Skeleton Diclofenac Potassium Sustained-release Pellet Capsules and Production Process

A technology of diclofenac potassium and sustained-release pellets, applied in the field of medicine, can solve the problems of unstable blood drug concentration, toxic and side effects, etc., and achieve the effects of lasting effective blood drug concentration, good reproducibility and excellent release curve

Active Publication Date: 2011-12-07
ZHEJIANG JINHUA CONBA BIO PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the oral dosage form of this drug in the domestic and foreign markets is mainly diclofenac potassium tablets, and the usage and dosage are 100-150 mg (calculated as diclofenac potassium) per day, divided into 2-3 times, and in severe cases it can reach 200 mg / day (4 tablets / day) ), frequent medication many times a day has brought great inconvenience to patients, and the blood drug concentration is not stable, and there are peaks and valleys, and high doses of medication have produced great toxic and side effects

Method used

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  • Skeleton Diclofenac Potassium Sustained-release Pellet Capsules and Production Process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 Production of 1000 skeleton-type diclofenac potassium sustained-release pellets and capsules (75 mg / grain in terms of diclofenac potassium), the used raw materials, adjuvant materials and their weight ratios are:

[0033] Diclofenac Potassium 75g

[0034] Carbomer 974P 12g

[0035] Microcrystalline Cellulose 192g

[0036] Sodium sulfite 3g

[0037] Calcium chloride 3g

[0038] Tween 80 15g

[0039] Its preparation method is as follows:

[0040] (1) Mix 75g of the main drug diclofenac potassium, 12g of the hydrophilic gel skeleton agent carbomer 974P and 192g of the diluent microcrystalline cellulose to obtain a solid powder mixture; mix 3g of the antioxidant sodium sulfite and 3g of the anti-sticking agent calcium chloride and absorption enhancer Tween-80 15g were respectively dissolved in wetting agent water to prepare solutions with a mass volume ratio of 6%, 6% and 15% respectively; the above soluti...

Embodiment 2

[0044] Embodiment 2 Production of skeleton type diclofenac potassium sustained-release pellet capsules 1000 (75mg / grain in terms of diclofenac potassium), used raw materials, adjuvant materials and weight ratio thereof are:

[0045] Diclofenac Potassium 75g

[0046] Carbomer 974P 9g

[0047] Microcrystalline Cellulose 180g

[0048] Sodium sulfite 3g

[0049] Calcium chloride 6g

[0050] Tween 80 15g

[0051] Its preparation method is as follows:

[0052] (1) Mix 75g of main drug diclofenac potassium, 21g of hydrophilic gel skeleton agent carbomer 974P and 180g of diluent microcrystalline cellulose; mix 3g of antioxidant sodium sulfite, 6g of anti-sticking agent calcium chloride and absorption promoter Tween-80 15g was dissolved in water respectively to prepare solutions with mass volume ratios of 6%, 12% and 15% respectively; the above solutions were respectively added to the above solid powder mixture, and stirred ev...

Embodiment 3

[0056] Embodiment 3 Production skeleton type diclofenac potassium sustained-release pellet capsule 1000 (75mg / grain in terms of diclofenac potassium), used bulk drug, auxiliary material and its weight ratio are:

[0057] Main ingredient Diclofenac Potassium 75g

[0058] Hydrophilic gel matrix agent Carbomer 974P 9g

[0059] Insoluble matrix ethyl cellulose 45g

[0060] Thinner Microcrystalline Cellulose 147g

[0061] Antioxidant Sodium Sulfite 3g

[0062] Anti-sticking agent calcium chloride 6g

[0063] Absorption enhancer Tween 80 15g

[0064] The release rate of the above-mentioned skeleton-type diclofenac potassium sustained-release pellets and capsules was measured by the slurry method, the rotation speed was 100 rpm, the phosphate buffer solution with pH 6.2 was used as the dissolution medium, and the water temperature was 37°C. According to the measurement, 32% of 0.5h dissolution, 53% of 2h dissolution, 8h dissolution of more than 70%.

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Abstract

The invention relates to matrix diclofenac potassium sustained-release pellet capsules and a production process thereof. The matrix diclofenac potassium sustained-release pellet capsules are prepared by filling matrix diclofenac potassium sustained-release pellets into gastric-soluble capsule shells. The matrix diclofenac potassium sustained-release pellets are prepared in one step by extrusion and rolling. The formula of the matrix diclofenac potassium sustained-release pellets comprises basic remedy diclofenac potassium 10-50%, matrix agent 1-20%, diluent 20-80%, antioxidant 0.1-5%, antisticking agent 0.1-5%, absorption promoting agent 1-10%, and any available wetting agent as balance, wherein the matrix agent is hydrophilic gel matrix agent, or hydrophilic gel matrix agent and erodiblematrix agent, or hydrophilic gel matrix agent and insoluble matrix agent. The matrix diclofenac potassium sustained-release pellet capsules provided by the invention have the advantages of high bioavailability, long in vivo holdup time, regular drug release, good in vivo (Beagle dogs) absorption and reproducibility, good sustained-release effect, simple production process, short production period, and no flying of dust during production, and are suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a sustained-release pharmaceutical preparation, in particular to a skeleton-type diclofenac potassium sustained-release pellet capsule and a production process thereof. Background technique [0002] Diclofenac potassium is a third-generation potent anthranilic acid non-steroidal anti-inflammatory analgesic. Its mechanism of action is to inhibit the activity of cyclooxygenase, thereby blocking the transformation of arachidonic acid into prostaglandins. At the same time, it can also promote the combination of arachidonic acid and triglyceride (triacylglycerol), reduce the concentration of free arachidonic acid in cells, and indirectly inhibit the synthesis of leukotrienes. At present, the oral dosage form of this drug in the domestic and foreign markets is mainly diclofenac potassium tablets, and the usage and dosage are 100-150 mg (calculated as diclofenac potassium) per day, divide...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/52A61K31/196A61K47/44A61K47/38A61K47/34A61K47/32A61K47/30A61P29/00
Inventor 金庆平付纪军唐星余斌
Owner ZHEJIANG JINHUA CONBA BIO PHARM CO LTD
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