Medicine urapidil composition capsule for treating hypertensive crisis of old people

A technology of urapidil and its composition, which is applied in the field of urapidil composition capsules for the treatment of elderly hypertensive crisis, which can solve the problems of increasing the risk of medication for patients, the toxicity of patients, and poor stability, and is suitable for clinical application , high bioavailability, improved fluidity

Inactive Publication Date: 2015-12-09
杨献美
View PDF2 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because urapidil hydrochloride is easily soluble in water and slightly soluble in organic solvents (such as ethanol), urapidil hydrochloride is not easy to be refined by general purification processes such as recrystallization, and the quality of urapidil hydrochloride after refining It cannot meet the requirements of the Chinese National Drug Standard WS-(X-116)-2003Z, especially the clarity>No. 2 standard turbidity liquid, and the quality cannot meet the purity requirements of injection medicines (see Comparative Examples 1 and 2), so , the purification of urapidil is particularly important
[0006] Urapidil in the prior art has disadvantages such as poor stability, easy decomposition and deterioration, and difficult storage under special circumstances (such as high temperature and light), which are largely limits the wide application of the drug
Find that there is a certain amount of oxidative degradation product I in the urapidil in the prior art through a large number of experimental studies simultaneously, as impurity, it shows the risk that has toxicity to patient or is harmful in other respects, has had a strong impact on the quality of medicine, increases patient risk
The existing technology solves the problems of water solubility and stability by changing the excipients and preparation methods of the preparation. It must rely on specific prescriptions and processes to achieve its stable effect, which brings certain limitations to the preparation of preparations and the selection of excipients. sex

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Medicine urapidil composition capsule for treating hypertensive crisis of old people
  • Medicine urapidil composition capsule for treating hypertensive crisis of old people
  • Medicine urapidil composition capsule for treating hypertensive crisis of old people

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Preparation of urapidil crystals

[0030] Get urapidil crude drug, add in the mixed solvent A of acetone, N-methylacetamide that the volume of 40 ℃ is 8 times of urapidil weight, acetone, N-methylacetamide volume ratio is 4:1.5, obtains solution; then applying a constant magnetic field with a magnetic field intensity of 0.5T in the horizontal direction of the liquid surface of the resulting solution, and under the condition of this constant magnetic field, in the solution, the volume is added dropwise to isobutanol and ether that are 5 times the weight of urapidil The volume ratio of the mixed solvent B, isobutanol and diethyl ether is 4:3; after the dropwise addition, the temperature was lowered to -5°C, allowed to stand for 2 hours, filtered, washed, and vacuum-dried to obtain the urapidil crystals.

[0031] The X-ray powder diffraction pattern obtained by measuring the obtained urapidil crystal using Cu-Kα ray is as follows: figure 1 shown.

Embodiment 2

[0032] Example 2: Preparation of Urapidil Capsules

[0033] Prescription: in parts by weight

[0034]

[0035] Preparation:

[0036] (1) Processing of raw and auxiliary materials: crush urapidil to 100 meshes;

[0037] (2) Weighing: Weighing according to the process prescription;

[0038] (3) Preparation of adhesive: dissolve povidone K30 in 95% ethanol and set aside;

[0039] (4) Mixing and granulation: Add urapidil, microcrystalline cellulose, and nicotinamide to the wet mixing granulator, turn on the stirring motor and dry mix for 10 minutes; add the prepared binder to wet mix and cut, and use 24 Mesh sieve soft material;

[0040] (5) Drying: Add the wet granules obtained from granulation into a fluidized bed dryer, set the temperature at 65-70°C, and dry for 150-180 minutes. After drying, the material is granulated at 24 mesh;

[0041] (6) Mixing: Put the granulated particles and micropowder silica gel into the three-dimensional motion mixer, set the pre-mixing s...

Embodiment 3

[0044] Example 3: Preparation of Urapidil Capsules

[0045] Prescription: in parts by weight

[0046]

[0047] Preparation:

[0048] (1) Processing of raw and auxiliary materials: crush urapidil to 100 meshes;

[0049] (2) Weighing: Weighing according to the process prescription;

[0050] (3) Preparation of adhesive: dissolve povidone K30 in 95% ethanol and set aside;

[0051] (4) Mixing and granulation: Add urapidil, microcrystalline cellulose, and nicotinamide to the wet mixing granulator, turn on the stirring motor and dry mix for 10 minutes; add the prepared binder to wet mix and cut, and use 24 Mesh sieve soft material;

[0052] (5) Drying: Add the wet granules obtained from granulation into a fluidized bed dryer, set the temperature at 65-70°C, and dry for 150-180 minutes. After drying, the material is granulated at 24 mesh;

[0053] (6) Mixing: Put the granulated particles and micropowder silica gel into the three-dimensional motion mixer, set the pre-mixing s...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention related to a medicine urapidil composition capsule for treating hypertensive crisis of old people and belongs to the technical field of medicine. The composition is prepared from urapidil, microcrystalline cellulose, nicotinamide, povidone K30, 95% ethyl alcohol and superfine dilica powder. The urapidil is a novel crystal form compound, an X-ray powder diffraction pattern measured through a Cu-K alpha ray is shown in the graph 1, the urapidil is different from urapidil reported in the prior art, it is found through tests that compared with the prior art, the novel crystal form compound is better in stability and extremely low in content of impurities I, and the total impurity content is also controlled within a low range and has small change along with the prolonging of storage time. The solubility in water and fluidity of the urapidil crystal form compound are obviously improved compared with those in the prior art, the capsule prepared through the novel crystal form compound is high in dissolution rate, good in stability, high in bioavailability and very suitable for clinical application.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a capsule of urapidil composition for treating senile hypertensive crisis. Background technique [0002] Hypertension is a kind of common disease, frequently-occurring disease. With the improvement of people's living standards, the number of hypertensive patients is increasing day by day, especially the number of hypertensive crisis and severe hypertensive patients is constantly increasing, but there are few safe and effective injection drugs clinically used for this type of disease. High blood pressure affects work and life, and high blood pressure is the most important risk factor for coronary heart disease and cerebrovascular disease. 50% of myocardial infarction patients are hypertensive patients, and 76% of stroke patients have a history of hypertension. Therefore, the risk of high blood pressure is sudden death or disability. Hypertensive patients should learn how to take ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K9/48A61K31/513A61P9/12C07D239/545
Inventor 杨献美
Owner 杨献美
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap