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Loxoprofen sodium matrix sustained-release tablet

A technology of loxoprofen sodium and skeleton sustained-release material, which is applied in the directions of non-active ingredient medical preparations, pill delivery, pharmaceutical formulations, etc., can solve the problems of increased adverse reactions, rapid initial release, and unfavorable blood drug concentrations, etc. Achieve the effect of increasing drug diffusion resistance, constant release rate and good control effect

Active Publication Date: 2012-07-04
北京天衡药物研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the clinically applied preparation is an ordinary quick-release preparation, the specification is 60 mg, and it is administered 3 times a day, which is likely to cause fluctuations in blood drug concentration and increase the occurrence of adverse reactions. Therefore, it is necessary to make it into a sustained-release preparation to reduce Dosing times, maintain a stable blood concentration, reduce the occurrence of adverse reactions, and improve patient compliance
[0004] The drug release rate of single-layer hydrophilic gel matrix sustained-release tablets is first-order or pseudo-first-order release, and its release characteristics are fast drug release in the early stage and slow drug release in the later stage, which is not conducive to stable control of blood drug concentration
For drugs with high water solubility, the single-layer gel matrix has insufficient ability to control the release rate. In the early stage of drug release, the drug on the surface is released before the formation of the hydration gel layer, resulting in a faster initial release. In order to control the initial release Generally, an excessive amount of sustained-release material is added. In this case, in the late stage of release, the release rate decreases due to the decrease in drug diffusion concentration difference, which may easily cause incomplete release.

Method used

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  • Loxoprofen sodium matrix sustained-release tablet
  • Loxoprofen sodium matrix sustained-release tablet
  • Loxoprofen sodium matrix sustained-release tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Comparative Example 1: Loxoprofen Sodium Common Single-Layer Sustained Release Tablet

[0079] 1. Prescription composition:

[0080]

[0081] Prescription composition 1000 tablets

[0082]

[0083] Loxoprofen Sodium 90g

[0084] Hydroxypropyl Methyl Cellulose K4M 95g

[0085] Hydroxypropyl Methyl Cellulose K100 60g

[0086] Microcrystalline Cellulose 30g

[0087] Lactose 60g

[0088] Stearic acid 15g

[0089] Micronized silica gel 20g

[0090] 8% povidone K30 ethanol solution appropriate amount

[0091] Magnesium Stearate 5g

[0092]

[0093] Second, the preparation process:

[0094] 1. Take the prescription amount of loxoprofen sodium, hypromellose K4M, hypromellose K100, microcrystalline cellulose, lactose, micropowder silica gel and stearic acid and mix evenly;

[0095] 2. 8% povidone K30 ethanol solution is used to make soft materials, and 24 m...

Embodiment 1

[0102] Comparative example 1 release test result

[0103]

[0104]

[0105] * n=6, the average value of 6 samples

[0106] The result shows, because the dissolubility of loxoprofen sodium is bigger, according to the loxoprofen sodium common matrix slow-release tablet of single-layer structure prepared by traditional process, has used a larger amount of matrix slow-release material, the result releases better in the early stage, but The release value at the end point 8h is on the low side, although it is still within the limit, the residue is serious (about 15-20%), and the ideal release effect has not been achieved.

Embodiment 2

[0107] Comparative Example 2: Loxoprofen Sodium Common Single-Layer Sustained Release Tablet

[0108] 1. Prescription composition:

[0109]

[0110] Prescription composition 1000 tablets

[0111]

[0112] Loxoprofen Sodium 90g

[0113] Hydroxypropyl Methyl Cellulose K4M 90g

[0114] Hydroxypropyl Methyl Cellulose K100 50g

[0115] Microcrystalline Cellulose 30g

[0116] Lactose 60g

[0117] Stearic acid 15g

[0118] Micronized silica gel 20g

[0119] 8% povidone K30 ethanol solution appropriate amount

[0120] Magnesium Stearate 5g

[0121]

[0122] Two, preparation technology: with comparative example 1.

[0123] Three, release measurement: method is with comparative example 1, and result is as shown in the table below:

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Abstract

The invention relates to a novel matrix sustained-release tablet containing loxoprofen sodium, in particular to a locoprofen sodium matrix sustained-release tablet with a regulation layer, which is capable of stably releasing for 8 hours, good in releasing effect, simple in process and low in cost.

Description

technical field [0001] The invention relates to a novel matrix sustained-release tablet containing loxoprofen sodium, in particular to a loxoprofen sodium matrix sustained-release tablet with a regulating layer, which can be sustained-release for 8 hours. Background technique [0002] Loxoprofen sodium belongs to phenylpropionic acid non-steroidal anti-inflammatory drugs and is used for the treatment of rheumatoid arthritis, osteoarthritis, low back pain, frozen shoulder, neck, shoulder and wrist syndrome, as well as after surgery, trauma and tooth extraction Analgesic and anti-inflammatory after treatment, antipyretic and analgesic for acute upper respiratory tract inflammation. Belongs to phenylpropionic acid non-steroidal anti-inflammatory drugs. [0003] At present, the clinically applied preparation is an ordinary quick-release preparation, the specification is 60 mg, and it is administered 3 times a day, which is likely to cause fluctuations in blood drug concentratio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/24A61K31/192A61K47/48A61P29/00
Inventor 姜庆伟刘全志杨文斌衣伟锋狄媛梁希葛振中张强
Owner 北京天衡药物研究院有限公司
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