Venlafaxine hydrochloride liquid slow-release preparation and its preparation method

A technology of venlafaxine hydrochloride and sustained-release preparations, which is applied in the field of medicine, can solve problems such as side effects, discomfort in taste, and difficulty in dividing doses, and achieve the effect of stable blood drug concentration and long duration of drug effect

Inactive Publication Date: 2005-07-06
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the differences in physiological functions between these patients and adults, in addition to the difference in dosage, there are also different requirements for dosage forms and compliance of medication. Oral controlled-release tablets or capsules and other solid preparations are often due to taste Discomfort or difficulty in swallowing and difficulty in dividing doses lead to inconvenience in taking such patients, affecting the completion of the normal treatment plan and the exertion of the drug effect. Some film-controlled tablets or sustained-release tablets are taken after being broken, and even severe side effect

Method used

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  • Venlafaxine hydrochloride liquid slow-release preparation and its preparation method
  • Venlafaxine hydrochloride liquid slow-release preparation and its preparation method

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preparation example Construction

[0030] 1. Preparation of Drug Resin

[0031] Method 1: add an appropriate amount of deionized water to the cation exchange resin, add the drug under stirring and mix evenly, take samples at regular intervals, and measure the concentration of the drug in the solution. When the drug concentration no longer changes with time, the equilibrium is reached, the unbound drug on the surface of the resin is washed away with deionized water, and the drug-loaded resin is obtained by drying at 40°C-60°C.

[0032] Method 2: Suspend the cation exchange resin in water and pour it into a suitable long glass tube, then slowly inject the high-concentration drug solution from the upper end of the adsorption column. Rinse with deionized water repeatedly to remove unbound drug on the surface, and dry at 40°C-60°C to obtain the drug-loaded resin.

[0033] 2. Impregnation of drug resin

[0034] Method 1: Take an appropriate amount of drug-loaded resin, add it to an aqueous solution of an impregnati...

Embodiment 1

[0043] Venlafaxine hydrochloride: 75mg;

[0044] Amberlite IRP69: 75mg;

[0045] PEG4000: 30mg;

[0046] PEG400: 2.5 mg;

[0047] Diethyl phthalate: 2.5mg;

[0048] EC (20cps) 20mg;

[0049] PVP (K90) 5mg

[0050] HPMC (K15M) 10mg

[0051] Carbopol (934P) 10mg

Embodiment 2

[0053] Venlafaxine hydrochloride: 75mg;

[0054] Amberlite IRP69: 100mg;

[0055] PEG4000: 35mg;

[0056] PEG400: 2.5 mg;

[0057] Diethyl phthalate: 2.5mg;

[0058] Eudragit RS100 20mg;

[0059] PVP (K30) 10mg

[0060] HPMC (K4M) 10mg

[0061] Avicel (RC591) 10mg

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Abstract

The invention discloses a Venlafaxine hydrochloride liquid slow-release preparation and its preparation method, wherein the preparation comprises venlafaxine hydrochloride 30-90%, adjuvant 10-70% for slow release action, and balancing adjuvant. The adjuvant with slow release action is cationic ion-exchange resin and acrylic resin and / or cellulose ethyl ether. The slow release preparation can sustain blood medicament concentration effectively within 24 hours.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a liquid sustained-release preparation of antidepressant venlafaxine hydrochloride administered once a day and a preparation method thereof. Background technique [0002] Venlafaxine Hydrochloride (hereinafter referred to as VL) is a new type of phenethylamine antidepressant, which is different from tricyclic antidepressants (TCAs) and monoamine oxidase inhibitors (MAOI), and is the first serotonin (5-HT) and norepinephrine (NE) dual reuptake strong inhibitors, dopamine (DA) weak inhibitors; has unique neuropharmacological effects, and M choline receptors, histamine H1 receptors, adrenaline α1, α2, and β receptors have almost no affinity. Compared with similar drugs, venlafaxine hydrochloride has the characteristics of rapid onset of action and fewer adverse reactions, so it can be used as a first-line treatment drug for major depression. [0003] Oral administration of venlaf...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/137A61P25/24
Inventor 潘卫三张春月刘宏飞
Owner SHENYANG PHARMA UNIVERSITY
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