Development of an Extended-Release Formulation for Apremilast and a Level A &lt;i&gt;in Vitro&lt;/i&gt;–&lt;i&gt;in Vivo&lt;/i&gt; Correlation Study in Beagle Dogs

Tang, Meiqiong; Hu, Ping; Shigui, Huang; Zheng, Qiang; Yu, Hao; He, Yun

doi:10.1248/cpb.c16-00519

Cited by 24 publications

(15 citation statements)

References 35 publications

(24 reference statements)

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“…The benefit of this approach is the effect of in vitro release rate on in vivo parameters like maximum plasma concentration ( C max ), time to reach C max ( t max ), AUC, and duration of action can be evaluated. A validated, two‐stage level A correlation has been reported with ER formulation of apremilasat by applying model dependent and numeric deconvolution approaches (Tang et al, ).…”

Section: Levels Of Ivivcmentioning

confidence: 99%

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An updated overview with simple and practical approach for developing in vitro–in vivo correlation

Jacob

Nair

2018

Drug Development Research

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Preclinical Research & Development An in vitro-in vivo correlation (IVIVC) is as a predictive mathematical model that demonstrates a key role in the development, advancement, evaluation and optimization of extended release, modified release and immediate release pharmaceutical formulations. A validated IVIVC model can serve as a surrogate for bioequivalence studies and subsequently save time, effort and expenditure during pharmaceutical product development. This review discusses about different levels of correlations, general approaches to develop an IVIVC by mathematical modelling, validation, data analysis and various applications. In the current setting, the dearth of success associated with IVIVC is due to complexity of underlying scientific principles as well as the practice of fitting/matching in vivo plasma level-time data with in vitro dissolution profile. Hence, a simple, straightforward practical means to predict plasma drug levels by convolution technique and percentage drug absorbed computed from in vitro dissolution profile based on deconvolution method are illustrated. The bioavailability/bioequivalence assessment and evaluation are frequently validated by the pharmacokinetic parameters such as maximum concentration, time to reach maximum concentration, and area under the curve. The implementation of a quality by design manufacturing based on in vivo bioavailability and clinically relevant dissolution specification are recommended because corresponding design safe space will guarantee that all batches from relevant products are met with sufficient quality and bioperformance. Recently, United States Food and Drug Administration and European Medicines Agency have proposed that in silico/physiologically based pharmacokinetic modelling can be used in decision making during preclinical experiments as well as to recognize the dissolution profiles that can forecast and ensure the desired clinical performance.

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Section: Levels Of Ivivcmentioning

confidence: 99%

“…Single stage or two-stage approach is generally used for estimating level A correlation. In a single stage approach, the plasma concentra- (Tang et al, 2016).…”

Section: Level a Model Approachmentioning

confidence: 99%

An updated overview with simple and practical approach for developing in vitro–in vivo correlation

Jacob

Nair

2018

Drug Development Research

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“…7,8 Therefore, an alternative Dovepress Dovepress 1588 anwer et al drug-delivery system is urgently required to overcome the tolerability and the frequent daily dosing and to improve the bioavailability of APM. Recently, Tang et al (2016) developed an extended release formulation of APM to resolve the dosing and tolerability issue. 9 Poly(D,L-lactide-coglycolide) (PLGA) is considered as a smart polymer, which is being used in order to sustain the release of drug and enhance the in vivo oral bioavailability and therapeutic efficacy of several poorly water-soluble drugs.…”

Section: Introductionmentioning

confidence: 99%

“…Recently, Tang et al (2016) developed an extended release formulation of APM to resolve the dosing and tolerability issue. 9 Poly(D,L-lactide-coglycolide) (PLGA) is considered as a smart polymer, which is being used in order to sustain the release of drug and enhance the in vivo oral bioavailability and therapeutic efficacy of several poorly water-soluble drugs. [10][11][12] The PLGA polymer also protects the drugs from premature degradation and hepatic pass metabolism.…”

