Steps for Development of a Dissolution Test for Sparingly Water-Soluble Drug Products

Noory, Carol; Tran, Nhan L.; Ouderkirk, Larry; Shah, Vinod P.

doi:10.14227/dt070100p16

Cited by 27 publications

(20 citation statements)

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“…The most common way to challenge the discriminatory power of the method is to test formulations with differences resulting from changes in the characteristics of the API, drug product composition, product manufacturing process, and stability conditions (11)(12)(13)(14)(15)(16). In general, mild agitation conditions should be maintained during dissolution testing to allow maximum discriminatory power (4).…”

Section: Discussionmentioning

confidence: 99%

Development of Discriminating Method for Dissolution of Aceclofenac Marketed Formulations

Soni¹,

Nagda²,

Gandhi³

et al. 2008

Dissolution Technol.

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The development of a meaningful dissolution procedure for drug products with limited water solubility has been a challenge to the pharmaceutical industry. Aceclofenac (BCS Class II drug) is a nonsteroidal anti-inflammatory drug. There is no official dissolution medium available in the literature. In the present study, parameters such as solubility, medium pH, surfactant type, dissolution behavior of formulations, influence of sink conditions, stability, and discriminatory effect of dissolution testing were studied for the selection of a proper dissolution medium. Results of solubility data revealed that solubility increased with an increase in pH. Sink conditions were exhibited in all media except double-distilled water and 0.1 N HCl. The drug and marketed formulations were stable in the dissolution media used. An agitation speed of 50 rpm showed a more discriminating drug release profile than 75 rpm. The discriminating dissolution method for aceclofenac formulation is paddle at 50 rpm, 900 mL pH 6.8 phosphate buffer, greater than 80% of the label amount is released over 60 minutes.

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Section: Discussionmentioning

confidence: 99%

Development of Discriminating Method for Dissolution of Aceclofenac Marketed Formulations

Soni¹,

Nagda²,

Gandhi³

et al. 2008

Dissolution Technol.

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“…If the concentration of surfactant is increased sufficiently, the bilayer becomes unstable and micelles are formed. The micelle consists of a hydrophilic shell and a hydrophobic core (10).…”

Section: Use Of Surfactants and Mixed Micellesmentioning

confidence: 99%

Dissolution Testing for Poorly Soluble Drugs: A Continuing Perspective

Kuppusamy¹

2010

Dissolution Technol.

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The development of a meaningful dissolution procedure for drug products with limited water solubility has been a challenge to both the pharmaceutical industry and the agencies that regulate them. These challenges include developing and validating the test methods, ensuring that methods are appropriately discriminatory, and addressing the potential for an in vivo-in vitro correlation (IVIVC). Dissolution test media selection should be justified for pH (recommended pH range is 1.2-7.5) as well as surfactant type (ionic versus non-ionic) and amount. If the drug is not soluble in the in vivo pH range, with or without surfactants, then the use of nonaqueous media can be preferred with proper justifications. Physical modifications of the drug, such as particle size reduction, use of metastable polymorphs, eutectic mixtures, solid dispersions, or complexation, are being widely used in the industry to enhance the drug dissolution characteristics. In recent years, newer physical modifications (e.g., microemulsions and nanocrystals) are giving promising results in enhancement of drug dissolution and bioavailability of poorly soluble drugs. Whatever method is used by the dissolution scientists, it must aim towards the cheaper but most effective approach to enhance the dissolution behavior of poorly soluble drugs.

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“…DAR was insoluble in acid mediums (0.1N HCl and acetate buffer pH 5.5) and showed a low solubility in sodium phosphate buffer pH 7.0. For poor soluble drugs, a percentage of surfactant can be used to enhance drug solubility [24,31]. Then, different concentrations of SLS (0.1, 0.25, 0.5 and 0.75%) were added to sodium phosphate buffer pH 7.0 medium to improve DAR solubility.…”

Section: Development Of Dissolution Test Conditionsmentioning

confidence: 99%

Development and Validation of a Dissolution Method with Spectrophotometric Analysis for Diacerhein Capsules

Borgmann¹,

Parcianello²,

Arend³

et al. 2008

Sci Pharm

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The aim of this work was to develop and validate a dissolution test for diacerhein in capsules using spectrophotometric method. The dissolution established conditions were: 900 mL of sodium phosphate buffer pH 7.0 with 0.75 % of sodium lauryl sulphate as dissolution medium, using a basket apparatus at a stirring rate of 50 rpm. The drug release was evaluated by UV spectrophotometric method at 258 nm. The method was validated to meet requirements for a global regulatory filing. The validation included specificity, linearity, precision and accuracy. In addition, filter suitability and drug stability in medium were demonstrated. The comparison of the obtained dissolution profiles of capsules, obtained from three different brands (denominate product A, B and C) of 50 mg diacerhein, was performed and the results showed no significative difference among the products.

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Steps for Development of a Dissolution Test for Sparingly Water-Soluble Drug Products

Cited by 27 publications

References 0 publications

Development of Discriminating Method for Dissolution of Aceclofenac Marketed Formulations

Development of Discriminating Method for Dissolution of Aceclofenac Marketed Formulations

Dissolution Testing for Poorly Soluble Drugs: A Continuing Perspective

Development and Validation of a Dissolution Method with Spectrophotometric Analysis for Diacerhein Capsules

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