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Preparation and preparation method of erythromycin and related drugs

A technology of erythromycin and preparations, which is applied in the field of preparation of pharmaceutical preparations, and can solve the problems of low bioavailability and instability of enteric-coated erythromycin preparations, and reduced curative effect of oral preparations of erythromycin

Inactive Publication Date: 2015-12-16
胡昌勤 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Restricted by this kind of thinking, although the prepared enteric-coated erythromycin preparation can avoid the degradation in the gastric acid environment and reduce the irritation to the gastric mucosa, it is difficult to ensure the effective absorption of erythromycin in the body, especially in the small intestine. The effective absorption of the upper part eventually leads to the peak time of erythromycin in vivo (T max ) more than double the delay, and cause the highest blood concentration (C max ) is low, resulting in low bioavailability of enteric-coated erythromycin preparations or large fluctuations due to individual differences, and ultimately leads to reduced and unstable efficacy of erythromycin oral preparations

Method used

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  • Preparation and preparation method of erythromycin and related drugs
  • Preparation and preparation method of erythromycin and related drugs
  • Preparation and preparation method of erythromycin and related drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] Embodiment 1: the preparation of erythromycin micropill pill

[0083] The prescription is shown in the table below

[0084] components Take the amount components Take the amount Erythromycin 125g Sodium carboxymethyl starch 1.25g~7.5g blank core 15～30g 3% hypromellose, 1% PEG6000 Appropriate amount Sodium dodecyl sulfate 0.3g~5g Vitamin C 0.5g~5g microcrystalline cellulose 15～30g

[0085] Isolation layer: 3% hypromellose, talcum powder, appropriate amount.

[0086] Operating process:

[0087] (1) Preparation of wetting agent: Take 100ml of water, heat to 80°C, add 3g of hydroxypropylmethylcellulose, stir to disperse evenly while adding, then add 1g of polyethylene glycol 6000, stir to fully dissolve, cool to Fully swell at room temperature and set aside;

[0088] (2) The original and adjuvant materials of prescription quantity are mixed uniformly by the method of equal quantity addition, and it is stand...

Embodiment 2

[0092] Embodiment 2: Preparation of erythromycin granules

[0093] The prescription is shown in the table below

[0094] components Take the amount components Take the amount Erythromycin 125g Sodium carboxymethyl starch 1.25g~7.5g 3% hypromellose, 1% ~ 2% Tween-80 Appropriate amount Vitamin C 0.5g~5g microcrystalline cellulose 15～30g

[0095] Isolation layer liquid: 9% white gastric soluble coating premix, appropriate amount.

[0096] Operating process:

[0097] (1) Preparation of wetting agent: Take 100ml of water, heat to 80°C, add 3g of hydroxypropylmethylcellulose, stir while adding to make the dispersion even, then add the prescribed amount of Tween-80, stir to fully dissolve, cool Fully swell at room temperature and set aside;

[0098] (2) The original and auxiliary materials of the prescription amount are mixed uniformly by the method of equal addition, and set aside;

[0099] (3) Add a wetting agent into the m...

Embodiment 3

[0104] Embodiment 3: the preparation of erythromycin microchip tablet core

[0105] The prescription is shown in the table below

[0106] components Take the amount components Take the amount Erythromycin 125g Crospovidone 1.25g~6.25g Vitamin C 0.5g~5g polyethylene glycol 1g~6g microcrystalline cellulose 20g 3% povidone, 1% ~ 2% Tween-80 Appropriate amount

[0107] Isolation layer: 9% white gastric soluble coating premix, appropriate amount.

[0108] Operating process:

[0109](1) Preparation of wetting agent: take 100ml of water, heat to 80°C, add 3g of povidone, stir while adding to disperse evenly, then add the prescribed amount of Tween-80, stir to fully dissolve, cool to room temperature and use Fully swollen, ready for use;

[0110] (2) The original and auxiliary materials of the prescription amount are mixed uniformly by the method of equal addition, and set aside;

[0111] (3) Add a wetting agent into the mixed pow...

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Abstract

The invention relates to a preparation method of new preparation of erythrocin, which is characterized in that an endothelin core of erythrocin is prepared, and then an isolating layer, a protective layer, a second isolating layer and an improved enteric-coating material layer are applied one by one. In this way, new preparation of the erythrocin which has certain feature of releasing (dissolving) in acid solution (hydrochloric acid solution 9 to 1000) can be formed. The technology of the new preparation can also be widely applied to drugs which, like erythrocin, when being taken orally by a patient, cause the patient to suffer the side effects of stimulation, sickness and the like after degradation in the stomach of the patient or contact with the stomach of the patient, and drugs which the patient needs to take orally to let the blood concentration to reach the peak value in a short time. Such drugs include macrolides of azithromycin, metronidazole of nitroimidazoles, tinidazole, acyclovir as an antiviral drug, ammonium chloride as a phlegm eliminating drug, bromhexine, chloroquine as an antimalarial, nitroquine, artemisinin, dihydroartemisinin, artesunate, primaquine, pyrimethamine, carbarsone and emetine amebicides and so on.

Description

technical field [0001] The present invention relates to erythromycin (English name: Erythromycin, molecular formula: C 37 h 67 NO 13 ) of a new pharmaceutical preparation and a preparation method of the pharmaceutical preparation. The purpose is to avoid the degradation of erythromycin in gastric acid, reduce the side effect of erythromycin on the gastrointestinal tract, improve the compliance of oral preparations of erythromycin, and reduce the degree of loss of bioavailability of oral preparations of erythromycin. [0002] The technical field that the present invention relates to also contains the side effects such as being similar to erythromycin in the stomach after oral administration and causing irritation, vomiting, etc. Concentrations of such drugs, such as macrolide azithromycin and other drugs, nitroimidazole metronidazole, tinidazole, antiviral drug acyclovir, expectorant drug ammonium chloride , bromhexine, anti-malarial drugs chloroquine, nitroquine, artemisin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/16A61K9/20A61K9/32A61K9/36A61K31/7048A61K47/32A61K47/34A61K47/38A61P31/04
CPCY02A50/30
Inventor 胡昌勤和琳琳刘英李思思高艺歌
Owner 胡昌勤
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