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Oral preparation of novel colonic positioning release medicine

A technology of colon-localized and oral preparations, applied in the field of olsalazine sodium colon-localized release tablets, which can solve problems such as irritation and obvious adverse reactions of the stomach, and achieve the effect of improving curative effect

Active Publication Date: 2010-06-16
TIANJIN LISHENG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Common oral preparations for the treatment of colitis disintegrate in the stomach, which may have obvious adverse reactions to the stomach. Common enteric-coated tablets are disintegrated, released and absorbed in the small intestine when taken orally, and the drug is affected by the digestive juice and the first-pass effect to stimulate the upper gastrointestinal tract , the patient had adverse reactions such as vomiting, anorexia, and nausea

Method used

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  • Oral preparation of novel colonic positioning release medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Core preparation

[0039] Tablet core prescription ①: 1000 tablets

[0040] Osalazine Sodium 250g

[0041] Starch 30g

[0042] Sodium carboxymethyl starch 37.5g

[0043] Microcrystalline Cellulose 25g

[0044] 6% PVPk30 Appropriate amount.

[0045] Tablet core prescription ②: 1000 tablets

[0046] Osalazine Sodium 250g

[0047] Modified starch 30g

[0048] Low-substituted hydroxypropyl cellulose 37.5g

[0049] Microcrystalline Cellulose 25g

[0050] 6% PVPk90 Appropriate amount.

[0051] Magnesium Stearate 1.5g.

[0052] Tablet core prescription ③: 1000 tablets

[0053] Osalazine Sodium 250g

[0054] Sodium chloride 30g

[0055] Sodium carboxymethyl starch 37.5g

[0056] Spray dried lactose 25g

[0057] 6% ethyl cellulose appropriate amount

[0058] Talc powder 1.5g.

[0059] Tablet core prescription ④: 1000 tablets

[0060] Osalazine Sodium 250g

[0061] Lactose 20g

[0062] Hydroxypropyl Cellulose 37.5g

[0063] Microcrystalline Cellulose 30g

[00...

Embodiment 2

[0083] Preparation of the isolation layer:

[0084] Isolation layer prescription ①: 1000 tablets

[0085] Hypromellose 9.6g

[0086] Macrogol 2000 2.4g

[0087] Diethyl phthalate 1.2g

[0088] 60% ethanol 140g.

[0089] Isolation layer prescription ②: 1000 tablets

[0090] Hypromellose 9.6g

[0091] Macrogol 2000 4.8g

[0092] Diethyl phthalate 1.8g

[0093] 80% ethanol 140g.

[0094] Isolation layer prescription ③: 1000 tablets

[0095] Hypromellose 9.6g

[0096] Macrogol 2000 4.8g

[0097] Triethyl citrate 2.4

[0098] 95% ethanol 140g.

[0099] Isolation layer prescription ④: 1000 tablets

[0100] Hypromellose 9.6g

[0101] Macrogol 2000 4.8g

[0102] Triethyl citrate 1.2

[0103] 95% ethanol 140g.

[0104] The isolation layer prescriptions ①-④ are all coated with high-efficiency coating machines, and the amount of coating solution varies with the amount of tablet cores. Efficient coating machine specific

[0105] The parameters are as follows:

[0106] ...

Embodiment 3

[0109] Colonic coating layer preparation:

[0110] Prescription of colonic coating layer ①: 1000 tablets

[0111] Eudregit S100 20.5g

[0112] Eudregit L100 5g

[0113] Macrogol 2000 4.8g

[0114] Diethyl phthalate 1.8g

[0115] 60% ethanol 500

[0116] Colonic coating layer prescription ②: 1000 tablets

[0117] Eudregit S100 20.5g

[0118] Eudregit L100 7g

[0119] Triethyl citrate 5g

[0120] Macrogol 2000 4.8g

[0121] Diethyl phthalate 1.8g

[0122] 60% ethanol 500

[0123] Colonic coating layer prescription ③: 1000 tablets

[0124] Eudregit S100 20g

[0125] Triethyl citrate 8g

[0126] 80% ethanol 500

[0127] Colonic coating layer prescription ④: 1000 tablets

[0128] Eudregit S100 20g

[0129] Macrogol 2000 2g

[0130] 95% ethanol 415

[0131] The formulations of the colonic coating layer are all coated by a high-efficiency coating machine, and the amount of coating solution varies with the amount of the tablet core. The specific parameters of the hi...

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Abstract

The invention discloses an oral preparation of a colonic positioning release medicine, which is formed in such a way that the effective component of olsalazine sodium and a medicinal carrier form a medicine tablet core together, the outside of the medicine tablet core is wrapt with isolation layer coating liquid comprising an imbibition type high molecular material, and the outermost layer of the medicine tablet core is wrapt with colonic dissolvable coating liquid containing a colonic dissolvable type high molecular material, wherein the weight ratio of the medicine tablet core to the isolation layer coating liquid to the colonic dissolvable coating liquid is 1:0.2-1.2:0.5-2. The olsalazine sodium colonic positioning enteric coated tablet avoids the first pass effect of the medicine, avoids stimulating the stomach and the small intestine, enables a coating to be dissolved according to the condition of high pH at the tail end of the small intestine and the position of the colon and acts as the function of colonic positioning release. In the invention, an azo bond is ruptured under the function of colonic bacteria and is split into 5-aminosalicylic acid with 2 molecules, thereby achieving the function of suppressing an inflammatory reaction and diarrhea.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to an oral preparation for colon-localized drug release, in particular to a colon-localized release tablet of olsalazine sodium. Background technique [0002] Colon-targeted release systems are divided into the following types: [0003] 1. Time-delayed drug release: After oral administration, the drug is transported through the gastrointestinal tract, and it takes a certain amount of time to reach the colon. According to this principle, the drug can be controlled to release after a period of time through appropriate preparation methods. Theoretically To achieve the purpose of colon target drug release. However, the gastric emptying time in the human body is affected by factors such as food, age, personal physiological and pathological characteristics, and there are large individual differences. Therefore, the time-delay release drug has a greater individual influe...

Claims

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Application Information

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IPC IPC(8): A61K9/30A61K31/655A61K47/38A61K47/36A61P29/00A61P1/00A61P1/04A61P1/12
Inventor 郁洋翟德志张晶
Owner TIANJIN LISHENG PHARM CO LTD
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