Acetazolamide tablet and preparation method thereof

A technology of acetazolamide tablets and acetazolamide, which is applied in the field of acetazolamide tablets and its preparation, can solve the problems that drug intraocular pressure cannot be well controlled, acetazolamide is difficult to dissolve in water, and its bioavailability is low. To achieve the effect of improving bioavailability, improving stability and improving solubility

Inactive Publication Date: 2017-05-31
HUAYI PHARMA ANHUI CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Acetazolamide is poorly soluble in water, and its bioavailability in ordinary tablets is low
In the cases where the application of acetazolamide failed, in a

Method used

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  • Acetazolamide tablet and preparation method thereof
  • Acetazolamide tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0020] Example 1

[0021] An acetazolamide tablet, including the following raw materials:

[0022] Acetazolamide 180g, poloxamer 40g, sorbitol 21g, lactose 100g, corn starch 50g, povidone 10g, magnesium stearate 4g, calcium sulfate 5g and sodium carboxymethyl starch 7g.

[0023] The preparation method includes the following steps:

[0024] 1) Pass acetazolamide through a 20-mesh sieve; poloxamer, sorbitol, lactose, corn starch, magnesium stearate, calcium sulfate and sodium carboxymethyl starch are passed through a 30-mesh sieve, and the povidone is dissolved in water Preparation of povidone aqueous solution;

[0025] 2) Weigh acetazolamide, poloxamer and sorbitol into a wet granulator for dry mixing, and then add povidone aqueous solution for wet granulation;

[0026] 3) The granules obtained in step 2) are sized and dried at 70°C for 5 minutes to obtain acetazolamide dry granules;

[0027] 4) After acetazolamide dry granules, corn starch, povidone, magnesium stearate, calcium sulfate a...

Example Embodiment

[0028] Example 2

[0029] An acetazolamide tablet, including the following raw materials:

[0030] Acetazolamide 200g, poloxamer 45g, sorbitol 30g, lactose 100g, corn starch 10g, pregelatinized starch 10g, povidone 7g, zinc stearate 2g, calcium sulfate 5g and sodium carboxymethyl starch 5g.

[0031] The preparation method includes the following steps:

[0032] 1) Pass acetazolamide through a 20-mesh sieve; poloxamer, sorbitol, lactose, corn starch, pregelatinized starch, zinc stearate, calcium sulfate and sodium carboxymethyl starch pass through a 30-mesh sieve. Polyvidone is dissolved in water to prepare an aqueous solution of povidone;

[0033] 2) Weigh acetazolamide, poloxamer and sorbitol into a wet granulator for dry mixing, and then add povidone aqueous solution for wet granulation;

[0034] 3) The granules obtained in step 2) are sized and dried at 65°C for 6 min to obtain acetazolamide dry granules;

[0035] 4) After acetazolamide dry granules, corn starch, pregelatinized starch,...

Example Embodiment

[0036] Example 3

[0037] An acetazolamide tablet, including the following raw materials:

[0038] Acetazolamide 200g, poloxamer 50g, sorbitol 15g, lactose 130g, corn starch 50g, povidone 15g, magnesium stearate 6g, calcium sulfate 5g and sodium carboxymethyl starch 11g.

[0039] The preparation method includes the following steps:

[0040] 1) Pass acetazolamide through a 20-mesh sieve; poloxamer, sorbitol, lactose, corn starch, magnesium stearate, calcium sulfate and sodium carboxymethyl starch are passed through a 30-mesh sieve. Vitone aqueous solution;

[0041] 2) Weigh acetazolamide, poloxamer and sorbitol into a wet granulator for dry mixing, and then add povidone aqueous solution for wet granulation;

[0042] 3) The granules obtained in step 2) are sized and dried at 60°C for 8 minutes to obtain acetazolamide dry granules;

[0043] 4) After acetazolamide dry granules, corn starch, povidone, magnesium stearate, calcium sulfate and sodium carboxymethyl starch are mixed uniformly, the...

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Abstract

The invention provides an acetazolamide tablet, which is prepared from the following raw and auxiliary materials in parts by weight: 160-200 parts of acetazolamide, 30-50 parts of poloxamer, 15-30 parts of sorbitol, 120-180 parts of filler, 5-15 parts of povidone, 2-6 parts of a lubricant and 10-16 parts of a disintegration material. The preparation method comprises the following steps: (1) sieving the raw and auxiliary materials except for the povidone for later use and preparing a water solution from the povidone; (2) adding weighed acetazolamide, poloxamer and sorbitol to a wet type granulator for dry mixing, adding a povidone water solution for wet granulation; (3) granulating and drying the particles prepared in the step (2) to obtain acetazolamide particles; and (4) mixing dry acetazolamide particles, the filler, the lubricant and the disintegration material evenly and then tabletting. With the tablet, the solubility of an active ingredient in water can be improved, the bioavailability is improved and the disintegration time is shortened.

Description

technical field [0001] The invention belongs to the field of ophthalmic drug preparations, and in particular relates to an acetazolamide tablet and a preparation method thereof. Background technique [0002] Acetazolamide is a carbonic anhydrase inhibitor, mainly used to reduce intraocular pressure and inhibit the activity of ciliary skin carbonic anhydrase, thereby reducing the production of aqueous humor and reducing intraocular pressure. It is suitable for the treatment of various types of glaucoma. Such as open-angle (chronic simple) glaucoma, angle-closure glaucoma and so on. [0003] Acetazolamide is insoluble in water, and its bioavailability in ordinary tablets is low. In the cases where the application of acetazolamide failed, except for the cases where its use was limited due to its side effects, the rest were due to poor control of intraocular pressure due to poor absorption of the drug. Contents of the invention [0004] The invention provides an acetazolamid...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/433A61K47/36A61K47/02A61K47/10A61K47/32A61P27/06A61K9/16
CPCA61K31/433A61K9/1623A61K9/2004A61K9/2027A61K9/2031A61K9/2059A61K9/2095
Inventor 高煜操铖
Owner HUAYI PHARMA ANHUI CO LTD
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