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In-situ gel slow-release preparation for anti-tuberculosis drugs and preparation method thereof

A technology of in-situ gel and sustained-release preparations, applied in pharmaceutical formulations, antibacterial drugs, drug delivery, etc.

Inactive Publication Date: 2011-08-17
INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] There have been a lot of literature reports on the preparation of drug slow-release particles, but the slow-release particles are dispersed in a biocompatible gel medium, so that they have environmental responsive gelling properties as a whole, and there are no similar reports at home and abroad.

Method used

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  • In-situ gel slow-release preparation for anti-tuberculosis drugs and preparation method thereof
  • In-situ gel slow-release preparation for anti-tuberculosis drugs and preparation method thereof
  • In-situ gel slow-release preparation for anti-tuberculosis drugs and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0448] Microsphere preparation of rifampicin:

[0449] Rifampicin (RFP) 15mg

[0450] Polylactic-co-glycolic acid (PLGA) 30mg

[0451] Polyvinyl alcohol (PVA) 0.5g

[0452] Dichloromethane 2ml

[0453] Deionized water 24ml

[0454] Preparation method of rifampicin microspheres: Weigh 30mg of PLGA and dissolve in dichloromethane, add 15mg of rifampicin, ultrasonically dissolve, as the organic phase; dissolve 0.5g of PVA in 24ml of deionized water, as the water phase. Under the condition of stirring at 1000rpm, slowly inject the organic phase into the water phase, stir at high speed for a certain period of time, stir at 600rpm until the organic phase is completely volatilized, collect the microspheres by suction filtration, wash with distilled water 3 times, and dry under reduced pressure to obtain the product.

[0455] The in situ gel preparation method is:

[0456] Poloxamer 407 25g

[0457] Poloxamer 188 3g

[0458] Sodium Alginate 2g

[0459] Hydroxypropyl methylcell...

Embodiment 2

[0464] Microsphere preparation of rifampicin:

[0465] Rifampicin (RFP) 19mg

[0466] Polylactic-co-glycolic acid (PLGA) 115mg

[0467] Polyvinyl alcohol (PVA) 1.7g

[0468] Dichloromethane 1ml

[0469] Deionized water 10ml

[0470] Preparation method of rifampicin microspheres: Weigh 115mg PLGA and dissolve in dichloromethane, add 19mg rifampicin, ultrasonically dissolve, as the organic phase; dissolve 1.7g PVA in 10ml deionized water, as the water phase. Under the stirring condition of 1200rpm, slowly inject the organic phase into the water phase, stir at high speed for a certain period of time, stir at 400rpm until the organic phase is completely volatilized, collect the microspheres by suction filtration, wash with distilled water 3 times, and dry under reduced pressure to obtain the product.

[0471] The in situ gel preparation method is:

[0472] Poloxamer 407 23.9g

[0473] Poloxamer 188 2g

[0474] Hydroxypropyl Methyl Cellulose 1.5g

[0475] Deionized water 10...

Embodiment 3

[0479] Microsphere preparation of rifampicin:

[0480] Rifampicin (RFP) 28mg

[0481] Polylactic-co-glycolic acid (PLGA) 40mg

[0482] Polyvinyl alcohol (PVA) 1.4g

[0483] Dichloromethane 1ml

[0484] Deionized water 21ml

[0485] Preparation method of rifampicin microspheres: Weigh 40mg PLGA and dissolve in dichloromethane, add 28mg rifampicin, ultrasonically dissolve, as the organic phase; dissolve 1.4g PVA in 21ml deionized water, as the water phase. Under the stirring condition of 1200rpm, slowly inject the organic phase into the water phase, stir at high speed for a certain period of time, stir at 400rpm until the organic phase is completely volatilized, collect the microspheres by suction filtration, wash with distilled water 3 times, and dry under reduced pressure to obtain the product.

[0486] The in situ gel preparation method is:

[0487] Sodium Alginate 1.3g

[0488] Hydroxypropyl methylcellulose 0.8g

[0489] Deionized water 100ml

[0490] Take the sodium a...

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PUM

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Abstract

The invention discloses an in-situ gel slow-release preparation for local drug delivery, which comprises drug active ingredient microspheres and in-situ gel. The in-situ gel slow-release preparation is characterized in that the gel forming temperature is kept within the scope of 15-25 DEG C and the calcium ion effect exists; the drug active ingredient is anti-tuberculosis drugs; the proportional relationship of the drug active ingredient microsphere and the temperature-ion sensitive gel is 5-50 mg:1-50 ml; the drug active ingredient microspheres are uniformly dispersed in the in-situ gel under the agitation condition; the in-situ gel slow-release preparation can restrain the excessive release of the drugs and lead the drugs to release stably and detain at the lung of a rat for 120 h at most; and a drug system detains at the local part for a long time, thereby realizing the treatment purpose.

Description

technical field [0001] The invention provides a pharmaceutical preparation and a preparation method thereof, in particular to an in-situ gel sustained-release preparation of an anti-tuberculosis drug and a preparation method thereof. Background technique [0002] One of the key points and difficulties in tuberculosis treatment: retreatment, refractory and multidrug-resistant tuberculosis. The conventional route of drug administration is poor in chemotherapy effect, and the patient has not healed for many years, and the sputum bacteria are continuously positive or become lifelong bacteria excretion. [0003] The slow-release drug delivery system for pulmonary interventional therapy via bronchoscope of the present invention solves the problem that the slow-release system has not yet been established in local interventional therapy, targeted interventional therapy for refractory, retreatment and multidrug-resistant tuberculosis, and shortens the closure of the cavity Time, pro...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K45/00A61K47/38A61K47/34A61K31/496A61K31/4409A61P31/06
Inventor 朱春燕胡春晖
Owner INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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