Formulation of controlled release microspheres containing nicardipine: The role of pharmacokinetic modeling and computer simulation

European Journal of Drug Metabolism and Pharmacokinetics

Volumn 24, Issue 1, 1999, Pages 55-61

  Mrhar, A ^a   Bogataj, M ^a   Grabnar, I ^a   Karba, R ^a  

^a UNIVERSITY OF LJUBLJANA   (Slovenia)

Author keywords

Controlled release microspheres; Formulation; Nicardipine; Pharmacokinetic modeling; Plasma levels

Indexed keywords

HYDROXYPROPYLMETHYLCELLULOSE PHTHALATE; MICROSPHERE; NICARDIPINE;

ARTICLE; COMPARTMENT MODEL; COMPUTER SIMULATION; CONTROLLED RELEASE FORMULATION; DRUG BLOOD LEVEL; DRUG RELEASE; EVAPORATION; PARTICLE SIZE; SCANNING ELECTRON MICROSCOPE;

EID: 0032991270     PISSN: 03787966     EISSN: None     Source Type: Journal    
DOI: 10.1007/BF03190011     Document Type: Article

References (18)

1. Sorkin E.M., Clissold S.P. (1987) : Nicardipine, a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy, in treatment of angina pectoris, hypertension and related cardiovascular disorders. Drugs, 33: 296-345.
2. Thuillez C., Gueret M., Duhaze P. et al. (1984) : Nicardipine: pharmacokinetics and effects on carotid and brachial blood flows in normal volunteers. Br J. Clin. Pharmacol., 18: 837-847.
3. Celentano A., Galderisi M., Tammaro P. et al. (1990) : Effects on casual and 24-h ambulatory blood pressure of slow-release nicardipine and chlorthalidone in arterial essential hypertension: double-blind, crossover study. Int. J. Clin. Pharmacol. Ther. Toxicol., 28: 190-196.
4. Sumimoto T., Hiwada K., Ochi T. et al. (1994): Effects of long term treatment with sustained-release nicardipine on left ventricular hypertrophy and function in patients with essential hypertension. J. Clin. Pharmacol., 34: 266-269.
5. Boissel J.P., Meillard O. Perrin-Fayol E. et al. (1996): Comparison between a bid and a tid regimen: improved compliance with no improved antihypertensive effect. Eur. J. Clin. Pharmacol., 50: 63-67.
6. Wallin J.D., Cook M.E., Blanski L. et al. (1988) : Intravenous nicardipine for the treatment of severe hypertension. Am. J. Med., 85: 331-338.
7. Anon (1991) : Efficacy and safety of intravenous nicardipine in the control of postoperative hypertension. Chest, 99: 393-398.
8. Graham D.J.M., Dow R.J., Hall D.J. et al. (1985) : The metabolism and pharmacokinetics of nicardipine hydrochloride in man. Br. J. Clin. Pharmacol., 20 (Suppl): 23S-28S.
9. Graham D.J.M., Dow R.J., Freedman D. et al. (1984) : Pharmacokinetics of nicardipine following oral and intravenous administration in man: Postgrad. Med. J., 60: 7-10.
10. Product Information (1996): Cardene R (SR), Nicardipine. Syntex Laboratories, Palo Alto, CA.
11. Washington C. (1996) : Drug release from microparticulate systems. In: Benita S. (Ed.). Microencapsulation, methods and industrial applications. New York: Marcel Dekker, 155-182.
12. Cvelbar P., Lenardic A., Milovac J. et al. (1990) : Bioavailability of different nicardipine formulations. Lek Pharmaceutical Works, Ljubljana, Slovenia.
13. Kristl A., Vojnovic D, Karba R., Mrhar A., Rubessa F. Zupancic, B. (1993) : Mixture design of theophylline retard formulation. Int. J. Pharm., 100: 33-40.
14. Vojnovic D., Rubessa F., Bogataj M., Mrhar A. (1993) : Formulation and evaluation of vinylpyrrolidone/vinylacetate copolymer microspheres with griseofulvin. J. Microencapsulation, 10: 89-99.
15. Cardot J.M., Beyssac E. (1993) : In vitro/in vivo correlations: scientific implications and standardisation. Eur. J. Drug Metab. Pharmacokinet., 18: 113-120.
16. Vidmar V., Jalsenjak I. (1982) : Kinetics and mechanism of release of a water-soluble drug from microcapsules, Acta Pharm. Techn., 28: 78-80
17. Forni, F., Coppi G., Vandelli M.A. et al. (1990) : An interpretation of the diffusion-type mechanism of drug release from microspheres. Int. J. Pharm., 60: 83-88.
18. Higuchi S., Shiobara Y. (1980) : Comparative pharmacokinetics of nicardipine hydrochloride, a new vasodilatator, in various species. Xenobiotica, 10: 447-454.