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Epalrestat sustained release preparation and preparation method thereof

A sustained-release preparation, the technology of epalrestat, is used in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc. problems, to increase compliance, avoid drug burst effects, and reduce the incidence of adverse reactions

Inactive Publication Date: 2020-12-29
南京康川济医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] CN201510313451.5 provides a kind of epalrestat enteric-coated sustained-release tablet, adopts sustained-release matrix material to prepare single-layer sustained-release tablet core and carries out enteric coating, also has sustained-release effect, but this single-layer sustained-release tablet core There is still a risk of being damaged by the environment of the gastrointestinal tract or accidentally bitten by the patient, leading to the risk of sudden release of the drug

Method used

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  • Epalrestat sustained release preparation and preparation method thereof
  • Epalrestat sustained release preparation and preparation method thereof
  • Epalrestat sustained release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] (1) Drug-containing sustained-release pellet core (per 1000 capsules)

[0040]

[0041]

[0042] (2) Isolation coating layer (per 1000 capsules)

[0043] Opadry YS-1-7003 17.1g

[0044] Purified water 154g

[0045] The coating weight gain was about 3%.

[0046] (3) Enteric coating layer (per 1000 capsules)

[0047] Sureteric 58.56g

[0048] Antifoam emulsion 0.19g

[0049] Purified water 331g

[0050] The coating weight gain was about 10%.

[0051] (4) Protective coating layer (per 1000 capsules)

[0052] Opadry YS-1-7003 19.3g

[0053] Purified water 174g

[0054] The coating weight gain was about 3%.

Embodiment 1

[0055] Embodiment 1——Example 10 Epalrestat sustained-release preparation preparation process:

[0056] The epalrestat raw material is micronized, particle size D 90 About 50μm, pass the auxiliary material through a 40-mesh sieve;

[0057] Preparation of soft material: weigh epalrestat, filler, release regulator, and sustained-release framework material according to the prescription amount, place them in a wet granulator and mix them evenly, spray an appropriate amount of binder aqueous solution with a certain concentration, and open Stirring knife for preparing soft materials;

[0058] Preparation of pellets: put the above-mentioned soft materials in an extrusion spheronizer to prepare pellets. Set the sieve aperture to 0.8 mm, the extrusion speed to 10-25 rpm, the rounding speed to 500-1700 rpm, and the rounding time to 2-5 minutes. Sieve, take 18-40 mesh pellets, and dry in a fluidized bed, set the drying temperature at 60°C, and dry for 20-25 minutes;

[0059] Fluidized...

Embodiment 2

[0066] Drug-containing sustained-release pellet core (per 1000 capsules)

[0067]

[0068] Hypromellose E5 (release modifier) ​​15g

[0069] Lactose G200 (filler) 90g

[0070] Microcrystalline Cellulose PH101 (Filler) 90g

[0071] Povidone K30 (adhesive) 8g

[0072] Appropriate amount of purified water

[0073] Other auxiliary materials category and dosage and preparation process are all the same as in Example 1.

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Abstract

The invention belongs to the field of pharmaceutical preparations, and provides an epalrestat sustained release preparation and a preparation method thereof. The epalrestat sustained release preparation is composed of 64%-92% of drug-containing sustained-release pellets, 1.0%-8.0% of a gastric-soluble isolation coating layer, 5.0%-20% of an enteric-soluble coating layer, and 2.0%-8.0% of a protective coating layer. The epalrestat sustained release preparation disclosed by the invention can effectively avoid the peak valley phenomenon of the blood concentration of a common preparation, reducesthe medicine taking frequency, reduces the occurrence rate of adverse reactions, and increases the compliance of a patient; and can avoid a possible drug burst release effect of a monobasic sustainedrelease preparation, reduces the toxicity and side effects of the drug, and further ensures the safety of clinical medication. The selected auxiliary materials are common, the preparation process is simple, the technical difficulty is low, the industrial mass production is easy to realize, and the market potential is large.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an epalrestat sustained-release preparation and a preparation method thereof. Background technique [0002] Epalrestat (Epalrestat) is a phenylpropenylthiazolidine carboxylic acid, structurally a carboxylic acid derivative, currently the only commercially available non-competitive ARIs for the treatment of diabetic neuropathy. Epalrestat was first found to inhibit AR, which may improve the delayed complications of diabetes. It was later prepared into oral preparations during the development process and was first listed in Japan in 1992. The trade name is (ONO-2235), for the treatment of neuropathy and retinopathy. Since its launch, epalrestat, as a drug for the treatment of diabetic neuropathy, can significantly improve the symptoms of neuropathy and improve the quality of life of patients. It has remarkable clinical efficacy and fewer side effects. It can be used alo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/60A61K47/38A61K31/426A61P3/10A61P25/00
CPCA61K9/5047A61K9/5073A61K31/426A61P3/10A61P25/00
Inventor 尹来生朱春莉陈金脱
Owner 南京康川济医药科技有限公司
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