Abstract
The drug level was calculated in the plasma, the lung tissue and bronchial secretion using ciprofloxacin as the drug with erosion-controlled dosage forms. A numerical model was built and tested for this calculation. It takes into account the following stages: the kinetics of drug release along the gastrointestinal tract time, the absorption into and elimination out of the plasma, the diffusion through the lung tissue and convection into the bronchial secretion. Emphasis is placed upon the effect of patient's non-compliance on the drug levels, with intake omission, intake omission followed by double dosing, wrong frequency. Calculation with erosion-controlled dosage form with a long time of full erosion able to remain in the gastrointestinal over a period of time much longer than the usual gastrointestinal tract time shows the interest of bioadhesion.
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REFERENCES
Aïnaoui, A. and Vergnaud, J. M. (1998). Assessment of blood level with controlled-release dosage forms. Effect of the rate constant of elimination of the drug. Eur. J. Drug Metab. Pharmacok. 23, 383–89.
Aïnaoui, A., Ouriemchi, E. M. and Vergnaud, J. M. (1999). Assessment of plasma drug level with erosion controlled dosage forms: effect of the shape and dimensions, and residence time in the gastrointestine, J. Reinforced Plastics Composites. 18, 798–814.
Amidon, G.L., Lennernäs, H., Shah, V. P., et al. (1995). A theoretical basis for a biopharmaceutical drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability, Pharm. Res. 12, 413–20.
Bakhouya, A., Saidna, M. and Vergnaud, J. M. (1997). Calculation of the blister fluid-time history with ciprofloxacin administered orally or by infusion, Int. J. Pharm. 146, 225–32.
Barza, M. and Cuchural, G. (1985). General principles of antibiotic tissue penetration, Antimicrob. Agents Chemother. 15, 59–75.
Bergogne-Berezin, E. (1988). Pharmacokinetics of antibiotics in respiratory secretions, in: Respiratory Infections: Diagnotics and Management, 2nd edn, Pennington, J. E. (ed.), pp. 608–31. Raven Press, New York, USA.
Bergogne-Berezin, E., Morel, C., Even, P., et al. (1978). Pharmacocinétique des antibiotiques dans les voies respiratoires, Nouv. Presse Med. 7, 2831–6.
Bergogne-Berezin, E., Berthelot, G., Even, P., et al. (1986). Penetration of ciprofloxacin into bronchial secretion, Eur. J. Clin Microbiol. 5, 197–200.
Breilh, D. (1994). Diffusion de la ciprofloxacine et de son principal métabolite la désethyl-ciprofloxacine dans le parenchyne pulmonaire humain. Etude des modélisations plasmatiques et tissulaires et simulation des concentrations pulmonaires de ciprofloxacine selon un modèle physiologique-pharmacocinétique. Diplome d'Etudes Approfondies, Pessac, France.
Caron, H. S. and Roth, H. P. (1968). Patients' cooperation with a medical regimen, J. Amer. Med. Ass. 203, 120–124.
Davis, M. S. (1966). Variation in patients compliance with doctors orders: analysis of congruency between survey responses and results of empirical investigations, J. Med. Educ. 41, 1037–48.
Fabre, D., Bressole, F., Gomeni, R., et al. (1991). Steady-state pharmacokinetics of ciprofloxacin in plasma from patients with Nosocomial pneumonia: penetration of the bronchial mucosa, Antimicrob. Agents Chemother. 35, 2521–5.
Gaffaro, R., De Salvator, F., Dellamonica, P., et al. (1988). Ciprofloxacin penetration in bronchial mucosa after oral treatment. Presented at the World Congress of the International Society for Infectious Diseases, Rio de Janeiro, 16–21 April, 1988.
Heilmann, K. (1984). Therapeutic Systems. George Thieme Verlag, Stuttgart.
Heller, J. (1984). Biodegradable polymers in Controlled drug delivery, CRC Critical Reviews in Ther. Drug Carrier Systems. 1, 39–90.
