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Aprepitant capsules

A technology of aprepitant and capsules, applied in the field of medicine, can solve the problems of failure to provide dissolution rate, etc., and achieve the effect of good dissolution rate, fast dissolution rate and simple process

Active Publication Date: 2015-05-06
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The prior art fails to provide an aprepitant preparation with high dissolution rate and simple preparation process

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019]

[0020] Preparation Process:

[0021] Dissolve aprepitant in diethylene glycol monoethyl ether, add hydroxypropyl cellulose, stir to dissolve, then add the prescribed amount of fumed silica for adsorption, and then mix with lactose, sodium carboxymethyl starch, stearin Magnesium Oxide is mixed well and made by direct filling capsules.

Embodiment 2

[0023]

[0024] Preparation Process:

[0025] Dissolve aprepitant in diethylene glycol monoethyl ether, add hydroxypropyl cellulose, stir to dissolve, then add the prescribed amount of fumed silica for adsorption, and then mix with microcrystalline cellulose and crospovidone , magnesium stearate, mixed evenly, and directly filled into capsules.

Embodiment 3

[0027]

[0028]

[0029] Preparation Process:

[0030] Dissolve aprepitant in diethylene glycol monoethyl ether, add hydroxypropyl cellulose, stir to dissolve, then add the prescribed amount of fumed silica for adsorption, and then mix with microcrystalline cellulose and crospovidone , magnesium stearate, mixed evenly, and directly filled into capsules.

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Abstract

The invention belongs to the technical field of medicines, and specifically relates to aprepitant capsules. The aprepitant capsules contain aprepitant, hydroxy propyl cellulose, diethylene glycol monoethyl ether, fumed silica and other pharmaceutically acceptable filler, disintegrant and lubricant. A preparation method of the aprepitant capsules comprises the following steps: dissolving aprepitant in diethylene glycol monoethyl ether, adding hydroxy propyl cellulose, stirring to dissolve, adding fumed silica to adsorb, then uniformly mixing with the other pharmaceutically acceptable filler, disintegrant and lubricant, and directly filling capsules. Compared with the prior art, the aprepitant capsules disclosed by the invention are fast in medicine dissolution speed, simple in process, and free from a surfactant and a micronization treatment. An acceleration test result indicates that the prepared aprepitant capsules are high in dissolution rate.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to an aprepitant capsule. Background technique [0002] Aprepitant (aprepitanl) is an NK-1 receptor antagonist currently on the market for antiemetic. The NK-1 receptor is the binding site for tachykinin (NKA) substance P (SP), located in the brainstem vomiting center and the gastrointestinal tract. Animal experiments have shown that SP can induce vomiting. Drugs that specifically block this receptor prevent vomiting from all emetogenic stimuli, including cisplatin. Aprepitant is an NK-1 receptor blocker, which blocks the action of substance P by binding to NK-1 receptors (mainly present in the central nervous system and its periphery). Aprepitant can pass through the blood-brain barrier and occupy the NK-1 receptors in the brain with selectivity and high affinity, but has low affinity for NK-2 and NK-3 receptors. Aprepitant is the only NK-1 receptor drug that has been marketed...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/5377A61K47/04A61P1/08
Inventor 张贵民秦守刚崔召元
Owner SHANDONG NEWTIME PHARMA
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