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

Urapidil composition granule for treating pregnancy-induced hypertension

A technology for gestational hypertension and urapidil, applied in the field of medicine, can solve the problems of patients with toxicity, affect drug quality, poor stability, etc., and achieve the effects of improved fluidity, high bioavailability and good stability

Inactive Publication Date: 2015-11-18
QINGDAO HUAZHICAO PHARMA CO LTD
View PDF6 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 China's national drug standard WS-(X-116)-2003Z, especially the clarity of which is >No. 2 standard turbidity liquid, and the quality cannot meet the purity requirements of injection drugs. Therefore, 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
  • Urapidil composition granule for treating pregnancy-induced hypertension
  • Urapidil composition granule for treating pregnancy-induced hypertension
  • Urapidil composition granule for treating pregnancy-induced hypertension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: Preparation of Urapidil Crystal

[0029] Dissolve urapidil in a mixed solvent of methanol and dimethyl sulfoxide whose volume is 6 times the weight of urapidil at 35°C. The volume ratio of methanol to dimethyl sulfoxide is 5:1.5; first at a speed of 40ml / min Add a mixed solvent of butanol and ether with a volume of 9 times the weight of urapidil. The volume ratio of butanol to ether is 2:3. Stir while adding, control the temperature at 35°C, and cultivate the crystal for 3 hours; then add 20ml Add petroleum ether with a total volume of 7 times the weight of urapidil at a speed of 1 hour, and then cool down to -5°C at a rate of 10°C / hour, and then keep the stirring speed at 90 revolutions / minute to crystallize. , Cultivate crystals for 3 hours; filter, wash, and dry under reduced pressure to obtain urapidil crystal compound.

[0030] The prepared urapidil crystal uses Cu-Kα rays to measure the X-ray powder diffraction pattern as shown in figure 1 Shown.

Embodiment 2

[0031] Example 2: Preparation of Urapidil Granules

[0032] Prescription: 2.5 parts by weight of the urapidil crystal compound prepared in Example 1, 22.0 parts by weight of sucrose, 0.3 parts by weight of hypromellose, 0.15 parts by weight of poloxamer, 3.0 parts by weight of anhydrous Ethanol.

[0033] Preparation:

[0034] (1) Raw and auxiliary materials processing: pulverize urapidil to 100 mesh;

[0035] (2) Weighing: Weigh according to the craft prescription;

[0036] (3) Preparation of binder: Dissolve the prescription amount of hypromellose and poloxamer in absolute ethanol, and set aside;

[0037] (4) Mixing granulation: Add urapidil and sucrose to the wet mixing granulator, turn on the mixing motor for dry mixing for 10 minutes; add the prepared binder for wet mixing and cutting, and use a 16-mesh sieve to make soft materials;

[0038] (5) Drying and sieving: evenly spread the wet granules obtained from granulation on the baking pan of the oven, set the temperature to 65-70℃, ...

Embodiment 3

[0041] Example 3: Preparation of Urapidil Granules

[0042] Prescription: 2.5 parts by weight of the urapidil crystal compound prepared in Example 1, 22.2 parts by weight of sucrose, 0.4 parts by weight of hypromellose, 0.2 parts by weight of poloxamer, 3.4 parts by weight of anhydrous Ethanol.

[0043] Preparation:

[0044] (1) Raw and auxiliary materials processing: pulverize urapidil to 100 mesh;

[0045] (2) Weighing: Weigh according to the craft prescription;

[0046] (3) Preparation of binder: Dissolve the prescription amount of hypromellose and poloxamer in absolute ethanol, and set aside;

[0047] (4) Mixing granulation: Add urapidil and sucrose to the wet mixing granulator, turn on the mixing motor for dry mixing for 10 minutes; add the prepared binder for wet mixing and cutting, and use a 16-mesh sieve to make soft materials;

[0048] (5) Drying and sieving: evenly spread the wet granules obtained from granulation on the baking pan of the oven, set the temperature to 65-70℃, a...

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 discloses a urapidil composition granule for treating pregnancy-induced hypertension, belonging to the technical field of medicines. The composition is prepared from urapidil, sucrose, hydroxypropyl methylcellulose, poloxamer and absolute ethyl alcohol. Urapidil is a compound in a new crystal form and is different from urapidil reported in the prior art. An X-ray powder diffraction pattern obtained through measurement by using a Cu-Kalpha ray is shown in a drawing 1 in the specification. Through tests, compared with the prior art, the compound in the new crystal form has good stability and lower impurity I content. The total impurity content is also controlled in a lower range and is slightly changed with increase of the storage time. The solubility and flowability of the urapidil crystalline compound provided by the invention in water are obviously improved compared with the solubility and flowability of the prior art. The granule prepared by utilizing the compound in the new crystal form has good stability and high bioavailability and is very suitable for clinical application.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a urapidil composition granule for treating pregnancy-induced hypertension syndrome. 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 h...

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): A61K9/16A61K31/513C07D239/545A61P9/12
Inventor 杨冬梅
Owner QINGDAO HUAZHICAO PHARMA CO LTD
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