Unlock instant, AI-driven research and patent intelligence for your innovation.

Compound double-layer tablet containing ritonavir pellets for treating novel coronavirus

A double-layer tablet, coronavirus technology, applied in the directions of antiviral agents, medical preparations containing active ingredients, pill delivery, etc., can solve the problems of high production cost, long process time, cumbersome production process, etc., and achieve production cost. Low, good drug compliance, simple production process effect

Pending Publication Date: 2022-06-28
乐普制药科技有限公司
View PDF6 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0020] Combination packaged medicines need to be taken according to the known instructions, and the production process is cumbersome, the process takes a long time, and the production cost is high

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
  • Compound double-layer tablet containing ritonavir pellets for treating novel coronavirus
  • Compound double-layer tablet containing ritonavir pellets for treating novel coronavirus
  • Compound double-layer tablet containing ritonavir pellets for treating novel coronavirus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Ritonavir layer:

[0051]

[0052] Its preparation method is:

[0053](1) After mixing the ritonavir of the recipe with the copovidone of the recipe, Span 20, and colloidal silicon dioxide, add it to the hot-melt extruder. The hot-melt extrusion temperature is 100-120°C for hot-melt extrusion to prepare a solid dispersion;

[0054] (2) After the solid dispersion is pulverized by a high-efficiency pulverizer, the particle size range is controlled to be 0.5 to 1 mm;

[0055] (3) After pulverization, the granules are coated, and a coating solution with a concentration of 15% is prepared. The granules are put into a fluidized bed granulation pot, preheated, and when the temperature of the material reaches 40 °C, spray slurry to control the temperature of the material to be about 40 °C. , the flow rate of the coating liquid is 50g / min, and the surface of the particles is coated with a gastrosoluble coating film. Finally, pellets containing ritonavir were obtained.

[...

Embodiment 2

[0068] Ritonavir layer:

[0069]

[0070] Its preparation method is

[0071] (1) add the hot melt extruder after mixing the ritonavir of the recipe quantity and the polyvinylpyrrolidone of the recipe quantity, sodium lauryl sulfate, talc. The hot-melt extrusion temperature is 100-120°C for hot-melt extrusion to prepare a solid dispersion;

[0072] (2) After the solid dispersion is pulverized by a high-efficiency pulverizer, the particle size range is controlled to be 0.5 to 1 mm;

[0073] (3) After pulverization, the granules are coated, and a coating solution with a concentration of 15% is prepared. The granules are put into a fluidized bed granulation pot, preheated, and when the temperature of the material reaches 40 °C, spray slurry to control the temperature of the material to be about 40 °C. , the flow rate of the coating liquid is 50g / min, and the surface of the particles is coated with a gastrosoluble coating film. Finally, pellets containing ritonavir were obtai...

Embodiment 3

[0085] Ritonavir layer:

[0086]

[0087] Its preparation method is:

[0088] (1) after the ritonavir of recipe quantity and the copovidone of recipe quantity, sodium lauryl sulfate, colloidal silicon dioxide are mixed and dissolved in methylene chloride, fluidized bed granulator is turned on hot air 80 ℃ , spray drying to prepare granules;

[0089] (2) The spray-dried granules are screened by a lifting dry granulator, and the screen aperture is 0.6 mm;

[0090] (3) Coat the granulated granules, prepare a coating solution with a concentration of 15%, put the granules into the fluidized bed granulation pot, preheat, when the temperature of the material reaches 40 °C, spray slurry, and control the temperature of the material to be about 40 °C , the flow rate of the coating liquid is 50g / min, and the surface of the particles is coated with a gastrosoluble coating film. Finally, pellets containing ritonavir were obtained.

[0091] (4) Mix the pellets with lactose and steari...

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

PropertyMeasurementUnit
Particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention discloses a double-layer compound tablet containing ritonavir pellets for treating new coronavirus 2019-nCoV (SARS-CoV-2), the tablet is the double-layer compound tablet containing the pellets, the active ingredients are ritonavir and Nirmatrevir, and the double-layer compound tablet provided by the invention can shorten the production cycle of the medicine and save the dosage of auxiliary materials. Nirmatrevir is an SARS-CoV-2 main protease (Mpro) inhibitor, and ritonavir is an HIV-1 (human immunodeficiency virus-1) protease inhibitor and a CYP3A (cytochrome Phosphate 3A) inhibitor. Clinical tests prove that the combination can be used for treating mild and moderate new coronavirus infection, and the death rate is clinically reduced by 89%. Compared with a new crown treatment medicine PAXLOVID (which is packaged by a combination of a Nirmatrevir tablet and a ritonavir tablet) of Ruy, the medicine disclosed by the invention is an innovative compound preparation, and the convenience in carrying and taking the medicine is improved. The pharmaceutical composition is more suitable for clinical medication selection, improves medication compliance of patients, is more suitable for commercialized production, saves production cost and shortens production cycle.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a compound bilayer tablet containing ritonavir pellets for treating novel coronavirus and a preparation method thereof. Background technique [0002] PAXLOVID is an oral antiviral drug developed by Pfizer, which can reduce the ability of the new coronavirus to reproduce in the body. The drug consists of the small molecule drug PF-07321332 (Nirmatrelvir) and ritonavir. PF-07321332 is an inhibitor against the main protease of the new coronavirus, and ritonavir is an antiviral drug synergist, which was used to fight AIDS. Virus. [0003] Nirmatrelvir structural formula: [0004] [0005] Chemical Name: [0006] (1R,2S,5S)-N-((1S)-1-Cyano-2-((3S)-2-oxopyrrolidin-3-yl)ethyl)-3-((2S)-3,3-dimethyl- 2-(2,2,2-trifluoroacetamido)butanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide] [0007] Molecular formula: C 23 H 32 F 3 N 5 O 4 [...

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): A61K9/24A61K9/28A61K31/427A61K31/4025A61P31/14
CPCA61K9/209A61K9/2081A61K9/2806A61K31/427A61K31/4025A61P31/14A61K2300/00
Inventor 潘裕生吴肖蒙俞悦陈盈王海翔
Owner 乐普制药科技有限公司