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Preparation method for indapamide microsphere sustained release capsules

A technology of indapamide and sustained-release capsules, which can be used in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. Difficulty in dapamide and other problems, to achieve the effect of improving fluidity, simplifying granulation process, and good fluidity

Inactive Publication Date: 2012-07-18
SHANXI MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, indapamide is insoluble in water, and the slow release delays the peak time and reduces the peak concentration, which may lead to low bioavailability.

Method used

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  • Preparation method for indapamide microsphere sustained release capsules
  • Preparation method for indapamide microsphere sustained release capsules
  • Preparation method for indapamide microsphere sustained release capsules

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Preparation of indapamide E-100 microspheres:

[0041] Indapamide 0.04g

[0042] Eudragit E-100 0.28g

[0043] Micropowder silica gel amount

[0044] According to the above prescription, dissolve the main ingredients indapamide and Eudragit E-100 in 5.2ml of acetone and dichloromethane mixed solvent, then add a small amount of micropowdered silica gel, shake to form a uniformly dispersed organic liquid; stir at 24°C and 600rpm Next, inject this organic liquid into 52 ml of sodium lauryl sulfate aqueous solution, continue to stir, and add the same amount of aqueous solution; continue to stir until the spherical particles are solidified, filter, dry, and collect stomach-soluble microspheres.

[0045] Preparation of indapamide HP-55 microspheres:

[0046] Indapamide 0.04g

[0047] Hypromellose Phthalate HP-55 0.20g

[0048] According to the above prescription, the main drug indapamide and HP-55 were dissolved in 4.0ml of absolute ethanol and dichloromethane mixed solv...

Embodiment 2

[0054] Indapamide extended-release capsules

[0055] Gastric Microspheres 1.9g

[0056] Enteric coated microspheres 10g

[0057] Colonic Microspheres 1.1g

[0058] Microcrystalline Cellulose 25g

[0059] Lactose 20g

[0060] Talc powder 2g

[0061] According to the composition of the above prescription, take 1.9g of gastric-coated microspheres, 10g of enteric-coated microspheres and 1.1g of colonic-coated microspheres and mix them uniformly by equal addition method; pass microcrystalline cellulose, lactose and talcum powder through an 80-mesh sieve and mix well; The microspheres and auxiliary materials are respectively packed into empty capsules to make 1000 capsules, each capsule weighs 60 mg, and each capsule contains 1.5 mg of indapamide.

Embodiment 3

[0063] Indapamide extended-release capsules

[0064] Gastric Dissolved Microspheres 2.5g

[0065] Enteric coated microspheres 9.3g

[0066] Colonic Microspheres 1.2g

[0067] Microcrystalline Cellulose 27g

[0068] Lactose 18g

[0069] Micronized silica gel 2g

[0070] According to the composition of the above prescription, take 2.5g of stomach-coated microspheres, 9.3g of enteric-coated microspheres and 1.2g of colonic-coated microspheres and mix them uniformly by equal addition method; pass microcrystalline cellulose, lactose and micronized silica gel through an 80-mesh sieve and mix well ; The microspheres and auxiliary materials are respectively packed into empty capsules to make 1000 capsules, each capsule weighs 60 mg, and the indapamide contained in each capsule is 1.5 mg.

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Abstract

Provided is a preparation method for indapamide microsphere sustained release capsules. The indapamide microsphere sustained release capsules, especially contents, are formed by microsphere of gastrointestinal tract release medicine manufactured by indapamide and high polymer materials with high potential of hydrogen (pH) dependency. The high polymer materials comprise polyacrylate E-100, hydroxypropyl methylcellulose phthalic ester HP-55 and hydroxypropyl methylcellulose succinate HAS which are respectively manufactured into stomach dissolving microsphere, intestines dissolving microshpere and colon dissolving microsphere with the indapamide. All microspheres are combined into particle dispersing capsules according to weight parts. After taken, medicine is released in the stomach and intestines according to pH gradient, blood concentration is stable, sustained release is achieved, medicine in the microsphere is highly dispersed and dissolved out to be completely absorbed, and biological utilization of oral medicine is improved. The medicine microsphere is simple in the preparation method and equipment and suitable for industrialization.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to indapamide sustained-release capsules, the contents of which are mainly composed of indapamide localized microspheres with pH-dependent gradient release, and the drug is released in the whole gastrointestinal tract after oral administration. Absorption, to achieve a sustained release effect, and improve the bioavailability of poorly soluble drugs. Background technique [0002] Hypertension is the most common cardiovascular disease in the world, and it is also one of the biggest epidemics. It often causes complications in the heart, brain, kidney and other organs, and seriously endangers human health. The "three highs" of high prevalence, high mortality, and high disability rate and the "three lows" of low awareness rate, low treatment rate, and low control rate are common in hypertension in my country. Among them, the treatment rate and control rate are according to the...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K9/16A61K31/404A61K47/38A61K47/32A61P9/12A61P7/10
Inventor 丁红赵志娟郭海丽赵智卉闫志飞谢茵
Owner SHANXI MEDICAL UNIV
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