Dry suspensoid of Repirinast and its prepn. method

A technology of dry suspension and repimilast, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problem of uneven distribution of active ingredients of drugs and inability of drugs to reach Therapeutic effect, poor dispersion of granules and other problems, to achieve the effect of good compliance, good absorption and high dispersion

Active Publication Date: 2007-01-31
JUMPCAN PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Since repimilast tablet is a common oral solid preparation, it must go through disintegration, dissolution and other processes before it can be absorbed by the gastrointestinal tract when absorbed in the body. It is difficult to disintegrate and the drug is difficult to dissolve, so that the drug cannot achieve the desired therapeutic effect
In addition, tablets are difficult to administer in children and patients with swallowing difficulties
For the granules taken by children, because repimilast is insoluble in water, the dispersion of the granules made is poor, the active ingredients of the drug are unevenly distributed, the taste is poor, the absorption is slow, and the bioavailability is low.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Take the crushed: 50g repimilast, 20g sodium carboxymethylcellulose as suspending agent, 50g lactose as filler, 100g sucrose as flavoring agent, after mixing, pass through 200 mesh sieve, then 5g talcum powder as Lubricant, mix evenly and dispense.

Embodiment 2

[0022] The proportioning and production method of this example and Example 1 are basically the same, the difference is only: 30g of sodium citrate is also used as a flocculant in the raw materials mixed for the first time.

Embodiment 3

[0024] A. Take the pulverized: 50g repimilast, 2g hydroxypropyl methylcellulose sodium as suspending agent, 500g microcrystalline cellulose as filler, 10g mannitol as flavoring agent, 30g sodium citrate as flocculation Agents were dried and mixed and passed through a 80-mesh sieve. B. Add 20g of 50% ethanol (i.e. pure ethanol 10g) as a binder system soft material, cross 18 mesh sieves for granulation, and make dry granules after drying. The drying time is sufficient when the water content in the material is less than or equal to 1%, usually about 2 hours. C. Add 0.1g of micropowder silica gel as lubricant and 0.05g of butter essence to the dry granules, mix evenly, and pack them separately.

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PUM

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Abstract

A mixed dry suspension of repirinast is proportionally prepared from repirinast, suspending aid, filler, flavouring and lubricant. Its preparing process is also disclosed.

Description

Technical field [0001] The invention relates to a preparation of repimilast and a preparation method thereof. Background technique [0002] Anti-inflammatory therapy remains the primary treatment option for bronchial asthma, making topical inhalation therapy the main form of drug delivery for this disease. However, in recent years, with the intensification of localization of asthma treatment drugs, tablets, injections and compound preparations have been promoted more and more, and the share of systemic drugs has increased year by year, surpassing inhalants. Following the widespread use of agonist bronchodilators, the use of xanthines is expected to decrease, while the use of steroids and prophylactics will increase. The trend in the treatment of asthma is towards the widespread use of anti-inflammatory or pro-inflammatory drugs, including inhaled steroids and cromolyn. [0003] Repimilast is a new type of oral antiallergic drug with the chemical name of 5,6-dihydro-7,8-dim...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/4741A61K47/38A61P11/06
Inventor 蔡骏黄衡
Owner JUMPCAN PHARMA GRP
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