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

Darunavir composition with improved dissolution speed

A technology for darunavir and dissolution rate, applied in the field of compositions with improved dissolution rate, can solve problems such as no darunavir involved, and achieve the effects of fast dissolution rate and good stability

Active Publication Date: 2020-10-27
SHENZHEN NYCRIST TECH CO LTD
View PDF13 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is worth noting that none of the above-mentioned literature patents involves darunavir that forms a salt with an acidic polymer

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
  • Darunavir composition with improved dissolution speed
  • Darunavir composition with improved dissolution speed
  • Darunavir composition with improved dissolution speed

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0060] Embodiment 2: the mensuration of darunavir content:

[0061] Agilent 1260 liquid chromatograph, Agilent C18 (15×0.46mm) chromatographic column, acetonitrile:water ratio of 1:1 as mobile phase, injection volume 20μL, flow rate 1mL / min, UV detection wavelength 267nm.

[0062] Take an appropriate amount of darunavir ethanol solvate, accurately weighed, add mobile phase to dissolve and quantitatively dilute to make a solution containing about 10 μg per 1 mL, as a reference solution, accurately measure 20 μL, inject it into a liquid chromatograph, and record the chromatogram picture.

[0063] In addition, get darunavir obtained in Example 1: an appropriate amount of acidic polymer salt composition, and measure with the same method, and calculate with the peak area by the external standard method, darunavir: darunavir in the acidic polymer salt composition The weight percentage of Wei is about 40%.

Embodiment 3

[0064] Embodiment 3: infrared spectrum measurement

[0065] A Fourier transform infrared spectrometer (Shimadzu) was used with a matched attenuated internal reflectance accessory fitted with a diamond crystal.

[0066] The spectral acquisition range is 4000-650cm-1, 32 scans, and the spectral resolution is 4.0cm-1. Before recording the spectrum of each sample, the measurement was performed with air as a blank.

[0067] In this disclosure, the term "mixture" or "physical mixture" refers to a simple physical mixture of darunavir and HPMCP obtained by combining the dry components and then physically stirring them together.

[0068] As is known in the art, co-powdering does not substantially alter the physical form of the drug, eg its crystalline or amorphous character, co-powdering is not intended to produce an amorphous drug / polymer dispersion.

[0069] Darunavir obtained in Example 1: the acidic polymer salt composition is carried out infrared spectrum test, and with 40% daru...

Embodiment 4

[0083] Example 4: X-Ray Powder Diffraction (XRPD)

[0084] X-ray powder diffraction was carried out using the Holland PANalytical X’Pert sharp shadow X-ray powder diffractometer (PW3040 / 60), using Cu-Kα radiation, wavelength The divergence slit is 1 / 8°, the X-ray light tube voltage is 45kV, the X-ray light tube current is 40mA, the scanning range is 2-40° (2θ), the step size is 0.0260°, and the scanning time of each step is 78.7950s.

[0085] Spread the sample on the sample tray for testing, data collection software X’Pert Data Collector, data viewing software HighScore Plus.

[0086] Darunavir of the present invention: physical state and physical stability of acidic polymer salt are measured, choose darunavir: HPMCP salt. image 3 For darunavir: the X-ray powder diffraction pattern of the HPMCP salt separated and measured immediately after spray-drying preparation shows diffuse peaks in the figure and does not show sharp diffraction peaks, which confirms that the product is 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 relates to a composition with an improved dissolution rate. The composition comprises a salt formed by darunavir and an acidic polymer. The darunavir: acidic polymer salt composition hasa faster dissolution rate and better stability. The composition can be applied to the treatment of viral infection diseases, such as acquired immunodeficiency syndrome (HIV), viral hepatitis and coronavirus infection.

Description

technical field [0001] The invention relates to the technical field of pharmacy, more specifically, to a composition with improved dissolution rate. Background technique [0002] Darunavir, the chemical name is [(1R,5S,6R)-2,8-dioxobicyclo[3.3.0-decane-6-yl-N-[(2S,3R)-4-[(4 -aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-hydroxyl-1-phenyl-butane-2-yl]carbamate, which has the following structural formula: [0003] [0004] Darunavir is an HIV protease inhibitor developed by a subsidiary of Johnson & Johnson in the United States. After marketing, it is often used in combination with ritonavir and other antiretroviral drugs for the late treatment of adult HIV-infected patients. The usual dose is 600mg orally (combined with ritonavir 100mg), twice a day; for newly treated patients, 800mg orally (combined with remdesivir 100mg), twice a day. Later studies showed that darunavir had in vitro inhibitory activity against novel coronavirus (COVID-19). [0005] Patents US7700645B2...

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): A61K31/635A61K9/08A61K9/10A61K9/02A61K9/72A61K47/38A61P31/14A61P31/20A61P31/18A61P31/12
CPCA61K9/0019A61K9/0053A61K9/007A61K9/02A61K9/08A61K9/10A61K31/635A61K47/38A61P31/12A61P31/14A61P31/18A61P31/20A61K2300/00
Inventor 田芳高明陈明安妮
Owner SHENZHEN NYCRIST TECH 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