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Drug resin salt containing Ziprasidone and salt thereof and preparation method of drug resin salt

A technology of ziprasidone and ziprasidone acid, which is applied in the field of medicine and can solve problems such as potential safety hazards, environmental pollution, and long-term

Inactive Publication Date: 2013-12-04
AVENTIS PHARMA HAINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] But above-mentioned technology still has deficiencies: because the solubility of ziprasidone compound in water is low, carry out β-cyclodextrin clathrate in water and need carry out very long time, need continuous stirring about to be up to 4 days, in water It is difficult to achieve practical results in actual mass production
However, the preparation of the β-cyclodextrin inclusion complex of ziprasidone by heating and refluxing in an organic solvent shortens the time to a great extent, but the concentration of the required organic solvent is large, which inevitably increases the production capacity. The cost and the cost of recycling organic solvents, in addition, there are safety hazards in the production process, causing environmental pollution, etc.

Method used

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  • Drug resin salt containing Ziprasidone and salt thereof and preparation method of drug resin salt

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Add 1 g of ziprasidone hydrochloride and 2 g of Amberlite IRP-88 into 100 ml of propylene glycol: water (1:1) solution, and let the resin powder evenly disperse in the solution in a constant temperature water bath shaker, shake overnight at room temperature. A vacuum filter is used to separate the resin salt from the liquid, and then the resin salt is washed three times with a small amount of water, and the filtered resin is dried overnight in a vacuum drying oven at 60 degrees Celsius to obtain the pharmaceutical resin salt of ziprasidone.

Embodiment 2

[0015] Add 1 g of ziprasidone and 1.5 g of Amberlite IRP-64 into 100 ml of propylene glycol:water (1:1) solution, and shake overnight at room temperature in a constant temperature water bath shaker. A vacuum filter is used to separate the resin salt from the liquid, and then the resin salt is washed three times with a small amount of water, and the filtered resin is dried overnight in a vacuum drying oven at 60 degrees Celsius to obtain the pharmaceutical resin salt of ziprasidone.

Embodiment 3

[0017] A generic tablet containing 20 mg of ziprasidone:

[0018] (a) Prescription of granular powder: Unit: mg

[0019] components

[0020] Croscarmellose Sodium

[0021] Preparation method: Prepare ziprasidone hydrochloride 11.3g and Amberlite IRP-64 resin 20g according to the method described in Example 1 to prepare a drug resin salt, then mix with mannitol 61.2g, croscarmellose sodium 5g and hydroxypropyl After mixing 2g of methylcellulose evenly, use water as a wetting agent to make a soft material, granulate with a 18-mesh sieve, and dry at 50°C until the moisture content is less than 3.0%; granulate with a 24-mesh sieve to obtain the prepared granule powder .

[0022] (b) Prescription for tablet granules: Unit: mg

[0023] components

[0024] Preparation method: Mix 99.5g of the granules in (a) above with 0.5g of magnesium stearate evenly, press with a Φ6 flat die, and press into tablets with a weight of 100mg and a hardness of 50-80 Newt...

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Abstract

The invention belongs to the field of medicine and particularly relates to drug resin salt containing Ziprasidone and salt thereof and a preparation method of the drug resin salt. The drug resin salt is a drug resin composite formed by the Ziprasidone or the salt thereof and weak-acid cation-exchange resin. The weak-acid cation-exchange resin is Amberlite-series resin and in the mole ratio of 1.5+ / -0.5:1 to the Ziprasidone. The final application form of the drug resin salt includes but not limited to tablets, capsules, granules or suspensions and the like with the purpose of providing patients with the preparation containing the Ziprasidone and the salt thereof and having quick absorption and high bioavailability.

Description

Technical field: [0001] The invention belongs to the field of medicine, and in particular relates to a resin salt containing ziprasidone and a salt thereof and a preparation method thereof. Background technique: [0002] Ziprasidone is an important antipsychotic drug, which is effective for auditory and visual hallucinations of schizophrenia, and is mainly used for the treatment of schizophrenia or affective psychosis. [0003] Since various forms of ziprasidone compounds have strong hydrophobicity, are difficult to wet in water and have low water solubility, the dissolution rate of ziprasidone in water is very slow, and it needs to be pulverized to a certain The particle size is below to increase the dissolution rate and play a clinical therapeutic role. However, the pulverization process will increase the production cost, cause the loss of the raw material medicine, and possibly cause the pollution of the raw material medicine. Therefore, a more effective solubilization ...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61K47/32A61P25/18
Inventor 王飞孟旻翟志瑞
Owner AVENTIS PHARMA HAINAN