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Preparation method of medical composition

A composition and drug technology, applied in the field of medicine, can solve the problems of good pharmaceutical composition products, difficult to obtain dissolution and release properties, etc.

Active Publication Date: 2019-09-17
WUHAN LL SCI & TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] However, the applicant found in further formulation process research that when neutral endopeptidase and the compound shown in formula (I) are used to prepare a pharmaceutical composition using an existing process such as a fluidized bed process, it is difficult to obtain Pharmaceutical composition products with good dissolution and release performance

Method used

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  • Preparation method of medical composition
  • Preparation method of medical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0151] Embodiment 1 prepares the first active component

[0152] Add Shakubiqu into acetone solvent, stir at room temperature, cool to 0-10°C, add a little excess of concentrated ammonia water dropwise, after the dropwise addition, continue stirring for 4 hours, filter, wash with acetone, and dry in vacuo to obtain AHU377 ammonium salt with a purity of Greater than 99.5%, MS: m / z=412.3 (M+H) + .

[0153] The preparation of AHU 377K is similar to this process, replacing concentrated ammonia with potassium hydroxide.

Embodiment 2

[0154] Embodiment 2 prepares the second active component: the preparation of compound 1K

[0155]

[0156] Dissolve compound 1 (1.0g) in dichloromethane (5ml), stir at room temperature to form a solution, add potassium phthalimide (0.27g) to the solution, keep warm for 4h, cool to -50°C, filter , and the solvent was spin-dried to obtain a solid compound 1K (amorphous).

[0157] Melting point: 135-145°C.

[0158] MS / HRMS m / z: 717[M+H] + ;677[M-K] - .

[0159] 1 H-NMR (400MHz, DMSO-d 6 )δ: 1.44(t, 3H), 1.46(t, 3H), 2.38(s, 3H), 2.41(s, 3H), 2.44(s, 3H), 4.64(q, 2H), 5.29(d, 1H ), 5.32(d, 1H), 5.52(d, 1H), 5.56(d, 1H), 6.86(q, 1H), 6.90(d, 2H), 7.18(m, 2H), 7.22(d, 2H) , 7.33 (m, 1H), 7.36 (m, 1H), 7.46 (d, 1H), 7.52 (dd, 1H), 7.75 (d, 1H).

[0160] The study found that: the composition (excluding preparation auxiliary materials) consisting only of the products of Examples 1 and 2 (100mg: 50mg), at a relative humidity of 92.5% and a temperature of 25°C, the moisture abso...

Embodiment 3

[0162]

[0163]

[0164] Weigh the compound 1K, AHU 377 ammonium salt, mannitol, microcrystalline cellulose, colloidal silicon dioxide, and crospovidone in the first auxiliary material, mix them through a 40-mesh sieve and put them into the mixer, and mix them for 6 minutes. Then add the first auxiliary material magnesium stearate in the added part, and mix for 3 minutes.

[0165] A dry granulator was used to prepare granules, and the specific granulation conditions were as follows: the roll width was 25mm, the roll diameter was 200mm, and the roll gap was 2mm; the feeding speed was 34rpm, the pressing wheel speed was 3rpm, and the granulation speed was 550rpm.

[0166] Take by weighing the colloidal silicon dioxide in the second auxiliary material of recipe quantity, after crossing 40 mesh sieves, mix with crospovidone, magnesium stearate (additional part) and the above-mentioned granules in the second auxiliary material, drop into mixer and mix for 3 Minutes, a blend o...

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Abstract

The invention belongs to the field of medicines, and particularly relates to a preparation method of a medical composition. The preparation technology can effectively solve the problem that the medical composition being good in properties cannot be prepared through a conventional technology, so that the problem that the preparation cannot be disintegrated is solved. A solid preparation can be promoted to disintegrate, and medicines are released. Through the adoption of the method, the flowing properties of materials are effectively improved, and the problem of decomposition of active components caused by high-temperature drying in the conventional technology can be solved. The preparation technology of the preparation is simple, and industrial mass production is easy to realize.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a preparation method of a pharmaceutical composition. Background technique [0002] Cardiovascular disease, also known as circulatory system disease, refers to a series of diseases involving the circulatory system. The circulatory system mainly includes the heart and blood vessels (arteries, veins, capillaries). According to statistics, cardiovascular disease is the number one cause of death in the world, and more people die from cardiovascular disease than any other cause of death every year. Common cardiovascular diseases include: hypertension, heart failure, coronary heart disease, heart disease, atherosclerosis, angina, left ventricular dysfunction, hypertrophic cardiomyopathy, diabetic cardiomyopathy, supraventricular and ventricular arrhythmias, atrial Fibrillation, cardiac fibrosis, atrial flutter, deleterious vascular remodeling, myocardial infarction and its sequela...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4245A61K31/497A61K31/216A61K45/06A61P9/12A61P9/04A61P9/10A61P3/10A61P9/06A61P9/00
CPCA61K31/4245A61K31/497A61K31/216A61K45/06A61P9/12A61P9/04A61P9/10A61P3/10A61P9/06A61P9/00A61K2300/00A61K31/501A61K31/4164A61K31/192A61K31/197
Inventor 胡晓婧钱丽娜张志超余峥嵘陈永凯冯伟祁雯雯王朝东
Owner WUHAN LL SCI & TECH DEV
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