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A kind of tablet of novel opioid delta receptor agonist hydrochloride and preparation method thereof

A δ receptor and agonist technology, applied in the field of chemical pharmaceuticals

Active Publication Date: 2021-03-12
YUNNAN INST OF MATERIA MEDICA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The forced swimming test in rats shows that the drug takes effect quickly, and the effect can be seen after only a single administration, while the current commonly used antidepressant drugs usually take 1-2 weeks to be effective

Method used

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  • A kind of tablet of novel opioid delta receptor agonist hydrochloride and preparation method thereof
  • A kind of tablet of novel opioid delta receptor agonist hydrochloride and preparation method thereof
  • A kind of tablet of novel opioid delta receptor agonist hydrochloride and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042]

[0043]

[0044] Pure water wet granulation, and then add the following materials

[0045]

[0046] Preparation: 4-{(αR)-α-[(2S,5R)-4-(3-fluorobenzyl)-2,5-dimethyl-1-piperazinyl]-3-hydroxybenzyl} -(4'-methylpiperidinyl)-benzamide dihydrochloride is mixed evenly with other excipients, binders and disintegrants. Granulate with aqueous solution, dry and granulate. Add disintegrant, filler, glidant and lubricant, and mix well. Tablet. Take 6 tablets and measure according to the method under the item of disintegration time limit determination in the appendix of Chinese Pharmacopoeia 2015 edition, and the average disintegration time of the obtained tablets is 4.83min.

Embodiment 2

[0048]

[0049] Pure water wet granulation, and then add the following materials

[0050]

[0051] The sample preparation method is the same as above, and the determination method is the same as above. The disintegration time of the obtained tablet was 5 minutes.

Embodiment 3

[0053]

[0054] Pure water wet granulation, and then add the following materials

[0055]

[0056] The sample preparation method is the same as above, and the determination method is the same as above. The disintegration time of the obtained tablet was 1 min.

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Abstract

The invention relates to a tablet of a novel opioid delta receptor agonist hydrochloride and a preparation method thereof. The invention solves the problem of slow tablet disintegration and dissolution by adopting a method of adding a disintegrating agent inside and outside. The delta receptor agonist is 4‑{(αR)‑α‑[(2S,5R)‑4‑(3‑fluorobenzyl)‑2,5‑dimethyl‑1‑piperazinyl]‑(3 ‑Hydroxybenzyl)}‑(4'‑methylpiperidinyl)‑benzamide. By screening the disintegrating agent and the method of adding the disintegrating agent, the disintegrating time limit of the tablet is less than 5 minutes, so that the drug can be released rapidly in the gastric juice and take effect quickly.

Description

technical field [0001] The invention belongs to the field of chemical pharmacy, in particular to a 4-{(αR)-α-[(2S,5R)-4-(3-fluorobenzyl)-2,5-dimethyl-1-piperazinyl ]-(3-hydroxybenzyl)}-(4'-methylpiperidinyl)-benzamide dihydrochloride tablet and a preparation method thereof. [0002] technical background [0003] With the rapid economic development and the accelerated pace of life, depression has become a common and frequently-occurring disease. Subsequently, different types of antidepressants such as selective serotonin reuptake inhibitors, tricyclic antidepressants, and aminoketone antidepressants have emerged on the market. Although the above-mentioned drugs are effective, side effects such as drowsiness, disordered thinking, sexual dysfunction and the like can be produced in varying degrees during the medication process, and the onset of effect is slow. The existing drugs for the treatment of depression mainly fall into the following categories: [0004] 1) Traditional ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K47/36A61K47/38A61K47/32A61K31/496A61P25/24
CPCA61K9/2027A61K9/2054A61K9/2059A61K9/2095A61K31/496
Inventor 王京昆孙文强田霞李丽云王泽人丁江生宋鹤孙敏
Owner YUNNAN INST OF MATERIA MEDICA