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Loxoprofen sodium sustained release preparation

A technology of loxoprofen sodium and sustained-release preparations, applied in the field of medicine, can solve the problems of inability to show curative effect, peak-to-valley phenomenon, side effects and the like

Inactive Publication Date: 2005-06-22
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because the biological half-life of loxoprofen sodium is very short, common preparations are usually administered three times a day, which is not only inconvenient to use, but also has a large fluctuation in blood drug concentration, with a "peak-valley" phenomenon, causing a short-term rise in blood drug concentration and then rapidly eliminated
When the blood concentration is high (peak), side effects or even poisoning may occur; when the blood concentration is low (trough), it may be below the therapeutic concentration, so that the curative effect cannot be shown

Method used

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  • Loxoprofen sodium sustained release preparation
  • Loxoprofen sodium sustained release preparation
  • Loxoprofen sodium sustained release preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] prescription:

[0052] Loxoprofen sodium (calculated as anhydrous substance) 180mg

[0053] Hypromellose 60mg

[0054] Ethylcellulose 160mg

[0055]Acrylic resin (Eudragit L100) 100mg

[0056] Magnesium Stearate Appropriate amount

[0057] 70% ethanol appropriate amount

[0058] Preparation method:

[0059] Loxoprofen sodium, hypromellose, ethyl cellulose and acrylic resin are crossed 80 mesh sieves respectively (if necessary, must be pulverized earlier), take each adjuvant by prescription quantity and mix homogeneously, add loxoprofen sodium, Mix evenly, add 70% ethanol to make soft material, granulate with 20-mesh sieve, dry at 50°C for 2 hours, granulate with 18-mesh sieve, add 2% magnesium stearate by dry granule weight, and press into tablets to obtain.

Embodiment 2

[0061] prescription:

[0062] Loxoprofen sodium (calculated as anhydrous substance) 180mg

[0063] Hypromellose 60mg

[0064] Ethylcellulose 60mg

[0065] Acrylic resin (Eudragit L100) 160mg

[0066] Lactose 40mg

[0067] Magnesium Stearate Appropriate amount

[0068] 70% ethanol appropriate amount

[0069] Preparation method:

[0070] Pass loxoprofen sodium, lactose, hypromellose, ethyl cellulose and acrylic resin through 80-mesh sieve respectively (if necessary, first pulverize), weigh each auxiliary material according to the prescription amount and mix evenly, add loxoprofen Sodium, mix well, add 70% ethanol to make soft material, granulate with 20-mesh sieve, dry at 50°C for 2 hours, granulate with 18-mesh sieve, add 2% magnesium stearate by weight of dry granules, compress into tablets, and obtain.

Embodiment 3

[0072] prescription:

[0073] Loxoprofen sodium (calculated as anhydrous substance) 180mg

[0074] Hypromellose 60mg

[0075] Ethylcellulose 180mg

[0076] Acrylic resin (Eudragit L100) 80mg

[0077] Magnesium Stearate Appropriate amount

[0078] 70% Alcohol Appropriate amount

[0079] Preparation method:

[0080] Loxoprofen sodium, hypromellose, ethyl cellulose and acrylic resin are crossed 80 mesh sieves respectively (if necessary, must be pulverized earlier), take each adjuvant by prescription quantity and mix homogeneously, add loxoprofen sodium, Mix evenly, add 70% ethanol to make soft material, granulate with 20-mesh sieve, dry at 50°C for 2 hours, granulate with 18-mesh sieve, add 2% magnesium stearate by dry granule weight, and press into tablets to obtain.

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Abstract

The invention provides a Loxoprofen sodium sustained release preparation, wherein the preparation comprises Loxiprofen sodium as active component and pharmaceutically acceptable carrier, the components include (1) skeleton type, membrane control type, or penetration pump type tablet or capsule, (2) microcapsule, small pill, microballoon, emulsion, and slow release preparation, (3) space or time delay type slow release preparation.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a composition containing loxoprofen sodium, more specifically, the invention relates to a slow-release preparation of loxoprofen sodium. Background technique [0002] Loxoprofen sodium is a phenylpropionic acid non-steroidal analgesic anti-inflammatory drug, the chemical name is 2-[4-(2-oxocyclopentane-1-ylmethyl)phenyl]propionate sodium dihydrate , the molecular formula is C 15 h 17 NaO 3 2H 2 O, the structural formula is as follows: [0003] [0004] Loxoprofen sodium is white crystal or crystalline powder. It is very soluble in water or methanol, easily soluble in ethanol, and almost insoluble in ether. Loxoprofen sodium has excellent analgesic and anti-inflammatory effects, characterized by strong analgesic effect, anti-inflammatory and antipyretic effects similar to other similar drugs, and weak activity on chronic inflammation. Clinically, it can be w...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/14A61K9/52A61K31/192A61P29/00
Inventor 印春华唐翠
Owner FUDAN UNIV
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