Hydroxychloroquine sulfate pharmaceutical composition and preparation method thereof

Abstract

The invention provides a hydroxychloroquine sulfate pharmaceutical composition and a preparation method thereof. The hydroxychloroquine sulfate pharmaceutical composition comprises the following components in percentage by weight: 60-70% of a pharmaceutical active component, 20-30% of a filler, 2-10% of an adhesive, 2-10% of a disintegrating agent, 0.5-2% of a lubricant and 2-6% of a coating material. The pharmaceutical composition and the preparation method have the advantages that the hygroscopicity is low, the compressibility and the reproducibility are good, the problem of tablet sticking caused by moisture absorption of hydroxychloroquine sulfate particles can be solved, and the production convenience and the stability are greatly improved.

Description

technical field

[0001] The invention belongs to the technical field of medicine, and in particular relates to a hydroxychloroquine sulfate pharmaceutical composition and a preparation method. Background technique

[0002] Hydroxychloroquine sulfate, chemical name: (±)-2-[[4-[(7-chloro-4-quinolyl)amino]pentyl]ethylamino]-ethanol sulfate, clinically used for rheumatoid arthritis, Juvenile chronic arthritis, discoid and systemic lupus erythematosus, and skin lesions triggered or exacerbated by sunlight. It is white or off-white crystalline powder; odorless and bitter. Soluble in water, almost insoluble in ethanol, chloroform or ether. The chemical structural formula is as follows:

[0003]

[0004] Hydroxychloroquine sulfate raw material is white or off-white crystalline powder, easily soluble in water and highly hygroscopic. In the process of making hydroxychloroquine sulfate into tablets, within the normal humidity range (45%~75%) of the GMP workshop, it is extremely...

Examples

Embodiment 1

[0026]

[0027] Preparation:

[0028] (1) Add active ingredients, fillers, and binders filtered through a 50-60 mesh screen into a wet mixing granulator for granulation, and then dry and granulate to obtain solid granules;

[0029] (2) Add the above-mentioned granules, disintegrating agent, and lubricant into the mixer and granulate again. After tableting, control the humidity between the tablets to ≤40%, control the tablet weight to 290-310mg, and the hardness to 6-10kg to obtain plain tablets ;

[0030] (3) Prepare the film coating premix into a 15% aqueous solution, coat the above-mentioned plain tablets, set the temperature of the coating machine at 50-70°C, atomize at 0.2-0.4MPa, and control the negative pressure of the coating machine at -100pa , Coating weight increase to 2.9-3.1% to stop coating, to obtain the finished product.

Embodiment 2

[0032]

[0033] Preparation:

[0034] (1) Add active ingredients, fillers, and binders filtered through a 50-60 mesh screen into a wet mixing granulator for granulation, and then dry and granulate to obtain solid granules;

[0035] (2) Add the above-mentioned granules, disintegrating agent, and lubricant into the mixer and granulate again. After tableting, control the humidity between the tablets to ≤40%, control the tablet weight to 290-310mg, and the hardness to 6-10kg to obtain plain tablets ;

[0036] (3) Prepare the film coating premix into a 15% aqueous solution, coat the above-mentioned plain tablets, set the temperature of the coating machine at 50-70°C, atomize at 0.2-0.4MPa, and control the negative pressure of the coating machine at -100pa , Coating weight increase to 2.9-3.1% to stop coating, to obtain the finished product.

Embodiment 3

[0038]

[0039] Preparation:

[0040] (1) Add active ingredients, fillers, and binders filtered through a 50-60 mesh screen into a wet mixing granulator for granulation, and then dry and granulate to obtain solid granules;

[0041] (2) Add the above-mentioned granules, disintegrating agent, and lubricant into the mixer and granulate again. After tableting, control the humidity between the tablets to ≤40%, control the tablet weight to 290-310mg, and the hardness to 6-10kg to obtain plain tablets ;

[0042] (3) Prepare the film coating premix into a 15% aqueous solution, coat the above-mentioned plain tablets, set the temperature of the coating machine at 50-70°C, atomize at 0.2-0.4MPa, and control the negative pressure of the coating machine at -100pa , Coating weight increase to 3.1-3.3% to stop coating, to obtain the finished product.

technical field

[0001] The invention belongs to the technical field of medicine, and in particular relates to a hydroxychloroquine sulfate pharmaceutical composition and a preparation method. Background technique

[0002] Hydroxychloroquine sulfate, chemical name: (±)-2-[[4-[(7-chloro-4-quinolyl)amino]pentyl]ethylamino]-ethanol sulfate, clinically used for rheumatoid arthritis, Juvenile chronic arthritis, discoid and systemic lupus erythematosus, and skin lesions triggered or exacerbated by sunlight. It is white or off-white crystalline powder; odorless and bitter. Soluble in water, almost insoluble in ethanol, chloroform or ether. The chemical structural formula is as follows:

[0003]

[0004] Hydroxychloroquine sulfate raw material is white or off-white crystalline powder, easily soluble in water and highly hygroscopic. In the process of making hydroxychloroquine sulfate into tablets, within the normal humidity range (45%~75%) of the GMP workshop, it is extremely...

Examples

Embodiment 1

[0026]

[0027] Preparation:

[0028] (1) Add active ingredients, fillers, and binders filtered through a 50-60 mesh screen into a wet mixing granulator for granulation, and then dry and granulate to obtain solid granules;

[0029] (2) Add the above-mentioned granules, disintegrating agent, and lubricant into the mixer and granulate again. After tableting, control the humidity between the tablets to ≤40%, control the tablet weight to 290-310mg, and the hardness to 6-10kg to obtain plain tablets ;

[0030] (3) Prepare the film coating premix into a 15% aqueous solution, coat the above-mentioned plain tablets, set the temperature of the coating machine at 50-70°C, atomize at 0.2-0.4MPa, and control the negative pressure of the coating machine at -100pa , Coating weight increase to 2.9-3.1% to stop coating, to obtain the finished product.

Embodiment 2

[0032]

[0033] Preparation:

[0034] (1) Add active ingredients, fillers, and binders filtered through a 50-60 mesh screen into a wet mixing granulator for granulation, and then dry and granulate to obtain solid granules;

[0035] (2) Add the above-mentioned granules, disintegrating agent, and lubricant into the mixer and granulate again. After tableting, control the humidity between the tablets to ≤40%, control the tablet weight to 290-310mg, and the hardness to 6-10kg to obtain plain tablets ;

[0036] (3) Prepare the film coating premix into a 15% aqueous solution, coat the above-mentioned plain tablets, set the temperature of the coating machine at 50-70°C, atomize at 0.2-0.4MPa, and control the negative pressure of the coating machine at -100pa , Coating weight increase to 2.9-3.1% to stop coating, to obtain the finished product.

Embodiment 3

[0038]

[0039] Preparation:

[0040] (1) Add active ingredients, fillers, and binders filtered through a 50-60 mesh screen into a wet mixing granulator for granulation, and then dry and granulate to obtain solid granules;

[0041] (2) Add the above-mentioned granules, disintegrating agent, and lubricant into the mixer and granulate again. After tableting, control the humidity between the tablets to ≤40%, control the tablet weight to 290-310mg, and the hardness to 6-10kg to obtain plain tablets ;

[0042] (3) Prepare the film coating premix into a 15% aqueous solution, coat the above-mentioned plain tablets, set the temperature of the coating machine at 50-70°C, atomize at 0.2-0.4MPa, and control the negative pressure of the coating machine at -100pa , Coating weight increase to 3.1-3.3% to stop coating, to obtain the finished product.

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