Development and Validation of a Discriminatory Dissolution Method for Rifaximin Products

Dharani, Sathish; Ali, Sogra F. Barakh; Afrooz, Hamideh; Khan, Mansoor A.; Rahman, Ziyaur

doi:10.1016/j.xphs.2019.01.020

Cited by 10 publications

(4 citation statements)

References 24 publications

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“…Physical Degradation: Bell shapes or plateaus during dissolution may also demonstrate (beyond the lack of enough solubility or medium volume to dissolve the full drug dose) that a polymorphic drug transition happens or that there is a polymorphic impurity in the drug substance. For example, the mixture of different polymorphic forms with different solubility values will lead to a variation in the rate and extent of dissolution . Precipitation from an amorphous to a crystalline form, or from a salt/cocrystal to its free form, will lead to a change in dissolution rate or even to complete stop of drug dissolution if the precipitation occurs on the surface of the drug product. , The presence of cosolvents or polymers can also change the rate and extent of surface precipitation, and, where relevant, such excipients should be considered critical to the product performance …”

Section: Discussionmentioning

confidence: 99%

“…For example, the mixture of different polymorphic forms with different solubility values will lead to a variation in the rate and extent of dissolution. 102 Precipitation from an amorphous to a crystalline form, or from a salt/cocrystal to its free form, will lead to a change in dissolution rate or even to complete stop of drug dissolution if the precipitation occurs on the surface of the drug product. 103,104 The presence of cosolvents or polymers can also change the rate and extent of surface precipitation, 105 and, where relevant, such excipients should be considered critical to the product performance.…”

Section: Q4: Which Are the Factors To Be Considered When Modeling Dis...mentioning

confidence: 99%

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Parameterization of Physiologically Based Biopharmaceutics Models: Workshop Summary Report

Pepin,

Arora,

Borges

et al. 2024

Mol. Pharmaceutics

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This Article shares the proceedings from the August 29th, 2023 (day 1) workshop "Physiologically Based Biopharmaceutics Modeling (PBBM) Best Practices for Drug Product Quality: Regulatory and Industry Perspectives". The focus of the day was on model parametrization; regulatory authorities from Canada, the USA, Sweden, Belgium, and Norway presented their views on PBBM case studies submitted by industry members of the IQ consortium. The presentations shared key questions raised by regulators during the mock exercise, regarding the PBBM input parameters and their justification. These presentations also shed light on the regulatory assessment processes, content, and format requirements for future PBBM regulatory submissions. In addition, the day 1 breakout presentations and discussions gave the opportunity to share best practices around key questions faced by scientists when parametrizing PBBMs. Key questions included measurement and integration of drug substance solubility for crystalline vs amorphous drugs; impact of excipients on apparent drug solubility/supersaturation; modeling of acid−base reactions at the surface of the dissolving drug; choice of dissolution methods according to the formulation and drug properties with a view to predict the in vivo performance; mechanistic modeling of in vitro product dissolution data to predict in vivo dissolution for various patient populations/species; best practices for characterization of drug precipitation from simple or complex formulations and integration of the data in PBBM; incorporation of drug permeability into PBBM for various routes of uptake and prediction of permeability along the GI tract.

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Section: Discussionmentioning

confidence: 99%

Section: Q4: Which Are the Factors To Be Considered When Modeling Dis...mentioning

confidence: 99%

Parameterization of Physiologically Based Biopharmaceutics Models: Workshop Summary Report

Pepin,

Arora,

Borges

et al. 2024

Mol. Pharmaceutics

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“…Dissolution testing, a method that measures the extent and rate of an active ingredient's release from a solid substance dose into a solution, is widely employed to characterize and control the quality of various drug dosage forms, and is also used as a surrogate of in vivo behavior of various dosage forms. [12][13] The U.S. Food and Drug Administration (FDA) Center for Tobacco Products recommended dissolution testing of STPs for substantial equivalence determination between products. 2 Similarly, it can be employed as a one of the quality control tests for STPs.…”

Section: Introductionmentioning

confidence: 99%

Development and Validation Of A Discriminatory Dissolution Method for Portioned Moist Snuff and Snus

Rahman

Mohamed

Dharani

et al. 2022

Journal of Pharmaceutical Sciences

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“…Dissolution is one of the quality control tests to measure the performance of a drug product and is required by regulatory agencies [ 1 , 2 ]. Even though it does not completely simulate in vivo conditions, it can be used as a surrogate of the in vivo behavior of certain drugs [ 3 , 4 , 5 ]. Dissolution determines whether dosage forms is an immediate or extended release formulations, which will eventually determine the duration of the in vivo action and hence the frequency of administration.…”

Section: Introductionmentioning

confidence: 99%

Development of a Multivariate Predictive Dissolution Model for Tablets Coated with Cellulose Ester Blends

et al. 2020

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The focus of the present investigation was to develop a predictive dissolution model for tablets coated with blends of cellulose acetate butyrate (CAB) 171-15 and cellulose acetate phthalate (C-A-P) using the design of experiment and chemometric approaches. Diclofenac sodium was used as a model drug. Coating weight gain (X1, 5, 7.5 and 10%) and CAB 171-15 percentage (X2, 33.3, 50 and 66.7%) in the coating composition relative to C-A-P and were selected as independent variables by full factorial experimental design. The responses monitored were dissolution at 1 (Y1), 8 (Y2), and 24 (Y3) h. Statistically significant (p < 0.05) effects of X1 on Y1 and X2 on Y1, Y2, and Y3 were observed. The models showed a good correlation between actual and predicted values as indicated by the correlation coefficients of 0.964, 0.914, and 0.932 for Y1, Y2, and Y3, respectively. For the chemometric model development, the near infrared spectra of the coated tablets were collected, and partial least square regression (PLSR) was performed. PLSR also showed a good correlation between actual and model predicted values as indicated by correlation coefficients of 0.916, 0.964, and 0.974 for Y1, Y2, and Y3, respectively. Y1, Y2, and Y3 predicted values of the independent sample by both approaches were close to the actual values. In conclusion, it is possible to predict the dissolution of tablets coated with blends of cellulose esters by both approaches.

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Development and Validation of a Discriminatory Dissolution Method for Rifaximin Products

Cited by 10 publications

References 24 publications

Parameterization of Physiologically Based Biopharmaceutics Models: Workshop Summary Report

Parameterization of Physiologically Based Biopharmaceutics Models: Workshop Summary Report

Development and Validation Of A Discriminatory Dissolution Method for Portioned Moist Snuff and Snus

Development of a Multivariate Predictive Dissolution Model for Tablets Coated with Cellulose Ester Blends

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