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Acetazolamide sustained-release capsule and preparation method thereof

A technology of acetazolamide and sustained-release capsules, which can be used in pharmaceutical formulations, medical preparations containing active ingredients, drug delivery and other directions, and can solve the problems of irreplaceable, high peak blood drug concentration, and too fast release rate of common dosage forms. , to achieve the effect of facilitating long-term treatment, less toxic and side effects, and reducing toxic and side effects

Active Publication Date: 2015-05-27
ZHONGSHUAI PHARMA SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because its mechanism of action is different from other ocular hypotensive drugs, and it has an additive effect with other types of ocular hypotensive drugs, it cannot be replaced clinically at present, especially for the maximum tolerated drug treatment of glaucoma
[0009] For the treatment of acute mountain sickness, there is still a gap in China and urgently needs to be filled; while acetazolamide on the domestic market is only oral regular-release tablets, but the release rate of the common dosage form is too fast, resulting in a high peak blood concentration, which induces various side effects , such as numbness in limbs, fatigue, drowsiness, depression, lethargy, etc.

Method used

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  • Acetazolamide sustained-release capsule and preparation method thereof
  • Acetazolamide sustained-release capsule and preparation method thereof
  • Acetazolamide sustained-release capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The raw and auxiliary materials of the acetazolamide sustained-release capsule of the present invention are composed of: according to the composition formula of the raw and auxiliary materials, the expansion is 6.3 times, expressed in parts by weight g, consisting of 500 g of acetazolamide, 130 g of microcrystalline cellulose, and 2.0 g of sodium lauryl sulfate And purified water 230g composition.

[0048] Explanation: The water in the adhesive added in this example goes through the preparation method and is finally dried to obtain the product. The added water is all evaporated, so the proportion of the above raw and auxiliary materials is calculated as solid matter.

[0049] The preparation method of acetazolamide sustained-release capsules of the present invention:

[0050] a. Prepare various raw and auxiliary materials according to the composition of the raw and auxiliary materials of the above-mentioned acetazolamide sustained-release capsules, dissolve the auxiliar...

Embodiment 2

[0052] Embodiment 2: basically the same as Embodiment 1, the difference is:

[0053] The raw and auxiliary materials of the acetazolamide sustained-release capsule of the present invention are composed of: according to the composition formula of the raw and auxiliary materials, the expansion is 6.4 times, expressed in parts by weight g, consisting of 500 g of acetazolamide, 125 g of microcrystalline cellulose, and 1.5 g of sodium lauryl sulfate , 6.3g of talcum powder and 225g of 2% hypromellose aqueous solution in mass percent concentration.

[0054] Explanation: The water in the adhesive added in this example goes through the preparation method and is finally dried to obtain the product. The added water is all evaporated, so the proportion of the above raw and auxiliary materials is calculated as solid matter.

[0055] The preparation method of the acetazolamide sustained-release capsule of the present invention is the same as in Example 1.

Embodiment 3

[0056] Embodiment 3: basically the same as Embodiment 1, the difference is:

[0057] The raw and auxiliary materials of the acetazolamide sustained-release capsule of the present invention are composed of: according to the composition formula of the raw and auxiliary materials, the expansion is 6.9 times, expressed in parts by weight g, consisting of 525g of acetazolamide, 110g of microcrystalline cellulose, and 1.0g of sodium lauryl sulfate , 50g of sucrose, 5g of talcum powder and 200g of purified water.

[0058] Explanation: The water in the adhesive added in this example is prepared through the preparation method and finally dried to obtain the product. The added water is all evaporated, so the proportion of the above raw and auxiliary materials is calculated as solid matter;

[0059] The preparation method of the acetazolamide sustained-release capsule of the present invention is the same as in Example 1.

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Abstract

The invention discloses an acetazolamide sustained-release capsule and a preparation method thereof. The acetazolamide sustained-release capsule is mainly composed of the following raw materials in accordance with parts by weight: 65 to 85 parts of acetazolamide, 15 to 35 parts of microcrystalline cellulose and 0.1 to 0.5 part of sodium dodecyl sulfate, and the acetazolamide sustained-release capsule further contains pharmaceutically acceptable pharmaceutic adjuvants. The preparation method comprises the following steps that the required raw materials and the adjuvants are smashed and uniformly mixed, and then the raw materials and adjuvants are prepared into soft materials after being uniformly mixed; a low-temperature refrigerator is turned on, the soft materials are put into an extrusion rolling machine to be extruded and rolled, and then drug containing micro pills with uniform particle sizes are formed; after the drug containing micro pills are dried, acetazolamide sustained-release micro pills are obtained; and the acetazolamide sustained-release micro pills are encapsulated to obtain the acetazolamide sustained-release capsule. The acetazolamide sustained-release capsule prepared by using the preparation method has little side effect and is convenient for patients to treat for a long time, and the drug compliance is improved. When the acetazolamide sustained-release capsule is taken once a day, the concentration of effective drugs in vivo can be guaranteed for 24 hours, and the toxic and side effects caused by a higher peak value of the blood drug concentration due to normal preparations can be reduced.

Description

technical field [0001] The invention relates to pharmaceutical preparations and a preparation method thereof in the field of pharmacy, in particular to an acetazolamide sustained-release capsule and a preparation method thereof. Background technique [0002] Acetazolamide is a carbonic anhydrase inhibitor that can be used to prevent or improve the symptoms of acute mountain sickness; it is also used for chronic simple (open-angle) glaucoma, secondary glaucoma, and acute angle-closure glaucoma. adjunct to pressure therapy. The chemical name of acetazolamide is N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide. Its molecular formula is: C 4 h 6 N 4 o 3 S 2 , the molecular weight is 222.25, and the structural formula is: [0003] [0004] Acetazolamide is white needle-like crystal or crystalline powder, odorless, slightly bitter taste. Slightly soluble in boiling water, very slightly soluble in water or ethanol, almost insoluble in chloroform or ether; easily soluble in...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K31/433A61P27/06A61P9/00
Inventor 马丽赵军霞吴会勤
Owner ZHONGSHUAI PHARMA SCI & TECH CO LTD