Pharmacoscintigraphic and pharmacokinetic evaluation on healthy human volunteers of sustained-release floating minitablets containing levodopa and carbidopa

International Journal of Pharmaceutics

Volumn 364, Issue 1, 2008, Pages 54-63

  Goole, J ^a   Van Gansbeke, B ^b   Pilcer, G ^a   Deleuze, Ph ^a   Blocklet, D ^b   Goldman, S ^b   Pandolfo, M ^b   Vanderbist, F ^c   Amighi, K ^a  

^a UNIVERSITÉ LIBRE DE BRUXELLES   (Belgium)

^b ERASME HOSPITAL   (Belgium)

^c Laboratoires SMB SA   (Belgium)

Author keywords

Carbidopa; Clinical study; Floating; Gamma scintigraphy; Levodopa; Minitablets; Pharmacokinetics; Sustained release

Indexed keywords

BENSERAZIDE PLUS LEVODOPA; BICARBONATE; CALCIUM CARBONATE; CARBIDOPA PLUS LEVODOPA; EUDRAGIT; GELUCIRE; GLYCEROL PALMITOSTEARATE; INDIUM 111; LACTOSE; METHYLCELLULOSE; TARTARIC ACID;

ADULT; AREA UNDER THE CURVE; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG DOSE COMPARISON; DRUG SOLUBILITY; FEMALE; GAMMA SCINTIGRAPHY; HUMAN; ISOTOPE LABELING; MALE; NORMAL HUMAN; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SINGLE DRUG DOSE; SUSTAINED RELEASE FORMULATION; TABLET FORMULATION;

ADULT; ANTIPARKINSON AGENTS; AREA UNDER CURVE; CARBIDOPA; CHEMISTRY, PHARMACEUTICAL; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CROSS-OVER STUDIES; DELAYED-ACTION PREPARATIONS; DRUG COMBINATIONS; FEMALE; HALF-LIFE; HUMANS; INDIUM RADIOISOTOPES; ISOTOPE LABELING; LEVODOPA; MALE; POWDERS; RADIONUCLIDE IMAGING; TABLETS; TISSUE DISTRIBUTION; YOUNG ADULT;

EID: 53949114854     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2008.08.016     Document Type: Article

References (36)

