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A kind of antihypertensive pharmaceutical composition

A composition and drug technology, applied in the direction of drug combination, active ingredients of hydroxyl compounds, pharmaceutical formulations, etc., can solve the problems of large differences in release speed, unfavorable drug compliance, and increased frequency of drug use, so as to ensure the antihypertensive effect, Effect of promoting microcirculation and delaying release rate

Active Publication Date: 2021-02-09
HUBEI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, the preparation level of the drug is still relatively backward, resulting in a very short half-life of the drug and low bioavailability, thereby shortening the duration of the effect. Therefore, it is necessary to increase the dosage and increase the frequency of medication, which is not conducive to improving medication compliance.
In addition, the synchronous release and absorption of the active ingredients is one of the necessary conditions to obtain the overall coordination of the system, and because this product is a Chinese and Western compound preparation, the release speed of each ingredient in the body varies greatly, resulting in poor coordination of the ingredients , the curative effect needs to be further improved

Method used

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  • A kind of antihypertensive pharmaceutical composition
  • A kind of antihypertensive pharmaceutical composition
  • A kind of antihypertensive pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029]

[0030] Preparation:

[0031] 1) Preparation of daidzein and honokiol liposomes: Weigh soybean phosphatidylcholine, cholesterol, polyethylene glycol-distearoylphosphatidylethanolamine, daidzein and honokiol, and vortex to make It is dissolved in a mixed solvent of chloroform and methanol (1:4, V / V), and then the liposome suspension is prepared according to the thin film ultrasonic dispersion method: firstly, the mixed solution is evaporated under reduced pressure at 40°C to remove the organic solvent to the inner wall of the container Form a layer of liposome film, then add ultrapure water to make the solid content 0.15%, stir the hydrated liposome film at 60°C, then ultrasonically break and homogenize the liposome in an ice bath, and finally filter through 0.22 μm The membrane is sized to prepare the daidzein and honokiol long-circulating liposome suspension.

[0032] The entrapment efficiency of daidzein and honokiol encapsulation liposomes was measured by dialys...

Embodiment 2

[0053] A kind of antihypertensive pharmaceutical composition, it is made up of the composition of following weight ratio:

[0054]

[0055] The preparation method comprises the following steps:

[0056] 1) Dissolve daidzein, honokiol, soybean phosphatidylcholine, cholesterol, polyethylene glycol-distearoylphosphatidylethanolamine in a mixed solvent of chloroform and methanol (1:4, V / V), Then make a liposome suspension with a solid content of 0.3% according to the thin-film ultrasonic dispersion method: first remove the organic solvent by rotary evaporation under reduced pressure at 40 ° C of the mixed solution to form a liposome film on the inner wall of the container, then add ultrapure water to make The solid content is 0.3%, stirring the hydrated liposome film at 60°C, then ultrasonically crushing and homogenizing the liposome in an ice bath, and finally passing through a 0.22 μm filter membrane for granulation, so as to obtain daidzein, and thick Parkinol long-circulat...

Embodiment 3

[0063] A kind of antihypertensive pharmaceutical composition, it is made up of the composition of following weight ratio:

[0064]

[0065]

[0066] The encapsulation efficiency of daidzein was measured to be 57.8%, and the encapsulation efficiency of honokiol was 95.6%.

[0067] The components of the tablet are basically completely released within 8 hours, and the similar factors of synchronous release are shown in Table 3.

[0068] Each component of table 3 embodiment 3 liposome tablet releases similar factor synchronously

[0069] substance f 2 Hydrochlorothiazide / Daidzein 53.78±2.01 Hydrochlorothiazide / rhynchophylline 66.83±10.24 Hydrochlorothiazide / Honokiol 67.35±1.20 Daidzein / Hynchophylline 53.39±2.32 Daidzein / Honokiol 61.88±1.92 Rhynchophylline / Honokiol 71.78±4.56

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Abstract

The present invention discloses a hypotensive pharmaceutical composition. The composition is prepared by dissolving daidzein, honokiol, soybean phosphatidylcholine, cholesterol, DSPE-PEG in an organicsolvent, then preparing a liposome suspension by a membrane-sonic method, then adding hydrochlorothiazide, rhynchophylline and a diluent into the liposome suspension, performing freeze-dying, uniformly mixing the dried material with a disintegrant and a lubricant, and finally performing tabletting. The invention uses the daidzein and the honokiol to prepare the encapsulated liposome so as to delay the release rate of the drug, and the liposome can be released simultaneously with the hydrochlorothiazide and the rhynchophylline, thereby improving the coordination of the action of drug components in the body and increasing the curative effect.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to an antihypertensive pharmaceutical composition. Background technique [0002] CN101297884A discloses a concentrated antihypertensive Maijunan tablet or capsule, the active ingredients of which are hydrochlorothiazide, total flavonoids of kudzu root and total alkaloids of Uncaria. The antihypertensive effect of this drug is found to be poor in clinical application, and long-term use is prone to produce antihypertensive resistance, so that the antihypertensive effect gradually declines. For this reason, the applicant applied for an improved antihypertensive pharmaceutical composition on November 16, 2017. The publication number is CN107951940A. Phenols can reduce systolic and diastolic blood pressure more significantly, and can also inhibit the body from developing drug resistance, making the antihypertensive effect more durable. [0003] However, the preparation level of the drug is still r...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61K31/05A61K31/549A61K31/437A61K9/127A61P9/12
CPCA61K9/127A61K31/05A61K31/352A61K31/437A61K31/549A61K47/28A61P9/12A61K2300/00
Inventor 陈勇刘红唐兰如王俏
Owner HUBEI UNIV
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