Immunomodulator slow-release preparation and preparation method thereof

Abstract

The invention discloses an immunomodulator slow-release preparation and a preparation method thereof. A lenalidomide slow-release tablet is composed of a slow-release layer and an optional quick-release layer, wherein the slow-release layer contains active ingredients of lenalidomide and a slow-release framework material simultaneously; the quick-release layer does not contain the slow-release framework material. The lenalidomide slow-release tablet disclosed by the invention is capable of slowly and uniformly releasing medicines by virtue of the slow-release framework material, so as to reduce the release speed, delay the time to peak, prolong the action time of lenalidomide, and provide a uniform and constant blood concentration. Moreover, The lenalidomide slow-release tablet disclosed by the invention is simple in prescription and excellent in quality stability; the preparation process is simple to operate, free from special treatment and production equipment, low in production cost, and beneficial to batch-enlarged industrial production for the product; the preparation method is high in yield, the granulation and crushing procedures are simple and practicable to operate, the intermediate material is good in stability, flowability, compressibility and content uniformity, and completely meets the requirements of tabletting, and the surface of the prepared tablet is smooth and beautiful.

Description

technical field

[0001] The invention relates to a sustained-release preparation and a preparation method thereof, in particular to a sustained-release tablet of an immunomodulator lenalidomide and a preparation method thereof. Background technique

[0002] Lenalidomide, chemical name 3-(7-amino-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione, molecular formula C 13 h 13 N 3 o 3 , its molecular weight is 259.2606, soluble in DMSO (100mg / ml), slightly soluble in methanol, ethanol, acetonitrile and water, it needs to be micronized, form strong acid salt or add solubilizer to improve its water solubility.

[0003] Lenalidomide is an antineoplastic drug developed by Celgene Biopharmaceutical Company of the United States for the treatment of myelodysplastic syndrome (MDS) and multiple myeloma (MM). It was approved by the FDA in 2005.

[0004] Lenalidomide is a representative drug of the new generation of immunomodulators, with a unique dual mechanism of action. On the one hand, l...

Examples

Embodiment 1

[0136] A lenalidomide sustained-release tablet, comprising the following components (calculated in 1000 tablets):

[0137] Lenalidomide 25.00 g

[0138] Hypromellose (3000mPa·s-8000 mPa·s)

[0139] (sustained release matrix material) 200.00 g

[0140] Povidone (adhesive) 25.00 g

[0141] Microcrystalline cellulose (filler) 112.50 g

[0142] Mannitol (bulking agent) 100.00 g

[0143] Povidone (solubilizer) 25.00 g

[0144] Talc powder (glidant) 5.00 g

[0145] Magnesium stearate (lubricant) 7.50 g

[0146] Opadry II (film coating material) 15.00 g

[0147] The method for preparing the above-mentioned lenalidomide sustained-release tablet comprises the following steps:

[0148] (1) According to the prescription, lenalidomide fine powder, slow-release matrix material, adhesive, filler and solubilizer are passed through a 40-mesh sieve, and the glidant and lubricant are passed through a 80-mesh sieve;

[0149] (2) Accurately weigh lenalidomide, sustained-release matrix ma...

Embodiment 2

[0157] A lenalidomide sustained-release tablet, comprising the following components (calculated in 1000 tablets):

[0158] Lenalidomide 25.00 g

[0159] Hypromellose (12000mPa·s-21000 mPa·s)

[0160] (sustained release matrix material) 150.00 g

[0161] Pregelatinized starch (binder) 100.00 g

[0162] Calcium hydrogen phosphate (filler) 635.00 g

[0163] Povidone (solubilizer) 10.00 g

[0164] Talc powder (glidant) 50.00 g

[0165] Magnesium stearate (lubricant) 30.00 g

[0166] Opadry II (film coating material) 30.00 g

[0167] The method for preparing the above-mentioned lenalidomide sustained-release tablet is the same as that in Example 1.

