Allopurinol dual-release preparation and preparation method thereof

Abstract

The invention relates to an allopurinol dual-release preparation and a preparation method thereof, which is characterized in that the dual-release preparation consists of a quick-release part and a slow-release part, wherein the ratio of the base allopurinol contained in the quick-release part to the base allopurinol contained in the slow-release part is 1:1 to 1:24. The invention belongs to the technical field of medicine preparation and aims at providing the allopurinol dual-release preparation with good patient compliance and small side effect and the preparation method thereof, wherein the allopurinol dual-release preparation has the advantages of taking effect quickly and maintaining effective blood concentration stably. The dual-release preparation can not only be used for reducing the side effect on the gastrointestinal tract, but also decreasing the administration times of a patient and adverse effect and promoting the patient compliance.

Description

technical field

[0001] The invention relates to an allopurinol double-release preparation and a preparation method thereof, which is characterized in that the double-release preparation is composed of an immediate-release part and a sustained-release part, wherein the immediate-release part and the sustained-release part contain the main drug allopurinol The specific gravity is 1:1-1:24. It belongs to the technical field of pharmaceutical preparations. Background technique

[0002] Allpurinol has a chemical structure of 1H-pyrazolo[3,4-d]pyrimidin-4-ol. Allopurinol is white or off-white crystalline powder; almost odorless and tasteless. Very slightly soluble in water or ethanol, insoluble in ether or chloroform; dissolved in alkaline solution. Allopurinol is currently the only drug that can inhibit the synthesis of uric acid. It and its metabolite oxypurinol inhibit the activity of xanthine oxidase, prevent the metabolism of hypoxanthine and xanthine into uric acid, and r...

Examples

Embodiment 1

[0026] quick release part

[0027] Allopurinol 50g

[0028] Microcrystalline Cellulose 101 20g

[0029] Starch 30g

[0030] Povidone K30 3g

[0031] Magnesium stearate 0.5g

[0032] Sustained release part

[0033] Allopurinol 200g

[0034] Hypromellose K100LV 40g

[0035] Microcrystalline Cellulose 101 50g

[0036] Povidone K30 15g

[0037] Magnesium stearate 0.8g

[0038]

[0039] Made into 1000 pieces / grain

[0040] Preparation:

[0041] (1) Preparation of immediate-release granules: crush allopurinol through an 80-mesh sieve, and set aside; weigh allopurinol, starch, povidone K30, and microcrystalline cellulose 101 of the prescribed amount, mix well, add appropriate amount of water, and carry out Wet granulation, wet granulation with a 16-mesh sieve, drying at 50°C, granulation with a 20-mesh sieve, calculate the yield, add magnesium stearate, mix, and set aside.

[0042] (2) Preparation of sustained-release granules: cr...

Embodiment 2

[0046] Quick release part:

[0047] Allopurinol 50g

[0048] Microcrystalline Cellulose 101 25g

[0049] Starch 26g

[0050] Povidone K30 3.7g

[0051] Magnesium stearate 0.5g

[0052] Sustained release part

[0053] Allopurinol 200g

[0054] Hypromellose K4M 25g

[0055] Hypromellose E5 26g

[0056] Microcrystalline Cellulose 101 45g

[0057] Povidone K30 15g

[0058] Magnesium stearate 0.8g

[0059]

[0060] Made into 1000 pieces / grain

[0061] Preparation method: with embodiment 1.

Embodiment 3

[0063] Quick release part:

[0064] Allopurinol 125g

[0065] Microcrystalline Cellulose 101 38g

[0066] Sodium carboxymethyl starch 23g

[0067] Povidone K 30 12g

[0068] Magnesium Stearate 1g

[0069] Sustained release part:

[0070] Allopurinol 125g

[0071] Hypromellose K100LV 55g

[0072] Microcrystalline Cellulose 101 40g

[0073] Povidone K 30 15g

[0074] Magnesium Stearate 1g

[0075]

[0076] A total of 1000 pieces / grain

[0077] Preparation method: with embodiment 1.

technical field

[0001] The invention relates to an allopurinol double-release preparation and a preparation method thereof, which is characterized in that the double-release preparation is composed of an immediate-release part and a sustained-release part, wherein the immediate-release part and the sustained-release part contain the main drug allopurinol The specific gravity is 1:1-1:24. It belongs to the technical field of pharmaceutical preparations. Background technique

[0002] Allpurinol has a chemical structure of 1H-pyrazolo[3,4-d]pyrimidin-4-ol. Allopurinol is white or off-white crystalline powder; almost odorless and tasteless. Very slightly soluble in water or ethanol, insoluble in ether or chloroform; dissolved in alkaline solution. Allopurinol is currently the only drug that can inhibit the synthesis of uric acid. It and its metabolite oxypurinol inhibit the activity of xanthine oxidase, prevent the metabolism of hypoxanthine and xanthine into uric acid, and r...

Examples

Embodiment 1

[0026] quick release part

[0027] Allopurinol 50g

[0028] Microcrystalline Cellulose 101 20g

[0029] Starch 30g

[0030] Povidone K30 3g

[0031] Magnesium stearate 0.5g

[0032] Sustained release part

[0033] Allopurinol 200g

[0034] Hypromellose K100LV 40g

[0035] Microcrystalline Cellulose 101 50g

[0036] Povidone K30 15g

[0037] Magnesium stearate 0.8g

[0038]

[0039] Made into 1000 pieces / grain

[0040] Preparation:

[0041] (1) Preparation of immediate-release granules: crush allopurinol through an 80-mesh sieve, and set aside; weigh allopurinol, starch, povidone K30, and microcrystalline cellulose 101 of the prescribed amount, mix well, add appropriate amount of water, and carry out Wet granulation, wet granulation with a 16-mesh sieve, drying at 50°C, granulation with a 20-mesh sieve, calculate the yield, add magnesium stearate, mix, and set aside.

[0042] (2) Preparation of sustained-release granules: cr...

Embodiment 2

[0046] Quick release part:

[0047] Allopurinol 50g

[0048] Microcrystalline Cellulose 101 25g

[0049] Starch 26g

[0050] Povidone K30 3.7g

[0051] Magnesium stearate 0.5g

[0052] Sustained release part

[0053] Allopurinol 200g

[0054] Hypromellose K4M 25g

[0055] Hypromellose E5 26g

[0056] Microcrystalline Cellulose 101 45g

[0057] Povidone K30 15g

[0058] Magnesium stearate 0.8g

[0059]

[0060] Made into 1000 pieces / grain

[0061] Preparation method: with embodiment 1.

Embodiment 3

[0063] Quick release part:

[0064] Allopurinol 125g

[0065] Microcrystalline Cellulose 101 38g

[0066] Sodium carboxymethyl starch 23g

[0067] Povidone K 30 12g

[0068] Magnesium Stearate 1g

[0069] Sustained release part:

[0070] Allopurinol 125g

[0071] Hypromellose K100LV 55g

[0072] Microcrystalline Cellulose 101 40g

[0073] Povidone K 30 15g

[0074] Magnesium Stearate 1g

[0075]

[0076] A total of 1000 pieces / grain

[0077] Preparation method: with embodiment 1.

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