Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Medicine urapidil composition tablet for treating hypertension

A technology of urapidil and composition, which is applied in the field of drug urapidil composition tablet for treating hypertension, can solve the problems of toxicity to patients, increase the risk of drug use for patients, poor stability, etc., and achieves high bioavailability, suitable for In clinical application, the effect of fluidity improvement

Inactive Publication Date: 2015-12-09
杨献美
View PDF2 Cites 0 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 tablet for treating hypertension
  • Medicine urapidil composition tablet for treating hypertension
  • Medicine urapidil composition tablet for treating hypertension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Preparation of urapidil crystals

[0030] Prepare urapidil crude product saturated acetone solution, then add the mixed solvent of isobutanol and sherwood oil whose volume is 8 times of the volume of saturated acetone solution, the volume ratio of described isobutanol and sherwood oil is 1:3, after stirring , stirring while cooling down, the cooling rate is 10°C / hour, the stirring speed is 105 rpm, and at the same time, add diethyl ether whose volume is 3 times the volume of the mixed solvent of isobutanol and petroleum ether, stop stirring after cooling down to 0°C, and let it stand After growing the crystal for 3 hours, filtering, and drying under reduced pressure, the crystal compound of urapidil was obtained.

[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 Tablets

[0033] Prescription: in parts by weight

[0034]

[0035] Preparation:

[0036] (1) Processing of raw and auxiliary materials: crush urapidil through a 100-mesh sieve, and sieve arginine through a 80-mesh sieve;

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

[0038] (3) Adhesive preparation: prepare starch slurry with the prescribed amount of starch and purified water by cooking slurry method, and cool to room temperature for use;

[0039] (4) Mixing and granulation: Add urapidil, lactose, calcium carbonate, polacrilin potassium, and arginine to the wet mixing granulator, turn on the stirring motor and dry mix for 10 minutes; add the prepared binder Wet mixing and cutting, using 18-mesh sieve to make soft materials;

[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 2-3 hours. After drying, the material i...

Embodiment 3

[0044] Example 3: Preparation of Urapidil Tablets

[0045] Prescription: in parts by weight

[0046]

[0047] Preparation:

[0048] (1) Processing of raw and auxiliary materials: crush urapidil through a 100-mesh sieve, and sieve arginine through a 80-mesh sieve;

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

[0050] (3) Adhesive preparation: prepare starch slurry with the prescribed amount of starch and purified water by cooking slurry method, and cool to room temperature for use;

[0051] (4) Mixing and granulation: Add urapidil, lactose, calcium carbonate, polacrilin potassium, and arginine to the wet mixing granulator, turn on the stirring motor and dry mix for 10 minutes; add the prepared binder Wet mixing and cutting, using 18-mesh sieve to make soft materials;

[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 2-3 hours. After drying, the material i...

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 belongs to the technical field of medicine and relates to a medicine urapidil composition tablet for treating hypertension. The composition is prepared from urapidil, lactose, calcium carbonate, polacrilin potassium, arginine, starch, purified water and magnesium stearate. 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, and the tablet 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 tablet of urapidil composition for treating hypertension. 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 care of life a...

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): A61K9/20A61K31/513A61K47/36C07D239/545A61P9/12
Inventor 杨献美
Owner 杨献美
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com