[0168]

Embodiment 3

[0170] A lenalidomide sustained-release tablet, comprising the following components (calculated in 1000 tablets):

[0171] Lenalidomide 25.00 g

[0172] Carbomer (sustained release matrix material) 180.00 g

[0173] Povidone (adhesive) 15.00 g

[0174] Compressible starch (filler) 52.50 g

[0175] Hydroxypropyl-β-cyclodextrin (solubilizer) 65.00 g

[0176] Micronized silica gel (glidant) 1.50 g

[0177] Magnesium stearate (lubricant) 1.50 g

[0178] Opadry II (film coating material) 12.00 g

[0179] The method for preparing the above-mentioned lenalidomide sustained-release tablet is the same as that in Example 1.

[0180]

technical field

[0001] The invention relates to a sustained-release preparation and a preparation method thereof, in particular to a sustained-release tablet of an immunomodulator lenalidomide and a preparation method thereof. Background technique

[0002] Lenalidomide, chemical name 3-(7-amino-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione, molecular formula C 13 h 13 N 3 o 3 , its molecular weight is 259.2606, soluble in DMSO (100mg / ml), slightly soluble in methanol, ethanol, acetonitrile and water, it needs to be micronized, form strong acid salt or add solubilizer to improve its water solubility.

[0003] Lenalidomide is an antineoplastic drug developed by Celgene Biopharmaceutical Company of the United States for the treatment of myelodysplastic syndrome (MDS) and multiple myeloma (MM). It was approved by the FDA in 2005.

[0004] Lenalidomide is a representative drug of the new generation of immunomodulators, with a unique dual mechanism of action. On the one hand, l...

Examples

Embodiment 1

[0136] A lenalidomide sustained-release tablet, comprising the following components (calculated in 1000 tablets):

[0137] Lenalidomide 25.00 g

[0138] Hypromellose (3000mPa·s-8000 mPa·s)

[0139] (sustained release matrix material) 200.00 g

[0140] Povidone (adhesive) 25.00 g

[0141] Microcrystalline cellulose (filler) 112.50 g

[0142] Mannitol (bulking agent) 100.00 g

[0143] Povidone (solubilizer) 25.00 g

[0144] Talc powder (glidant) 5.00 g

[0145] Magnesium stearate (lubricant) 7.50 g

[0146] Opadry II (film coating material) 15.00 g

[0147] The method for preparing the above-mentioned lenalidomide sustained-release tablet comprises the following steps:

[0148] (1) According to the prescription, lenalidomide fine powder, slow-release matrix material, adhesive, filler and solubilizer are passed through a 40-mesh sieve, and the glidant and lubricant are passed through a 80-mesh sieve;

[0149] (2) Accurately weigh lenalidomide, sustained-release matrix ma...

Embodiment 2

[0157] A lenalidomide sustained-release tablet, comprising the following components (calculated in 1000 tablets):

[0158] Lenalidomide 25.00 g

[0159] Hypromellose (12000mPa·s-21000 mPa·s)

[0160] (sustained release matrix material) 150.00 g

[0161] Pregelatinized starch (binder) 100.00 g

[0162] Calcium hydrogen phosphate (filler) 635.00 g

[0163] Povidone (solubilizer) 10.00 g

[0164] Talc powder (glidant) 50.00 g

[0165] Magnesium stearate (lubricant) 30.00 g

[0166] Opadry II (film coating material) 30.00 g

[0167] The method for preparing the above-mentioned lenalidomide sustained-release tablet is the same as that in Example 1.

[0168]

Embodiment 3

[0170] A lenalidomide sustained-release tablet, comprising the following components (calculated in 1000 tablets):

[0171] Lenalidomide 25.00 g

[0172] Carbomer (sustained release matrix material) 180.00 g

[0173] Povidone (adhesive) 15.00 g

[0174] Compressible starch (filler) 52.50 g

[0175] Hydroxypropyl-β-cyclodextrin (solubilizer) 65.00 g

[0176] Micronized silica gel (glidant) 1.50 g

[0177] Magnesium stearate (lubricant) 1.50 g

[0178] Opadry II (film coating material) 12.00 g

[0179] The method for preparing the above-mentioned lenalidomide sustained-release tablet is the same as that in Example 1.

[0180]

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