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Gel microsphere capable of being injected with rifamycinoid antibiotics and preparation method thereof

A technology of rifamycin and gel microspheres, which is applied in the directions of antibacterial drugs, pharmaceutical formulations, medical preparations with inactive ingredients, etc. It can achieve the effect of good slow-release and controlled-release effect, low cost, and uniform drug dispersion.

Inactive Publication Date: 2013-01-02
中国人民解放军第三0九医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The object of the present invention is to solve the problem of poor dispersion of rifamycin antibiotics (rifampicin, rifapentine and rifabutin) in calcium alginate gel microspheres, the sustained release time is shorter, the gel microspheres To solve the technical problems of low drug loading and drug encapsulation efficiency, an injectable rifamycin sustained-release gel microsphere containing rifamycin antibiotic-polyethylene succinate solid dispersion is provided and its rapid preparation method

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] 1. Preparation of Injectable Rifapentine Gel Microspheres

[0032] (1) Dissolve 4.5 g of rifapentine in 20 mL of dimethyl sulfoxide solvent to obtain rifapentine dimethyl sulfoxide solution (solution A).

[0033] (2) Weigh 2.2g of polyethylene succinate and dissolve in solution A to obtain solution B.

[0034] (3) Weigh 1.8 g of sodium alginate and dissolve it in 100 mL of distilled water to obtain a 1.8% sodium alginate solution (solution C).

[0035] (4) Add solution B dropwise to 400 mL of distilled water, and stir continuously at 700 r / min to form a precipitate of rifapentine solid dispersion. After centrifugal precipitation, the supernatant was discarded, and 100 mL of distilled water was added to wash the solid dispersion precipitate once.

[0036] (5) The rifapentine solid dispersion obtained in the previous step was precipitated and dried, weighed, and suspended in 100 mL of solution C to obtain rifapentine sodium alginate glue.

[0037] (6) Take 7.5g of anhy...

Embodiment 2

[0044] 1. Preparation of Injectable Rifabutin Gel Microspheres

[0045] (1) Dissolve 3.2 g of rifabutin in 20 mL of dimethyl sulfoxide solvent to obtain rifabutin dimethyl sulfoxide solution (solution A).

[0046] (2) Weigh 2.0 g polyethylene succinate and dissolve in solution A to obtain solution B.

[0047] (3) Weigh 1.8 g of sodium alginate and dissolve it in 100 mL of distilled water to obtain a 1.8% sodium alginate solution (solution C).

[0048] (4) Add solution B dropwise to 400 mL of distilled water, and stir continuously at 700 r / min to form a solid dispersion of rifabutin. After centrifugal precipitation, the supernatant was discarded, and 100 mL of distilled water was added to wash the solid dispersion precipitate once.

[0049] (5) Suspend the rifabutin solid dispersion precipitate obtained in the previous step in 100 mL of solution C to obtain rifabutin sodium alginate glue.

[0050] (6) Take 7.5g of anhydrous calcium chloride and dissolve in 500mL distilled wa...

Embodiment 3

[0057] 1. Preparation of Injectable Rifapentine Gel Microspheres

[0058] (1) Dissolve 2.5 g of rifapentine in 20 mL of dimethyl sulfoxide solvent to obtain rifapentine dimethyl sulfoxide solution (solution A).

[0059] (2) Weigh 2g of polyethylene succinate and dissolve in solution A to obtain solution B.

[0060] (3) Weigh 1.8 g of sodium alginate and dissolve it in 100 mL of distilled water to obtain a 1.8% sodium alginate solution (solution C).

[0061] (4) Add solution B dropwise to 400 mL of distilled water, and stir continuously at 700 r / min to form a solid dispersion of rifapentine. After centrifugal precipitation, the supernatant was discarded, and 100 mL of distilled water was added to wash the solid dispersion precipitate once.

[0062] (5) Suspend the rifapentine solid dispersion precipitate obtained in the previous step in 100 mL of solution C to obtain rifapentine sodium alginate glue.

[0063] (6) Take 5g of anhydrous calcium chloride and dissolve it in 500mL...

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Abstract

The invention relates to a gel microsphere capable of being injected with rifamycinoid antibiotics comprising 4-6 wt% of rifamycinoid antibiotics, 1-3 wt% of polyethylene succinate, 3.2-4.0 wt% of calcium alginate and 87.0-91.8 wt% of water, and a preparation method for the gel microsphere, comprising the steps of: A. dissolving rifamycinoid antibiotics and polyethylene succinate in dimethyl sulfoxide; B. dispersing the dimethyl sulfoxide in water to form a rifamycinoid antibiotics-polyethylene succinate solid dispersoid; C. suspending the solid dispersoid in a sodium alginate aqueous solution to obtain a rifamycinoid antibiotics-polyethylene succinate-sodium alginate sol solution; and D. using an electrostatic droplet generation device for dropping the sol solution in a calcium chloride aqueous solution, curing the succinate-sodium alginate medicated sol solution to form the gel microsphere. The gel microsphere medicine has good dispersity, good slow release and controlled release effects, high medicine entrapment rate and high loading rate.

Description

technical field [0001] The invention relates to an anti-tuberculosis slow-release drug microsphere preparation and a preparation method thereof, in particular to an injectable rifamycin antibiotic gel microsphere and a preparation method thereof. Background technique [0002] Medical microspheres are a kind of medical biomaterial products that have gradually emerged with the development of biomaterial science, clinical medicine and pharmacology. The administration methods of drug-loaded microspheres include oral administration, subcutaneous implantation, intramuscular injection, intravenous injection, intraperitoneal injection, bronchial injection, etc. Injectable microspheres are extremely small in diameter to allow administration by syringe. Microspheres for injection have the advantages of sustained release, long-acting and targeted drug delivery, and can be administered every 2 weeks or even 3 months. For tuberculosis patients, it greatly improves the convenience of dru...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/395A61K31/438A61K31/496A61K47/36A61P31/06
Inventor 黎立张广宇杨楠史迎昌陈志
Owner 中国人民解放军第三0九医院