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Sodium picosulfate enteric-coated tablet and preparation method thereof

A technology of sodium picosulfate and enteric-coated tablets, which can be used in pharmaceutical formulations, drug delivery, and the digestive system, and can solve problems such as irritation and instability of sodium picosulfate, so as to reduce adverse reactions and avoid gastrointestinal discomfort Effect

Active Publication Date: 2015-04-22
SHANDONG INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the listed products of sodium picosulfate include solutions, tablets, and granules, all of which are stomach-soluble preparations. Sodium picosulfate is extremely unstable to acid and degrades about 29%, of which the main degradation products are diphenols (impurity B in the European Pharmacopoeia). Although diphenols are active ingredients, they can stimulate the gastrointestinal mucosa above the colon. The role of sodium picosulfate The effective time is 6 to 12 hours after taking, and the premature release of the active ingredient will cause adverse reactions such as nausea, vomiting, borborygmi, abdominal distension, abdominal pain, etc. Therefore, it is necessary to improve the common gastric-soluble preparation of sodium picosulfate

Method used

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  • Sodium picosulfate enteric-coated tablet and preparation method thereof
  • Sodium picosulfate enteric-coated tablet and preparation method thereof
  • Sodium picosulfate enteric-coated tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1 Preparation of sodium picosulfate immediate-release tablet core

[0051]

[0052] Preparation method: ①Binder solution preparation: Weigh the prescription amount of hypromellose or hypromellose to prepare a 3% (w / w) aqueous solution. ②Material pretreatment: the particle size of sodium picosulfate is controlled below 80 mesh, and the particle size of other auxiliary materials is controlled below 60 mesh. ③ Mixing: Weigh the prescribed amount of sodium picosulfate, sodium starch glycolate or croscarmellose sodium, lactose, starch, and microcrystalline cellulose into a mixed wet granulator and mix well. ④ Granulation: Add the binder solution to the above materials, stir and granulate. ⑤Drying and granulating: drying at 45~55℃ and then granulating. ⑥Total mixing and tableting: Add magnesium stearate and silicon dioxide to the dry granules, then mix and tablet them for later use.

Embodiment 2

[0053] Example 2 Preparation of isolation layer of sodium picosulfate tablets

[0054]

[0055] Preparation method: ①Weigh hypromellose, polyethylene glycol 6000 or commercial film coating premix Opadry according to the prescription ? Ⅱ Dissolve in an appropriate amount of ethanol solution to make a coating solution, with a solid content of about 15%. ②The sodium picosulfate immediate-release tablet core is coated in a high-efficiency coating machine. The film-forming temperature is about 40~50℃, and the weight gain of the isolation layer is about 2~5% of the total weight of the immediate-release tablet core.

Embodiment 3

[0056] Example 3 Preparation of enteric coating layer of sodium picosulfate tablets

[0057]

[0058] Note: Eudragit ? FS 30D is a 30% water dispersion containing dry powder of methacrylic acid / methyl acrylate / methyl methacrylate (1:1:1) copolymer.

[0059] Preparation method: ①Weigh methacrylic acid / methyl methacrylate (1:2) copolymer according to the prescription [Eudragit ? S100] or methacrylic acid / methyl acrylate / methyl methacrylate (1:1:1) copolymer [Eudragit ? FS 30D], triethyl citrate, talc or micro-powder silica gel or monostearoyl glyceride and polysorbate 80, titanium dioxide are dispersed in an appropriate amount of ethanol solution or water to prepare a coating liquid, the solid content is about 15%. ② Put the sodium picosulfate immediate-release tablet core coated with the isolation layer into a high-efficiency coating machine, and the film-forming temperature is about 30℃. The weight gain of the enteric coating layer is about the total of the immediate-release tablet ...

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PUM

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Abstract

The invention belongs to the field of pharmaceutical compositions for treating constipation, and in particular relates to a sodium picosulfate enteric-coated tablet and a preparation method thereof. In vitro leaching test results show that according to the sodium picosulfate enteric-coated tablet prepared by the preparation method disclosed by the invention, the vast majority of active components can be released in an physiological environment which simulates the colon with pH greater than 7, so that gastrointestinal discomfort caused by premature release of sodium picosulfate can be effectively avoided so as to alleviate the adverse reaction of the tablet.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical compositions for treating constipation, and specifically relates to sodium picosulfate enteric-coated tablets and a preparation method thereof. Background technique [0002] Sodium picosulfate is a laxative synthesized by De Angeli, Italy in 1964. The efficacy of phenolic laxatives is mainly based on free hydroxyl groups. Therefore, the way to synthesize these compounds is to add other groups to the hydroxyl groups to evaluate the efficacy of a large number of such compounds. Studies have shown that almost all of these compounds are There is no gastrointestinal reaction. Diphenols are produced after hydrolysis by the colonic flora to play a laxative effect. Among them, sodium picosulfate shows good intestinal and laxative effects. The site of action of sodium picosulfate is the colon, which is hydrolyzed by the enzyme produced by the colonic flora to produce diphenols, which can directly stimulate the in...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/36A61K31/4402A61P1/10
Inventor 张雯刘晓琰李兆明曹冲
Owner SHANDONG INST OF PHARMA IND
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