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Vilazodone inclusion complexes, compositions and preparation thereof

A technology of composition and clathrate, applied in the direction of drug combination, non-active ingredients of polymer compounds, pharmaceutical formulations, etc., can solve the problem of low bioavailability

Pending Publication Date: 2019-06-21
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Containing vilazodone hydrochloride crystal form IV Tablets, which were approved by the U.S. Food and Drug Administration in 2011 for the treatment of major depressive disorder, The instructions clearly stipulate that the drug must be taken with food, and the bioavailability is very low when taken on an empty stomach

Method used

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  • Vilazodone inclusion complexes, compositions and preparation thereof
  • Vilazodone inclusion complexes, compositions and preparation thereof
  • Vilazodone inclusion complexes, compositions and preparation thereof

Examples

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Comparison scheme
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specific Embodiment approach

[0090] Those skilled in the art will appreciate that the following examples are intended to illustrate the invention and are not to be construed as limiting the invention. Various modifications and variations of the present invention will occur to those skilled in the art. Unless otherwise specified, if no specific technique or condition is explicitly described in the following embodiments, those skilled in the art can perform the procedure according to the commonly used technique or condition in the field or according to the product specification. The medicines, reagents or instruments used were not indicated by the manufacturer, and they were all commercially available conventional products.

[0091] Among them, the reference preparation Vilazodone hydrochloride tablets with a specification of 10 mg / tablet developed for Merck in Germany.

Embodiment approach

[0092] Unless otherwise specified, the following embodiments adopt the following detection methods:

[0093] HPLC instrument model: Agilent 1260

[0094] Chromatographic conditions: detection wavelength: UV242nm, chromatographic column: kromasil 100-5C18 4.6mm×150mm, 5 microns, mobile phase: 0.02M pH6.0 dipotassium hydrogen phosphate and acetonitrile are 54:46 (V / V, volume ratio), Flow rate: 1.0mL / min, injection volume: 10 microliters, running time: 4.5min.

Embodiment 1

[0109] In Example 1, vilazodone hydrochloride (API) and sulfobutyl-β-cyclodextrin (SBE-β-CD) were stirred in a water bath at 80°C for 4 hours according to the prescription ratio in Table 4 to obtain the clathrate solution, and then freeze-dried to obtain a powder clathrate composition.

[0110] Table 4 The prescription ratio of vilazodone hydrochloride and sulfobutyl-β-cyclodextrin

[0111]

[0112] Each sample of the clathrate solution was filtered through a 0.45 micron filter membrane, and the filtrate was taken for HPLC testing to determine the content of the drug in the clathrate solution. Inclusion rate=included drug amount / total drug amount×100%. The results are shown in Table 5.

[0113] Table 5 drug inclusion amount and inclusion rate

[0114]

[0115]

[0116] According to the method in Comparative Example 1, in 0.1N HCl and pH 6.8 buffer solution, the vilazodone inclusion complex 1-0 to 1-5, C1 and the reference preparation (RLD) (each 10mg) were carried ...

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PUM

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Abstract

Disclosed herein are inclusion complexes comprising vilazodone or a pharmaceutically acceptable salt thereof and an inclusion material, compositions and pharmaceutical formulations comprising the inclusion complexes, and methods for preparing the inclusion complexes, compositions or pharmaceutical formulations.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a vilazodone pharmaceutical preparation and a preparation method. Background technique [0002] Vilazodone is an antidepressant that belongs to the group of selective serotonin reuptake inhibitors and partial agonists of 5-HT1A receptors. Containing vilazodone hydrochloride crystal form IV Tablets, which were approved by the U.S. Food and Drug Administration in 2011 for the treatment of major depressive disorder, The instructions clearly stipulate that the drug must be taken with food, and the bioavailability is very low when taken on an empty stomach. [0003] Summary of the invention [0004] In one aspect, the present invention provides an clathrate, which comprises an active ingredient and an inclusion material, wherein the active ingredient is vilazodone or a pharmaceutically acceptable salt thereof, and the inclusion material is cyclodextrin or its derivatives. [0005] In so...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61K47/40A61P25/24
CPCA61K31/496A61P25/24A61K9/1652A61K9/2018A61K9/205A61K9/2054A61K47/40
Inventor 奉水旺黄心游劲松黄芳芳
Owner SUNSHINE LAKE PHARM CO LTD
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