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Bezafibrate sustained release tablet and preparation method thereof

A technology of bezafibrate and sustained-release tablets, which is applied in the direction of pharmaceutical formulas, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., can solve the problems of large doses and low solubility of bezafibrate, Achieve the effect of reducing side effects, lasting blood concentration and improving compliance

Active Publication Date: 2012-05-23
BEIJING YILING BIOENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Bezafibrate has low solubility and high dosage, so it is difficult to develop a once-daily sustained-release formulation of bezafibrate within a reasonable tablet weight range

Method used

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  • Bezafibrate sustained release tablet and preparation method thereof
  • Bezafibrate sustained release tablet and preparation method thereof
  • Bezafibrate sustained release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Tablet formula:

[0069] Bezafibrate API 400mg Silicon dioxide 5mg Sodium lauryl sulfate 30mg Propylmethylcellulose 100mg Spray-dried lactose 45mg Magnesium stearate 6mg

[0070] Coating film coating material:

[0071] 15% Opadry II in water.

[0072] Preparation method: first mix 400mg of bezafibrate raw material with 5mg of silicon dioxide and 30mg of sodium lauryl sulfate for 5 minutes, then add 100mg of direct pressure grade hydroxypropylmethylcellulose and 45mg of spray-dried lactose, and mix well Finally, after adding 6 mg of magnesium stearate and mixing for 2 minutes, tableting was performed to obtain tablet cores. Place the obtained tablet cores in the coating pan, spray 15% Opadry aqueous solution at a uniform speed at a spray speed of 5ml / min, tablet bed temperature of 40°C, and coating pan rotation speed of 45r / min until the coating weight increases 2%.

[0073] Technical effect: cumulative release of 23%, 45%, 63%, 77%, 87%, and 93% in 2, 4, 6, 8, 10, a...

Embodiment 2

[0075] Tablet core formula: bezafibrate 400mg polyoxyethylene 80mg ethyl cellulose 40mg polyethylene glycol 6000 30mg magnesium stearate 5mg

[0076] Coating film coating material:

[0077] Hydroxypropyl Methyl Cellulose 20% Titanium Dioxide 1% Triacetyl Glyceride 3% Ethanol 5% Water 71%.

[0078] Preparation:

[0079] Mix the prescribed amount of medicine with polyoxyethylene, ethyl cellulose, and polyethylene glycol evenly, granulate with 95% ethanol, granulate after drying, add the prescribed amount of magnesium stearate, mix evenly, compress into tablets, and obtain tablet cores . Place the obtained tablet cores in the coating pan, spray the above coating solution at a uniform speed at a spray speed of 5ml / min, a tablet bed temperature of 40°C, and a coating pan rotation speed of 45r / min until the coating weight gain is 3 %.

[0080] Technical effect: cumulative release of 24%, 45%, 64%, 82%, 92%, and 93% in 2, 4, 6, 8, 10, and 12 hours respectively, see the in vitro r...

Embodiment 3

[0082] Tablet core formula: bezafibrate 400mg hydroxypropyl methylcellulose 60mg pregelatinized starch 22mg lactose 30mg sodium lauryl sulfate 26mg silicon dioxide 6mg talcum powder 3mg.

[0083] Coating film coating material:

[0084] none

[0085] Preparation:

[0086] Mix the prescription amount of bezafibrate raw material with hydroxypropyl methylcellulose, pregelatinized starch, lactose, and sodium lauryl sulfate evenly, then granulate with 5% hydroxypropylmethylcellulose E5 aqueous solution, After drying, granulate, add the prescribed amount of talcum powder and silicon dioxide, mix evenly, and press into tablets to obtain tablet cores.

[0087] Technical effect: Cumulative release of 21%, 42%, 60%, 75%, 88%, and 98% in 2, 4, 6, 8, 10, and 12 hours respectively, see the in vitro release curve image 3 .

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Abstract

The invention provides a bezafibrate sustained release tablet, comprising a sustained release tablet core and a film coated on the tablet core. The bezafibrate sustained release tablet comprises, by weight, 400 parts of bezafibrate, 60-120 parts of skeletal material and 50-150 parts of accessory facilitating release of drug; and the coating film accounts for 1-5wt% of the tablet. The bezafibrate sustained release tablet of the invention can effectively adjust release rate of the medicament and obtain stationary and lasting effective plasma concentration, so as to reduce side-effect and drug administration frequency; and absorption of medicament is not influenced by food intake and internal environment, so as to increase compliance of a patient. Therefore, the bezafibrate sustained release tablet can be widely applied to prevention and treatment of disease like hyperlipidemia.

Description

technical field [0001] The benzene invention relates to a bezafibrate sustained-release tablet and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] There are many types of lipid-lowering drugs currently in clinical use, but there are mainly two categories that are more commonly used: statins and fibrates. Statins lipid-lowering drugs are the first choice for cholesterol-lowering treatment, their effects on triglyceride and HDL-C are far less obvious than those on cholesterol, and fibrate lipid-lowering drugs have been clinically used for a longer time than statins, Its effect of lowering triglycerides is more obvious than that of statins. For its obvious effect of raising HDL-C and lowering TG levels, fibrates can make up for the deficiency of statins. According to literature reports, bezafibrate can also inhibit the expression of inflammatory cytokines in the blood circulation by adjusting dyslipid...

Claims

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Application Information

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IPC IPC(8): A61K31/192A61K9/22A61K9/36A61K47/38A61P3/06
Inventor 孙光美田书彦贾卫东李向军安军永王超
Owner BEIJING YILING BIOENG
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