Pharmaceutical composition containing fesoterodine and preparation method thereof

Abstract

The invention brings forward a pharmaceutical composition containing fesoterodine and a preparation method thereof. The pharmaceutical composition also comprises a stabilizing agent, which is dextrin, maltodextrin, mannitol, propylene glycol and / or cane sugar. The preparation method of the pharmaceutical composition comprises steps of sieving, mixing, wetting, granulating, drying, tabletting and coating. According to the pharmaceutical composition, the problem that fesoterodine is easy to decompose under conditions of high temperature and high humidity is solved, and the problem that a medicinal excipient in an existing pharmaceutical composition containing fesoterodine has side effect on intestines and stomach is also solved.

Description

technical field

[0001] The invention relates to a pharmaceutical composition of fesoterodine or a pharmaceutically acceptable salt thereof and a preparation method thereof. Background technique

[0002] Fesoterodine fumarate, which may be known chemically as 2-[(R)-3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenyliso Butyrate hydrogen fumarate, its structural formula is as follows:

[0003]

[0004] Fesoterodine fumarate is used to treat overactive bladder (OAB). The sustained-release tablet developed by Pfizer was approved by the FDA in 2008. This product treats overactive bladder once a day, which can significantly reduce urgency Onset of incontinence and frequency of voiding in 24 hours.

[0005] Fesoterodine fumarate is a competitive blocker of muscarinic receptors. After oral administration, it is rapidly and extensively hydrolyzed by non-specific esterases into the active metabolite 5-hydroxymethyl tolterodine, which exerts the anti-inflammatory effect ...

Examples

Embodiment 1

[0041] With dextrin as stabilizer, prepare fesoterodine fumarate sustained-release tablet, its prescription is shown in Table 1 (1000 tablet quantity):

[0042] Table 1

[0043] Fesoterodine fumarate

4g

Dextrin

120g

lactose

65g

microcrystalline cellulose

25g

Hypromellose K15M

50g

Hypromellose K100M

50g

Glyceryl behenate

15g

[0044] Its preparation method is as follows:

[0045]Weigh the raw and auxiliary materials according to Table 1, mix fesoterodine fumarate and dextrin, pass through a 100-mesh sieve and mix evenly, then mix with lactose, microcrystalline cellulose, hypromellose and pass through a 100-mesh sieve to mix uniform. Mix the powder and add 95% ethanol as a wetting agent to make a soft material, pass through a 20-mesh sieve to make wet granules, and dry the wet granules at 45°C until the water content is less than 4.0%, to obtain dry granules. The dry granules are passed thro...

Embodiment 2

[0048] Do stabilizer with maltodextrin, prepare fesoterodine fumarate sustained release tablet, its prescription is shown in Table 2 (quantity of 1000):

[0049] Table 2

[0050] Fesoterodine fumarate

4g

Maltodextrin

100g

lactose

65g

microcrystalline cellulose

25g

Hypromellose K15M

50g

Hypromellose K100M

50g

Talc powder

9g

[0051] Its preparation method is as follows:

[0052] Refer to Table 2 to weigh the raw and auxiliary materials, mix fesoterodine fumarate and maltodextrin, pass through a 120-mesh sieve and mix evenly, then mix with lactose, microcrystalline cellulose, hypromellose and mix with a 40-mesh sieve Uniform; mixed with powder, 80% ethanol as wetting agent, made into soft material, passed through 14 mesh sieve to make wet granules, dried at 45°C until the moisture content was less than 4.0%, to obtain dry granules. The dry granules are passed through a 14-mesh sieve for gran...

Embodiment 3

[0055] Make stabilizer with mannitol, prepare fesoterodine fumarate sustained-release tablet, its prescription is shown in Table 3 (1000 tablet quantities):

[0056] table 3

[0057] Fesoterodine fumarate

4g

Mannitol

80g

lactose

65g

microcrystalline cellulose

25g

Hypromellose K15M

50g

Hypromellose K100M

50g

Glyceryl behenate

12g

Magnesium stearate

3g

[0058] Its preparation method is as follows:

