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Novel anti-hypertension compound slow release tablets and production process thereof

A slow-release tablet and anti-hypertensive technology, which is applied in pill delivery, pharmaceutical formulations, cardiovascular system diseases, etc., can solve the problems of poor water solubility, high cost, and low bioavailability of quercetin, and achieve prevention Cardiovascular and other dangerous diseases, low toxicity, and the effect of inhibiting myocardial remodeling

Inactive Publication Date: 2017-07-07
SHANGHAI PHARMA DONGYING JIANGSU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the medical community and patients are mainly concerned about three issues about high blood pressure drugs: first, whether the antihypertensive effect is mild and stable, and whether it can protect other organs from damage; Whether the quality is not affected or the impact is very small; Third, as a chronic common disease, hypertension requires long-term control by patients, and whether the resulting costs are too expensive, which requires that the drug itself should be economical, so that the treatment of patients and the society is equal. able to bear
However, quercetin has poor water solubility and low bioavailability when used directly as a drug

Method used

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  • Novel anti-hypertension compound slow release tablets and production process thereof
  • Novel anti-hypertension compound slow release tablets and production process thereof
  • Novel anti-hypertension compound slow release tablets and production process thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] 1. The formulation and preparation of the quercetin and pinoresinol diglucoside PVP dispersion preparation stage:

[0050] formula:

[0051] Quercetin 20mg

[0052] Pinoresinol Diglucoside 20mg

[0053] PVP-k30 60mg

[0054] Preparation Process:

[0055] Take 20 mg of quercetin and 20 mg of pinoresinol diglucoside in a mixer and mix them evenly, add 60 mg of PVP-k30 to the reaction flask, add an appropriate amount of 95% ethanol, and stir in a water bath at 50°C for 3 hours until the solution is clear, then vacuum The solvent was removed by evaporation, freeze-dried, pulverized into powder, and sieved with 80 meshes to obtain a PVP dispersion of quercetin-pinoresinol diglucoside, which was stored in a desiccator for later use.

[0056] 2. Preparation of quercetin-pininol diglucoside gel matrix sustained-release granules:

[0057] Formula (calculated at 200mg / grain):

[0058]

[0059] Preparation Process:

[0060] The above-mentioned 100 mg of the quercetin-pin...

Embodiment 2

[0073] 1. The formulation and preparation of the quercetin and pinoresinol diglucoside PVP dispersion preparation stage:

[0074] formula:

[0075] Quercetin 18mg

[0076] Pinoresinol Diglucoside 20mg

[0077] PVP-k30 50mg

[0078] Preparation Process:

[0079] Take 18 mg of quercetin and 20 mg of pinoresinol diglucoside in a mixer and mix them evenly. Add 50 mg of PVP-k30 to the reaction flask, add an appropriate amount of 95% ethanol, and stir in a water bath at 50 °C for 3 hours until the solution is clear. The solvent was removed by evaporation, freeze-dried, pulverized into powder, and sieved with 80 meshes to obtain a PVP dispersion of quercetin-pinoresinol diglucoside, which was stored in a desiccator for later use.

[0080] 2. Preparation of quercetin-pininol diglucoside gel matrix sustained-release granules:

[0081] Formula (calculated at 200mg / grain):

[0082]

[0083] Preparation Process:

[0084] The above-mentioned 88 mg of the quercetin-pinoresinol diglu...

Embodiment 3

[0098] 1. The formulation and preparation of the quercetin and pinoresinol diglucoside PVP dispersion preparation stage:

[0099] formula:

[0100] Quercetin 20mg

[0101] Pinoresinol Diglucoside 15mg

[0102] PVP-k30 50mg

[0103] Preparation Process:

[0104] Take 20 mg of quercetin and 15 mg of pinoresinol diglucoside in a mixer and mix them evenly, add 50 mg of PVP-k30 to the reaction flask, add an appropriate amount of 95% ethanol, stir in a water bath at 50°C for 3 hours until the solution is clear, vacuum The solvent was removed by evaporation, freeze-dried, pulverized into powder, and sieved with 80 meshes to obtain a PVP dispersion of quercetin-pinoresinol diglucoside, which was stored in a desiccator for later use.

[0105] 2. Preparation of quercetin-pininol diglucoside gel matrix sustained-release granules:

[0106] Formula (calculated at 200mg / grain):

[0107]

[0108] Preparation Process:

[0109] The above-mentioned 85 mg of the quercetin-pinoresinol d...

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PUM

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Abstract

The invention relates to novel medical anti-hypertension compound slow release tablets. The tablets are mainly prepared from four bioactive components of 5 mg-20 mg of quercetin, 5 mg-20 mg of pinoresinol diglucoside (effective ingredient of the bark of eucommia), 0.4 mg-1.60 mg of sulfonamide diuretic indapamide and 2 mg-10 mg of angiotensin reductase II inhibitor (ACEI) perindopril salt and pharmaceutical adjuvants of 20 mg-60 mg of PVP-k30, 10 mg-30 mg of hydroxyl propyl cellulose (HPMC-K15M), 30 mg-60 mg of lactose, 53 mg-80 mg of microcrystalline cellulose (MCC), 1 mg-2 mg of magnesium stearate (lubricating agent), 2 mg-4 mg of low hydroxypropyl cellulose (LHPC, disintegrating agent), 1 mg-20 mg of starch and 1 mg-10 mg of talcum powder. The novel anti-hypertension compound slow release tablets provide a safe and effective medicine help for adjusting and stabilizing blood pressure of patients, improving heart functions, relieving heart and cerebral vessel lesions and avoiding occurrence of other cardiovascular disease risks.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a novel antihypertensive compound sustained-release tablet and a production process. 0.4~1.60mg of sulfonamide diuretic indapamide, 2mg~10mg of angiotensin reductase II inhibitor (ACEI) perindopril salt, four biologically active substances, and 20mg~60mg of pharmaceutical excipients PVP-k30 , 10mg~30mg hydroxypropyl cellulose (HPMC-K15M), 30mg~60mg lactose, 53mg~80mg microcrystalline cellulose (MCC), 1mg~2mg magnesium stearate (lubricant), 2mg~4mg low hydroxypropyl Cellulose (LHPC, disintegrant), 1mg~20mg starch, 1mg~10mg talc powder. The new antihypertensive compound sustained-release tablet provided by this formula provides safe and effective drug help for patients to regulate and stabilize blood pressure, improve heart function, improve cardiovascular and cerebrovascular diseases, and avoid the risk of other cardiovascular diseases. Background technique [0002] Hypertension ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/05A61K9/24A61P9/12A61K31/352A61K31/404A61K31/7048
CPCA61K9/0002A61K9/2059A61K9/2086A61K31/352A61K31/404A61K31/7048A61K38/05A61K2300/00
Inventor 姜丽华甄国艳吴进玉刘春香孙伯兰李鑫华
Owner SHANGHAI PHARMA DONGYING JIANGSU PHARMA CO LTD
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