Preparation of powder injection pharmaceutical composition from high-purity papaverine hydrochloride

A technology of papaverine hydrochloride and its mixture, which is applied in the field of medicine and can solve problems such as insignificant curative effect

Active Publication Date: 2020-10-30
山东北大高科华泰制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has no significant curative effect on hypertension, angina pectoris, pyloric spasm, biliary colic, intestinal colic, bronchial asthma, etc.

Method used

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  • Preparation of powder injection pharmaceutical composition from high-purity papaverine hydrochloride
  • Preparation of powder injection pharmaceutical composition from high-purity papaverine hydrochloride
  • Preparation of powder injection pharmaceutical composition from high-purity papaverine hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0167] Embodiment 1: Preparation of papaverine hydrochloride powder injection pharmaceutical composition

[0168] formula:

[0169]

[0170]

[0171] Preparation method:

[0172] (a) Take by weighing papaverine hydrochloride and pharmaceutical excipients of the prescribed amount, add an appropriate amount (accounting for 65% of the prescription volume) of water for injection to dissolve, then add 0.5% of the volume of the medicinal liquid with active carbon for needles, stir, filter and decarbonize;

[0173] (b) Add water for injection to the prescribed amount, stir evenly, measure the pH value of the solution and optionally measure the active ingredient content, and adjust to the specified pH value with an acid-base regulator if necessary;

[0174] (c) The medicinal liquid is sterilized and filtered with a microporous membrane, and filled in vials;

[0175] (d) Freeze-drying to remove moisture, and stoppering, to obtain. This powder injection sample can be record...

Embodiment 2

[0176] Embodiment 2: Preparation of papaverine hydrochloride powder injection pharmaceutical composition

[0177] formula:

[0178]

[0179] Preparation method:

[0180] (a) Take by weighing papaverine hydrochloride and pharmaceutical excipients of the prescribed amount, add an appropriate amount (accounting for 50% of the prescription volume) of water for injection to dissolve, then add 0.5% of the volume of the medicinal liquid with active carbon for needles, stir, filter and decarbonize;

[0181] (b) Add water for injection to the prescribed amount, stir evenly, measure the pH value of the solution and optionally measure the active ingredient content, and adjust to the specified pH value with an acid-base regulator if necessary;

[0182] (c) The medicinal liquid is sterilized and filtered with a microporous membrane, and filled in vials;

[0183] (d) Freeze-drying to remove moisture, and stoppering, to obtain. This powder injection sample can be recorded as Ex2. ...

Embodiment 3

[0184] Embodiment 3: Preparation of papaverine hydrochloride powder injection pharmaceutical composition

[0185] formula:

[0186]

[0187]

[0188] Preparation method:

[0189] (a) Take by weighing papaverine hydrochloride and pharmaceutical excipients of the prescribed amount, add an appropriate amount (accounting for 90% of the prescription volume) of water for injection to dissolve, then add 0.8% of the volume of the medicinal liquid with active carbon for needles, stir, and decarbonize by filtration;

[0190] (b) Add water for injection to the prescribed amount, stir evenly, measure the pH value of the solution and optionally measure the active ingredient content, and adjust to the specified pH value with an acid-base regulator if necessary;

[0191] (c) The medicinal liquid is sterilized and filtered with a microporous membrane, and filled in vials;

[0192] (d) Freeze-drying to remove moisture, and stoppering, to obtain. The powder injection sample can be ...

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Abstract

The invention relates to preparation of a powder injection pharmaceutical composition from high-purity papaverine hydrochloride, in particular to a preparation method of papaverine hydrochloride. Themethod comprises the following steps of: heating 3, 4-dimethoxy-beta-phenyl-ethylamine and 3, 4-dimethoxy-phenyl-acetic acid to melting, and then carrying out reaction in a mixture of benzene and chlorethoxyfos to obtain 6, 7, 3', 4'-tetramethoxy-1-benzyl-dihydro-isoquinoline hydrochloride; then dissolving the wet product in tetrahydronaphthalene after the wet product becomes free alkali, and carrying out dehydrogenation reaction at 180DEG C in the presence of a Raney nickel catalyst; after dehydrogenation is finished, directly filtering the tetrahydronaphthalene reaction mixture from the Raney nickel catalyst into a mixture of a hydrochloric acid aqueous solution and methanol; filtering out precipitates, and performing recrystallizing from the ethanol-water solution in an inert gas environment to obtain off-white 6, 7, 3', 4'-tetramethoxy-1-benzyl isoquinoline hydrochloride, namely papaverine hydrochloride. The invention also relates to a papaverine hydrochloride powder injection pharmaceutical composition, and a preparation method and a quality detection method thereof. The invention achieves excellent technical effects as described in the specification.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to an opiate alkaloid used as a vasodilator, in particular to a freeze-dried powder injection of papaverine. The invention also relates to a quality detection method of the papaverine freeze-dried powder injection, especially a method for determining the content of specific impurities therein. In addition, the present invention also relates to a method for preparing high-purity papaverine hydrochloride, and a method for preparing its powder injection pharmaceutical composition by using the high-purity papaverine hydrochloride. The freeze-dried powder injection of papaverine of the present invention exhibits excellent technical effects as described herein. Background technique [0002] Papaverine, its hydrochloride is commonly used clinically, the English name is Papaverine Hydrochloride, the molecular formula of papaverine hydrochloride is C20H21NO4·HCl, the molecular weight is 375.8...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D217/20A61K31/472A61P9/08A61K9/19A61K47/26
CPCC07D217/20A61P9/08A61K9/0019A61K9/19A61K47/26
Inventor 张庚伦周洪娟张爽夏肖丽
Owner 山东北大高科华泰制药有限公司
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