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Enteric pore-foaming agent, preparation method of enteric pore-foaming agent and enteric capsule

A technology of enteric-coated capsules and porogens, which is applied in capsule delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc. It can solve the problems of slow dissolution and pore formation, and achieve the effect of strong solubility

Active Publication Date: 2021-04-02
HUBEI HUMANWELL PHARMACEUTICAL EXCIPIENTS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above organic acids and hydrophilic polymers are easy to dissolve in the gastric acid environment, and the rate of dissolution and pore formation in the alkaline environment of the intestinal tract is slow, so it is necessary to improve

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] First, the γ-cyclodextrin metal-organic framework@cellulose acetate fiber composite was prepared:

[0037] (1) 100 g of cellulose acetate fibers with a size of 1 μm were soaked in potassium hydroxide solution for 6 hours, and 12 g of γ-cyclodextrin with a size of 100 nm was added to form a mixed solution;

[0038] (2) Put the mixed solution in a closed environment of methanol, heat it to volatilize methanol into the mixed solution, remove the precipitation after centrifugation, add methanol and cetyltrimethylammonium bromide, let stand for 28 hours, and take out the cellulose acetate fiber, washed and dried to obtain a γ-cyclodextrin metal organic framework@cellulose acetate fiber composite.

[0039] The specific surface area of ​​the tested γ-cyclodextrin metal organic framework@cellulose acetate fiber composite is: 42m 2 / g.

[0040] Next, prepare the enteric porogen:

[0041] (3) The supersaturated solution of calcium chloride is mixed with the γ-cyclodextrin meta...

Embodiment 2

[0043] First, the γ-cyclodextrin metal-organic framework@cellulose acetate fiber composite was prepared:

[0044] (1) 100 g of cellulose acetate fibers with a size of 2 μm were placed in potassium hydroxide solution and soaked for 7 hours, and 15 g of γ-cyclodextrin with a size of 120 nm was added to form a mixed solution;

[0045] (2) Put the mixed solution in a closed environment of methanol, heat it to volatilize methanol into the mixed solution, remove the precipitation after centrifugation, add methanol and cetyltrimethylammonium bromide, let stand for 30 hours, and take out the cellulose acetate fiber, washed and dried to obtain γ-cyclodextrin metal-organic framework@cellulose acetate fiber composite.

[0046] The specific surface area of ​​the tested γ-cyclodextrin metal organic framework@cellulose acetate fiber composite is: 45m 2 / g.

[0047] Next, prepare the enteric porogen:

[0048] (3) The supersaturated solution of calcium gluconate is mixed with the γ-cyclode...

Embodiment 3

[0050] First, the γ-cyclodextrin metal-organic framework@cellulose acetate fiber composite was prepared:

[0051] (1) 100 g of cellulose acetate fibers with a size of 3 μm were placed in a potassium hydroxide solution to soak for 8 hours, and 20 g of γ-cyclodextrin with a size of 150 nm was added to form a mixed solution;

[0052] (2) Put the mixed solution in a closed environment of methanol, heat it to volatilize methanol into the mixed solution, remove the precipitation after centrifugation, then add methanol and cetyltrimethylammonium bromide, let stand for 32 hours, and take out the cellulose acetate fiber, washed and dried to obtain γ-cyclodextrin metal-organic framework@cellulose acetate fiber composite.

[0053] The specific surface area of ​​the tested γ-cyclodextrin metal organic framework@cellulose acetate fiber composite is: 50m 2 / g.

[0054] Next, prepare the enteric porogen:

[0055] (3) The supersaturated solution of potassium chloride is mixed with the γ-cy...

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Abstract

The invention discloses an enteric pore-foaming agent, a preparation method of the enteric pore-foaming agent and an enteric capsule. A gamma-cyclodextrin metal organic framework@cellulose acetate fiber composite material is adopted to coat soluble salt, the hydrolysis of the material in a gastric acid environment is prevented by utilizing the hydrophilic and acidophobic characteristics of cellulose acetate fibers, meanwhile the material can be slowly hydrolyzed in an intestinal alkaline environment to release the soluble salt in the material, and the soluble salt is extremely high in solubility in an aqueous solution, so that pores can be quickly formed; starch is used as a main material in the enteric capsule, and the cost is low, but the problems of poor water locking performance and brittleness and easiness in cracking after drying also exist; and by adding hydroxypropyl methylcellulose, the water absorption and water retention performance can be effectively improved, and the overall toughness is improved.

Description

technical field [0001] The invention relates to the technical field of enteric-coated capsules, in particular to an enteric-coated porogen and a preparation method thereof, and an enteric-coated capsule. Background technique [0002] The digestive organs of the human body are mainly the stomach and intestines. The stomach is mainly acidic and the intestines are alkaline. So now there are generally two kinds of capsules, one is dissolved in the stomach, the other is dissolved in the intestines. Enteric-coated capsules, in fact, only add special medicinal polymer materials to the capsule shell or undergo special treatment to make them insoluble in gastric juice and only disintegrate and dissolve in intestinal juice. The current enteric-coated capsules generally use gelatin or starch as the main component. In order to accelerate the dissolution in the intestinal tract, a pore-forming agent can be added to the enteric-coated capsules. Commonly used enteric porogens include org...

Claims

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Application Information

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IPC IPC(8): A61K47/40A61K47/38A61K47/36A61K47/02A61K47/12A61K47/26A61K9/48
CPCA61K9/4816Y02A50/30
Inventor 黄猛孙平飞黄建华任海民柯丽烂卢大林周峰詹欢欢闫莹莹
Owner HUBEI HUMANWELL PHARMACEUTICAL EXCIPIENTS CO LTD
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