Perspectives of in vitro dissolution tests in establishing in vivo/in vitro correlations

Siewert, Martin

doi:10.1007/bf03220004

Cited by 29 publications

(9 citation statements)

References 13 publications

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“…15,16,17,18,19,20 In general, there is increased uncertainty associated with developing an IVIVC for IR oral dosage forms, because the in vivo apparent drug absorption is often a function of a multitude of variables, many of which are difficult to isolate or mimic in vitro . For example, an IVIVC for IR dosage forms of highly water-soluble drugs (BCS classes I and III) may not be possible, 2 because gastric emptying or membrane permeation is usually the rate-limiting step.…”

Section: Ivivc and Product Developmentmentioning

confidence: 99%

In Vitro–In Vivo Correlations

Qiu¹

2009

Developing Solid Oral Dosage Forms

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Section: Ivivc and Product Developmentmentioning

confidence: 99%

In Vitro–In Vivo Correlations

Qiu¹

2009

Developing Solid Oral Dosage Forms

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“…Moreover, the last purpose is to take advantage of the plasma drug profiles obtained using this method in solving in a quantitative way the following two main problems: the effect of the intervariability of the patients defined by their pharmacokinetic parameters and the effect of the noncompliance of the patients; the effect of stirring the liquid around the dosage form either with in vitro or in vivo test (Siewert 1993); and finally the effect of the transit time along the GI (Ouriemchi and Vergnaud 1996) and thus the time over which the drug is released into the patient's body.…”

Section: Introductionmentioning

confidence: 99%

Survey: calculation of the characteristics of oral diffusion-controlled release dosage forms related to the drug

Rosca

Vergnaud²

2010

Eur J Drug Metab Pharmacokinet

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Oral dosage forms with controlled release exhibit various advantages over their immediate release counterparts, but they must be built adequately by dispersing the drug through the well-defined polymer matrix. This study is concerned with diffusion-controlled dosage forms to resolve the problems that appear: in vitro tests generally used for determining the kinetics of drug release do not take into account the nature of the drug. On the contrary, the plasma drug profiles obtained through in vivo tests strongly depend on the nature of the drug, through their typical pharmacokinetic parameters. Moreover, the effect of the stirring rate is difficult to evaluate. Following the demand from the FDA concerned with the in vitro/in vivo correlation, a numerical model was built so as to evaluate the plasma drug profile obtained with any drug delivered from a diffusion-controlled release dosage form. The results are expressed by connecting the half-life times of the drugs obtained either with bolus injection or with the dosage forms, for various values of the parameters of interest: the diffusivity of the matrix polymer and the size of the dosage form. Thus, these diagrams make it possible to promptly determine the characteristics of the dosage forms able to give the desired plasma drug profile for any drug. Of course, for each drug being defined by its pharmacokinetic parameters, the polymer matrix should be selected as a function of its diffusivity. Finally, the evaluation of the plasma drug profile is of effective help to determine quantitatively the effect of the intervariability of the patients as well as the effect of the patient's noncompliance.

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“…The kinetics of dru~ release can be determined by in-vitro tests, while the measurement of plasma drut levels through in-vivo tests necessitates tedious and highly time-consuming experi ments. This is why the Food and Drug Administration (FDA) have conducted studie for establishing in-vitro/in-vivo correlation by means of two workshops [16,17[ However, these correlations were found not able "to provide meaningful data at th~ time" [18] and three levels of correlation were defined [19]. Another approach was t build numerical models taking all the known facts into account, namely the kinetics ( drug release from the dosage form, whatever the process of drug release, and tl~ following stages of absorption into, and elimination from, the plasma compartmel [20].…”

Section: Introductionmentioning

confidence: 99%

Calculation of the antibiotic level in the lung tissue and bronchial secretion with an oral controlled-release dosage form

Saïdna¹,

Ouriemchi²,

Vergnaud³

1998

Inflammopharmacol

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The drug level-time history in plasma and lung tissue was calculated with an antibiotic orally delivered in either an immediate-release or a controlled-release dosage form. The drug profiles were compared with experiment results given in the literature. In the same way, the drug level was evaluated in the bronchial secretion in contact with lung tissue. A numerical model, based on finite differences taking all the known facts into account was built and tested with the data found in the literature. Transport of the drug was looked at, including a stage of diffusion through the thickness of the lung tissue and a stage of convection into the bronchial secretion. A few parameters were thus considered, including the thickness of the lung tissue and the diffusivity of the antiobiotic through the tissue, the thickness of the bronchial secretion and the coefficient of convective transport into the sputum which characterizes its viscosity. Two partition factors were also introduced for the drug: between the tissue and the serum and between the lung tissue and the bronchial secretion.

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Perspectives of in vitro dissolution tests in establishing in vivo/in vitro correlations

Cited by 29 publications

References 13 publications

In Vitro–In Vivo Correlations

In Vitro–In Vivo Correlations

Survey: calculation of the characteristics of oral diffusion-controlled release dosage forms related to the drug

Calculation of the antibiotic level in the lung tissue and bronchial secretion with an oral controlled-release dosage form

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