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Clarithromycin enteric-coated preparation and preparation method thereof

A clarithromycin enteric and clarithromycin technology, applied in the field of pharmaceutical preparations, can solve the problems of decreased bioavailability, impact on curative effect, poor patient compliance, etc., and achieve the effect of ensuring bioavailability and good enteric coating effect

Active Publication Date: 2017-02-08
HAINAN PULIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, clarithromycin has a strong bitter taste, and patients' compliance is poor
The Chinese patent application with the publication number CN1759844A discloses a clarithromycin enteric-coated preparation, which is released and absorbed in the intestinal tract, although it solves the problem that clarithromycin is easily degraded in the gastric environment and the adverse reactions in the stomach
However, there are still some problems in the enteric-coated preparation of clarithromycin. Clarithromycin is a poorly soluble substance, and the dissolution effect after entering the intestinal tract is not good, resulting in a decrease in bioavailability and affecting the curative effect.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] To prepare clarithromycin enteric-coated dry suspension, the following materials are used:

[0018] Clarithromycin 200g Acrylic Eudragit L100 200g

[0019] Starch 500g Sucrose 500g Mannitol 720g

[0020] Lemon essence 20g Aspartame 20g Xanthan gum 20g Silica 20g

[0021] Preparation Process:

[0022] (1) First mix 200g of clarithromycin raw material with 100g of acrylic resin Eudragit L100, add it to the hot-melt extrusion equipment, heat to melt the enteric material, and form a uniform suspension system with clarithromycin raw material, then cool and extrude, then Use a granulator to granulate to get 80~45 mesh granules;

[0023] (2) Prepare the remaining enteric-coated material acrylic resin Eudragit L100 into a coating solution; add the above granules into the fluidized bed equipment for coating, and sieve the 80-45 mesh coated granules;

[0024] (3) Mix the coated granules obtained in step (2) with the prescribed amount of titanium dioxide, xanthan gum, lemon es...

Embodiment 2

[0026] Embodiment 2: To prepare 1000 clarithromycin enteric-coated tablets, the following materials were used:

[0027] Clarithromycin 250g Acrylic S100 250g

[0028] Microcrystalline Cellulose 370g Magnesium Stearate 20g

[0029] Silica 10g Crospovidone 100g

[0030] Preparation Process:

[0031] (1) First mix 250g of clarithromycin raw material with 120g of acrylic resin Eudragit S100, add it to the hot-melt extrusion equipment, heat to melt the enteric material, and form a uniform suspension system with clarithromycin raw material, then cool and extrude, then Use a granulator to granulate to get 80~45 mesh granules;

[0032] (2) Prepare the remaining enteric-coated material acrylic resin Eudragit S100 into a coating solution; add the above particles into the fluidized bed equipment for coating, and sieve the 80-45 mesh coated particles;

[0033] (3) Mix the obtained coated granules with other excipients and press into tablets to obtain clarithromycin enteric-coated tabl...

Embodiment 3

[0034] Embodiment 3: Prepare 1000 granulomycin enteric-coated capsules, using the following materials:

[0035] Clarithromycin 250g Acrylic Eudragit S100 250g

[0036] Silica 10g

[0037] Preparation Process:

[0038] (1) First mix 250g of clarithromycin raw material with 120g of acrylic resin Eudragit S100, add it to the hot-melt extrusion equipment, heat to melt the enteric material, and form a uniform suspension system with clarithromycin raw material, then cool and extrude, then Use a granulator to granulate to get 80~45 mesh granules;

[0039] (2) Prepare the remaining enteric-coated material acrylic resin Eudragit S100 into a coating solution; add the above particles into the fluidized bed equipment for coating, and sieve the 80-45 mesh coated particles;

[0040] (3) Mix the clarithromycin-coated granules with silicon dioxide evenly, and cover them with capsule shells to obtain granulamycin enteric-coated capsules.

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Abstract

The invention relates to a clarithromycin enteric-coated preparation and a preparation method thereof. The clarithromycin enteric-coated preparation is obtained through using clarithromycin enteric coating particles, the particle sizes of the clarithromycin enteric coating particles are 80-45 meshes, and the clarithromycin enteric-coated preparation comprises 30-60% of clarithromycin and 40-70% of an enteric material. The preparation method of the clarithromycin enteric-coated preparation comprises a step of mixing a clarithromycin raw material with parts of the enteric material, a step of carrying out hot melting granulation to form a solid dispersion, and a step of coating the outside of the obtained granulated particles by the enteric coating. The obtained clarithromycin enteric-coated preparation has the advantages of very good enteric effect, no dissolve-out of clarithromycin in the stomach, effective guarantee of no degradation of clarithromycin in the stomach, high dispersiveness of clarithromycin in the intestinal tract, generation of the curative effect through rapid dissolve-out in the intestinal tract, and guarantee of the bioavailability of medicines.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a clarithromycin enteric-coated preparation and a preparation method thereof. Background technique [0002] Clarithromycin is a semi-synthetic macrolide antibiotic produced by methylation of the 6-hydroxyl group of erythromycin A. After methylation, clarithromycin effectively improves its pharmacokinetic properties due to its increased lipid solubility, rapid oral absorption, good cell penetration, and wide tissue distribution. The antibacterial mechanism of clarithromycin is to act on the ribosome 50S subunit in the bacterial 70S system, hindering the synthesis of bacterial proteins, and is a long-term antibacterial agent. It has inhibitory effect on Gram-positive bacteria such as Staphylococcus aureus, Streptococcus, pneumococcus, etc., and has inhibitory effect on some Gram-negative bacteria such as Haemophilus influenzae, Bordetella pertussis, Neisseria gonorrhoeae...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K9/20A61K9/48A61K31/7048A61K47/32A61K47/36A61K47/38A61P31/04
Inventor 范敏华姜双瑜刘华
Owner HAINAN PULIN PHARMA
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