Novel long-acting antipyretic analgesic ibuprofen composition and preparation method thereof

An antipyretic and analgesic composition technology, which is applied in the field of pharmaceutical chemical synthesis, can solve the problems of reducing the antipyretic and analgesic time of ibuprofen, the large fluctuation of ibuprofen blood drug concentration, and the single type of ibuprofen. Avoid the peaks and valleys of the drug effect, improve the effect of the drug effect, and reduce the effect of blood concentration fluctuations

Pending Publication Date: 2019-10-08
NINGXIA MEDICAL UNIV
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But at present, there is a single type of ibuprofen in the ibuprofen suspension, which is released too quickly in the human body, which reduces the antipyretic and analgesic time of ibuprofen in the human body, and at the same time, due to its longer half-life, it reaches 1.8-2 hours , taken 2-3 times a day, resulting in large fluctuations in the blood concentration of ibuprofen in the human body, causing patients to often experience hemolysis after taking the drug, causing patients to experience gastric burning, stomach pain, nausea, vomiting and other adverse reactions, which aggravated Bleeding tendency, especially in patients with hemophilia or other bleeding disorders, ibuprofen should be used with caution

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
  • Novel long-acting antipyretic analgesic ibuprofen composition and preparation method thereof
  • Novel long-acting antipyretic analgesic ibuprofen composition and preparation method thereof
  • Novel long-acting antipyretic analgesic ibuprofen composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0021] A preparation method of a novel long-acting antipyretic and analgesic ibuprofen composition, characterized in that it comprises the following steps:

[0022] Step a), the synthesis of ibuprofen imidazolate, ibuprofen is dissolved in dichloromethane, N, N'-carbonyldiimidazole (CDI) is dissolved in dichloromethane, and then the dichloromethane of ibuprofen The methane solution is added dropwise into the dichloromethane solution of CDI through the dropping funnel, stirred evenly until the reaction is completed, and dried after acid-base extraction and n-hexane precipitation to obtain imidazolate ibuprofen;

[0023] The synthetic route of ibuprofen imidazolate is:

[0024]

[0025] Step b), the synthesis of ibuprofen-beta-cyclodextrin second side derivatives, the ibuprofen imidazolate prepared in step a) is dissolved in N, N-dimethylformamide (DMF), forming The DMF solution of ibuprofen imidazolate, add β-cyclodextrin in the DMF solution of ibuprofen imidazolate, stir e...

Embodiment 1

[0044] The preparation of ibuprofen imidazolate: ibuprofen 0.01mol (2.06g) is dissolved in 30ml dichloromethane; CDI0.015mol (2.43g) is dissolved in 60ml dichloromethane; The dichloromethane solution of ibuprofen is passed through The dropping funnel was added dropwise into the dichloromethane solution of CDI, reacted for 12-24 hours, extracted with acid and alkali, precipitated with n-hexane and dried to obtain imidazolate ibuprofen (yield 80%).

[0045] The ibuprofen imidazolate that this embodiment makes, nuclear magnetic data is as follows:

[0046] 1 H NMR (400MHz, DMSO-d 6 ):8.49,7.71,7.32,7.30,7.13,7.11,7.01, 4.76,4.74,2.51,2.39,2.37,1.82-1.72,1.49,1.47,0.82,0.80; 13 C NMR (400MHz, DMSO-d 6 ): 171.8, 140.88, 137.63, 130.75, 130.07, 127.53, 117.24, 44.61, 44.36, 40.60-39.44, 29.99, 22.59, 19.59.

[0047] Preparation of ibuprofen-β-cyclodextrin second derivatives: Ibuprofen imidazolate 0.015mol (3.84g) was dissolved in 600mL N,N-dimethylformamide (DMF), and β was adde...

Embodiment 2

[0053] The preparation of ibuprofen imidazolate: ibuprofen 0.01mol (2.06g) is dissolved in 30ml dichloromethane; CDI0.015mol (2.43g) is dissolved in 60ml dichloromethane; The dichloromethane solution of ibuprofen is passed through The dropping funnel was added dropwise into the dichloromethane solution of CDI, reacted for 5-10 hours, extracted with acid and alkali, precipitated with n-hexane and dried to obtain imidazolate ibuprofen (yield 68%).

[0054] Preparation of ibuprofen-β-cyclodextrin second derivatives: Ibuprofen imidazolate 0.015mol (3.84g) was dissolved in 600mL N,N-dimethylformamide (DMF), and β was added under stirring at room temperature - CD 0.0225mol (25.5g), while adding triethylamine (65ml). Continue to stir the reaction at room temperature for 12-24h, and evaporate the solvent under reduced pressure. The residue was chromatographed with excess acetone and filtered to obtain a crude product. The crude product was purified on a C18 reverse-phase column and ...

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 relates to a novel long-acting antipyretic analgesic ibuprofen composition. The novel long-acting antipyretic analgesic ibuprofen composition is composed of an ibuprofen-beta-cyclodextrin secondary derivative and ibuprofen. The invention further discloses a preparation method of the novel long-acting antipyretic analgesic ibuprofen composition. The preparation method of the novel long-acting antipyretic analgesic ibuprofen composition comprises the steps that first ibuprofen and N,N'-carbonyl diimidazole (CDI) are used as raw materials to prepare an intermediate product ibuprofenimidazolate, the ibuprofen imidazolate reacts with beta-cyclodextrin to obtain the ibuprofen-beta-cyclodextrin derivative, and then the ibuprofen-beta-cyclodextrin derivative and additional weighed ibuprofen are separately added into water for even stirring; and an ibuprofen suspension and an ibuprofen-beta-cyclodextrin derivative suspension are evenly stirred to form a mixed suspension of the ibuprofen-beta-cyclodextrin derivative and the ibuprofen, the mixed suspension is subjected to freezing of a refrigerator and drying of a freeze dryer to obtain the ibuprofen composition. The ibuprofencomposition has a high inclusion rate, and solves the problems of short curative effect duration, excessively-large release rate, and large fluctuation of blood concentration of ibuprofen.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical chemical synthesis, in particular to a novel long-acting antipyretic and analgesic ibuprofen composition and a preparation method thereof. Background technique [0002] Ibuprofen (Ibuprofen (INN), chemical name: 2-methyl-4-(2-methylpropyl) phenylacetic acid, also known as ibuprofen), commonly used names: profen, ibuprofen, etc., It is a non-steroidal antipyretic drug (NSAID), which is often used to relieve arthritis, menstrual pain, fever and other symptoms. It is also an analgesic, especially for pain caused by inflammation. Ibuprofen has a platelet inhibitory effect, but the duration is shorter than that of aspirin. Ibuprofen (Ibuprofen) is one of the most successful antipyretic and analgesic antipyretic drugs developed in recent years. my country has listed ibuprofen as a pillar product for realizing the structural renewal of antipyretic and analgesic drugs. In addition to the antipyr...

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
Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K31/192A61P29/00
CPCA61K47/6951A61K31/192A61P29/00
Inventor 王玉营黄青褚慧敏魏世杰王志忠
Owner NINGXIA MEDICAL UNIV
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