PDF herunterladen
Arzneimittelforschung 2012; 62(06): 280-284
DOI: 10.1055/s-0032-1306305
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Pharmacokinetic Equivalence of Taxotere and SID530, a Novel Docetaxel Formulation Containing Hydroxypropyl-beta-cyclodextrin in Monkeys

T. K. Kim   *
1   College of Pharmacy, Seoul National University, Seoul, Republic of Korea
2   Life Science R&D Center, SK Chemicals, Seongnam, Gyeonggi-do, Republic of Korea
,
H. H. Yoo   *
3   College of Pharmacy, Hanyang University, Ansan, Gyeonggi-do, Republic of Korea
,
E. J. Kim
2   Life Science R&D Center, SK Chemicals, Seongnam, Gyeonggi-do, Republic of Korea
,
B.-Y. Lee
2   Life Science R&D Center, SK Chemicals, Seongnam, Gyeonggi-do, Republic of Korea
,
J. H. Park
1   College of Pharmacy, Seoul National University, Seoul, Republic of Korea
› Institutsangaben
Weitere Informationen

Publikationsverlauf

received 03. Januar 2012

accepted 17. Februar 2012

Publikationsdatum:
16. April 2012 (online)

    Lizenzen und Reprints

Abstract

SID530 is a new parenteral formulation of docetaxel containing hydroxypropyl-beta-cyclodextrin (HP-β-CD). In this study, a comparative pharmacokinetic study of 2 docetaxel parenteral solutions, SID530 and Taxotere, was carried out. In a crossover experimental design, 6 male cynomolgus monkeys received each formulation by intravenous infusion of a single dose. The concentration of docetaxel in whole blood and plasma was determined using liquid chromatography-tandem mass spectrometry (LC-MS/MS). The 2 formulations showed similar pharmacokinetic parameters in both whole blood and plasma, and displayed comparable values for maximum serum concentration (Cmax), time to peak concentration (Tmax), and area under the concentration-time curve (AUC). The 90% confidence intervals for the ratios of Cmax and AUC values for SID530 to Taxotere were within the acceptable range of 0.80–1.20 in both plasma and whole blood. These findings indicate that SID530 and Taxotere are comparable in terms of their distribution in the blood and their plasma profile; consequently, these drugs are bioequivalent in the monkey.

Key words

docetaxel - bioequivalence - HP-β-CD - polysorbate 80 - LC-MS/MS
*

*  These 2 authors contributed equally to this work.


 

  • References

  • 1 Clarke SJ, Rivory LP. Clinical pharmacokinetics of docetaxel. Clin Pharmacokinet 1999; 36: 99-114
    CrossrefPubMedGoogle Scholar
  • 2 Lyseng-Williamson KA, Fenton C. Docetaxel: a review of its use in metastatic breast cancer. Drugs 2005; 65: 2513-2531
    CrossrefPubMedGoogle Scholar
  • 3 Michael A, Syrigos K, Pandha H. Prostate cancer chemotherapy in the era of targeted therapy. Prostate Cancer Prostatic Dis 2009; 12: 13-16
    CrossrefPubMedGoogle Scholar
  • 4 Gould S, Scott RC. 2-Hydroxypropyl-beta-cyclodextrin (HP-beta-CD): A toxicology review. Food Chem Toxicol 2005; 43: 1451-1459
    PubMedGoogle Scholar
  • 5 Brewster ME, Loftsson T. Cyclodextrins as pharmaceutical solubilizers. Adv Drug Deliv Rev 2007; 59: 645-666
    CrossrefPubMedGoogle Scholar
  • 6 Burris HA. Optimal use of docetaxel (T 235 axotere): maximizing its potential. Anticancer Drugs 1996; 7 (Suppl. 02) 25-28
    PubMedGoogle Scholar
  • 7 Hennenfent KL, Govindan R. Novel formulations of taxanes: a review. Old wine in a new bottle?. Ann Oncol 2006; 17: 735-749
    CrossrefPubMedGoogle Scholar
  • 8 ten Tije AJ, Verweij J, Loos WJ et al. Pharmacological effects of formulation vehicles : implications for cancer chemotherapy. Clin Pharmacokinet 2003; 42: 665-685
    CrossrefPubMedGoogle Scholar
  • 9 Crispens Jr CG, Sorenson JR. Treatment of reticulum cell sarcoma in SJL/J mice with Tween 80. Anticancer Res 1988; 8: 1341-1343
    PubMedGoogle Scholar
  • 10 Loos WJ, Baker SD, Verweij J et al. Clinical pharmacokinetics of unbound docetaxel: role of polysorbate 80 and serum proteins. Clin Pharmacol Ther 2003; 74: 364-371
    CrossrefPubMedGoogle Scholar
  • 11 Fleuren HL, van Rossum JM. Nonlinear relationship between plasma and red 245 blood cell pharmacokinetics of chlorthalidone in man. J Pharmacokinet Biopharm 1977; 5: 359-375
    CrossrefPubMedGoogle Scholar
  • 12 Hinderling PH. Red blood cells: a neglected compartment in pharmacokinetics and pharmacodynamics. Pharmacol Rev 1997; 49: 279-295
    PubMedGoogle Scholar
  • 13 Kurata D, Wilkinson GR. Erythrocyte uptake and plasma binding of diphenylhydantoin. Clin Pharmacol Ther 1974; 16 (02) 355-362
    PubMedGoogle Scholar
  • 14 Hinderling PH. Kinetics of partitioning and binding of digoxin and its analogues in the subcompartments of blood. J Pharm Sci 1984; 73: 1042-1053
    CrossrefPubMedGoogle Scholar
  • 15 Musumeci T, Ventura CA, Giannone I et al. PLA/PLGA nanoparticles for sustained release of docetaxel. Int J Pharm 2006; 325: 172-179
    CrossrefPubMedGoogle Scholar
  • 16 Yang M, Ding Y, Zhang L et al. Novel thermosensitive polymeric micelles for docetaxel delivery. J Biomed Mater Res A 2007; 81: 847-857
    PubMedGoogle Scholar
  • 17 Du W, Hong L, Yao T et al. Synthesis and evaluation of water-soluble docetaxel prodrugs-docetaxel esters of malic acid. Bioorg Med Chem 2007; 15: 6323-6330
    CrossrefPubMedGoogle Scholar
  • 18 Gao K, Sun J, Liu K et al. Preparation and characterization of a submicron lipid emulsion of docetaxel: submicron lipid emulsion of docetaxel. Drug Dev Ind Pharm 2008; 34: 1227-1237
    CrossrefPubMedGoogle Scholar
  • 19 Zhao L, Wei YM, Zhong XD et al. PK and tissue distribution of docetaxel in rabbits after i. v. administration of liposomal and injectable formulations. J Pharm Biomed Anal 2009; 49: 989-996
    CrossrefPubMedGoogle Scholar
  • 20 Quaglia F, Ostacolo L, Mazzaglia A et al. The intracellular effects of non-ionic amphiphilic cyclodextrin nanoparticles in the delivery of anticancer drugs. Biomaterials 2009; 30: 374-382
    CrossrefPubMedGoogle Scholar
  • 21 Huang XX, Zhou CL, Wang H et al. Pharmacokinetics, efficacy, and safety evaluation of docetaxel/hydroxypropyl sulfobutyl-β-cyclodextrin inclusion complex. AAPS PharmSciTech 2011; 12: 665-672
    CrossrefPubMedGoogle Scholar