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Aprepitant compound and its preparation method

An aprepitant and compound technology, which is applied in the field of highly soluble aprepitant compound and its preparation, can solve the problems of fast elimination, difficult drug absorption, poor bioavailability, etc. Great clinical application value and the effect of improving bioavailability

Active Publication Date: 2015-02-25
SHANGHAI SUNTECH PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is often difficult to make products with clinical efficacy for such drugs, because the drugs are difficult to be absorbed by the body, the elimination speed in the body is too fast, and the bioavailability is poor.

Method used

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  • Aprepitant compound and its preparation method
  • Aprepitant compound and its preparation method
  • Aprepitant compound and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Preparation of Aprepitant Complex

[0036] Aprepitant, sucrose and suspending agents hypromellose and poloxamer were wet milled.

[0037] formula:

[0038] name

[0039] *: Removed during process

[0040] preparation:

[0041] Connect the wet grinding machine ECM-AP 05 and the liquid distribution tank (with jacket and stirring paddle) to the water cooling system respectively, and the temperature of the cold water is 10°C. Aprepitant, Poloxamer F127 and Hypromellose E5 were mixed into a homogeneous solid mixture. Put another purified water in the liquid mixing tank, turn on the stirring, slowly add aprepitant, poloxamer F127 and hypromellose E5 into the above liquid mixing tank, and add while stirring to form a uniform mixture. Suspension, keep stirring, set aside. Connect the outlet of the liquid dispensing tank to the inlet of the wet grinder with a pipeline, connect the outlet of the wet grinder to the inlet of the liquid dispensing tank with ...

Embodiment 2

[0049] Aprepitant, fructose, and suspending agent, sodium carboxymethylcellulose, were wet milled.

[0050] formula:

[0051] name

[0052] Aprepitant

[0053] *: Removed during process

[0054] preparation:

[0055] Connect the wet grinding machine ECM-AP 05 and the liquid distribution tank (with jacket and stirring paddle) to the water cooling system, and the temperature of the cold water is 8 degrees. Mix aprepitant and sodium carboxymethylcellulose to form a homogeneous solid mixture. Weigh a certain amount of purified water into the liquid mixing tank, turn on the stirring, slowly add aprepitant and carboxymethylcellulose sodium into the above liquid mixing tank, add while stirring to form a uniform suspension, keep Stirring state, set aside. The above-mentioned liquid preparation tank is connected with the wet grinding machine with a pipeline, the grinding machine is turned on, the grinding administration speed is 3 L / min, and the grinding bead pa...

Embodiment 3

[0062] Aprepitant, dextrose and suspending agent hydroxyethylcellulose were wet milled.

[0063] formula:

[0064] name

[0065] *: Removed during process

[0066] preparation:

[0067] Connect the wet grinding machine ECM-AP 05 and the liquid distribution tank (with jacket and stirring paddle) to the water cooling system, and the temperature of the cold water is 7 degrees. Aprepitant and hydroxyethylcellulose were mixed into a homogeneous solid mixture. Weigh a certain amount of purified water into the liquid mixing tank, turn on the stirring, slowly add aprepitant and hydroxyethyl cellulose into the above liquid mixing tank, add while stirring to form a uniform suspension, keep stirring status, standby. Connect the above-mentioned liquid preparation tank to the wet grinder with a pipeline, turn on the grinder, grind the dosing speed to 4 L / min, and the grinding bead particle size is 0.1 mm. After the grinding starts, slowly add the prescribed amount of glucose...

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Abstract

The invention provides an aprepitant compound. The compound comprises 30-70wt% of aprepitant, 20-60wt% of monosaccharide and 10-50wt% of a suspending agent. The monosaccharide in the compound is helpful for forming aprepitant nanocrystals; and the suspending agent can avoid local non-uniformity caused by wet grinding and settlement of a suspension in the spray drying process. The prepared aprepitant compound greatly improves the solubility of aprepitant, is helpful for improving the bioavailability of aprepitant, and has great clinical application values. The method of the invention is simple, and is suitable for industrial production.

Description

technical field [0001] The invention relates to pharmaceutical preparations, in particular to a highly soluble aprepitant complex and a preparation method thereof. Background technique [0002] Aprepitant is the first neurokinin NK-1 receptor blocker approved by the US FDA in 2003. The developer of its original research product is Merck & Co. of the United States, which is mainly used for the prevention of postoperative vomiting, as well as the prevention and control of vomiting after the use of chemotherapy drugs. Its chemical name is 5-[[(2R,3S)-2-[(R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorobenzene Base) morpholino] methyl] -1 hydrogen -1,2,4-triazol-3 (2 hydrogen) -one, the molecular formula is C 23 h 21 f 7 N 4 o 3 . Its structural formula is as follows: [0003] [0004] Aprepitant is almost insoluble in water, and its Log P (P is the oil-water partition coefficient) at pH 7.0 is 4.8. Therefore, according to the classification of biopharmaceutic...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/20A61K9/16A61K9/48A61K31/5377A61K47/26A61P1/08
Inventor 何平钱晓明龚援梁思齐
Owner SHANGHAI SUNTECH PHARMA
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