Slow-releasing Tamoxifen citrate tablet

Abstract

The present invention relates to a slow-releasing preparation of Tamoxifen citrate as an anti-tumor medicine and its preparation method. Every tablet of Tamoxifen citrate contains 1 mg-100 mg, and the rest is slow-releasing material and auxiliary material.

Description

Technical field

[0001] The invention relates to a sustained-release preparation of the anti-tumor drug tamoxifen citrate (Tamoxifen citrate) and a preparation method thereof. Background technique

[0002] Tamoxifen citrate (Tamoxifen citrate), also known as tamoxifen, chemical name (Z)-2-[p-(1,2-diphenyl-1-butenyl)phenoxy]-N, The citrate of N-dimethylethylamine is a tristyrene non-steroidal anti-estrogen anti-tumor drug. By competitively binding with the estrogen receptor in the target cytoplasm, it blocks the effect of excessive estrogen on the breast tissue and reduces the excessive stimulation of estrogen on the ducts and interstitium of the breast. Therefore, it can be used for the treatment of breast cancer. In addition, the drug also has anti-oxidation, membrane regulation, multi-drug resistance (Multi-drug Resistance, MDR), cardioprotective function, anti-viral, anti-candida, and has an effect on insulin growth factor (can significantly reduce blood IGF- I (Level of Insuli...

Examples

Embodiment 1

[0191] Prescription (contains per 1000 tamoxifen citrate sustained-release tablets)

[0192] Tamoxifen Citrate 100g

[0193] Hypromellose (HPMC K4M) 90g

[0194] Polyvinylpyrrolidone (PVP K30) 100g

[0195] Lactose 85g

[0196] Micronized silica gel 100g

[0197] Magnesium stearate 10g

[0198] 80% ethanol aqueous solution

[0199] (1) Pass the prescribed amount of hydroxypropyl methylcellulose and polyvinylpyrrolidone through a 40-mesh sieve three times and mix them thoroughly.

[0200] (2) The tamoxifen citrate and the materials in (1) are first mixed in equal amounts by progressive addition, and then passed through a 40-mesh sieve three times to fully mix.

[0201] (3) Pass the lactose and the material in (2) through a 40-mesh sieve three times and mix them thoroughly.

[0202] (4) Pass the powdered silica gel and the materials in (3) through a 40-mesh sieve three times and mix them thoroughly.

[0203] (5) Add an appropriate amount of 80% ethanol solution to the above-mentione...

Embodiment 2

[0206] Prescription (contains per 1000 tamoxifen citrate sustained-release tablets)

[0207] Tamoxifen Citrate 1g

[0208] Hypromellose (HPMC K4M) 3g

[0209] Polyvinylpyrrolidone (PVP K30) 1g

[0210] Lactose 5g

[0211] Micronized silica gel 1g

[0212] Magnesium stearate 0.1g

[0213] 80% ethanol aqueous solution

[0214] (1) Pass the prescribed amount of hydroxypropyl methylcellulose and polyvinylpyrrolidone through a 40-mesh sieve three times and mix them thoroughly.

[0215] (2) The tamoxifen citrate and the materials in (1) are first mixed in equal amounts by progressive addition, and then passed through a 40-mesh sieve three times to fully mix.

[0216] (3) Pass the lactose and the material in (2) through a 40-mesh sieve three times and mix them thoroughly.

[0217] (4) Pass the powdered silica gel and the materials in (3) through a 40-mesh sieve three times and mix them thoroughly.

[0218] (5) Add an appropriate amount of 80% ethanol solution to the above-mentioned unifo...

Embodiment 3

[0221] Prescription (contains per 1000 tamoxifen citrate sustained-release tablets)

[0222] Tamoxifen Citrate 50g

[0223] Hypromellose (HPMC K4M) 45g

[0224] Polyvinylpyrrolidone (PVP K30) 50g

[0225] Lactose 42g

[0226] Micronized silica gel 50g

[0227] Magnesium stearate 5g

[0228] 80% ethanol aqueous solution

[0229] (1) Pass the prescribed amount of hydroxypropyl methylcellulose and polyvinylpyrrolidone through a 40-mesh sieve three times and mix them thoroughly.

[0230] (2) The tamoxifen citrate and the materials in (1) are first mixed in equal amounts by progressive addition, and then passed through a 40-mesh sieve three times to fully mix.

[0231] (3) Pass the lactose and the material in (2) through a 40-mesh sieve three times and mix them thoroughly.

