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Modified release tamsulosin tablets

A tamsulosin and tablet technology, which is applied in the field of monolithic drug tablets, capsules, and unit dosage forms, to treat symptoms of benign prostatic hyperplasia, and can solve problems such as food effects that have not been proposed

Inactive Publication Date: 2005-03-02
SYNTHON BV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the food effect of commercial tamsulosin capsules is well documented, no solution to the food effect has been proposed so far

Method used

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  • Modified release tamsulosin tablets
  • Modified release tamsulosin tablets
  • Modified release tamsulosin tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] Three batches of monolithic tablets were prepared by step-blending and direct compression with the following properties:

[0083] (％)

Tamsulosin Hydrochloride

0.4mg

0.5

anhydrous lactose

26.4mg

33.0

Dicalcium Phosphate Anhydrous

26.4mg

33.0

Hydroxypropyl Methyl Cellulose (HPMC)

26.4mg

33.0

Magnesium stearate

0.4mg

0.5

total

80mg

100

[0084] The difference from batch to batch is only the viscosity value of the selected hydroxypropyl methylcellulose:

[0085] Batch A contains METHOCEL K4M CR PREMIUM

[0086] Batch B contains METHOCEL K15M CR PREMIUM

[0087] Batch C containing METHOCEL K100M CR PREMIUM

[0088] b) Operation method

[0089] Tamsulosin hydrochloride was blended (15 minutes) with anhydrous lactose in a 1:9 ratio (10% active substance), ground (15 seconds) and then blended again (5 minutes). This pre-blend was then mixed with the remainde...

Embodiment 2

[0098] Three batches of monolithic tablets were prepared by step-blending and direct compression with the following properties:

[0099] D

E

F

Tamsulosin Hydrochloride

0.4mg

0.4mg

0.4mg

anhydrous lactose

35.2mg

30.8mg

22.0 mg

Dicalcium Phosphate Anhydrous

35.2mg

30.8mg

22.0 mg

Hydroxypropyl Methyl Cellulose (HPMC)

8.8mg

17.6mg

35.2mg

Magnesium stearate

0.4mg

0.4mg

0.4mg

total

80mg

80mg

80mg

[0100] The difference from batch to batch is only the concentration of hydroxypropyl methylcellulose used:

[0101] Lot D contains 11% METHOCEL K100M CR PREMIUM

[0102] Lot E contains 22% METHOCEL K100M CR PREMIUM

[0103] Batch F contains 44% METHOCEL K100M CR PREMIUM

[0104] b) Operation method

[0105] Tamsulosin hydrochloride was blended (15 minutes) with anhydrous lactose in a 1:9 ratio (10% active substance), ground (15 seconds) and then...

Embodiment 3

[0111] Two batches of monolithic tablets were prepared by step-blending and direct compression with the following properties:

[0112] a) Tablet composition

[0113] (％)

Tamsulosin Hydrochloride

0.4mg

0.5

anhydrous lactose

25.6mg

32.0

Dicalcium Phosphate Anhydrous

25.6mg

32.0

Hydroxypropyl Methyl Cellulose (HPMC)

28.0mg

35.0

Magnesium stearate

0.4mg

0.5

total

80mg

100

[0114] The differences between the two batches are mainly in scale-up, mixing time and physical parameters.

[0115] G batch enlarged to 20000 units

[0116] Batch H enlarged to 40000 units

[0117] b) Operation method

[0118] Tamsulosin hydrochloride was blended (Turbula; 15 minutes) with anhydrous lactose in a 1:9 ratio (10% active substance), ground (IKA; 30 seconds) and then blended again (Turbula; 5 minutes). This pre-blend was then mixed with the remainder of the lactose, dical...

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PUM

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Abstract

The invention relates to an adjustment release tablet comprising a tablet matrix having dispersed tamsulosin or a pharmaceutically acceptable salt thereof, and optionally having an enteric coating over said matrix, wherein said tablet has a dissolution profile such that in each of the media SIF, FaSSIF, and FeSSIF, said tablet releases not more than 60% of said tamsulosin at 2 hours elapsed time in USP 2 apparatus using 500 ml of said media at 50-100 rpm paddle speed.

Description

[0001] Pursuant to 35 U.S.C. §119(e), this application claims priority to earlier U.S. Provisional Application 60 / 331,055, filed November 7, 2001, which is hereby incorporated by reference in its entirety. Background of the invention [0002] The present invention relates to modified release tamsulosin tablets showing little or no food effect, and to unit dosage forms prepared therefrom. [0003] Tamsulosin is the common name for 5-[2-[[2-(2-ethoxyphenoxy)ethyl]amino]propyl]-2-methoxy-benzenesulfonamide of the following formula (1) . [0004] [0005] It is disclosed in EP 34432 and US 4731478 as a pharmaceutically active substance having alpha-adrenergic blocking activity for the treatment of cardiac insufficiency and benign prostatic hyperplasia. [0006] (R)-Tamsulosin hydrochloride is marketed under various trade names, including FLOMAX in the U.S.  (Boehringer Ingelheim), HARNAL in Japan  (Yamanouchi) and OMNIC in Europe  (Yamanouchi), used to treat symptoms of ...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/26A61K9/28A61K9/48A61K31/18A61K47/02A61K47/04A61K47/12A61K47/26A61K47/32A61K47/38A61P13/08
CPCA61K9/2054A61K9/2009A61K31/18A61K9/2027A61K9/2846A61K9/2095A61K9/4808A61K9/2018A61P13/00A61P13/08A61P43/00A61P9/00A61K47/02
Inventor 雅各布斯·玛丽亚·莱曼斯约翰尼斯·简·普拉特尤弗朗斯·范达伦阿图罗·西勒斯·奥特加胡安·库卡拉·艾斯科伊
Owner SYNTHON BV
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