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5’-deoxy-5-fluoro-N-[(pentyloxy)carbonyl]-cytidine tablet content

IP.com Disclosure Number: IPCOM000171312D
Publication Date: 2008-Jun-04
Document File: 4 page(s) / 114K

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The IP.com Prior Art Database

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5'-deoxy-5-fluoro-N-[(pentyloxy)carbonyl]-cytidine tablet content

    5'-deoxy-5-fluoro-N-[(pentyloxy)carbonyl]-cytidine("CTN") of the following formula

    is a fluoropyrimidine carbamate with antineoplastic activity. It is an orally administered systemic prodrug of 5'-deoxy-5-fluorouridine (5'-DFUR) which is converted to 5-fluorouracil. Trade name of the product (tablets) is XELODA®.

CTN is marketed under the trade name XELODA®.

    CTN is a white to off-white crystalline powder with an aqueous solubility of 26 mg/mL at 20°C.

The purity of commercial CTN is reported herein.

Sample Preparation of XELODA®:
Operating in a glove-box three tablets of XELODA® were grinded. The mixture obtained was then accurately weighed to prepare a solution of about 0.6 mg/mL of CTN (about 80 mg in a 100ml volumetric flask). The weighed mixture was diluted with diluent and, after sonication, filtered trough a 0.45 μm membrane filter (the first 5 mL of solution were disregarded).

    The clear solution obtained was injected in an HPLC instrument.

Batch PURITY% Imp. rrt 0.18

Rel.Comp. A

XELODA®

U8202 99.68% 0.10% <0.02% 0.22% <0.02% XELODA®

U3031 99.67% 0.14% <0.02% 0.19% <0.02%

Imp. rrt 0.19

Rel.Comp. B Imp. rrt 0.95

Imp. rrt 1.11

Rel.Comp. C

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The identity of the above impurities as provided by the USP is a...