Feasibility of Biowaiver Extension to Biopharmaceutics Classification System Class III Drug Products

Jantratid, Ekarat; Prakongpan, Sompol; Amidon, Gordon L.; Dressman, Jennifer B.

doi:10.2165/00003088-200645040-00004

Cited by 57 publications

(71 citation statements)

References 23 publications

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“…According to the Biopharmaceutics Classification System, piroxicam is classified as a class II drug exhibiting low solubility and high permeability (10,11). Cimetidine is assigned as a class III drug (10,12), a drug with high solubility and poor permeability. A combination of these two drugs may lead changes in the dissolution profile of piroxicam.…”

Section: Introductionmentioning

confidence: 99%

Crystal Structure Transformations and Dissolution Studies of Cimetidine–Piroxicam Coprecipitates and Physical Mixtures

et al. 2009

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Abstract. We have recently demonstrated that coprecipitation of cimetidine (C) and piroxicam (P) at a mole ratio of 1:1 results in the transformation of the crystalline forms of both drugs to an amorphous state. In this study, coprecipitates and physical mixtures of cimetidine and piroxicam were further investigated at C/P mole ratios of 1:10, 1:5, 1:4, 1:2, 10:1, 20:1, 30:1, 40:1, and 52.5:1, the latter being the composition of a clinically used dosage. The physicochemical properties of these samples were examined using X-ray diffraction and Fourier transform infrared spectroscopy. Additionally, dissolution of piroxicam in the samples at C/P mole ratios of 10:1, 20:1, 30:1, 40:1, and 52.5:1 was investigated at pH 1.2 and pH 4. In coprecipitates with C/P mole ratios of 10:1, 20:1, 30:1, and 40:1, crystalline forms of both drugs were transformed to amorphous states. A mixture of an amorphous state and cimetidine crystalline form A was observed for the coprecipitate with a C/P mole ratio of 52.5:1. For the coprecipitates with C/P mole ratios of 1:2, 1:4, 1:5, and 1:10, cimetidine form A was transformed to form C, whereas piroxicam form II was modified to form I. It is interesting that small molecules, instead of polymers or solvents, can cause such crystal structure transformations. The dissolution of piroxicam at pH 4 is lower than that at pH 1.2. Additionally, the coprecipitates and physical mixtures with C/P mole ratios of 10:1, 20:1, 30:1, 40:1, and 52.5:1 demonstrate substantially higher dissolution of piroxicam compared to that of drug alone.

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Section: Introductionmentioning

confidence: 99%

Crystal Structure Transformations and Dissolution Studies of Cimetidine–Piroxicam Coprecipitates and Physical Mixtures

et al. 2009

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“…5 shows the regression analysis data. The IVIVC did not show a characteristic linear distribution of its dosage form either in the modified or immediate release of class II drugs (reference), instead an inverted L-shaped distribution was obtained which has been observed by others (45). This indicated that the method utilized for the dissolution study of the efavirenz tablets resulted in a fast dissolution of the drug.…”

Section: In Silico Studiesmentioning

confidence: 61%

In Vitro–In Vivo Correlation of Efavirenz Tablets Using GastroPlus®

et al. 2013

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Abstract. The aim of the present work was to use GastroPlus™ software for the prediction of pharmacokinetic profiles and in vitro-in vivo correlation (IVIVC) as tools to optimize the development of new generic medications. GastroPlus™ was used to simulate the gastrointestinal compartment and was based on the advanced compartmental absorption and transit model. Powder dissolution and efavirenz tablet dissolution studies were carried out to generate data from which correlation was established. The simulated plasma profile, based on the physicochemical properties of efavirenz, was almost identical to that observed in vivo for biobatches A and B. A level A IVIVC was established for the dissolution method obtained for the generic candidate using the Wagner-Nelson (r 2 =0.85) and for Loo-Riegelman models (r 2 =0.92). The percentage of fraction absorbed indicated that 0.5% sodium lauryl sulfate may be considered a biorelevant dissolution medium for efavirenz tablets. The simulation of gastrointestinal bioavailability and IVIVC obtained from immediate-release tablet formulations suggests that GastroPlus™ is a valuable in silico method for IVIVC and for studies directed at developing formulations of class II drugs.KEY WORDS: bioavailability; computational simulation; efavirenz; GastroPlus™; in vivo-in vitro correlation.

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“…A bioavailability study in a patient with a massive bowel restriction demonstrated reduced absorption of cimetidine which was attributed to rapid transit of drug through the GIT tract 45 . Both the absorption and clearance of cimetidine are linear in the therapeutic range 19,46 . Using the everted d ring technique the uptake of cimetidine from the rat jejunum and colon was show to be linear in the range 0.005-40 nM 47. After oral administration in the fasted state cimetidine usually show erratic double peak or multiple peak phenomenon in plasma drug concentration-time profile 19,44,48 . The phenomenon has been described extensively and still under discussion.…”

Section: 43mentioning

confidence: 99%

Cimetidine : A Review

2018

IJCTR

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Feasibility of Biowaiver Extension to Biopharmaceutics Classification System Class III Drug Products

Cited by 57 publications

References 23 publications

Crystal Structure Transformations and Dissolution Studies of Cimetidine–Piroxicam Coprecipitates and Physical Mixtures

Crystal Structure Transformations and Dissolution Studies of Cimetidine–Piroxicam Coprecipitates and Physical Mixtures

In Vitro–In Vivo Correlation of Efavirenz Tablets Using GastroPlus®

Cimetidine : A Review

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