In Vitro–In Vivo Correlation for Desvenlafaxine Succinate Monohydrate Extended Release Tablets

Silva, Jéssica Domingos da; Sousa, Valéria Pereira de; Cabral, Lúcio Mendes; Davanço, Marcelo Gomes; Meulman, Jessica; Carvalho, Patrícia de Oliveira; Campos, Daniel Rossi de

doi:10.1208/s12249-020-01740-x

Cited by 4 publications

(4 citation statements)

References 23 publications

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“…When comparing this specification with the one presented by Da Silva et al (2020) [ 16 ], a difference can be observed, mainly at 4 h and 8 h, since the authors proposed a slightly lower range (4 h: 28–48%; 8 h: 48–68%), which may be attributed to the use of basket apparatus. It is worth mentioning that each specification is related to the dissolution method employed.…”

Section: Resultsmentioning

confidence: 62%

“…Thus, it was maintained as 0.9% NaCl, as suggested by the FDA for desvenlafaxine ER tablets [ 9 ]. In a recent study, Da Silva et al (2020) [ 16 ] suggested the use of the basket apparatus at 75 rpm and a reduced volume of dissolution medium (500 mL) as a biorelevant method. However, according to the low hydrodynamics of the basket, as previously discussed, we decided to consider, as biopredictive, the following dissolution method: 900 mL of 0.9% NaCl and paddle at 50 rpm with sinker, which does not interfere with the performance of the matrix system.…”

Section: Resultsmentioning

confidence: 99%

“…The release profiles obtained from different dissolution test conditions as described in Table 3 were used as input data in the software. For each dissolution profile, a drug record was created in which the plasma concentration–time curve of the reference drug product Pristiq™ 50 mg ER tablets was used as an opd file, from a bioequivalence study conducted with 44 healthy volunteers aged between 18–50 years [ 16 ].…”

Section: Methodsmentioning

confidence: 99%

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Development of Biopredictive Dissolution Method for Extended-Release Desvenlafaxine Tablets

Carapeto,

Duque,

Issa

et al. 2023

Pharmaceutics

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This study aimed to develop a biopredictive dissolution method for desvenlafaxine ER tablets using design of experiments (DoE) and physiologically based biopharmaceutics modeling (PBBM) to address the challenge of developing generic drug products by reducing the risk of product failure in pivotal bioequivalence studies. For this purpose, a PBBM was developed in GastroPlus® and combined with a Taguchi L9 design, to evaluate the impact of different drug products (Reference, Generic #1 and Generic #2) and dissolution test conditions on desvenlafaxine release. The influence of the superficial area/volume ratio (SA/V) of the tablets was observed, mainly for Generic #1, which presented higher SA/V than the others, and a high amount of drug dissolved under similar test conditions. The dissolution test conditions of 900 mL of 0.9% NaCl and paddle at 50 rpm with sinker showed to be biopredictive, as it was possible to demonstrate virtual bioequivalence for all products, despite their release-pattern differences, including Generic #3 as an external validation. This approach led to a rational development of a biopredictive dissolution method for desvenlafaxine ER tablets, providing knowledge that may help the process of drug product and dissolution method development.

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Section: Resultsmentioning

confidence: 62%

Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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Development of Biopredictive Dissolution Method for Extended-Release Desvenlafaxine Tablets

Carapeto,

Duque,

Issa

et al. 2023

Pharmaceutics

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“…O -desmethylvenlafaxine ( Deecher et al, 2006 ; Sopko et al, 2008 ; Venu et al, 2008 ; Liu et al, 2016 ; Da Silva et al, 2020 ; Gahr et al, 2020 ) is the major active metabolite of the third serotonin-norepinephrine reuptake inhibitor (SNRI) venlafaxine approved by the US Food and Drug Administration for major depressive disorder (MDD), used to treat mild or severe depression, anxiety, and other mental disorders with superior clinical advantages ( Klamerus et al, 1992 ; Safer and Zito, 2019 ; Zhang et al, 2019 ; Agüera-Ortiz et al, 2020 ). The efficacy, safety, or tolerability of preparation prescription drugs developed through O -desmethylvenlafaxine succinate (@Pristiq) has been favored by more and more psychiatrists as their first choice for the treatment of depression and anxiety ( Khandpekar et al, 2014 ; Llorca et al, 2019 ).…”

Section: Introductionmentioning

confidence: 99%

Advances in Research at Synthesis Process Optimization and Quality Standard Improvement of O-desmethylvenlafaxine Succinate

et al. 2022

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We herein describe an optimal approach for the efficient synthesis of O-desmethylvenlafaxine succinate monohydrate (DVS) with high yield and high purity through 5-step reactions, including benzyl protection of the phenolic hydroxyl group, cyclohexanone condensation, deprotection, cyano reduction, dimethylation, and succinic acid salt formation from p-hydroxybenzene acetonitrile as a starting material. 4-Benzyloxyphenylacetonitrile (Intermediate I) was prepared by the hydroxyl protection of the bromide benzyl-p-hydroxyphenylacetonitrile catalyzed by potassium carbonate with 99.83% purity and 98.92% yields. The 1, 2-nucleophilic addition of intermediate I to cyclohexanone promoted by sodium hydroxide with the homogeneous catalyst (n-Bu)4N+Br− to the preparation of 1-[Cyano(4-benzyloxyphenyl)methyl]cyclohexanol (Intermediate II) was obtained by 99.13% purity and 99.71% yields. Cyclohexanone residues and benzyl bromide residues were trace, and tetrabutylammonium bromide residues were UNDER 0.7 ppm, which further improves the residual standards for genotoxic impurities (GIs). 1-[2-amino-1-(4-hydroxyphenyl)ethyl]cyclohexanol hydrochloride (Intermediate III) was prepared by 10% palladium-carbon under 2.0 MPa up to 98.32% purity and 94.20% yields. O-desmethylvenlafaxine (ODV) was synthesized by dimethylation of intermediate III with 37% formaldehyde solution and 85% formic acid solution. The highest purity was up to 99.20% and the yield was up to 84.77%. O-desmethylvenlafaxine succinate monohydrate (DVS) was formed from succinic acid and O-desmethylvenlafaxine (ODV) and crystallized in a mixed solvent of acetone and water (3:1) to obtain 99.92% purity and 90.27% yields. The 5-step total yields of desvenlafaxine succinate monohydrate is 71.09%, and its crystal form has characteristic peaks at 5, 10, 21, and 26 min by XRD powder diffraction, which is consistent with the crystalline form I. Compared with conventional synthesis strategy, we revealed a novel and green process with a high total yield, high atomic economy, low environmental pollution, high operational safety, and high residual standards for genotoxic impurities (GIs), which improves drug safety.

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Recent Advances in Dissolution Testing and Their Use to Improve In Vitro–In Vivo Correlations in Oral Drug Formulations

Ranjan

Jha

2021

J Pharm Innov

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In Vitro–In Vivo Correlation for Desvenlafaxine Succinate Monohydrate Extended Release Tablets

Cited by 4 publications

References 23 publications

Development of Biopredictive Dissolution Method for Extended-Release Desvenlafaxine Tablets

Development of Biopredictive Dissolution Method for Extended-Release Desvenlafaxine Tablets

Advances in Research at Synthesis Process Optimization and Quality Standard Improvement of O-desmethylvenlafaxine Succinate

Recent Advances in Dissolution Testing and Their Use to Improve In Vitro–In Vivo Correlations in Oral Drug Formulations

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