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Medicinal composition of pharmaceutically-acceptable salt containing clopidogrel and preparation method thereof

A composition and pharmaceutical technology, applied in the field of medicine, can solve problems such as product quality and clinical curative effect, and achieve the effects of solving crystal form and electrostatic problems, shortening peak time, and improving bioavailability

Inactive Publication Date: 2012-10-03
SHIJIAZHUANG SAIRUI MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, micro-powdered silica gel brings new challenges to the dust prevention and delamination prevention of material mixing and tableting process.
In addition, the current clopidogrel sulfide tablet stipulates that except for the main crystal form, the amount of other crystal forms shall not exceed 5%. Therefore, no matter how the production process is controlled, the phenomenon of crystal transformation will still occur during production or storage, thus Have a significant impact on product quality and clinical efficacy

Method used

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  • Medicinal composition of pharmaceutically-acceptable salt containing clopidogrel and preparation method thereof
  • Medicinal composition of pharmaceutically-acceptable salt containing clopidogrel and preparation method thereof
  • Medicinal composition of pharmaceutically-acceptable salt containing clopidogrel and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] The preparation of embodiment 1 clopidogrel thiohydrogen soft capsules

[0056] The composition of the prescription is as follows: (g)

[0057] Clopidogrel Sulfuric Acid 24.46

[0058] PEG400 842

[0059] 1,2-Propanediol 150

[0060] TW80 8.5

[0061] A total of 1024.96g, made into 1000 soft capsules.

[0062] Preparation process: Weigh the prescribed amount of PEG400, 1,2-propanediol, TW80, add to the dissolving tank, stir and mix evenly at 45-70°C; pass the drug through a 60-mesh sieve, and weigh the prescribed amount of thiohydrogen Clopidogrel (crystal form is not limited), add to the mixed medium, after the drug dissolves, filter and transfer to the liquid medicine tank, keep warm at 30-38°C, connect to a soft capsule machine, press into soft capsules, dry, and divide after passing the quality inspection Packing, labeling, and packaging, the clopidogrel sulfide soft capsules are obtained.

Embodiment 2

[0063] Embodiment 2 Preparation of Clopidogrel Sulfate Soft Capsules

[0064] The composition of the prescription is as follows: (g)

[0065] Clopidogrel Sulfuric Acid 24.46

[0066] PEG200 716

[0067] 1,2-Propanediol 80

[0068] ethanol 7

[0069] HS-15 0.8

[0070] A total of 828.26g, made into 1000 soft capsules.

[0071] Preparation process: Weigh the prescribed amount of PEG200, 1,2-propylene glycol, ethanol, HS-15, add to the dissolution tank, stir at 45-70°C to mix evenly; pass the drug through a 60-mesh sieve, weigh Prescribed amount of clopidogrel sulfide (crystal form is not limited), add to the mixed medium, after the drug dissolves, filter and transfer to the liquid medicine tank, keep warm at 30-38°C, connect to a soft capsule machine, press into soft capsules, and dry , after passing the quality inspection, subpackage, label, and pack to obtain the clopidogrel sulfide soft capsules.

Embodiment 3

[0072] The preparation of embodiment 3 clopidogrel hydrobromide soft capsules

[0073] The composition of the prescription is as follows: (g)

[0074] Clopidogrel hydrobromide 23.80

[0075] PEG600 500

[0076] 1,2-Propanediol 50

[0077] Tween 80 29

[0078] A total of 602.8g, made into 1000 soft capsules.

[0079] Preparation process: Weigh PEG600, 1,2-propanediol, and Tween 80 in the prescribed amount, add them to the dissolving tank, stir at 45-70°C to mix them evenly; pass the drug through a 60-mesh sieve, and weigh the prescribed amount Clopidogrel hydrobromide (crystal form is not limited), added to the mixed medium, after the drug is dissolved, filtered and transferred to the liquid medicine tank, kept at 30-38 ° C, connected to a soft capsule machine, compressed into soft capsules, dried, quality After passing the test, it is subpackaged, labeled, and packaged to obtain the finished product of clopidogrel hydrobromide soft capsules.

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Abstract

The invention discloses a medicinal composition of a pharmaceutically-acceptable salt, i.e., (+)-(s)-alpha-(2-chlorphenyl)-6,7-dihydrothieno-[3,2-c]pyridine-5(4H) and a preparation method thereof. According to the medicinal composition, the limitations of polycrystalline types and electrostatic properties of bulk pharmaceuticals on the preparation of solid oral preparations with stable product quality and high bioavailability are broken through. A medicinal composition and an appropriate medicinal medium construct a novel medicinal composition creatively, so that possible adverse effects of crystal transformation caused in the preparation process of bulk pharmaceuticals on the product quality and a clinical treatment effect are eliminated completely, and the bioavailability is enhanced remarkably. The medicinal composition is suitable for industrially preparing soft capsules or liquid hard capsules.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a pharmaceutical composition containing a pharmaceutically acceptable salt of clopidogrel and a preparation method thereof. The composition completely eliminates the adverse effects of the polymorphic form of the pharmaceutically acceptable salt of clopidogrel on the therapeutic effect and product quality, improves the bioavailability, and the production process is more suitable for industrial production. Background technique [0002] Clopidogrel sulfide is a new generation of anti-platelet aggregation drug developed by French pharmaceutical company Sanofi (Sanofi). Clopidogrel must be converted by CYP450 enzymes to produce active metabolites to exert anti-platelet focusing effect. Its active metabolite can selectively inhibit the binding of adenosine diphosphate (ADP) to its platelet receptor and the activation of glycoprotein GPⅡb / Ⅲa complex mediated by ADP, and inhibit platelet...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K31/4365A61K47/44A61K47/34A61P7/02
Inventor 袁悦许骥张岳江
Owner SHIJIAZHUANG SAIRUI MEDICAL TECH
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