Revising Pharmacokinetics of Oral Drug Absorption: II Bioavailability-Bioequivalence Considerations

Chryssafidis, Pavlos; Tsekouras, Athanasios A.

doi:10.1007/s11095-021-03078-w

Cited by 23 publications

(4 citation statements)

References 21 publications

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“…Moreover, to our knowledge, this is the first time that the distribution of specnuezhenide in the brain is reported. Usually, bioavailability is used to evaluate the efficiency of drug absorption in the blood (Chryssafidis et al, 2021). In this study, we analysed the average transfer rate of the drug to the tissues, which might be a new concept and an addition to the evaluation of drug bioavailability because it evaluates the absorption of the same drug into the tissues of the body instead of blood, at different formulations or routes of administration.…”

Section: Discussionmentioning

confidence: 99%

Establishment of a multicomponent quality control method and the transfer characteristics of five markers from Qidongning Formula to rat tissues by HPLC-QQQ-MS/MS

Zhou,

Chen,

Yang

et al. 2023

Front. Pharmacol.

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Introduction: Traditional Chinese medicine compound preparations have become an increasingly utilized strategy for tumour treatment. Qidongning Formula (QDN) is a kind of antitumour compound preparation used in hospitals, and it can inhibit the growth of lung cancer cells. However, due to the complexity of botanical drugs, the quality evaluation of QDN is inconsistent, affecting clinical efficacy and posing potential safety risks for clinical application. Additionally, tissue distribution is an integral part of the drug development process.Methods: To study the distribution characteristics of markers in compound preparations and rat tissues, a novel HPLC-QQQ-MS/MS quantitative analytical method was established to determine five markers in QDN simultaneously, and the method was verified.Results and discussion: The analytical results showed that the contents of salidroside (51.6 ± 5.75 μg/g), calycosin-7-O-β-D-glucoside (94.2 ± 15.4 μg/g), specnuezhenide (371 ± 72.5 μg/g), formononetin (23.8 ± 5.39 μg/g), and polyphyllin I (87.7 ± 10.6 μg/g) were stable in different batches of QDN. After intragastric administration (13.5 g/kg) in rats for 1 h, four markers in the QDN, except polyphyllin I, were distributed in most tissues. QDN was distributed chiefly in the stomach and small intestine, followed by the liver or kidney. The study also found that specnuezhenide had the highest concentration in both QDN and rat tissues (102 ± 22.1 μg/g in the stomach), while formononetin had the highest transfer rate (0.351%) from QDN to rat intestines. The above research lays a quality research foundation for the antitumour application of QDN and provides a scientific reference for the quality control of Chinese medicine compound preparations.

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Section: Discussionmentioning

confidence: 99%

Establishment of a multicomponent quality control method and the transfer characteristics of five markers from Qidongning Formula to rat tissues by HPLC-QQQ-MS/MS

Zhou,

Chen,

Yang

et al. 2023

Front. Pharmacol.

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“…This linear differential ( 1) is a widely used model. It should be noted, however, that recent studies demonstrate that oral drug absorption is completed in finite time [14][15][16][17][18][19] Hill's Model…”

Section: First-order Absorption Modelmentioning

confidence: 99%

An Analytical Solution for Saturable Absorption in Pharmacokinetics Models

Sorzano

Moreno²,

Vilas

2022

Pharm Res

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Objective The first-order absorption is a common model used in Pharmacokinetics. The absorption of some drugs follows carrier mediated transport. It has been proposed that the amount of drug available may saturate the transport mechanism resulting in an absorption slower than the one predicted by the first-order model. Saturable absorption has been modeled at the differential equation level by substituting the constant rate absorption by a Hill kinetics absorption. However, its exact solution is so far unknown. The goal of this is to know the exact solution of different Hill kinetic absorption models. Methods We start defining different absorption models and increasing then their complexity. The simplest case is the first-order absorption model and the most complex will be a generalized Hill kinetic absorption model. The differential equation of each model is integrated. Results The complexity of the models their solutions may be not expressed in a close-form, or in term of elementary functions. We obtain and discuss the exact solutions of the different Hill kinetics absorption models. To do that, the solutions are studied according to the possible values of the free parameters of the models. We show the differences between models through simulations. Conclusions The knowledge of closed-form solutions allows to illustrate the differences between the different absorption models and minimizes the errors of numerical integration.

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“…The concept of "finite time" of absorption has been used in various Physiologically Based Pharmacokinetic (PBPK) models. However, the formal development of Physiologically Based Finite Time Pharmacokinetic (PBFTPK) models was published recently (2)(3)(4)(5). The PBFTPK models were built on two principles: i) drugs are absorbed passively for a finite period of time, τ and ii) time absorption constrains linked with the gastrointestinal transit times of drug in the stomach, the small intestines and the colon were applied (2)(3)(4)(5).…”

Section: Introductionmentioning

confidence: 99%

“…However, the formal development of Physiologically Based Finite Time Pharmacokinetic (PBFTPK) models was published recently (2)(3)(4)(5). The PBFTPK models were built on two principles: i) drugs are absorbed passively for a finite period of time, τ and ii) time absorption constrains linked with the gastrointestinal transit times of drug in the stomach, the small intestines and the colon were applied (2)(3)(4)(5). Zero-or first-order input is used for the (PBFTPK) 0 and (PBFTPK) 1 models, respectively.…”

Section: Introductionmentioning

confidence: 99%

Drugs are Absorbed in Finite Time: A New Era in Biopharmaceutics and Pharmacokinetics

Macheras

2021

APH

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Revising Pharmacokinetics of Oral Drug Absorption: II Bioavailability-Bioequivalence Considerations

Cited by 23 publications

References 21 publications

Establishment of a multicomponent quality control method and the transfer characteristics of five markers from Qidongning Formula to rat tissues by HPLC-QQQ-MS/MS

Establishment of a multicomponent quality control method and the transfer characteristics of five markers from Qidongning Formula to rat tissues by HPLC-QQQ-MS/MS

An Analytical Solution for Saturable Absorption in Pharmacokinetics Models

Drugs are Absorbed in Finite Time: A New Era in Biopharmaceutics and Pharmacokinetics

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