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Enteric-coated azithromycin preparation and its preparing process

A technology for enteric azithromycin and azithromycin, which is applied in the field of enteric-coated azithromycin preparations and the preparation thereof, can solve the problems of poor water solubility, destruction of azithromycin, influence on the clinical efficacy of azithromycin, etc., and achieves the effects of improving bioavailability and accelerating absorption

Active Publication Date: 2005-01-26
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because azithromycin is unstable in gastric juice, there is almost no prototype in artificial gastric juice (pH=1.3) for 10 minutes; according to literature reports, after oral administration of azithromycin, the amount of azithromycin degraded into declardinose is about 15% of the administered dose , and after intravenous injection of the same dose of azithromycin, the amount of declardinose azithromycin is less than 0.5% of the dose, which further proves the destructive effect of gastric acid on azithromycin, resulting in low bioavailability of common oral preparations of azithromycin. between 37 and 46%, which affects the clinical efficacy of azithromycin
However, enteric-coated preparations prepared by conventional methods, because azithromycin is alkaline and has poor water solubility, the dissolution and release in the intestinal tract become the restrictive factors for drug absorption.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1: Enteric-coated tablets using Azithromycin salt as raw material

[0053] (1) Core materials

[0054] Azithromycin hydrochloride 250g (based on azithromycin) 50%

[0055] Sodium lauryl sulfate 10g 2%

[0056] Lactose 100g 20%

[0057] Hydroxypropyl cellulose 70g 14%

[0058] Crospovidone 20g 4%

[0059] 95% ethanol

[0060] Magnesium stearate 6g 1.2%

[0061] 1000 pieces

[0062] (2) Coating liquid

[0063] Ethyl cellulose 30g 6%

[0064] Polyethylene glycol 6000 14g 2.8%

[0065] 95% ethanol 1000ml

[0066] Weigh the azithromycin hydrochloride, filler, and part of the disintegrant that have passed through the 80 mesh sieve according to the prescription, add an appropriate amount of 10% povidone, granulate, and mix the remaining part of the disintegrant with the dry particles after drying. , After the semi-finished product has passed the inspection, add lubricant, mix well and press the tablet.

[0067] The prepared plain tablets are weighed and placed in a coating...

Embodiment 2

[0068] Example 2: Enteric-coated tablets of azithromycin and acid salt

[0069] Component weight weight percentage

[0070] (1) Core materials

[0071] Azithromycin 125g 31.25%

[0072] Citrate 15g 3.75%

[0073] Sodium lauryl sulfate 6g 1.5%

[0074] Microcrystalline cellulose 100g 25%

[0075] Hydroxypropyl cellulose 70g 17.5%

[0076] Sodium starch glycolate 30g 7.5%

[0077] Magnesium stearate 4g 1%

[0078] Crospovidone 10g 2.5%

[0079] 95% ethanol

[0080] 1000 pieces

[0081] (2) Coating liquid:

[0082] Polyacrylic resin No. II 30g 7.5%

[0083] Polyethylene glycol 1000 5g 1.25%

[0084] Polyethylene glycol 6000 5g 1.25%

[0085] 95% ethanol 1000ml

[0086] After pulverizing citric acid, add 20 times the amount of 95% ethanol solution until the acid is completely dissolved, then slowly add azithromycin, adding while grinding, until the azithromycin is completely dissolved and transparent and has no particles. Dry under reduced pressure at 40°C to obtain solid salt, which ...

Embodiment 3

[0088] Example 3: Azithromycin enteric-coated capsules

[0089] Component weight weight percentage

[0090] (1) Core materials:

[0091] Azithromycin 250g 38.46%

[0092] Tartaric acid 26g 4%

[0093] Tween 80 13g 2%

[0094] Microcrystalline cellulose 195g 30%

[0095] Hydroxypropyl cellulose 62g 9.54%

[0096] Crospovidone 26g 4%

[0097] 95% ethanol

[0098] Made into 1000 tablets

[0099] (2) Coating liquid:

[0100] Polyacrylic resin No. II 65g 10%

[0101] Polyethylene glycol 1000 6.5g 1%

[0102] Polyethylene glycol 6000 6.5g 1%

[0103] 95% ethanol 1500ml

[0104] The granules prepared according to the preparation method are weighed and placed in a coating pan or a boiling fluidized bed, while spraying the coating liquid and blowing hot air to obtain enteric-coated granules.

[0105] Fill enteric-coated particles into capsules to obtain azithromycin enteric-coated capsules.

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PUM

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Abstract

The invention discloses an enteric-coated azithromycin preparation and its preparing process, which comprises effective dosage of azithromycin or medicinal excipient, wheein the medicinal excipient include surface active agent, bulking agent, crumbling agent, lubricating agent, moistening agent or binding agent, intestine solution dressing material and plasticizer.

Description

Technical field [0001] The invention relates to an azithromycin enteric preparation and a preparation method thereof. technical background [0002] Azithromycin is a new-generation derivative of erythromycin and the only 15-membered macrocyclic antibiotic in this class of drugs. It has the characteristics of broad antibacterial spectrum, strong action and long half-life. It is widely used clinically to treat various sensitive bacteria. Infection of the respiratory tract, skin, soft tissue and genitourinary system is effective, with few adverse reactions. Because azithromycin is unstable in gastric juice, there is almost no prototype in artificial gastric juice (pH=1.3) for 10 minutes. According to literature reports, after oral administration of azithromycin, the amount of azithromycin degraded into declading sugar is about 15% of the administered dose However, after intravenous injection of the same dose of azithromycin, the amount of declatinose azithr...

Claims

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Application Information

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IPC IPC(8): A61K31/7052A61P31/04
Inventor 杨亚青张育孙鹏郭卫芹黄印陈霞张彬
Owner CSPC OUYI PHARM CO LTD
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