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Azithromycin enteric casing microsphere and its preparing process

An azithromycin enteric and azithromycin technology, which is applied in the field of azithromycin enteric-coated microspheres and the preparation thereof, can solve the problems of low bioavailability, low bioavailability and fast degradation speed of common oral preparations, and achieves the improvement of bioavailability and avoidance of cross-fertilization. Combined reaction, the effect of simple process steps

Inactive Publication Date: 2008-04-23
NANJING TECH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Recent studies also show that azithromycin is degraded by 68% in 0.1mol / L hydrochloric acid solution for 30 minutes, which shows that azithromycin is unstable in gastric juice, and the degradation speed is fast. Most of the drug has been destroyed in the stomach, which obviously affects the clinical efficacy.
According to other reports in the literature, after oral administration of azithromycin, the amount of azithromycin degraded into declardinose is about 15% of the administered dose, while after intravenous injection of the same dose of azithromycin, the amount of declaridine azithromycin is less than 0.5% of the administered dose. %, which further proves the destructive effect of gastric acid on azithromycin, resulting in low bioavailability of common oral preparations of azithromycin, which is only between 37% and 46% in literature reports, thus affecting the clinical efficacy of azithromycin
[0004] Although some enteric-coated preparations about azithromycin have been reported in the prior art, it is found that the enteric-coated preparations currently used and disclosed in the prior art usually have low bioavailability in vivo, slow onset of action, and large dosage of preparation auxiliary materials. , high dosage and other issues

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Precisely weigh 6.0 grams of polymeric enteric-coated material—methacrylic acid-methyl methacrylate copolymer (Udragit L100) and dissolve it in 300 ml of 95% ethanol to obtain a 2% enteric-coated material solution, which is set aside. Precisely weigh 1.2g of azithromycin and dissolve it in polymeric enteric-coated material, add 4.5ml of plasticizer castor oil and stir well, then add 3.0g of micropowder silica gel, under stirring conditions, according to the inlet air temperature 82 ℃, the outlet air temperature : 61°C, feed rate: 20ml / min, air flow 600nl / h, spray-dry it, and remove the organic solvent to obtain azithromycin enteric-coated microspheres.

[0026] The release rate after 2h in 0.1mol / L hydrochloric acid solution was 3.015±2.379% (n=3); the release rate after 2h in artificial intestinal juice (pH 6.8) was 92.141±2.379% (n=3).

Embodiment 2

[0028] Precisely weigh 4.5 grams of polymer enteric-coated material - methacrylic acid-methyl methacrylate copolymer (a mixture of Eudragit L100 and Eudragit S100 in equal proportions) and dissolve it in 300ml of 95% ethanol to obtain 1.5% enteric acid Dissolving material solution, set aside. Precisely weigh 3.0g of azithromycin and dissolve it in polymeric enteric-coated material, add 1.5ml of plasticizer castor oil and stir well. Then add 0.5g of micropowdered silica gel. : 61°C, feed rate: 20ml / min, air flow 600nl / h, spray-dry it, and remove the organic solvent to obtain azithromycin enteric-coated microspheres.

[0029] The release rate after 2h in 0.1mol / L hydrochloric acid solution was 6.015±2.451% (n=3); the release rate after 2h in artificial intestinal juice (pH 6.8) was 94.285±2.258% (n=3).

Embodiment 3

[0031] Precisely weigh 2.5 grams of the high-molecular enteric-coated material—hydroxypropyl methylcellulose phthalate and dissolve it in 65 ml of 80% ethanol to obtain a 1.5% enteric-coated material solution, which is set aside. Precisely weigh 1.2g of azithromycin and dissolve it in polymer enteric-coated material, add 3.0ml of plasticizer castor oil and stir well, then add 2.2g of micropowdered silica gel, under stirring conditions, according to the inlet air temperature 82 ℃, the outlet air temperature : 61°C, feed rate: 20ml / min, air flow 600nl / h, spray-dry it, and remove the organic solvent to obtain azithromycin enteric-coated microspheres.

[0032] The release rate after 2h in 0.1mol / L hydrochloric acid solution was 8.623±1.584% (n=3); the release rate after 2h in artificial intestinal juice (pH 6.8) was 93.854±2.584% (n=3).

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Abstract

The invention relates to enteric-coated Azithromycin microballoons and the preparing process, wherein the preparation comprises (by weight percent) Azithromycin 8-32%, macromolecular enteric-coating material 28-60%, antisticking agent 15-34% and plasticizer 5-25%.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to azithromycin enteric-coated microspheres and a preparation method thereof. Background technique [0002] Azithronycin is a broad-spectrum macrolide antibiotic obtained by modifying the structure of erythromycin. It mainly achieves antibacterial effect by inhibiting the synthesis of ribosomal 50s subunit protein in bacterial cells. At present, it has been widely used in gastrointestinal tract, genitourinary system, respiratory tract and other infections, with obvious curative effect and less drug resistance. Azithromycin is rapidly absorbed after oral administration, and can be rapidly distributed in multiple organs and tissues throughout the body, making the tissue concentration 10 to 100 times higher than the blood concentration, and it can last for several days. At the same time, azithromycin can also be rapidly taken up by phagocytes and carried to the infection sit...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7052A61K9/16A61P31/04A61P11/00A61P13/00A61P15/00
Inventor 李学明徐元龙
Owner NANJING TECH UNIV
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