Acceptable Analytical Practices for Dissolution Testing of Poorly Soluble Compounds

Brown, Cynthia K.; Chokshi, Hitesh; Nickerson, Beverly; Reed, Robert A.; Rohrs, Brian R.; Shah, Pankaj A.

doi:10.14227/dt120405p6

Cited by 57 publications

(80 citation statements)

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“…[12][13][14] The selection of dissolution apparatus also plays a key role for the establishment of discriminatory dissolution methodologies. 15,16) The United States Pharmacopeia (USP) Apparatus 3 (Reciprocating cylinder or BioDis) was specifically designed for dissolution evaluation of MR dosage forms because it can mimic physicochemical and mechanical changes experienced by a MR dosage form in the GIT. [17][18][19] In addition, this apparatus demonstrates superior hydrodynamic controls in comparison to USP apparatuses 1 and 2 and provides numerous options in terms of instrumental parameters, such as composition of the media, pH and agitation rate.…”

mentioning

confidence: 99%

Development of a Dissolution Method for Gliclazide Modified-Release Tablets Using USP Apparatus 3 with <i>in Vitro–in Vivo</i> Correlation

Bezerra

Pinto

Cabral

et al. 2018

CHEMICAL & PHARMACEUTICAL BULLETIN

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Gliclazide (GLZ) is a second generation hypoglycemic drug used for the treatment of Type 2 diabetes mellitus. The low solubility of GLZ has been described as the rate limiting step for drug dissolution and absorption, thus a prediction of its in vivo behavior based on a discriminative dissolution test should lead to a relevant in vitro-in vivo correlation (IVIVC). The aim of this study was to develop a dissolution method for GLZ modified-release (MR) tablets using an United States Pharmacopeia (USP) apparatus 3 through its evaluation by an IVIVC analysis. Various dissolution parameters were evaluated to establish an in vitro method for GLZ tablets. The final dissolution conditions, referred to as method 3, utilized a 400 µm mesh and 30 dips per minute over a total period of 10 h that included 1h in HCl media (pH 1.2), 2h in acetate buffer solution (pH 4.5), 1 h in phosphate buffer solution (PBS; pH 5.8), 5h in PBS (pH 6.8) and finally 1h in PBS (pH 7.2). The calculated point-to-point IVIVC (R 2 0.9970) was significantly greater than other methods. The robustness of method 3 suggests it could be applied to pharmaceutical equivalence studies and for quality control analyses of GLZ.

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mentioning

confidence: 99%

Development of a Dissolution Method for Gliclazide Modified-Release Tablets Using USP Apparatus 3 with <i>in Vitro–in Vivo</i> Correlation

Bezerra

Pinto

Cabral

et al. 2018

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Subsequently, the method should be able to identify changes that occur during the production process and drug formulation. Therefore, the appropriate apparatus, rotation speed, volume and composition of the dissolution medium, pH, ionic strength, and surfactant must be selected (37,39). The dissolution apparatus commonly used for ER are Apparatus 1 (basket), 2 (paddle), and 3 (reciprocating cylinder).…”

Section: Development Of the Dissolution Testmentioning

confidence: 99%

“…Conditions such as mild agitation are commonly used to provide discriminating power of the dissolution method (28,39). In the case of Apparatus 1, rotation speeds between 50 and 100 rpm are usually employed (28,32), thus the rotation speeds of 50, 75, and 100 rpm were evaluated in this work.…”

Section: Dissolution Profile Using a Basket (Usp Apparatus 1)mentioning

confidence: 99%

Development of a Dissolution Test for Extended-Release Bromopride Pellets with In Vivo–In Vitro Correlation

Giovani¹,

Silva²,

Volpato³

et al. 2015

Dissolution Technol.

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The aim of this study was the development of a dissolution test with IVIVC for extended-release bromopride (BPD) pellets using bioavailability data. BPD is a Biopharmaceutics Classification System Class 2 drug, and its absorption is primarily limited by its dissolution rate. Despite this, there are no reports describing a dissolution test for BPD dosage forms. The dissolution medium was selected based upon the sink condition and the gastrointestinal pH. Furthermore, USP Apparatus 1 and 3 were tested, and the dissolution method was compared with that outlined by the manufacturer of the reference drug. Deconvolution by the Wagner-Nelson method was used to obtain the fraction of drug absorbed. The dissolution test that yielded IVIVC for both the fasted and fed states (R 2 > 0.97) and also the discriminative power used Apparatus 1 at 75 rpm in 900 mL of HCl. The dissolution medium (900 mL PBS pH 7.2) was changed after 1 h. Additionally, quantitative analysis was successfully validated by UV absorption (273 nm). Drug release is controlled by the pellet coating and by BPD solubility. The Higuchi release kinetics model best describes the dissolution of commercial BPD pellets batches.

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“…The selection of a dissolution medium may be based on the solubility data and dosage range of the drug product [24,30]. Hydrochloric acid, acetate buffer, phosphate buffer and purified water are typical mediums used to dissolution test [24], and these mediums were evaluated.…”

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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Acceptable Analytical Practices for Dissolution Testing of Poorly Soluble Compounds

Cited by 57 publications

References 0 publications

Development of a Dissolution Method for Gliclazide Modified-Release Tablets Using USP Apparatus 3 with <i>in Vitro–in Vivo</i> Correlation

Development of a Dissolution Method for Gliclazide Modified-Release Tablets Using USP Apparatus 3 with <i>in Vitro–in Vivo</i> Correlation

Development of a Dissolution Test for Extended-Release Bromopride Pellets with In Vivo–In Vitro Correlation

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

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