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A kind of buflodil hydrochloride compound and pharmaceutical composition thereof

A technology of buflomedil hydrochloride and its compound, which is applied in the field of medicine, can solve problems affecting product stability, effectiveness and safety, internal quality of drug effect, decreased fluidity, and unsatisfactory effect, etc., to achieve excellent drug release behavior, Effect of reducing solubility and improving hygroscopicity

Active Publication Date: 2018-12-11
王珍 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the above-mentioned slow-release tablets have improved the release behavior of buflomedil hydrochloride to a certain extent, its effect is not ideal enough
And the research of prior art shows, buflomedil hydrochloride crude drug is easier to absorb moisture when placed under high-humidity conditions, and after absorbing moisture, it will cause changes in physical and chemical properties such as caking, fluidity decline, and deliquescence, thereby affecting product stability. Intrinsic qualities such as effectiveness, safety, and efficacy

Method used

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  • A kind of buflodil hydrochloride compound and pharmaceutical composition thereof
  • A kind of buflodil hydrochloride compound and pharmaceutical composition thereof
  • A kind of buflodil hydrochloride compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] [embodiment 1] the preparation of buflomedil hydrochloride compound

[0047] 1) Preparation of solution A: Sterile filter 600L of mixed solvent A of tetrahydrofuran and n-butanol (the volume ratio of tetrahydrofuran and n-butanol is 3:1) into a crystallization tank, cool down to 5°C and wait for use, which is solution A;

[0048] 2) Preparation of solution B: at room temperature, add 110L of mixed solvent B of water and methanol (the volume ratio of water and methanol is 5:1) into the dissolving tank, then add buflomedil hydrochloride crude product 30kg, dissolve and add activated carbon 0.45kg, stirring and decolorizing for 25 minutes, sterile filtering, washing with water, collecting the filtrate and washing liquid to obtain solution B;

[0049] 3) Add solution B into solution A, cool down to 5°C, keep the temperature, and stir at a stirring speed of 18 rpm for 25 minutes;

[0050] 4) Then lower the temperature to -5°C, control the stirring speed to 10 rpm, and contr...

Embodiment 2

[0052] [embodiment 2] the preparation of buflomedil hydrochloride compound

[0053] 1) Preparation of solution A: sterile filter 600L of mixed solvent A of tetrahydrofuran and n-butanol (the volume ratio of tetrahydrofuran and n-butanol is 8:1) into a crystallization tank, cool down to 10°C and wait for use, which is solution A;

[0054] 2) Preparation of solution B: at room temperature, add 90L of mixed solvent B of water and methanol (the volume ratio of water and methanol is 7:1) into the dissolution tank, then add 30kg of crude buflomedil hydrochloride, and add activated carbon after dissolving 0.45kg, stirring and decolorizing for 35 minutes, sterile filtering, washing with water, collecting the filtrate and washing liquid to obtain solution B;

[0055] 3) Add solution B into solution A, cool down to 8°C, keep the temperature, and stir at a stirring speed of 22 rpm for 35 minutes;

[0056] 4) Then lower the temperature to 0° C., control the stirring speed to 15 rpm, cont...

Embodiment 3

[0058] [embodiment 3] the preparation of buflomedil hydrochloride compound

[0059] 1) Prepare A solution: Sterile filter 600L of mixed solvent A of tetrahydrofuran and n-butanol (the volume ratio of tetrahydrofuran and n-butanol is 6:1) into a crystallization tank, cool down to 8°C and set aside for use, which is A solution;

[0060] 2) Preparation of solution B: at room temperature, add 100L of mixed solvent B of water and methanol (the volume ratio of water and methanol is 6:1) into the dissolution tank, then add 30kg of crude buflomedil hydrochloride, and add activated carbon after dissolving 0.45kg, stirring and decolorizing for 30 minutes, sterile filtering, washing with water, collecting the filtrate and washing liquid to obtain solution B;

[0061] 3) Add solution B into solution A, cool down to 6°C, keep the temperature, and stir at a stirring speed of 20 rpm for 30 minutes;

[0062] 4) Then lower the temperature to -2°C, control the stirring speed to 12 rpm, and con...

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Abstract

The invention belongs to the technical field of medicine, and particularly relates to a bullomedil hydrochloride compound and a pharmaceutical composition thereof. The structural formula of the bullomedil hydrochloride compound is as follow (see the formula in the description). An X-ray powder diffraction spectrogram obtained by measuring the bullomedil hydrochloride compound with Cu-Kalpha rays is shown as the figure one. The provided bullomedil hydrochloride compound reduces solubility of bullomedil hydrochloride bulk drugs in water to a certain degree, is in a new crystal form and has improved hygroscopicity. Meanwhile, it is indicated through tests that a sustained release tablet prepared from the bullomedil hydrochloride compound shows better drug release behaviors on the condition of the same prescription and the same preparing method.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a buflomedil hydrochloride compound and a pharmaceutical composition thereof. Background technique [0002] Buflomedil hydrochloride, chemical name: 4-(1-pyrrolidinyl)-1-(2,4,6-trimethoxyphenyl)-1-butanone hydrochloride. [0003] Molecular formula: C 17 h 25 NO 4 .HCl [0004] Molecular weight: 343.85 [0005] Pharmacological type: This product is an α-adrenergic receptor inhibitor, and has weak non-specific calcium ion antagonism. Improves microcirculatory blood flow in the brain and extremities by inhibiting the spasm of the anterior capillary sphincter. This product also has the functions of inhibiting platelet aggregation and improving red blood cell deformability. [0006] Pharmacokinetics: After intravenous infusion, buflomedil hydrochloride is widely distributed in tissues and body fluids, metabolized by the liver, and the elimination half-life is abou...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D295/104A61K31/40A61P7/02A61P9/00A61P9/10A61P25/00A61P25/28
CPCC07B2200/13C07D295/104
Inventor 刘华军王珍
Owner 王珍
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