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Controlled-release medicinal composition containing demethyl venlafaxine benzoate compounds

A sustained-release drug and composition technology, applied in the field of sustained-release pharmaceutical composition and its preparation, can solve the problems of low bioavailability of preparations, unfavorable preparation development, and reduced solubility

Active Publication Date: 2013-01-16
SHANDONG LUYE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it has been found through research that the lipophilicity of the above-mentioned methylvenlafaxine benzoate compounds is enhanced, which is beneficial to the absorption of the drug, but due to the reduced solubility, it is not conducive to the development of its preparations, resulting in low bioavailability of the preparations.

Method used

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  • Controlled-release medicinal composition containing demethyl venlafaxine benzoate compounds
  • Controlled-release medicinal composition containing demethyl venlafaxine benzoate compounds
  • Controlled-release medicinal composition containing demethyl venlafaxine benzoate compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Prescription: 4-[2-dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenyl 4-methylbenzoic acid hydrochloride 42g, HPMC K4M CR 112g, citric acid 7g, microcrystalline Cellulose 187.25g, magnesium stearate 1.75g

[0029] Preparation method: The raw and auxiliary materials are all passed through an 80-mesh sieve for later use; weigh 4-[2-dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenyl hydrochloride of 4-methylbenzoate according to the prescription Salt, hydroxypropyl methylcellulose, microcrystalline cellulose, citric acid, mixed evenly; dry granulation machine granulation; adding magnesium stearate, mixed evenly and pressed into tablets, tablet weight 350±15mg, hardness 6±1kg, Make 1000 pieces, that is.

Embodiment 2

[0031] Prescription: 4-[2-dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenyl 4-methylbenzoic acid hydrochloride 112g, HPMC K4M CR112g, citric acid 8.75g, microcrystalline Cellulose 106.75g, 5% PVP absolute ethanol solution 140ml, magnesium stearate 3.5g

[0032] Preparation method: Weigh 4-[2-dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenyl hydrochloride, hydroxypropyl methylcellulose, Mix microcrystalline cellulose and citric acid evenly; add an appropriate amount of 5% PVP ethanol solution to the above mixed powder to prepare a soft material, and granulate with a 20-mesh sieve; dry the granules at 50°C, granulate with a 20-mesh sieve; add magnesium stearate , mixed and pressed into tablets, the weight of the tablet is 350±15mg, the hardness is 6±1kg, and it is made into 1000 tablets, that is to say.

Embodiment 3

[0034] Prescription: 4-[2-dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenyl 4-methylbenzoate hydrochloride 80g, HPMC K1500PH 105g, citric acid 17.5g, microcrystalline Cellulose 140.5g, 80% ethanol solution 180ml, sodium stearyl fumarate 7g

[0035]Preparation method: Weigh 4-[2-dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenyl hydrochloride, hydroxypropyl methylcellulose, Mix microcrystalline cellulose and citric acid evenly; add an appropriate amount of 80% ethanol solution to the above mixed powder to prepare a soft material, and granulate with a 20-mesh sieve; dry the granules at 50°C, and granulate with a 20-mesh sieve; Sodium maleate, mixed and pressed into tablets, tablet weight 350±15mg, hardness 6±1kg, made into 1000 tablets, ready to go.

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Abstract

The invention provides a controlled-release medicinal composition containing demethyl venlafaxine benzoate compounds which contain a compound represented by a general formula (I), an acidity regulator and a controlled-release framework material. The ontrolled-release medicinal composition provided by the invention can remarkably improve oral bioavailability of the demethyl venlafaxine benzoate compound preparations, and a preparation technology is simple and convenient, and an effect on improving the bioavailability of preparation can be reached, and active compounds are not needed to be additionally preprocessed.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a sustained-release pharmaceutical composition containing desmethylvenlafaxine benzoate compounds and a preparation method thereof. Background technique [0002] Depression is a common and serious mental illness. It has become the fourth major disease that endangers human health. At present, the incidence of depression in the world can reach 5% to 12%. About 15% of patients with depression commit suicide every year. . Drug intervention is an effective means to relieve symptoms and improve the quality of life of patients with depression. There are many drugs for the traditional treatment of depression, but the treatment of depression is limited due to reasons such as large adverse reactions and poor compliance. Selective serotonin reuptake inhibitors (SSRIs) and serotonin-norepinephrine reuptake inhibitors (SNRIs) are currently widely used clinically as new antidepress...

Claims

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Application Information

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IPC IPC(8): A61K31/235A61K47/12A61K9/22A61K9/16A61P25/24
Inventor 张雪梅袁志瞾盖芸芸王麒麟林东海
Owner SHANDONG LUYE PHARMA CO LTD
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