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Clopidogrel hydrogen sulfate tablet and preparation method thereof

A clopidogrel bisulfate tablet and a technology of clopidogrel bisulfate, which are applied in the field of medicine, can solve problems such as lack of anti-platelet aggregation, and achieve the effect of improving safety, effectiveness and stability

Inactive Publication Date: 2009-12-02
ZHEJIANG JINGXIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But present clopidogrel bisulfate tablet has the following problems: the clopidogrel in the clopidogrel bisulfate tablet is more easily converted into clopidogrel acid, and the dextro isomer of clopidogrel is more easily converted into levoisomer body
Existing reports indicate that the left-handed isomer of clopidogrel has almost no anti-platelet aggregation effect, and animal test results show that the toxicity of the left-handed isomer of clopidogrel is significantly higher than that of the right-handed isomer of clopidogrel

Method used

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  • Clopidogrel hydrogen sulfate tablet and preparation method thereof
  • Clopidogrel hydrogen sulfate tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] Embodiment 1 prescription: (make 1000)

[0011] Main drug

[0012] Preparation method: mix vitamin C with microcrystalline cellulose according to the method of equal amount addition, and then mix with the main drug, mannitol, polyethylene glycol 4000, part of croscarmellose sodium, part of micro-powdered silica gel, and part of talcum powder Finally, the granules are prepared by dry granulation, and the obtained granules are mixed evenly with the remaining croscarmellose sodium, micronized silica gel, and talcum powder, pressed into tablets, coated with film, and packaged.

Embodiment 2

[0013] Embodiment 2 prescription: (make 1000)

[0014] Main drug

[0015] Preparation method: Mix vitamin C with microcrystalline cellulose according to the method of equal amount addition, and then granulate with the main drug, lactose, pregelatinized starch, polyethylene glycol 6000, and part of carboxymethyl starch sodium, and use water as the wetting agent. Drying, granulation, adding the remaining sodium starch glycolate, micropowder silica gel, and talcum powder, mixing evenly, pressing into tablets, coating with film, and packaging.

Embodiment 3

[0017] Prescription: (makes 1000 tablets)

[0018] Main drug

[0019] Preparation method: Dissolve vitamin C in a certain amount of water, add 95% ethanol solution to make an ethanol solution containing 50% alcohol, and obtain a wetting agent. After mixing mannitol and microcrystalline cellulose, completely wet it with a wetting agent, and dry it to obtain material 1. Take the main drug, material 1, pregelatinized starch, polyethylene glycol 6000, part of cross-linked povidone, part of micropowder silica gel, part of talc powder and mix them to make granules by dry granulation method. Vitone, micropowder silica gel, and talcum powder are mixed uniformly, pressed into tablets, and coated with a film.

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Abstract

The invention relates to a clopidogrel hydrogen sulfate tablet and a preparation method thereof. Clopidogrel is more easily converted into clopidogrel acid and a clopidogrel dextroisomer is more easily converted into a levoisomer in the prior clopidogrel hydrogen sulfate tablet. The clopidogrel hydrogen sulfate tablet takes clopidogrel hydrogen sulfate as a main medicine and is matched with filling agent, disintegrant, flow agent and lubricant, and a mixture with the weight percent of 0.05-5 of one or two of vitamin C and butylated hydroxyanisole are added into the clopidogrel hydrogen sulfate tablet. The vitamin C and / or the butylated hydroxyanisole can well inhibit the clopidogrel from being converted into the clopidogrel acid and inhibit the clopidogrel dextroisomer from being converted into the levoisomer, thereby improving the stability of the clopidogrel hydrogen sulfate tablet and the safety and the effectiveness of clinical medicines.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a clopidogrel bisulfate tablet and a preparation method thereof. Background technique [0002] Clopidogrel is a platelet aggregation inhibitor that selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptor and the subsequent ADP-mediated activation of the glycoprotein GPIIb / IIIa complex to achieve Inhibition of platelet aggregation. Clopidogrel is a prodrug that undergoes oxidation to form 2-oxo-clopidogrel, which is then hydrolyzed to form the active metabolite (a thiol derivative); oxidation is primarily mediated by cytochrome P450 isoenzymes 2B6 and 3A4 regulate, and 1A1, 1A2 and 2C19 also have certain regulatory effects. In vitro isolation of this active metabolite shows that it rapidly and irreversibly binds to platelet receptors, thereby inhibiting platelet aggregation. Clopidogrel reduces the chance of arterial blockage by inhibiting platelet aggre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4365A61K47/22A61P7/02
Inventor 梁志寿李黄强张利锋王光强
Owner ZHEJIANG JINGXIN PHARMA
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