Section: Introductionmentioning

confidence: 99%

<p>Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats</p>

Anwer

Mohammad

Ezzeldin

et al. 2019

IJN

115

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Background Apremilast (APM) is a novel, orally administered small molecule drug approved for treatment of psoriasis or psoriatic arthritis. Due to its low solubility and permeability, it is classified as a class IV drug according to BCS classification. Dose titration is recommended during APM treatment due to its tolerability and twice-daily dosing regimen issues. Materials and Methods In this study, three different APM-loaded PLGA nanoparticles (F1–F3) were prepared by single emulsion and evaporation method. Based on particle size, PDI, zeta potential (ZP), entrapment efficiency (%EE), drug loading (%DL), and spectral characterization, the nanoparticles (F3) were optimized. The F3 nanoparticles were further evaluated for in vitro release and in vivo pharmacokinetic studies in rats. Results The optimized nanoparticles (F3) had particles size 307.3±8.5 nm with a low PDI value 0.317, ZP of −43.4±2.6 mV, EE of 61.1±1.9% and DL of 1.9±0.1%. The in vitro release profile showed a sustained release pattern of F3 nanoparticles of APM. The pharmacokinetic results showed 2.25 times increase in bio-availability of F3 nanoparticles compared to normal APM suspension. Moreover, significant increase in half-life and mean residence time confirms long-term retention of F3 nanoparticles. Conclusion Bioavailability enhancement along-with long-term retention of the APM-loaded PLGA nanoparticles might be helpful for the once-daily regimen treatment.

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“…Molecular form is C 22 H 24 N 2 O 7 S with mass of 460.5. 2-4 A through literature survey reveals that various analytical and bioanalytical methods were published to describe the quantification of Apremilast in active pharmaceutical ingredient and pharmaceutical dosage forms to study the purity, degradation products by UV-Spectrophotometric method, 5-6 FTIR, 7 RP-HPLC, [8][9][10][11][12][13][14][15][16][17][18][19][20][21] Pharmacokinetic studies in beagle dog plasma, 22 human plasma and cerebro spinal fluid, [23][24][25][26][27] rat plasma [28][29][30] by LC-MS/MS. The published methods by LC-MS/MS was calibrated 0.1-100 ng/m.L of apremilast in biological samples.…”

Section: Introductionmentioning

confidence: 99%

LC-MS/MS Determination and Pharmacokinetics Study of Apremilast after Oral Administration in Rabbits

Rao¹,

Reddy²,

Babu³

2020

IJPER

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Objectives:A selective and reproducible method has been optimised for evaluation of Apremilast in rabbit biological matrices by UPLC-ESI-MS/MS. Methods: The analytical technique was implemented to quantify the apremilast in rabbit plasma samples with Apremilast-D5 as deuterated internal standard. The chromatographic separation tuned with 10mM Ammonium Acetate Buffer (pH: 4.0): Methanol: Acetonitrile, (20:40:40%, v/v/v) using the CORTECS C 18 , 2.7 µ.m, 4.6 m.m X 150 m.m analytical column with analysis time four minutes. The flow of mobile phase through column is 0.5 m.L/min. The mass spectrometric ions of Apremilast and Apremilast-D5 obtained were m/z 461.5→257.1 and 466.5→257.1. Results: The curve indicates correlation coefficient (r 2 ) was superior than 0.998 with linear range of 0.03-48.0 n.g/m.L. The developed method was tuned to apply efficaciously for analyzing the pharmacokinetic parameters of Apremilast in rabbit plasma samples. Conclusion: An accurate and reproducible novel method was fabricated for estimation of Apremilast in rabbit biological matrices by UPLC-ESI-MS/MS will be used for regular analysis and appropriate for therapeutic drug monitoring.

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Development of an Extended-Release Formulation for Apremilast and a Level A <i>in Vitro</i>–<i>in Vivo</i> Correlation Study in Beagle Dogs

Cited by 24 publications

References 35 publications

An updated overview with simple and practical approach for developing in vitro–in vivo correlation

An updated overview with simple and practical approach for developing in vitro–in vivo correlation

<p>Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats</p>

LC-MS/MS Determination and Pharmacokinetics Study of Apremilast after Oral Administration in Rabbits

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