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Fenofibrate delayed-release pellets, preparation method and application

A fenofibrate and pellet technology, which is applied in the field of fenofibrate pellets and preparation, can solve the problems that hinder the bioavailability of fenofibrate, the difficulty of fenofibrate delayed-release preparations, and the lack of fenofibrate. problems such as delayed-release preparations, to achieve the effect of high bioavailability, low process equipment requirements, and high yield

Active Publication Date: 2018-10-23
上海市生物医药技术研究院 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, the purpose of the present invention is to delay the release rate of fenofibrate, and the release of the delayed drug will hinder the improvement of fenofibrate bioavailability to a large extent, so the preparation of fenofibrate with high bioavailability Delayed-release formulations of fibrate are very difficult
In the open literature, there is no related report on fenofibrate delayed-release formulations

Method used

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  • Fenofibrate delayed-release pellets, preparation method and application
  • Fenofibrate delayed-release pellets, preparation method and application
  • Fenofibrate delayed-release pellets, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] The preparation of embodiment 1 loaded pill core

[0050] A prescription

[0051] Table 1:

[0052]

[0053]

[0054] *In the table, q.s. means appropriate amount.

[0055] B preparation process

[0056] Preparation of fenofibrate drug-loaded pellet core by fluidized bed powder drug loading method:

[0057] Fenofibrate bulk drug powder (Jiangsu Nhua Pharmaceutical Co., Ltd.) was micronized by a jet mill (Shanghai Huali Sofi Technology Co., Ltd., model: JGM-H100). The feed rate is 3kg / h, the working pressure is 8Mpa, and the fine powder obtained after continuous pulverization twice is measured by a laser particle size analyzer. The results showed that the drug particle size was 7.7 μm. Mix micronized fenofibrate powder and glidant evenly and add it into the feeder; use the blank pellet core as the mother core, and place it in the material tank of the tangential spray device; adjust the fluidization air volume to 100m 3 / h, the rotary speed of the turntable is...

Embodiment 2

[0058] The preparation of embodiment 2 delayed-release pellets

[0059] A prescription

[0060] Table 2:

[0061]

[0062]

[0063] *: PO: powder of copolymer of ethyl acrylate, methyl methacrylate and trimethylaminoethyl methacrylate (molar ratio 1:2:0.1) (purchased from Evonic Company)

[0064] 100: Particles of ethyl acrylate, methyl methacrylate and trimethylaminoethyl methacrylate chloride (molar ratio 1:2:0.1) copolymer (purchased from Evonic Company)

[0065] 100: particles of butyl methacrylate, dimethylaminoethyl methacrylate and methyl methacrylate (molar ratio 1:2:1) copolymer (purchased from Evonic Company)

[0066] PO: Powder of butyl methacrylate, dimethylaminoethyl methacrylate and methyl methacrylate (molar ratio 1:2:1) copolymer (purchased from Evonic Company)

[0067] B preparation process

[0068] a. Preparation of coating liquid: take respectively the plasticizer of the prescription amount shown in Table 2 and place it in a beaker, add eth...

Embodiment 3

[0071] Drug cumulative release test

[0072] (i) Method for determination of release rate:

[0073] Get an appropriate amount of fenofibrate delayed-release pellets (equivalent to fenofibrate 250mg), according to the release assay method (Chinese Pharmacopoeia 2010 edition appendix XD), with pH 4.0 aqueous solution 1000mL containing sodium lauryl sulfate (SLS) As a solvent, the rotating speed is 60 revolutions per minute. Operate according to the law. Take 2mL of the solution at 1, 4, 7, 10, and 18 hours respectively, centrifuge for 1min (10000rpm), and take the supernatant as the test solution.

[0074] In addition, accurately weigh an appropriate amount of fenofibrate reference substance, add 1 mL of methanol, ultrasonically dissolve, and dilute with a pH 4.0 aqueous solution containing sodium lauryl sulfate (SLS) to a 0.125 mg / mL solution as the reference substance solution.

[0075] Take 10 μL each of the test solution and the reference solution and inject them into the l...

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Abstract

The invention discloses a Fenofibrate delayed-release pellet high in bioavailability and a preparing method thereof. The pellet is composed of a carrier core and a single-layer controlled-release coating which covers the carrier core; the single-layer controlled-release coating accounts for 6% to 11% of total weight of the carrier core; based on the total weight of the carrier core; the carrier core comprises 60% to 85% of Fenofibrate, 5% to 35% of a hollow core, 1% to 5% of glue, and 1% to 5% of flow agent; based on the total weight of the single-layer controlled-release coating, the coating comprises 45% to 50% of copolymer of ethyl acrylate, methyl methacrylate, methacrylic chlorinated trimethylamine ethyl ester according to a molar ratio: 1:2:0.1, 9% to 12.5% of copolymer of butyl methacrylate, dimethylaminoethyl methacrylate and dimethylaminoethyl methacrylate according to a molar ratio: 1:2:1, 5% to 20% of plasticizer and 20% to 35% of anti-sticking agent. The Fenofibrate delayed-release pellet has the advantages that by the simple formulation of the quick-release coating, the unexpected delayed-release is achieved, and the bioavailability is higher.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a fenofibrate pellet, a preparation method and an application thereof. Background technique [0002] At present, the clinically available lipid-lowering drugs are divided into 5 categories: statins, fibrates, nicotinic acid, resins, cholesterol absorption inhibitors and others. Different types of drugs have different lipid-lowering effects due to their different chemical structures and mechanisms of action. [0003] Fenofibrate (fenofibrate) is the third generation of phenoxyacetic acid (i.e. fibrates) lipid-regulating drugs, the chemical name is 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl Isopropyl Propionate. Studies have shown that it can reduce total triglyceride (TG) by 25-59%, increase high-density lipoprotein cholesterol (HDL-C) by 1-34%, and reduce total cholesterol (TC) by 6%-27%. It has a remarkable effect in reducing TG and is currently the drug of...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/216A61P3/06
Inventor 李芳俸灵林郑昕曾佳朱芷涵潘峰余丽宁陈建兴
Owner 上海市生物医药技术研究院
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