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Solid preparation containing insoluble thienopyridine composition and preparation method

A technology for solid preparations and compositions, which is applied in the field of solid preparations and preparations containing insoluble thienopyridine compositions, can solve the problems of reduced bioavailability and slow dissolution speed, and achieve improved dissolution rate, low production cost, and preparation The effect of simple process

Active Publication Date: 2020-06-09
CHENGDU SHIBEIKANG BIOLOGICAL MEDICINE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the process of rapid disintegration and absorption of solid preparations, the rate-limiting step of drug absorption is often the dissolution rate of the drug, especially for poorly soluble drugs, the slow dissolution rate will lead to a decrease in bioavailability

Method used

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  • Solid preparation containing insoluble thienopyridine composition and preparation method
  • Solid preparation containing insoluble thienopyridine composition and preparation method
  • Solid preparation containing insoluble thienopyridine composition and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] This embodiment discloses the preparation method of the compound of formula II, specifically:

[0041] N-Oxo-(S)-2-(2-chlorophenyl)-2-((S)-2-oxo-2,6,7,7a-tetrahydrothiopheno[3,2-c]pyridine Synthesis of -5(4H)yl)methyl Acetate

[0042] Step 1. Resolution of the racemic product

[0043]

[0044] Referring to the patent CN104245707A, after we synthesized the structure of the SMX compound, the obtained racemic product 4.6gSMX was resolved by preparing a chiral column to obtain two relatively pure corresponding chiral isomers SMX-1 and SMX-2, 1.24g and 1.51g respectively. g. (Yield 59.8%) LC-MS (ESI) [M+H + ] + =338.8(M+H + ) is consistent with the structure.

[0045] The preparation of step 2 formula II compound:

[0046]

[0047] Put 1.51g of SMX-1 and 10mL of glacial acetic acid into a 50mL three-necked flask at room temperature, add 1ml of hydrogen peroxide dropwise in an ice bath, raise the temperature to 80°C for 2 hours after the addition, and monitor the...

Embodiment 2

[0048] Embodiment 2: the research of the different ratio of formula II compound and formula I compound

[0049] In this example, the pure products of the compound of formula I and compound of formula II in the thienopyridine composition with different proportions were added to conduct research to investigate their quality stability. Specifically: using the same amount of thienopyridine composition and auxiliary materials, only the ratio of the formula II compound to the formula I compound is different, and the same preparation method is used to make tablets. The content of the related substances was determined on the tablet at 0 days and accelerated at 6 months. Its prescription composition is calculated by 1000 tablets, as shown in Table 1:

[0050] Table 1 Prescription Composition Table 1

[0051]

[0052]

[0053] The preparation method is:

[0054]1. Weigh the pure products of the compound of formula I and the compound of formula II respectively; after mixing even...

Embodiment 3

[0066] Embodiment 3: control the ratio of formula II compound and formula I compound, the preparation method of refinement

[0067] According to the method disclosed in Example 2 of CN 104245707, prepare the compound crude product (containing II compound) synthesized and placed for a period of time shown in I, get 1.0g of the compound crude product shown in formula I and add in a 50mL eggplant-shaped bottle, add 30mL tetrahydrofuran, and heat up to Stir and dissolve at 60°C, basically dissolve, filter while hot, stir the filtrate in a 50mL beaker, and slowly cool down to room temperature, stir overnight to crystallize, and dry to obtain 0.50g of the finished compound. The mass ratio of the compound II to the compound of formula I in the finished product If it is less than or equal to 0.5:100, it can be refined repeatedly, so as to further reduce the mass ratio of the compound II to the compound of formula I.

[0068] The assay method of formula II compound and formula I compou...

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Abstract

The invention discloses a solid preparation containing an insoluble thienopyridine composition and a preparation method. The preparation is low in impurity content and can be rapidly dissolved out. According to the solid preparation containing the insoluble thienopyridine composition, disclosed by the invention, the composition comprises a compound with a structure represented by a formula I and acompound with a structure represented by a formula II, wherein a mass ratio of the compound II to the compound I is smaller than or equal to 1: 100.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a solid preparation containing an insoluble thienopyridine composition and a preparation method. Background technique [0002] The compound whose structure is shown in formula I, its chemical name is: (S)-2-(2-chlorophenyl)-2-((S)-2-oxo-2,6,7,7a-tetrahydro Thieno[3,2-c]pyridin-5(4H)yl)methyl acetate. [0003] [0004] The compound of formula I is the metabolite of clopidogrel in human body. Clopidogrel is the first-line drug for the prevention and treatment of heart, brain and other arterial circulation disorders caused by high platelet aggregation. However, there are significant individual differences in the efficacy of clopidogrel, especially in Asians, that is, clopidogrel resistance (CPGR). Recent studies have shown that the cause of CPGR is due to the differences in the activity of CYP enzymes in the liver of individuals. The specific ma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/48A61K9/16A61K31/4365A61K47/38A61P7/02
CPCA61K9/2059A61K9/2095A61K9/4866A61K9/1652A61K31/4365A61P7/02A61K2300/00Y02A50/30
Inventor 牟霞杨茂廷谭少军江杰陆瑶
Owner CHENGDU SHIBEIKANG BIOLOGICAL MEDICINE TECH CO LTD
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