Bezafibrate controlled release formulation and preparation method thereof

A technology of bezafibrate and controlled-release preparations, which is applied in the field of pharmacy, can solve the problems that the drug dissolution rate cannot reach the expected effect, the drug effect is not long-lasting, and it is not convenient for patients to take it. It is easy to produce industrialization and standardization, Fewer gastrointestinal side effects and long-lasting effects

Active Publication Date: 2009-01-14
TIANJIN TASLY LIAONING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This is inconvenient for patients to take, and the curative effect of the drug is not long-lasting, and the ideal effect of slow and long-acting drug release will not be achieved.
[0004] Furthermore, the dissolution rate of the drug is related to the drug excipients and the particle size of the particles, especially for drugs with poor water solubility, if the excipients are not properly selected, the dissolution rate of the drug will not reach the expected effect

Method used

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  • Bezafibrate controlled release formulation and preparation method thereof
  • Bezafibrate controlled release formulation and preparation method thereof

Examples

Experimental program
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Effect test

experiment example 1

[0043] Tablet core formula:

[0044] Benzafib 40g

[0045] Sodium carbonate 2g

[0046] Sodium lauryl sulfate 5g

[0047] Polyoxyethylene N80 8g

[0048] Sodium chloride 10g

[0049] Magnesium stearate 0.6g

[0050] Coating liquid formula:

[0051] Cellulose acetate 15g

[0052] Polyethylene glycol 4000 5g

[0053] Acetone 500ml

[0054] Water 30ml

[0055] Preparation process: fully mix the bezafibrate, sodium carbonate, sodium lauryl sulfate, polyoxyethylene N80 and sodium chloride in the formula, add 95% ethanol to make soft material, and granulate on a 20-mesh sieve. Dry at ℃, size with 16 mesh sieve, add proper amount of magnesium stearate, mix well, and compress. The tablet cores are coated with the coating liquid, and the weight of each tablet is about 35mg. Place the coated tablet in a drying box at 40°C for 8 hours and then punch a 0.8μm hole on each side of the tablet.

experiment example 2

[0057] Tablet core formula:

[0058] The first layer: bezafibrate 30g

[0059] Sodium carbonate 2g

[0060] Sodium lauryl sulfate 3g

[0061] Sodium chloride 8g

[0062] Hypromellose K4M amount

[0063] Magnesium stearate 0.4g

[0064] The second layer: bezafibrate 10g

[0065] Polyoxyethylene N80 8g

[0066] Sodium chloride 2g

[0067] Magnesium stearate 0.2g

[0068] Coating liquid formula:

[0069] Cellulose acetate 15g

[0070] Polyethylene glycol 4000 7g

[0071] Acetone 500ml

[0072] Water 30ml

[0073] Preparation process: Mix the bezafibrate, sodium carbonate, sodium lauryl sulfate and sodium chloride in the first layer of the formula fully and uniformly, add 2% hypromellose solution to make soft material, 20 Mesh granulation, drying at 45℃, 16 mesh granules, then add appropriate amount of magnesium stearate, mix well, and take the proportion of bezafibrate, polyoxyethylene N80 and sodium chloride in the second layer Mix well, add 95% ethanol to make soft material, granul...

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Abstract

The invention relates to a controlled release preparation of bezafibrate. The controlled release preparation of bezafibrate contains a bezafibrate core and a semi-permeability film coating. The outer layer of the semi-permeability film coating is provided with a pore. The semi-permeability film coating is made of following components by mass proportion: 60 to 80 percent of polymer materials of the semi-permeability film coating and 20 to 40 percent of plasticizer. The polymer materials of the semi-permeability film coating are made by the mixture of one or more than one of cellulose acetate, ethyl cellulose, cellulose propionate, polycarbonate, polythene and PVA. The controlled release preparation of bezafibrate overcomes the 'peak valley' phenomenon of blood concentration existing in a common preparation and only needs to be taken once per day with the little adverse effect of a gastrointestinal tract, so a curative effect is ensured and patient compliance is also improved. The invention also relates to a preparation method of the controlled release preparation of bezafibrate.

Description

Technical field [0001] The invention relates to the field of pharmacology, in particular to a controlled-release preparation of bezafibrate medicine and a preparation method thereof. Background technique [0002] Bezafibrate is a blood lipid regulator of clofibrate derivatives, which can lower blood low-density lipoprotein and cholesterol. [0003] Solid preparations need to undergo a process of disintegration, dissolution, and absorption, which is unfavorable for the effectiveness of poorly soluble drugs. However, bezafibrate is a poorly water-soluble drug, which will dissolve limited in the digestive tract, which affects the patient's absorption of the effective ingredients of bezafibrate, and ultimately leads to a decline in efficacy. Moreover, the blood concentration of bezafibrate in the conventional dosage form reaches its peak at about 2 to 3 hours after taking the drug, and then the blood concentration drops rapidly. The patient needs to take bezafibrate again within 5 to...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/195A61K9/24A61K9/52A61K47/38A61K47/32A61K47/34A61P3/06A61K47/10A61K47/26
Inventor 徐立元
Owner TIANJIN TASLY LIAONING PHARMA
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