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High-dissolubility fenofibrate tablet and preparation method thereof

A technology of fenofibrate and dissolution, which is applied in the direction of non-active ingredient medical preparations, pharmaceutical formulas, medical preparations containing active ingredients, etc., which can solve the problems of poor bioavailability, difficulty in controlling drug quality, and low solubility, etc. problems, to achieve better results, improve bioavailability, and improve solubility

Inactive Publication Date: 2017-09-05
SHANGHAI SINE WANXIANG PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] The present invention aims at the fact that fenofibrate is an insoluble drug with low solubility in water and is difficult to be absorbed by the body, resulting in poor bioavailability, and the traditional preparation method has many restrictions on the process and excipients, resulting in the problem that it is difficult to control the quality of the drug in production. Propose a kind of high dissolution rate fenofibrate tablet and preparation method thereof

Method used

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  • High-dissolubility fenofibrate tablet and preparation method thereof
  • High-dissolubility fenofibrate tablet and preparation method thereof
  • High-dissolubility fenofibrate tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Example 1 The preparation of high-dissolution fenofibrate tablets specifically includes the following steps:

[0050] (1) Preparation of clathrate

[0051] (a) Dissolving 90g of fenofibrate raw material in 250g of acetone, stirring until completely dissolved;

[0052] (b) Dissolve 290 g of sulfobutyl ether-β-cyclodextrin in 700 g of purified water, and stir until completely dissolved;

[0053] (c) Mix the above two solutions, stir evenly and ultrasonically disperse for 45min to prepare clathrate solution;

[0054] (d) Pass the clathrate solution through a 100-mesh sieve, and dry it in a spray dryer at a drying temperature of 70-72°C to obtain 380 g of clathrate;

[0055] (2) Tablet

[0056] (e) Pass 380g of clathrate, 30g of microcrystalline cellulose, 6g of lactose, 18g of povidone K30, 25g of sodium carboxymethyl starch, and 4g of magnesium stearate through a 30-mesh sieve;

[0057] (f) Weigh 1 / 4 of the inclusion compound of the prescription amount and mix it with...

Embodiment 2

[0059] Embodiment 2 The preparation of high-dissolution fenofibrate tablets specifically includes the following steps:

[0060] (1) Preparation of clathrate

[0061] (a) Dissolve 80 g of fenofibrate raw material in 220 g of acetone, and stir until completely dissolved;

[0062] (b) Dissolve 300 g of sulfobutyl ether-β-cyclodextrin in 650 g of purified water, and stir until completely dissolved;

[0063] (c) Mix the above two solutions, stir evenly and ultrasonically disperse for 50 minutes to prepare clathrate solution;

[0064] (d) Pass the clathrate solution through a 100-mesh sieve, and dry it in a spray dryer at a drying temperature of 75-77°C to obtain 380 g of clathrate;

[0065] (2) Tablet

[0066] (e) Pass 380g of clathrate, 32g of microcrystalline cellulose, 10g of lactose, 13g of povidone K30, 16g of sodium carboxymethyl starch, and 6g of magnesium stearate through a 30-mesh sieve;

[0067] (f) Weigh 2 / 4 of the inclusion compound of the prescription amount and mi...

Embodiment 3

[0069] Example 3 The preparation of high-dissolution fenofibrate tablets specifically includes the following steps:

[0070] (1) Preparation of clathrate

[0071] (a) Dissolving 120g of fenofibrate raw material in 550g of acetone, stirring until completely dissolved;

[0072] (b) Dissolve 340 g of sulfobutyl ether-β-cyclodextrin in 1300 g of purified water, and stir until completely dissolved;

[0073] (c) Mix the above two solutions, stir evenly and ultrasonically disperse for 50 minutes to prepare clathrate solution;

[0074] (d) Pass the clathrate solution through a 100-mesh sieve, and dry it in a spray dryer at a drying temperature of 75-77°C to obtain 460 g of clathrate;

[0075] (2) Tablet

[0076] (e) Pass 460g of clathrate, 40g of microcrystalline cellulose, 15g of lactose, 18g of povidone K30, 28.5g of sodium carboxymethyl starch, and 9g of magnesium stearate through a 30-mesh sieve;

[0077] (f) Weigh 2 / 4 of the inclusion compound of the prescribed amount and mix...

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Abstract

The invention discloses a high-dissolubility fenofibrate tablet and a preparation method thereof. The high-dissolubility fenofibrate tablet is prepared by coating a fenofibrate raw material with docosahexaenoic acid-beta-cyclodextrin, performing spray-drying and mixing and directly tabletting with auxiliary materials. By adopting the preparation method disclosed by the invention, the problems that by using a conventional method, the dissolubility is low and the bioavailability is poor as the mass of medicines is hard to control are solved; and compared with a conventional direct tabletting and wet-method pelleting process, the preparation method has the advantages that the dissolubility of medicines is effectively improved, the medicines are relatively good in dissolubility effect and the bioavailability is improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a solid oral preparation, in particular to a high-dissolution fenofibrate tablet and a preparation method thereof. Background technique [0002] Fenofibrate (Fenofibrate, FNB) is a clofibrate blood lipid regulator, its molecular formula is C20H21ClO4, its molecular weight is 360.84, its chemical name is 2-methyl-2-[4-(4-chlorobenzoyl)phenoxy Base] isopropyl propionate is a white or off-white crystalline powder, odorless and tasteless. It was first used clinically in 1975, mainly for the treatment of hyperlipidemia with unsatisfactory diet control therapy in adults. It is to reduce glycerol One of the first-choice drugs for triglycerides. Its effect of lowering triglycerides and mixed hyperlipidemia is more obvious than that of cholesterol. At the same time, it can also reduce blood uric acid levels. It also has a good effect on the treatment of type 2 diabetes and metabol...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/61A61K31/216A61P3/06
CPCA61K9/205A61K31/216
Inventor 姜丽莉高静董佳丽顾煜顾珽郭晶晶王平嵇栋梁
Owner SHANGHAI SINE WANXIANG PHARMA
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