[0232] (4) Pass the powdered silica gel and the materials in (3) through a 40-mesh sieve three times and mix them thoroughly.

[0233] (5) Add an appropriate amount of 80% ethanol solution to the above-mentioned un...

Technical field

[0001] The invention relates to a sustained-release preparation of the anti-tumor drug tamoxifen citrate (Tamoxifen citrate) and a preparation method thereof. Background technique

[0002] Tamoxifen citrate (Tamoxifen citrate), also known as tamoxifen, chemical name (Z)-2-[p-(1,2-diphenyl-1-butenyl)phenoxy]-N, The citrate of N-dimethylethylamine is a tristyrene non-steroidal anti-estrogen anti-tumor drug. By competitively binding with the estrogen receptor in the target cytoplasm, it blocks the effect of excessive estrogen on the breast tissue and reduces the excessive stimulation of estrogen on the ducts and interstitium of the breast. Therefore, it can be used for the treatment of breast cancer. In addition, the drug also has anti-oxidation, membrane regulation, multi-drug resistance (Multi-drug Resistance, MDR), cardioprotective function, anti-viral, anti-candida, and has an effect on insulin growth factor (can significantly reduce blood IGF- I (Level of Insuli...

Examples

Embodiment 1

[0191] Prescription (contains per 1000 tamoxifen citrate sustained-release tablets)

[0192] Tamoxifen Citrate 100g

[0193] Hypromellose (HPMC K4M) 90g

[0194] Polyvinylpyrrolidone (PVP K30) 100g

[0195] Lactose 85g

[0196] Micronized silica gel 100g

[0197] Magnesium stearate 10g

[0198] 80% ethanol aqueous solution

[0199] (1) Pass the prescribed amount of hydroxypropyl methylcellulose and polyvinylpyrrolidone through a 40-mesh sieve three times and mix them thoroughly.

[0200] (2) The tamoxifen citrate and the materials in (1) are first mixed in equal amounts by progressive addition, and then passed through a 40-mesh sieve three times to fully mix.

[0201] (3) Pass the lactose and the material in (2) through a 40-mesh sieve three times and mix them thoroughly.

[0202] (4) Pass the powdered silica gel and the materials in (3) through a 40-mesh sieve three times and mix them thoroughly.

[0203] (5) Add an appropriate amount of 80% ethanol solution to the above-mentione...

Embodiment 2

[0206] Prescription (contains per 1000 tamoxifen citrate sustained-release tablets)

[0207] Tamoxifen Citrate 1g

[0208] Hypromellose (HPMC K4M) 3g

[0209] Polyvinylpyrrolidone (PVP K30) 1g

[0210] Lactose 5g

[0211] Micronized silica gel 1g

[0212] Magnesium stearate 0.1g

[0213] 80% ethanol aqueous solution

[0214] (1) Pass the prescribed amount of hydroxypropyl methylcellulose and polyvinylpyrrolidone through a 40-mesh sieve three times and mix them thoroughly.

[0215] (2) The tamoxifen citrate and the materials in (1) are first mixed in equal amounts by progressive addition, and then passed through a 40-mesh sieve three times to fully mix.

[0216] (3) Pass the lactose and the material in (2) through a 40-mesh sieve three times and mix them thoroughly.

[0217] (4) Pass the powdered silica gel and the materials in (3) through a 40-mesh sieve three times and mix them thoroughly.

[0218] (5) Add an appropriate amount of 80% ethanol solution to the above-mentioned unifo...

Embodiment 3

[0221] Prescription (contains per 1000 tamoxifen citrate sustained-release tablets)

[0222] Tamoxifen Citrate 50g

[0223] Hypromellose (HPMC K4M) 45g

[0224] Polyvinylpyrrolidone (PVP K30) 50g

[0225] Lactose 42g

[0226] Micronized silica gel 50g

[0227] Magnesium stearate 5g

[0228] 80% ethanol aqueous solution

[0229] (1) Pass the prescribed amount of hydroxypropyl methylcellulose and polyvinylpyrrolidone through a 40-mesh sieve three times and mix them thoroughly.

[0230] (2) The tamoxifen citrate and the materials in (1) are first mixed in equal amounts by progressive addition, and then passed through a 40-mesh sieve three times to fully mix.

[0231] (3) Pass the lactose and the material in (2) through a 40-mesh sieve three times and mix them thoroughly.

[0232] (4) Pass the powdered silica gel and the materials in (3) through a 40-mesh sieve three times and mix them thoroughly.

[0233] (5) Add an appropriate amount of 80% ethanol solution to the above-mentioned un...