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A kind of enteric-coated dry suspension of rabeprazole and its dextrorotatory isomer and preparation method thereof

A technology of rabeprazole and dry suspension, which is applied in the field of medicine, can solve problems such as difficulty in swallowing ordinary enteric-coated tablets, irritation of the gastrointestinal tract of raw and auxiliary materials, and uneven release in the body, and achieve good bioavailability and Fast-acting, easy-to-split dosage effect

Inactive Publication Date: 2018-10-19
河南省健康伟业生物医药研究股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, ordinary enteric-coated tablets are difficult to swallow as a whole, are easily destroyed by patients and lose their active effect, are released unevenly in the body, and are prone to burst release, which may cause gastrointestinal irritation due to excessive local concentration of raw materials and excipients
Moreover, it is inconvenient to divide the dose during clinical use; it is not suitable for patients with dysphagia, especially infants and young children

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] In the present embodiment, the enteric-coated dry suspension of rabeprazole and its dextrorotatory isomer consists of the following components by weight:

[0031] Sustained-release microspheres A: Rabeprazole sodium 10g, glyceryl behenate 442g, poloxamer 148g,

[0032] Coating solution A: hypromellose 10g, water 190g,

[0033] Coating solution B: Eudragit L100-5530g EVONIC), sodium hydroxide 0.4g (in the process of preparing the above-mentioned enteric coating polymer material powder into an aqueous dispersion, a small amount of alkali or organic base needs to be added to neutralize the carboxyl groups in the polymer to obtain a pH value of about 5.2 Latex dispersion), talcum powder 15g, triethyl citrate 3g, water 52g;

[0034] Microspheres C945g,

[0035] Flavoring agent: 973g sucrose, 2g apple essence,

[0036] Suspending agent: hydroxypropyl cellulose 60g, xanthan gum 20g.

[0037] The preparation method of the enteric-coated dry suspension of rabeprazole and i...

Embodiment 2

[0044] In the present embodiment, the enteric-coated dry suspension of rabeprazole and its dextrorotatory isomer consists of the following components by weight:

[0045] Sustained-release microspheres A: dex-rabeprazole sodium 10g, mixed fatty acid glycerides 442g, poloxamer 148g,

[0046] Coating solution A: hypromellose 10g, water 190g,

[0047] Coating solution B: HPMCP HP-556g (Shin-Etsu), talc powder 1.5g, diethyl phthalate 0.6g, ethanol 28g, water 64g;

[0048] Microsphere C818g,

[0049] Flavoring agent: sorbitol 1100g, sodium saccharin 2g,

[0050] Suspending agent: sodium carboxymethylcellulose 60g, gum arabic 20g.

[0051] The preparation method of the enteric-coated dry suspension of rabeprazole and its dextrorotatory isomer in the present embodiment comprises the following steps:

[0052] (1) Accurately take each component according to the parts by weight, mix dextro-rabeprazole sodium, mixed fatty acid glycerides, and poloxamer evenly, melt the mixture at 90°C t...

Embodiment 3

[0058] In the embodiment, the enteric-coated dry suspension of rabeprazole and its dextrorotatory isomer consists of the following components by weight:

[0059] Sustained-release microspheres A: dex-rabeprazole sodium 10g, polyethylene glycol 6000590g,

[0060] Coating solution A: hypromellose 10g, water 190g,

[0061] Coating Solution B: Eudragit L1006g EVONIC), talc powder 1.2g, triethyl citrate 0.6g, ethanol 92g;

[0062] Microspheres C810g,

[0063] Flavoring agent: mannitol 1120g, stevia essence 10g,

[0064] Suspending agent: hypromellose 60g.

[0065] The preparation method of the enteric-coated dry suspension of rabeprazole and its dextrorotatory isomer in the present embodiment comprises the following steps:

[0066] (1) Accurately take each component according to the parts by weight, mix the preferred rabeprazole sodium and polyethylene glycol 6000 evenly, melt the mixture at 80°C through twin-screw extrusion, and then spray and condense to make a particle siz...

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Abstract

The invention discloses an enteric dry suspension of rabeprazole and dextroisomer thereof, and a preparation method thereof, and belongs to the technical field of medicines. The enteric dry suspension is composed of 30-59% by weight of rabeprazole enteric microspheres, 40-69% by weight of a corrective agent and 1-30% by weight of a suspending aid. Sustained-release microspheres A are prepared by a rabeprazole salt and a sustained-release skeleton material through a hot-melt spray method; the sustained-release microspheres A are coated by an isolation coating layer and an enteric coating layer in sequence; and then the sustained-release microspheres A are mixed with the corrective agent and the suspending aid. The prepared enteric dry suspension of rabeprazole and dextroisomer thereof is dispersed uniformly in intestinal tracts, and does not produce burst release. Compared with tablets or capsules, the enteric dry suspension has good stability, is convenient to separate dosage, is taken by adding water to form a solution, is good in absorptive capacity, fast in efficacy and good in bioavailability, has a good taste, is particularly suitable for patients suffering from difficult swallowing, especially for infant patients, and increases compliance of the patients. Besides, the preparation method is simple and is suitable for large-scale production and application.

Description

technical field [0001] The invention specifically relates to an enteric-coated dry suspension of rabeprazole and its dextro-isomer, and a preparation method of the enteric-coated dry suspension, belonging to the technical field of medicine. Background technique [0002] H2 receptor antagonists and proton pump inhibitors are the most common second class of drugs in the treatment of acid-related peptic disorders, both of which increase gastric pH. But proton pump inhibitors act on H + / K + -ATPase blocks the last channel of gastric acid secretion, so it can inhibit the secretion of basic gastric acid and the acid secretion caused by histamine, acetylcholine, gastrin and food stimulation, and cause a large and lasting increase in gastric pH. Proton pump inhibitors are currently recognized as the drug of choice for the treatment of peptic ulcer disease. [0003] Rabeprazole sodium is the latest proton pump inhibitor with a higher pKa value. Compared with omeprazole and esomep...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/4439A61P1/04
Inventor 杨艳丽张胜华陈蕴郭奇根于振艳
Owner 河南省健康伟业生物医药研究股份有限公司
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