Sustained release microsphere carrying rifapentine and linezolid as well as preparation method and applications of sustained release microsphere

A technology of linezolid and rifapentine, applied in the field of pharmaceutical preparations, can solve the problems of poor patient compliance, short duration of effective drug concentration, and poor sustained release effect, and achieve good compliance, fewer adverse reactions, and antibacterial effects. strong effect

Inactive Publication Date: 2017-04-26
THE 309TH HOSPITAL OF CHINESE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In order to solve the above problems, the object of the present invention is to provide a sustained-release microsphere loaded with rifapentine and linezolid, which can solve the problem of

Method used

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  • Sustained release microsphere carrying rifapentine and linezolid as well as preparation method and applications of sustained release microsphere
  • Sustained release microsphere carrying rifapentine and linezolid as well as preparation method and applications of sustained release microsphere
  • Sustained release microsphere carrying rifapentine and linezolid as well as preparation method and applications of sustained release microsphere

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Add 600 mg of polylactic acid-glycolic acid, 250 mg of rifapentine and 250 mg of linezolid into a volumetric flask filled with 10 mL of dichloromethane, vortex for 2 minutes to fully dissolve the drugs, and make a drug solution. Add 2g of polyvinyl alcohol into a beaker containing 100mL of water and heat it to dissolve to prepare a 2% wt polyvinyl alcohol solution and place it in a constant temperature water bath at 30°C, and set the stirring speed of the rotor of the water bath to 800, 1000 , 1400 rpm. Then use a syringe with a specification of 2 mL to drop the medicinal solution into the polyvinyl alcohol aqueous solution drop by drop, and continue stirring for 3 hours to completely volatilize the dichloromethane in the polyvinyl alcohol aqueous solution. Use a disposable straw to suck off the foam and impurities on the surface of polyvinyl alcohol, centrifuge the remaining solution at a low speed of 1000 rpm for 5 minutes, collect the slow-release microspheres prepar...

Embodiment 2

[0048] 600mg polylactic acid-glycolic acid, (group 1: 250mg rifapentine and 250mg linezolid; group 2: 150mg rifapentine and 350mg linezolid; group 3: 200mg rifapentine and 300mg Linezolid) was added into a volumetric flask containing 10 mL of dichloromethane, and vortexed for 2 minutes to fully dissolve the drug to prepare a drug solution. Add 2g of polyvinyl alcohol into a beaker filled with 100mL of water and heat it to dissolve to prepare a 2%wt polyvinyl alcohol solution and place it in a constant temperature water bath at 30°C, and set the stirring speed of the rotors of the water bath to 1000 rpm / point. Then use a syringe with a specification of 2 mL to drop the medicinal solution into the polyvinyl alcohol aqueous solution drop by drop, and continue stirring for 3 hours to completely volatilize the dichloromethane in the polyvinyl alcohol aqueous solution. Use a disposable straw to suck off the foam and impurities on the surface of polyvinyl alcohol, centrifuge the re...

Embodiment 3

[0059] Embodiment 3 draws release curve in vitro

[0060] Put 10 mg of microspheres prepared under optimal conditions into a sealed dialysis bag (molecular weight cut off 8000 or more) and place the dialysis bag in 50 mL full of release medium-phosphate buffer (PBS, pH=7.4, 0.1 mg / mL vitamin C) in a test tube with a screw cap. Put the test tube into a dissolution tester that shakes back and forth at a frequency of 100 rpm, and maintain the water temperature at 37±0.5°C. At 30min, 2h, 6h, 1d, 2mL samples were taken at 1d intervals, and the same volume of fresh release medium was added at the same time. The release medium was filtered with a microporous membrane and the drug content was measured by HPLC. The experiment was repeated three times. Finally, the in vitro cumulative release rate and release rate curves of rifapentine and linezolid were drawn respectively. The vitamin C in it can prevent rifapentine from being oxidized and decomposed and maintain the stability of rif...

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Abstract

The invention provides a sustained release microsphere carrying rifapentine and linezolid as well as a preparation method and applications of the sustained release microsphere. The sustained release microsphere contains rifapentine, linezolid and a medicinal carrier, wherein the medicinal carrier wraps rifapentine and linezolid, and the medicinal carrier is poly lactic-co-glycolic acid. The invention further provides the preparation method of the sustained release microsphere. The sustained release microsphere can treat pulmonary tuberculosis, especially, cavity tuberculosis through bronchoscope local administration; the problems that the existing medicines are poor in sustained release effect, the keeping time of the effective medicine concentration is short, and the compliance of patients is poor, are solved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a sustained-release microsphere and a preparation method thereof, in particular to a sustained-release microsphere loaded with rifapentine and linezolid and a preparation method thereof. Background technique [0002] According to the World Health Organization's 2015 Global Tuberculosis Report, 9.6 million people worldwide suffer from tuberculosis, and 40%-87% of tuberculosis patients suffer from cavitary tuberculosis, and these patients are also the main source of tuberculosis infection. Compared with other tuberculosis patients, patients with cavitary tuberculosis have stronger drug resistance to anti-tuberculosis drugs, and are the main population of tuberculosis treatment failure and retreatment. For cavitary pulmonary tuberculosis, anti-tuberculosis drugs can be delivered to the lesion site through bronchoscopy in clinic to solve the problems of poor treatment effect ...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K47/34A61K31/496A61K31/5377A61P31/06A61P11/00
CPCA61K9/5031A61K31/496A61K31/5377A61K2300/00
Inventor 张广宇黄洁云陈志黎立敖国昆
Owner THE 309TH HOSPITAL OF CHINESE PEOPLES LIBERATION ARMY
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