Abstract:
:For use in chronic oral chemotherapeutic regimens, the potent anticancer drug docetaxel needs a solid oral dosage form. Because docetaxel has a very low permeability and a very low aqueous solubility (biopharmaceutical classification system class IV), a pharmacokinetic booster was combined with a newly developed solid dispersion formulation to improve the oral bioavailability of docetaxel. The best performing solid dispersion was a 1/9/1 w/w/w ternary mixture of docetaxel, polyvinylpyrrolidone (PVP)-K30 and sodium lauryl sulphate (SLS). In a phase I clinical trial, with ritonavir as pharmacokinetic booster, the docetaxel premix solution (TAXOTERE) was pharmacokinetically evaluated against the solid dispersion formulation filled into hard gelatin capsules (ModraDoc001 15 mg capsules). There were no significant differences between the pharmacokinetic parameters of docetaxel after administration of docetaxel premix solution or ModraDoc001 15 mg capsules, although there was a trend towards a higher and more variable exposure to docetaxel after oral administration of docetaxel premix solution (513 ± 219 vs. 790 ± 669 ngh/mL). The low inter-individual variability of docetaxel exposure (44%), the dosing accuracy, and the absence of ethanol and polysorbate are major advantages of ModraDoc001 15 mg capsules over docetaxel premix solution.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Moes JJ,Koolen SL,Huitema AD,Schellens JH,Beijnen JH,Nuijen Bdoi
10.1016/j.ijpharm.2011.08.041subject
Has Abstractpub_date
2011-11-28 00:00:00pages
244-50issue
2eissn
0378-5173issn
1873-3476pii
S0378-5173(11)00812-Xjournal_volume
420pub_type
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