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Formulations of 5-fluorocytosine and uses thereof

A preparation, 5-FC technology, applied in the field of 5-flucytosine preparations

Inactive Publication Date: 2011-05-25
TOCAGEN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Monotherapy with 5-FC has limitations due to frequent occurrence of resistance

Method used

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  • Formulations of 5-fluorocytosine and uses thereof
  • Formulations of 5-fluorocytosine and uses thereof
  • Formulations of 5-fluorocytosine and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0100] Materials. Materials used in the preparation of the dosage forms described herein were obtained as follows. Flucytosine (5-FC), USP was purchased from Scinopharm (Taiwan); Carbomer 71-G was purchased from Noveon (Cleveland, Ohio, USA); HPMC, NF (Benecel MP874, hydroxypropyl methylcellulose) and HPC, NF (Klucel -HXF, hydroxypropyl cellulose) was purchased from Aqualon (Wilmington, Delaware, USA); Kollidon - SR (PVA-PVP copolymer, matrix retarding polymer based on polyvinyl acetate and povidone) was purchased from BASF (Ludwigshafen am Rhein, Rhineland-Palatinate, Germany); directly compressible dicalcium phosphate, NF (Emcompress ) was purchased from JRS Pharma (Patterson, New York, U.S.); maltodextrin was purchased from Grains Processing Corp. (GPC, Muscatine, Iowa); magnesium stearate NF was purchased from Spectrum Chemicals (Gardena, California, U.S.) and could be directly Compressed anhydrous lactose (DCL-21) was purchased from DMV (Veghel, Netherlands). Sodi...

Embodiment 2

[0106] Repeat the above method using the following ingredients:

[0107] Element

Embodiment 3

[0109] Repeat the above method using the following ingredients:

[0110] Element

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PUM

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Abstract

The disclosure provides an extended release formulation of 5- f luorocytosine. In another aspect, a method of treating a fungal disease is provided. The method comprises administering to a subject in need thereof a fungus-treating effective amount of a composition comprising 5-f luorocytosine. In yet another aspect, a method of treating a cancer is provided. The method comprises administering to a subject in need thereof a sufficient amount of an expression vector to induce expression of cytosine deaminase which is capable of converting 5-f luorocytosine to 5-f luorourcail in cells of the cancer and a cancer-treating effective amount of a composition comprising 5-f luorocytosine.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Provisional Application Serial No. 61 / 077,142, filed June 30, 2008, the disclosure of which is incorporated herein by reference. technical field [0003] The present application relates to 5-fluorocytosine preparations and to methods of using 5-fluorocytosine preparations for the treatment of fungal diseases, pneumocystis carinii pneumonia and other infectious diseases or cancer. Background technique [0004] The pyrimidine analog 5-fluorocytosine (5-FC) is a synthetic drug (Ancobon ), which has antifungal activity and can also be used in the treatment of cancer. Ancobon It is an immediate-release capsule formulation with a short half-life of the drug, which is quickly cleared from the body, so in order to maintain the effective level of the drug, high-frequency administration of 4-16 times a day is required. [0005] In addition, 5-FC is effective at blood drug concentration...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N43/04A61K31/70
CPCA61K38/51A61K9/2054A61K31/513A61K31/505A61K9/2018A61K31/496A61K9/2027A61K31/7048A61K9/2009A61K31/4196A61K9/2013C12Y305/04001A61K2300/00A61K38/50A61P31/00A61P31/10A61P31/12A61P35/00A61P43/00A61K9/0053
Inventor 哈利·E·格鲁贝尔道格拉斯·乔利K·奥尔姆斯蒂德
Owner TOCAGEN
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