of these compounds given orally was soluble in 250 mL of these BDMs. Lipophilicity as described by the log D(oct) value was identified as a good predictor of the solubilization ratio (R(2) = 0.74), and computed molecular descriptors were also shown to successfully predict the solubilities in BDM for this data set. To conclude, the physiological solubility of "grease ball" molecules may be largely underestimated in in vitro solubility assays unless BDM is used. Moreover, the results herein indicate that the improvement obtained in BDM may be possible to predict from chemical features alone.

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Section: Discussionmentioning

confidence: 99%

“…The three compounds were essentially neutral at pH 5.0 and 6.5. The apparent decline of solubility with danazol FeSSIF above 400 min is likely due to photodecomposition of the compound 36. Only the early time points were therefore used to characterize the solubility reported.…”

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confidence: 99%

Dissolution Rate and Apparent Solubility of Poorly Soluble Drugs in Biorelevant Dissolution Media

et al. 2010

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“…The danazol content in the formulations was determined by reversed-phase HPLC, a slightly modified version of a validated method previously described by Gadkariem et al (28). A Hitachi system from Merck (Darmstadt, Germany) was used, equipped with a D-7000 interface, an L-7200 autosampler, an L-7100 pump, an L-7300 column oven (30°C), and an L-7400 UV detector.…”

Section: Quantitative Analysis Of Danazol In Vehicles and Formulationsmentioning

confidence: 99%

Lipid-based Formulations for Danazol Containing a Digestible Surfactant, Labrafil M2125CS: In Vivo Bioavailability and Dynamic In Vitro Lipolysis

et al. 2008

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“…A quantitative TLC method has been reported for the validation of the purity analysis of DZ and its capsules [5]. HPLC has been frequently applied to the analysis of DZ in bulk form [6] pharmaceutical formulations [7][8][9][10][11] and biological fluids [11][12][13][14][15][16][17]. Gas chromatography [18,19] and immunoassay [20,21] was also reported.…”

Section: Introductionmentioning

confidence: 99%

Voltammetric study of danazol and its determination in capsules and spiked biological fluids

Al-Omar

Al-Majed

Sultan

et al. 2005

Journal of Pharmaceutical and Biomedical Analysis

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Photodegradation kinetic study and stability-indicating assay of danazol using high-performance liquid chromatography

Cited by 22 publications

References 5 publications

Dissolution Rate and Apparent Solubility of Poorly Soluble Drugs in Biorelevant Dissolution Media

Dissolution Rate and Apparent Solubility of Poorly Soluble Drugs in Biorelevant Dissolution Media

Lipid-based Formulations for Danazol Containing a Digestible Surfactant, Labrafil M2125CS: In Vivo Bioavailability and Dynamic In Vitro Lipolysis

Voltammetric study of danazol and its determination in capsules and spiked biological fluids

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