Honeybourne, D., Andrews, J. M., Ashby, J. P., et al. (1988). Evaluation of the penetration of ciprofloxacin and amoxycillin into the bronchial mucosa, Thorax. 43, 715–19.
Lambert, H. P. (1978). Clinical significance of tissue penetration of antibiotics in the respiratory tract, Scand. J. Infect. Dis. 14, 262–6.
Le Bel, M., Vallée, F. and Bergeron, M. (1986). Tissue penetration of ciprofloxacin after single and multiple doses, Antimicrob. Agents Chemother. 29, 501–5.
Marlin, G. E., Nicholls, A. J., Funnell, G. R., et al. (1984). Penetration of cefaclor into bronchial mucosa, Thorax. 39, 813–17.
Nia, B., Ouriemchi, E. M. and Vergnaud, J. M. (1995). Calculation of the blood level of a drug taken orally with diffusion controlled dosage forms, Int. J. Pharm. 119, 165–171.
Ouriemchi, E. M. and Vergnaud, J. M. (1996a). Calculation of the plasma drug level with oral controlled release dosage forms. Effect of the dose frequency, Int. J. Pharm. 127, 177–184.
Ouriemchi, E. M. and Vergnaud, J. M. (1996b). Prediction of in-vivo blood level with controlled-release dosage forms. Effect of the gastrointestinal tract time, J. Pharm. Pharmacol. 48, 390–4.
Pennington, J. E. (1981). Penetration of antibiotics into respiratory secretions, Rev. Infect. Dis. 3, 67–73.
Saïdna, M., Ouriemchi, E. M. and Vergnaud, J. M. (1998a). Calculation of the antibiotic level in the lung tissue and bronchial secretion with an oral controlled-release dosage forms, Inflammophar-macology 6, 321–37.
Saïdna, M., Ouriemchi, E. M. and Vergnaud, J. M. (1998b). Assessment of antibiotic levels in lung tissue with erosion-contolled dosage form, Eur. J. Drug Metab. Pharmacokinet. 22, 237–43.
Siewert, M. (1993). Perspectives of in vitro dissolution tests in establishing in vivo/ in vitro correlation, Eur. J. Drug Metab. Pharmacokinet. 18, 7–18.
Skelly, J. P., Barr, W. H., Benet, L. Z., et al. (1987). Report of the workshop on controlled-release dosage forms: issues and controversies, Pharm. Res. 4, 75–7.
Skelly, J. P., Amidon, G. L., Barr, W. H., et al. (1990). In vitro and in vivo testing and correlations for oral controlled, modified release dosage forms, Pharm. Res. 7, 975–82.
Skelly, J. P. and Shiu, G. H. (1993). In vitro/ in vivo correlation in biopharmaceutics: scientific and regulatory implications, Eur. J. Drug Metab. Pharmacok. 18, 121–9.
Smith, B. R. and Le Frocq, J. L. (1983). Bronchial tree penetration of antibiotics, Chest. 6, 904–8.
Smith, M. J., White, L. O., Bouryer, H., et al. (1986). Pharmacokinetics and sputum penetration of ciprofloxacin in patients with cystic fibrosis, Antimicrob. Agents Chemother. 30, 614–16.
Valcke, Y., Pauwels, R. and Van der Straeten, M. (1990). Pharmacokinetics of antibiotics in the lungs, Eur. Resp. J. 3, 715–22.
Vergnaud, J. M. (1993). Controlled Drug Release of Oral Dosage Forms, Vol. 10, pp. 199–259. Ellis Horwood Publishers, Chichester, UK.
Winter, J. and Sweeney, G. (1991). Reproducibility of the measurement of ciprofloxacin concentration in bronchial mucosa, J. Antimicrob. Chemother. 27, 329–33.
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Ouriemchi, E.M., Vergnaud, J.M. Assessment of the drug level in bronchial secretion with patient's noncompliance and oral dosage forms with controlled release. Inflammopharmacology 8, 267–283 (2000). https://doi.org/10.1163/156856000750260513
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DOI: https://doi.org/10.1163/156856000750260513