1. Belveal D., Bugge C.J., Garcia D.B., Keller K., Sowell K., Sullivan M.P., 2007, Determination of levodopa and carbidopa in human plasma by solid-phase extraction and LC/MS/MS, AAPPS Poster 003000 Exposition.
2. Bezard E., Brotchie J.M., and Gross C.E. Pathophysiology of levodopa-induced dyskinesia: potential for new therapies. Nat. Rev. Neurosci. 2 (2001) 577-588
3. Cedarbaum J.M., Kutt H., and Mc Dowell F.H. A pharmacokinetic and pharmacodynamic comparison of Sinemet CR (50/200) and standard Sinemet (25/100). Neurology 39 (1989) 38-44
4. Clarke's. Isolation and Identification of drugs in Pharmaceutics, Body Fluids, and Post-mortem Material. 2nd ed. (1986), The Pharmaceutical Press, London
5. Crevoisier Ch., Hoevels B., Zürcher G., and Da Prada M. Bioavailability of levodopa after Madropar HBS administration in healthy subjects. Eur. Neurol. 27 (1987) 36-46
6. Duvoisin R.C. Variation in the "on-off" phenomenon. Adv. Neurol. 5 (1974) 339-340
7. Forte G., Alimonti A., Violante N., Di Gregorio M., Senofonte O., Petrucci F., Sancesario G., and Bocca B. Calcium, copper, iron, magnesium, silicon and zinc content of hair in Parkinson's disease. J. Trace Elements Med. Biol. 19 (2005) 195-201
8. Gasser U.E., Crevoisier Ch., Ouwerkerk M., Lankhaar G., and Dingemanse J. Comparative single- and multiple-dose pharmacokinetics of levodopa and 3-O-methyldopa following a new dual-release and a conventional slow-release formulation of levodopa and benserazide in healthy subjects. Eur. J. Pharm. Biopharm. 46 (1998) 223-228
9. Guidance for Industry, Extended Release Oral Dosage Forms: Development, Evaluation, and Application of In Vitro/In Vivo Correlations, September 1997, U.S. Department of Health and Human Services, Food and Drug Administration, Center of Drug Evaluation and Research.
10. Goole J., Vanderbist F., and Amighi K. Development and evaluation of new multiple-unit levodopa sustained-release floating dosage forms. Int. J. Pharm. 334 (2007) 35-41
11. Goole J., Deleuze Ph., Vanderbist F., and Amighi K. New levodopa sustained-release floating minitablets coated with insoluble acrylic polymer. Eur. J. Pharm. Biopharm. 68 (2008) 310-318
12. Goole J., Vanderbist F., and Amighi K. Evaluation and floating enhancement of levodopa sustained-release floating minitablets coated with insoluble acrylic polymer. Drug Dev. Ind. Pharm. 34 (2008) 827-833
13. Grahnén A., Eckernäs S.A., Collin C., Ling-Anderson A., Tiger G., and Nilsson M. Comparative multiple-dose pharmacokinetics of slow-release levodopa products. Eur. Neurol. 32 (1992) 343-348
14. Griffiths G.H., Owen G.M., Kirkman S., and Shields R. Measurement of the rate of gastric emptying using chromium 51. Lancet 51 (1966) 1244-1245
15. Hamdani J., Moës A.J., and Amighi K. Development and evaluation of prolonged release pellets obtained by the melt pelletization process. Int. J. Pharm. 245 (2002) 167-177
16. Hoffman A., and Stepensky D. Pharmacodynamic aspects of modes of drug administration for optimization of drug therapy. Crit. Rev. Ther. Drug Carrier Syst. 16 (1999) 571-639
17. Kamba M., Seta Y., Kusai A., Ikeda M., and Nishimura K. A unique dosage form to evaluate the mechanical destructive force in the gastrointestinal tract. Int. J. Pharm. 208 (2000) 61-70
18. Kedzierewicz F., Thouvenot P., Lemut J., Etienne A., Hoffman M., and Maincent P. Evaluation of peroral silicone dosage forms in humans by gamma-scintigraphy. J. Control. Release 58 (1999) 195-205
19. Kiil S., and Dam-Johansen K. Controlled drug delivery from swellable hydroxypropylmethylcellulose matrices: model-based analysis of observed radial front movements. J. Control. Release 90 (2003) 1-21
20. Kordower J.H., and Goetz C.G. The first miracle in neurodegenerative disease: the discovery of oral levodopa. Brain Res. Bull. 50 (1999) 377-378
21. Mardsen C.D., and Parkes J.D. Success and problems of long-term L-dopa therapy in Parkinson's disease. Lancet (1977) 345-349
22. Moës A.J. Gastroretentive drug-delivery systems. Crit. Rev. Therapeutic Drug Carrier Syst. 15 (1993) 243-284
23. Monville C., Torres E.M., and Dunnett S.B. Validation of the L-dopa-induced dyskinesia in the 6-OHDA model and evaluation of the effects of selective dopamine receptor agonists and antagonists. Brain Res. Bull. 68 (2005) 16-23
24. Pinder R.M., Brogden R.N., Sawyer P.R., Speight T.M., and Avery G.S. Levodopa and decarboxylase inhibitors: a review of their clinical pharmacology and use in the treatment of Parkinsonism. Drugs 11 (1976) 329-377
25. Rouge N., Buri P., and Doelker E. Drug absorption sites in the gastrointestinal tract and dosage forms for site-specific delivery. Int. J. Pharm. 136 (1996) 117-139
26. Seth P.R., and Tossounian J. The hydrodynamically balanced system (HBS™): a novel drug delivery system for oral use. Drug Dev. Ind. Pharm. 10 (1984) 313-339
27. 2. Pharm. Res. 15 (1998) 889-896
28. Sharstry B.S. Parkinson disease: etiology, pathogenesis and future of gene therapy. Neur. Sci. Res. 41 (2001) 5-12
29. Siepmann J., Lecomte F., and Bodmeier R. Diffusion-controlled drug delivery systems: calculation of the required composition to achieve desired release profiles. J. Control. Release 60 (1999) 379-389
30. Stocchi F., Quinn N.P., Barbato L., Patsalos P.N., O'Connel M.T., Ruggieri S., and Mardsen C.D. Comparison between a fast and a slow release preparation of levodopa and combination of the two: a clinical and pharmacokinetic study. Clin. Neuropharmacol. 17 (1994) 38-44
31. Stops F., Fell J.T., Collett J.H., Martini L.G., Sharma H.L., and Smith A.-M. Citric acid prolongs the gastro-retention of a floating dosage form and increases bioavailability of riboflavin in the fasted state. Int. J. Pharm. 308 (2006) 14-24
32. Timmermans J., Van Gansbeke B., and Moes A.J. Assessing by gamma scintigraphy the in vivo buoyancy of dosage forms having known size and floating force profiles as a function of time. Proc. 5th APGI Int. Conf. Pharm. Technol. 1 (1989) 42-51
33. Timmermans J., and Moës A.J. Measuring the resultant-weight of an immersed test material. I. Validation of an apparatus and a method dedicated to pharmaceutical applications. Acta Pharm. Technol. 36 (1990) 171-175
34. Tothill P., McLoughlin G.P., and Heading R.C. Techniques and errors in scintigraphic measurements of gastric emptying. J. Nucl. Med. 19 (1978) 256-261
35. Wilding I.R., Coupe A.J., and Davis S.S. The role of γ-scintigraphy in oral drug delivery. Adv. Drug Del. Rev. 46 (2001) 103-124
36. Zhang L., Chen G., Hu Q., and Fang Y. Separation and determination of levodopa and carbidopa in composite tablets by capillary zone electrophoresis with amperometric detection. Anal. Chim. Acta 431 (2001) 287-292