Pharmaceutical preparation

A preparation and mucosal drug delivery technology, applied in the field of pharmaceutical preparations of enteric polymers, can solve the problems of reduced bioavailability of bicalutamide, increased systemic exposure, and limited maximum systemic exposure

Inactive Publication Date: 2004-06-09
ASTRAZENECA AB
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This may result in suboptimal treatment outcomes for a proportion of patients
In addition, the maximum systemic exposure obtained after administration of conventional tablets is limited, resulting in significantly lower bioavailability of bicalutamide at doses exceeding 150 mg in conventional tablets
Conventional tablets above 300 mg do not provide further significant increases in systemic exposure
Again, no specific mention of bicalutamide

Method used

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Embodiment Construction

[0046] The inventors chose to investigate solid dispersions as a possible means of increasing the efficacy of bicalutamide. The aim is to improve efficacy by increasing the bioavailability of bicalutamide or reducing interpatient variability in bicalutamide plasma concentrations, or both.

[0047] In order to increase drug bioavailability in general, the prior art teaches various possible polymers for solid dispersions. The present inventors have now surprisingly found that the efficacy of bicalutamide can be enhanced by specifically formulating bicalutamide with an enteric polymer having a pKa of 3 to 6 in a solid dispersion. As part of a non-limiting example, the following demonstrates that the use of other polymers does not bring about an increase in the efficacy of bicalutamide.

[0048] A variety of substances are routinely used to coat pharmaceutical tablets, capsules and granules, and the coated granules can be compressed into tablets or used to fill capsules. See Sch...

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Abstract

The present invention relates to a pharmaceutical formulation comprising bicalutamide and an enteric polymer having a pKa from 3 to 6. The invention also relates to a daily pharmaceutical dose of bicalutamide provided by such a formulation. In addition, the invention relates to the use of such an enteric polymer in solid dispersion with bicalutamide for increasing the bioavailability of the bicalutamide; for reducing inter-patient variability in plasma concentrations of bicalutamide; or for treating and / or reducing the risk of prostate cancer in a patient.

Description

technical field [0001] The present invention relates to a pharmaceutical formulation comprising bicalutamide and an enteric polymer with a pKa of 3 to 6. The invention also relates to a daily pharmaceutical dosage form of bicalutamide provided by the formulation. Furthermore, the present invention relates to the use of said enteric polymer present in solid dispersion together with bicalutamide to increase the bioavailability of bicalutamide, to reduce the variability of bicalutamide blood concentration between patients, Or use to treat prostate cancer and / or reduce the risk of prostate cancer in a patient. Background technique [0002] Bicalutamide, a nonsteroidal antiandrogen, is 4-cyano-α',α',α'-trifluoro-3-(4-fluorophenylsulfonyl)-2-hydroxy-2 - Racemate of methacryl-m-toluidine, trade name CASODEX given by AstraZeneca TM . EP-100172 discloses 4'-cyano-α', α', α'-trifluoro-3-(4-fluorophenylsulfonyl)-2-hydroxyl-2-methylpropionyl-m-toluidine ( In EP-100172 it is called ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/00A61K9/16A61K9/32A61K9/36A61K31/167A61K31/277A61K47/32A61K47/38A61P5/28A61P13/08A61P35/00
CPCA61K9/006A61K9/1647A61K9/1652A61K31/167A61K47/38A61K31/277A61P13/08A61P35/00A61P35/04A61P5/28A61K47/30
Inventor N·巴特曼J·卡希尔
Owner ASTRAZENECA AB
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