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Preparation method of high-purity nateglinide capsule

A nateglinide and high-purity technology, applied in the field of preparation of high-purity nateglinide capsules, can solve the problems of unstable quality, low bioavailability, poor dissolution rate, etc. The effect of uniform dispersion and improved dissolution

Pending Publication Date: 2021-12-07
HAINAN HAILING CHEMIPHARMA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The traditional preparation method uses steam as a means of temperature control, which is more likely to generate multiple crystal forms, isomers, and other impurities of B, H, and S. The resulting product has low purity and unstable quality. However, the patent CN109369443A provides A new preparation method of nateglinide H crystal form, its dissolution rate is not good; patent CN102813636B, nateglinide tablet and its preparation method, its dissolution rate is poor during storage, difficult to dissolve in water, oral bioavailability low degree

Method used

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  • Preparation method of high-purity nateglinide capsule
  • Preparation method of high-purity nateglinide capsule

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Embodiment 1

[0026] A preparation method of high-purity nateglinide capsules: comprising the following steps:

[0027] Preparation of S1 and H-type nateglinide: after condensing trans-4-isopropylcyclohexanecarbonyl chloride with D-phenylalanine, the crude crystal of nateglinide type B was obtained, and then at 15°C Perform low-temperature pulverization to obtain microparticle crystal seeds, add a crystallizing agent and then heat to 35 ° C to guide crystallization. The crystallizing agent is mixed with water-soluble phenolic and nicotinamide with a mass ratio of 0.3:1, and water with a mass-to-volume ratio of 2:1 is added to obtain crystals. agent to obtain white crystals of H-type nateglinide;

[0028] S2, the preparation of nanoemulsion: nanoemulsion comprises the following raw materials by weight: 13 parts of H-type nateglinide, 20 parts of triethanolamine, 10 parts of polysorbate 80, 3 parts of camellia oil, 2 parts of cyclohexyl propylene glycol, 2 parts of cross-linked carboxyl 1 pa...

Embodiment 2

[0032] A preparation method of high-purity nateglinide capsules: comprising the following steps:

[0033] Preparation of S1 and H-type nateglinide: after condensing trans-4-isopropylcyclohexanecarbonyl chloride with D-phenylalanine, a crude crystal of nateglinide type B is obtained, which is then pulverized at low temperature to obtain Microparticle seed crystals, add crystallization agent and then heat to 40 °C to guide crystallization to obtain H-type nateglinide white crystals. :1 water;

[0034] S2. Preparation of nanoemulsion: The nanoemulsion includes the following raw materials in parts by weight: 30 parts of H-type nateglinide, 25 parts of triethanolamine, 10 to 15 parts of polysorbate, 3 to 8 parts of castor oil, and 4 parts of polysorbate 400 , 1-3 parts of cross-linked polyvinylpyrrolidone, 1.5 parts of cationic polyacrylamide emulsion;

[0035] The preparation method of the nanoemulsion: dissolving the H-type nateglinide white crystal obtained by S1 in an alcohol...

Embodiment 3

[0038] A preparation method of high-purity nateglinide capsules: comprising the following steps:

[0039] Preparation of S1 and H-type nateglinide: after condensing trans-4-isopropylcyclohexanecarbonyl chloride with D-phenylalanine, the crude crystal of nateglinide type B was obtained, and then at 18°C Perform low-temperature pulverization to obtain microparticle seed crystals, add a crystallizing agent and then heat to 38 ° C to guide crystallization to obtain white crystals of H-type nateglinide. Water with a volume ratio of 3:1;

[0040] S2, the preparation of nanoemulsion: nanoemulsion comprises the following raw materials by weight: 18 parts of H-type nateglinide, 23 parts of n-propyl ester, 12 parts of polysorbate 60, 5 parts of olive oil, 3 parts of polyethylene glycol, 2 parts of copolyvidone, 1.0 part of acrylic acid;

[0041] The preparation method of the nanoemulsion: dissolving the H-type nateglinide white crystal obtained from S1 in an alcohol solvent, adding n-...

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Abstract

The invention provides a preparation method of a high-purity nateglinide capsule, and the preparation method comprises the following steps: S1, preparation of H-type nateglinide, S2, preparation of a nano-emulsion, and S3, preparation of the nateglinide capsule. Through combination and proportioning of the raw materials, a diluent, a cosolvent, an oil phase, an emulsifier, a disintegrating agent, a coagulant and a dissolution promoting substance are reasonably selected, the substance dissolution is promoted, the dissolution rate of nateglinide is improved, the medicine is uniformly dispersed and is stably absorbed by a human body, and the bioavailability is improved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of high-purity nateglinide capsules. Background technique [0002] Nateglinide (English name: Nateglinide), the content is off-white; it is a D-phenylalanine derivative, which belongs to the non-sulfonylurea hypoglycemic drug, and its mechanism of action is mainly through the interaction with sulfonylurea on islet B cells. Combined with urea receptors, it blocks the opening of ATP-sensitive potassium channels in pancreatic islet cells, leading to depolarization of the cell membrane, causing the opening of calcium channels and promoting insulin secretion; it is a new generation of hypoglycemic drugs with amino acid structure, and is the first in the treatment of type 2 diabetes. It is an amino acid derivative that promotes insulin secretion. It has a unique structure and is superior to other oral hypoglycemic agents in terms of chemistry and pharmacology. It ...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K9/107A61K47/44A61K47/38A61K47/32A61K31/198A61P3/10
CPCA61K9/5015A61K9/5026A61K9/5047A61K9/1075A61K31/198A61P3/10
Inventor 蔡亲
Owner HAINAN HAILING CHEMIPHARMA CORP
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