Azithromycin sustained-release microsphere and dry suspension, preparation method and application thereof

A technology of azithromycin and slow-release microspheres, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, respiratory diseases, etc., and can solve the problems of unsuitable simple, environmentally friendly and non-toxic extrusion-spheronization methods, etc., to achieve Good sustained release effect, reduced dosage, high yield effect

Active Publication Date: 2011-05-18
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The technical problem to be solved by the present invention is to overcome that the azithromycin composition in the prior art needs to be prepared by the spray-freezing method or in the presence of a large amount of organic solvents, and it is not suitable for the simple, environmenta

Method used

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  • Azithromycin sustained-release microsphere and dry suspension, preparation method and application thereof
  • Azithromycin sustained-release microsphere and dry suspension, preparation method and application thereof
  • Azithromycin sustained-release microsphere and dry suspension, preparation method and application thereof

Examples

Experimental program
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Embodiment 1

[0047] 1. The formulation of azithromycin sustained-release microspheres:

[0048] Azithromycin 52%, stearyl alcohol 16%, microcrystalline cellulose 8%, ethyl cellulose 9%, and ethyl cellulose aqueous dispersion 15% (content of solid matter).

[0049] 2. Preparation process of azithromycin sustained-release microspheres:

[0050] Adopt the known method of pharmaceutical industry, mix azithromycin with stearyl alcohol, microcrystalline cellulose and ethyl cellulose according to the above formula, add binder ethyl cellulose aqueous dispersion (Surelease ) to prepare a soft material, extrude it with a sieve plate with an aperture of 0.2mm, and carry out spheronization with a rotating speed of 900rpm. The obtained microspheres were dried in an oven at 40°C for 2 hours to remove moisture, and then heat-treated at 70°C for 2 hours. After cooling to room temperature, the particles were sized to collect microspheres with particle diameters between 60 and 100 mesh, and the yield was...

Embodiment 2

[0052] 1. The formulation of azithromycin sustained-release microspheres:

[0053] Azithromycin 35%, glyceryl monostearate 25%, microcrystalline cellulose 7%, ethyl cellulose 22.9%, and ethyl cellulose aqueous dispersion 0.1% (content of solid matter).

[0054] 2. Preparation process of azithromycin sustained-release microspheres:

[0055] Using methods known in the pharmaceutical industry, azithromycin is mixed with glyceryl monostearate, microcrystalline cellulose and ethyl cellulose according to the above formula, and the binder ethyl cellulose aqueous dispersion (Aquacoat ) to prepare a soft material, extrude it with a sieve plate with a pore size of 0.2 mm, and carry out spheronization with a rotating speed of 1200 rpm. The obtained microspheres were dried in an oven at 40°C for 1 hour to remove moisture, and then heat-treated at 70°C for 2 hours. After cooling to room temperature, the particles were sized to collect microspheres with a particle size between 60 and 100...

Embodiment 3

[0057] 1. The formulation of azithromycin sustained-release microspheres:

[0058] Azithromycin 70%, Glyceryl Behenate 18%, Ethylcellulose 5%, and Ethylcellulose aqueous dispersion 7% (solid matter content).

[0059] 2. Preparation process of azithromycin sustained-release microspheres:

[0060] Adopt the known method of pharmaceutical industry, mix azithromycin and glyceryl behenate according to the above-mentioned formula, add binder ethyl cellulose aqueous dispersion (Yishida ) to prepare a soft material, extrude it with a sieve plate with an aperture of 0.25mm, and carry out spheronization with a rotating speed of 500rpm. The obtained microspheres were heat-treated at 75°C for 3 hours. After cooling to room temperature, the particles were sized to collect microspheres with a particle size between 60 and 100 mesh. The yield is 91%.

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Abstract

The invention discloses an azithromycin sustained-release microsphere which comprises 30-70% of azithromycin, 5-25% of wax ester sustained-release framework material, 5-45% of other water-insoluble framework material except the wax ester sustained-release framework material and 0.1-25% of binder based on the total weight of the azithromycin sustained-release microsphere, wherein the binder is aqueous dispersion coating fluid, and the weight percentage of the binder is the weight percentage of solid substances except the solvent in the binder. The invention also discloses a preparation method and application of the azithromycin sustained-release microsphere, a suspension containing the azithromycin sustained-release microsphere and application of the suspension. According to the invention,the defect that the spraying-congelation or a large amount of organic solvent or coating is required in the prior art is solved, and the invention is particularly suitable for the preparation with anenvironmentally friendly and nontoxic extrusion-rounding method with simple steps.

Description

technical field [0001] The present invention relates to the field of pharmaceutical preparations, in particular to azithromycin sustained-release microspheres and a preparation method thereof. The present invention also relates to a dry suspension containing the azithromycin sustained-release microspheres, as well as azithromycin sustained-release microspheres and its containing Use of dry suspensions. Background technique [0002] Azithromycin is a 15-membered ring macrolide antibiotic derived from erythromycin. It works by inhibiting the synthesis of bacterial ribosomal 50S subunit protein. It is mainly used clinically to treat various community-acquired infections. , including respiratory tract infections (such as community-acquired pneumonia, acute exacerbation of chronic bronchitis, acute pharyngitis and tonsillitis, acute otitis media), urogenital infections (such as Neisseria gonorrhoeae and non-gonococcus urethritis, cervicitis, Chancroid), sinusitis, otitis media a...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/00A61K31/7052A61P31/04A61P11/00A61P11/02A61P13/00A61P27/16A61P17/02
Inventor 陶涛柴旭煜顾小燕赵雁吴大鹏
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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