[0059] Refer to Table 3 to weigh the raw and auxiliary materials, mix fesoterodine fumarate and mannitol, pass through a 40-mesh sieve and mix evenly, then mix with lactose, microcrystalline cellulose, hypromellose and mix evenly with a 100-mesh sieve ; Mix the powder and add 100% ethanol as a wetting agent to make soft materials, pass through a 20-mesh sieve to make wet granules, and dry the wet granules at 45°C until the water content is less than 4.0%. Obtain dry granules; pass the...

technical field

[0001] The invention relates to a pharmaceutical composition of fesoterodine or a pharmaceutically acceptable salt thereof and a preparation method thereof. Background technique

[0002] Fesoterodine fumarate, which may be known chemically as 2-[(R)-3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenyliso Butyrate hydrogen fumarate, its structural formula is as follows:

[0003]

[0004] Fesoterodine fumarate is used to treat overactive bladder (OAB). The sustained-release tablet developed by Pfizer was approved by the FDA in 2008. This product treats overactive bladder once a day, which can significantly reduce urgency Onset of incontinence and frequency of voiding in 24 hours.

[0005] Fesoterodine fumarate is a competitive blocker of muscarinic receptors. After oral administration, it is rapidly and extensively hydrolyzed by non-specific esterases into the active metabolite 5-hydroxymethyl tolterodine, which exerts the anti-inflammatory effect ...

Examples

Embodiment 1

[0041] With dextrin as stabilizer, prepare fesoterodine fumarate sustained-release tablet, its prescription is shown in Table 1 (1000 tablet quantity):

[0042] Table 1

[0043] Fesoterodine fumarate

4g

Dextrin

120g

lactose

65g

microcrystalline cellulose

25g

Hypromellose K15M

50g

Hypromellose K100M

50g

Glyceryl behenate

15g

[0044] Its preparation method is as follows:

[0045]Weigh the raw and auxiliary materials according to Table 1, mix fesoterodine fumarate and dextrin, pass through a 100-mesh sieve and mix evenly, then mix with lactose, microcrystalline cellulose, hypromellose and pass through a 100-mesh sieve to mix uniform. Mix the powder and add 95% ethanol as a wetting agent to make a soft material, pass through a 20-mesh sieve to make wet granules, and dry the wet granules at 45°C until the water content is less than 4.0%, to obtain dry granules. The dry granules are passed thro...

Embodiment 2

[0048] Do stabilizer with maltodextrin, prepare fesoterodine fumarate sustained release tablet, its prescription is shown in Table 2 (quantity of 1000):

[0049] Table 2

[0050] Fesoterodine fumarate

4g

Maltodextrin

100g

lactose

65g

microcrystalline cellulose

25g

Hypromellose K15M

50g

Hypromellose K100M

50g

Talc powder

9g

[0051] Its preparation method is as follows:

[0052] Refer to Table 2 to weigh the raw and auxiliary materials, mix fesoterodine fumarate and maltodextrin, pass through a 120-mesh sieve and mix evenly, then mix with lactose, microcrystalline cellulose, hypromellose and mix with a 40-mesh sieve Uniform; mixed with powder, 80% ethanol as wetting agent, made into soft material, passed through 14 mesh sieve to make wet granules, dried at 45°C until the moisture content was less than 4.0%, to obtain dry granules. The dry granules are passed through a 14-mesh sieve for gran...

Embodiment 3

[0055] Make stabilizer with mannitol, prepare fesoterodine fumarate sustained-release tablet, its prescription is shown in Table 3 (1000 tablet quantities):

[0056] table 3

[0057] Fesoterodine fumarate

4g

Mannitol

80g

lactose

65g

microcrystalline cellulose

25g

Hypromellose K15M

50g

Hypromellose K100M

50g

Glyceryl behenate

12g

Magnesium stearate

3g

[0058] Its preparation method is as follows:

[0059] Refer to Table 3 to weigh the raw and auxiliary materials, mix fesoterodine fumarate and mannitol, pass through a 40-mesh sieve and mix evenly, then mix with lactose, microcrystalline cellulose, hypromellose and mix evenly with a 100-mesh sieve ; Mix the powder and add 100% ethanol as a wetting agent to make soft materials, pass through a 20-mesh sieve to make wet granules, and dry the wet granules at 45°C until the water content is less than 4.0%. Obtain dry granules; pass the...

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