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Preparation containing 1-(cinnamoyl)-4-(cyclopentylamine acetyl) piperazidine and/or salt thereof and pharmaceutic adjuvant

A technology of amylamine acetyl group and cinnamoyl group, applied in the field of medicine, can solve the problems of increased content of cis-isomer of cinnamate maleate, great influence on drug safety, high toxicity and the like

Inactive Publication Date: 2011-05-11
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, after long-term storage, the content of the cis-isomer of cinepacid maleate in the related substances will increase significantly, and the cis-isomer of cinepacid maleate has greater toxicity and has a greater impact on the safety of the drug. Bring certain risks to clinical application

Method used

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  • Preparation containing 1-(cinnamoyl)-4-(cyclopentylamine acetyl) piperazidine and/or salt thereof and pharmaceutic adjuvant
  • Preparation containing 1-(cinnamoyl)-4-(cyclopentylamine acetyl) piperazidine and/or salt thereof and pharmaceutic adjuvant
  • Preparation containing 1-(cinnamoyl)-4-(cyclopentylamine acetyl) piperazidine and/or salt thereof and pharmaceutic adjuvant

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] One of the most preferred prescriptions and processes for solution injections:

[0043] 1. Prescription:

[0044] 1-(cinnamoyl)-4-(cyclopentylaminoacetyl)piperazine maleate 40g

[0045] D-Sorbitol 25.2g

[0046] Disodium hydrogen phosphate 2.5g

[0047] Add water for injection to 1000ml

[0048]

[0049] A total of 500 sticks were prepared

[0050]2. Process: Add D-sorbitol into 75% water for injection, dissolve within 1 minute at 60°C, then add the main drug to the above solution until it is partially dissolved, add 3 / 4 of disodium hydrogen phosphate to completely dissolve the main drug , slowly add the remaining disodium hydrogen phosphate solution, adjust the pH to 4.1; then add 0.1% needle-shaped activated carbon, keep stirring at 60°C for 15 minutes, filter while it is hot, and adjust the volume to the full amount; the intermediate product is obtained, and its pH is measured , if not within 3....

Embodiment 2

[0057] 1. Prescription

[0058] 1-(cinnamoyl)-4-(cyclopentylaminoacetyl)piperazine maleate 30g

[0059] D-Sorbitol 27.5g

[0060] Disodium hydrogen phosphate 2.4g

[0061] Add water for injection to 1000ml

[0062]

[0063] A total of 500 sticks were prepared

[0064] 2. Preparation process: Reference Example 1

Embodiment 3

[0066] 1. Prescription

[0067] 1-(cinnamoyl)-4-(cyclopentylaminoacetyl)piperazine maleate 35g

[0068] D-Sorbitol 26.8g

[0069] Disodium hydrogen phosphate 2.47g

[0070] Add water for injection to 1000ml

[0071]

[0072] A total of 500 sticks were prepared

[0073] 2. Preparation process: Reference Example 1

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Abstract

The invention provides 1-(cinnamoyl)-4-(cyclopentylamine acetyl) piperazidine and a preparation containing 1-(cinnamoyl)-4-(cyclopentylamine acetyl) piperazidine and a pharmaceutic adjuvant. 1-(cinnamoyl)-4-(cyclopentylamine acetyl) piperazidine maleate is a derivate of cinepazide, and experiments verify obvious pharmacological effect thereof. The invention concretely provides two injections of the compound, namely solution type and liposome type injections and preparation processes thereof. The solution type injection contains 30-45g of the compound, 20-30g of D-sorbierite, 2-3.5g of disodium hydrogen phosphate and an appropriate amount of water for injection. The preparation method of the solution type injection comprises the following steps: adding the D-sorbierite into water to be dissolved, adding the derivate into the D-sorbierite solution, stirring to partly dissolve the derivate, adding partial disodium hydrogen phosphate solution to completely dissolve the derivate, then regulating the pH value, and filtering, thus the injection preparation is obtained. The liposome type injection contains 1g of the derivate, 1-13g of phospholipid and 0.6-6g of cholesterol. The invention provides a compound with obvious pharmaceutical effect and also provides two safe and stable formulations of the compound and preparation methods thereof.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a preparation comprising 1-(cinnamoyl)-4-(cyclopentylaminoacetyl)piperazine and / or its salt and pharmaceutical excipients, wherein 1-(cinnamoyl) -4-(Cyclopentylaminoacetyl)piperazine is a derivative of Cinopazide, which has related significant pharmacological activities. Background technique [0002] Cinipacide is a new type of Ca2+ channel blocker, which has endogenous adenosine potentiation, calcium antagonism, cyclic adenosine monophosphate (CAMP) potentiation and 5-hydroxytryptamine (5-HT) neuron activation. It can not only relieve cerebrovascular resistance, increase cerebral blood flow, improve cell degeneration ability, improve microcirculation, increase tissue uptake of glucose in blood, reduce oxygen consumption, protect brain tissue, but also have better selective expansion Vascular action, can prevent vasospasm, protect neurons, reduce blood viscosity and ...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61K9/08A61K9/127A61P9/00A61P9/08A61P25/00
Inventor 吴正红陈钦恩和多黄欣谢开智
Owner CHINA PHARM UNIV
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