Doxazosin-mesylate controlled-releasing tablet and preparation method thereof

A technology of doxazosin mesylate and controlled-release tablets is applied in the directions of pharmaceutical formulations, medical preparations with inactive ingredients, medical preparations containing active ingredients, etc. application, increasing the difficulty of quality control, restricting large-scale production and other issues, to meet the needs of clinical medication, overcome technical difficulties, and reduce side effects.

Active Publication Date: 2008-04-30
HEFEI LIFEON PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The entire production process is complicated and technically difficult, and there are many production control points, which increases the difficulty of quality control and restricts large-scale production
[0005] Osmotic pumps with a monolithic core structure have the simple structure of primary osmotic pumps, and are currently a hot spot in the development of insoluble drugs, but the application of doxazosin mesylate in this area has not been found yet.

Method used

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  • Doxazosin-mesylate controlled-releasing tablet and preparation method thereof
  • Doxazosin-mesylate controlled-releasing tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] (1) Tablet core prescription

[0040] Composition g / 1000 tablets

[0041] Doxazosin mesylate 4.86

[0042] Tartaric acid 30

[0043] Sodium dodecyl sulfonate 5

[0044]Lactose 70

[0045] Mannitol 70

[0046] Polyethylene oxide (200,000 molecular weight) 3

[0047] Gum Arabic 17

[0048] Polyethylene oxide (5 million molecular weight) 5

[0049] Dextrin 44

[0050] Magnesium Stearate 1

[0051] (2) Preparation method

[0052] Raw and auxiliary materials are respectively passed through 80 mesh sieves. Weigh according to the prescription ratio, mix evenly, use ethanol as wetting agent to make soft material, granulate with a 20-mesh sieve, dry the wet granules at 50°C, granulate with an 18-mesh sieve, and mix the dry granules with a lubricant Compress the tablet to get the tablet core.

[0053] Dissolve cellulose acetate and polyethylene glycol 1500 (weight ratio 5:1) in a mixed solvent of acetone and isopropanol to prepare a semipermeable membrane coating solu...

Embodiment 2

[0055] (1) Tablet core prescription

[0056] Composition g / 1000 tablets

[0057] Doxazosin mesylate 4.86

[0058] Citric acid 35

[0059] Sodium dodecyl sulfonate 5

[0060] Sucrose 40

[0061] Lactose 80

[0062] Polyethylene oxide (100,000 molecular weight) 5

[0063] Gum Arabic 20

[0064] Sodium Alginate 20

[0065] Starch 40

[0066] Magnesium Stearate 1

[0067] (2) Preparation method

[0068] Raw and auxiliary materials are respectively passed through 80 mesh sieves. Weigh according to the prescription ratio, mix evenly, use ethanol as wetting agent to make soft material, granulate with a 20-mesh sieve, dry the wet granules at 50°C, granulate with an 18-mesh sieve, and mix the dry granules with a lubricant Compress the tablet to get the tablet core.

[0069] Dissolve cellulose acetate and polyethylene glycol 1500 (weight ratio 5:1) in a mixed solvent of acetone and isopropanol to prepare a semipermeable membrane coating solution. Coat the tablet cores in a ...

experiment example 1

[0070] Experimental example 1 Determination experiment of release degree

[0071] 1. Sample

[0072] The doxazosin mesylate controlled-release tablet of the present invention is prepared according to Example 1 of the present invention; "Keduohua" is purchased from the market.

[0073] 2. Experimental method

[0074] With Chinese Pharmacopoeia version in 2005 two appendices X D first method (adopting the device of dissolution rate second method, rotating speed is 75 revolutions per minute), measure the cumulative release of doxazosin mesylate, and preparation of the present invention and Marketed Kaduohua (produced by Pfizer of the United States, repackaged by Pfizer of Dalian) was compared. In order to further illustrate that the controlled release of the drug by the osmotic pump preparation is not affected by the environment, according to the relevant guiding principles and methods of the Chinese Pharmacopoeia 2005 edition, the standard medium (hydrochloric acid solution (7...

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Abstract

The invention discloses methanesulfonic acid doxazosin controlling releasing tablets and a process for preparation, which contains a single-layer core, insoluble semi-permeable membrane, single drug-releasing eyelet on each side of the tablet, and depends on the osmotic pressure difference between inside and outside of the semi-permeable membrane medium. The invention realizes the control of linear releasing of methanesulfonic acid doxazosin by single-layer core structure, and can remain effective and steady blood and drug concentration. The curative effect is improved, the generation rate of side effect is reduced, and the productive technology is greatly simplified.

Description

technical field [0001] The invention relates to a doxazosin mesylate controlled-release preparation, in particular to an oral doxazosin mesylate single-chip single-chamber osmotic pump controlled-release tablet and a preparation method thereof. Background technique [0002] Doxazosin Mesylate (Doxazosin Mesylate) is a selective α-receptor blocker developed by Pfizer of the United States. It is clinically applicable to hypertension and can also treat benign prostatic hyperplasia; benign prostatic hyperplasia refers to The enlargement of the prostate volume can cause symptoms such as dysuria in male patients, including frequent urination (especially nocturia), urgency, hesitancy to urinate, and thinning of the urinary stream. Among the men over 50 years old, more than 30% are troubled by benign prostatic hyperplasia (BPH), and about 50% of the elderly men over 60 years old. As a result, urinary function is increasingly damaged. [0003] Pfizer has improved the original ordina...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/517A61K9/22A61K47/36A61K47/40A61P9/12A61P13/08
Inventor 季俊虬高美华陈军夏军
Owner HEFEI LIFEON PHARMA
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