New Results on an in Vitro Model for the Study of the Influence of Fatty Meals on the Bioavailability of Theophylline Controlled-Release Formulations

Aiache, Jean-Marc; Pierre, NgeneJean; Beyssac, Eric; Prasad, Vadlamani K.; Skelly, Jerome P.

doi:10.1002/jps.2600780319

Cited by 19 publications

(4 citation statements)

References 2 publications

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“…The USP Level A correlation "...represents a point-to-point relationship between in vitro dissolution and...in vivo dissolution." [1][2][3][4][5][6][7][8][9][10][11][12] Drug products which are strongly permeation-rate-limited (R , 1) will yield a "reverse L" correlation plot and may be the case for very rapidly dissolving immediate release products. Not surprisingly, based upon this definition for Level A correlation, "successful" correlation attempts in the literature have focused on extended release products.…”

Section: Resultsmentioning

confidence: 99%

“…1,2,[4][5][6][7][8]10,11 Points from eq 15 were generated by varying R between 1000 and 0.001 and fa between 0.1 and 1. A USP Level A correlation approach was pursued.…”

Section: Methodsmentioning

confidence: 99%

“…Dissolution-rate-limited absorption (e.g., absorption from extended release products [1][2][3][4][5][6][7][8][9][10][11][12] in particular has been emphasized in the literature and has shown high in vitro-in vivo correlation. For orally-administered drugs, dissolution and intestinal permeation have long been recognized as two possible rate-limiting phenomena in the absorption process.…”

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confidence: 99%

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Novel Approach to the Analysis of in Vitro–in Vivo Relationships**Presented in part at the Ninth Annual Meeting and Exposition of the American Association of Pharmaceutical Scientists, San Diego, CA, November 1994.

Polli

Crison

Amidon

1996

Journal of Pharmaceutical Sciences

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The objective of this study was to quantify the dependence of degree of in vitro-in vivo correlation on the relative rates of dissolution and intestinal permeation and on the fraction of dose absorbed. The following equation was derived assuming first-order dissolution and permeation after oral drug administration: Fa = fa-1(1 - alpha(alpha - 1)-1 (1 - Fd) + (alpha - 1)-1(1 - Fd)alpha), where Fa is the fraction of the total amount of drug absorbed at time t, fa the fraction of the dose absorbed at t = infinitive, alpha is the ratio of the first-order permeation rate constant to the first-order dissolution rate constant, and Fd is the fraction of dose dissolved in vitro at time t. This equation was examined in order to pursue a theoretical treatment of in vitro-in vivo correlation. The degree of in vitro-in vivo correlation between Fa and Fd was measured by r2. alpha was varied between 1000 and 0.001. fa was varied between 0.1 and 1.0. Points employed in the linear regression were geometrically balanced about the derived equation. r2 values decreased as alpha decreased for all values of fa. r2 values were virtually independent of fa for all values of alpha, except for 0.01 < alpha < 1.0. The slope of the regression was modulated by both alpha and fa; larger alpha and smaller fa each increased slope. Application of the equation to a piroxicam data set demonstrated the equation's utility relative to the USP Level A correlation approach. It is concluded that the degree of in vitro-in vivo correlation depends on the relative rates of dissolution and intestinal permeation and on the fraction of dose absorbed and that the derived model merits further study.

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Section: Resultsmentioning

confidence: 99%

“…1,2,[4][5][6][7][8]10,11 Points from eq 15 were generated by varying R between 1000 and 0.001 and fa between 0.1 and 1. A USP Level A correlation approach was pursued.…”

Section: Methodsmentioning

confidence: 99%

mentioning

confidence: 99%

See 1 more Smart Citation

Novel Approach to the Analysis of in Vitro–in Vivo Relationships**Presented in part at the Ninth Annual Meeting and Exposition of the American Association of Pharmaceutical Scientists, San Diego, CA, November 1994.

Polli

Crison

Amidon

1996

Journal of Pharmaceutical Sciences

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“…Moreover, dissolution and intestinal permeation have been recognized as two possible rate‐limiting phenomena in the absorption process. Dissolution‐rate‐limited absorption (Aiache et al ., 1989; Davi et al ., 1989; Hussein & Friedman, 1990; Mojaverian et al ., 1992; Caramella et al ., 1993; Fassihi & Rislel, 1993; Harrison et al ., 1993; Humbert et al ., 1994) in particular has been emphasized in the literature and has shown high in vitro – in vivo correlation (IVIVC). Far fewer studies have emphasized permeation‐rate‐limited absorption in some cases of immediate‐release products (Strum et al ., 1978; Sylvestri & Uda, 1979; Yau & Meyer, 1981; Welling et al ., 1982; Yau & Meyer, 1983; El‐Yazigi & Sawchuk, 1985; Chung & Shim, 1987; Mayer et al ., 1992) where, as this analysis predicts, IVIVC is low.…”

Section: Introductionmentioning

confidence: 99%

The effect of soybean oil refuse powder used as vehicle on the absorption of oxolinic acid in chickens under fasting and nonfasting conditions and the correlation with in vitro dissolution

Hamamoto

Koike

Machida

2001

Vet Pharm & Therapeutics

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The effect of soybean oil refuse powder (SOR) when used as a vehicle on the absorption of oxolinic acid (OXA) powder in chicken, the dissolution profile of OXA and the correlation between in vivo and in vitro study were examined. To examine in vivo bioavailability, chickens fed or fasted were studied using a 2 x 2 crossover design. The OXA was administered OXA or OXA-SOR (1 : 9) mixture 20 mg OXA/kg. In vitro dissolution rates for OXA and OXA-SOR were measured using the paddle (PD) and the rotatory dialysis cell dissolution (PTSW) methods. Maximum plasma concentration (Cmax) and area under the curve (AUC) were significantly increased by the addition of SOR to OXA. Differences between OXA and OXA-SOR were more remarkable under fasted as compared with fed condition. In vitro dissolution rates of OXA-SOR pH 1.2, 6.5 and 7.2 as determined by the PD and the PTSW methods were increased in the presence of SOR vehicle. Differences between OXA and OXA-SOR in vitro dissolution rates were greater than in vivo bioavailability. Correlation between in vitro release (%) and in vivo absorption (%) showed good linearity (gamma=0.8805-0.9999).

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Kurzfassungen der Diskussions‐ und Postervorträge

1991

Archiv der Pharmazie

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New Results on an in Vitro Model for the Study of the Influence of Fatty Meals on the Bioavailability of Theophylline Controlled-Release Formulations

Cited by 19 publications

References 2 publications

Novel Approach to the Analysis of in Vitro–in Vivo Relationships**Presented in part at the Ninth Annual Meeting and Exposition of the American Association of Pharmaceutical Scientists, San Diego, CA, November 1994.

Novel Approach to the Analysis of in Vitro–in Vivo Relationships**Presented in part at the Ninth Annual Meeting and Exposition of the American Association of Pharmaceutical Scientists, San Diego, CA, November 1994.

The effect of soybean oil refuse powder used as vehicle on the absorption of oxolinic acid in chickens under fasting and nonfasting conditions and the correlation with in vitro dissolution

Kurzfassungen der Diskussions‐ und Postervorträge

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