Dipeptidyl peptidase inhibitor and vitamin-B pharmaceutical composition and application thereof

Inactive Publication Date: 2013-12-04
SHENZHEN AUSA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, DPP-4 inhibitors also have some shortcomings: First, compared with traditional hypoglycemic drugs, the clinical application history of DPP-4 inhibitors is short, and there is a lack of evidence-based medical data in the prevention and treatment of diabetic vascular complications, so there is no Second, in my country, DPP-4 inhibitor drugs are all imported, the drug cost is relatively high, and they are at a price disadvantage in market competition; third, because DPP-8 and DPP-9 belong to the same The enzyme family, DPP-4 inhibitors may also inhibit these enzymes. Although no adverse reactions related to the inhibition of the above two enzymes have been found so far, since these drugs have not been on the market for a long time, we should be cautious about the information on adverse reactions
[0008] At present, the antidiabetic drugs on the market focus on correcting the abnormal state of blood sugar and metabolic disorders of diabetes, while ignoring the early intervention of the composite risk factors that lead to diabetic complications (such as diabetic vascular disease) to a certain extent

Method used

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  • Dipeptidyl peptidase inhibitor and vitamin-B pharmaceutical composition and application thereof
  • Dipeptidyl peptidase inhibitor and vitamin-B pharmaceutical composition and application thereof
  • Dipeptidyl peptidase inhibitor and vitamin-B pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1 prepares compound sitagliptin / folic acid sheet (1000 pieces amount)

[0034]

[0035] Preparation method: pass the raw and auxiliary materials through a 80-mesh sieve, and dry for later use. Take the prescribed amount of folic acid and sitagliptin and mix them uniformly according to the method of equal increase, weigh the prescribed amount of microcrystalline cellulose, low-substituted hydroxypropyl cellulose (L-HPC), sodium carboxymethyl starch, and mix them with the raw materials The powder is fully mixed according to the method of equal increase, and an appropriate amount of 5% povidone 95% ethanol solution is added to make a soft material, granulated with a 20-mesh sieve, dried at 50°C for about 6 hours, and granulated with a 20-mesh sieve to control the water content of the granules. 2-3%, the dried granules are uniformly mixed with the prescribed amount of magnesium stearate, the intermediate is tested, and pressed into 1000 tablets. Pay attention...

Embodiment 2

[0036] Embodiment 2 prepares compound saxagliptin / folic acid sheet (1000 pieces amount)

[0037]

[0038] Preparation method: pass the raw and auxiliary materials through a 80-mesh sieve, and dry for later use. Take the prescribed amount of folic acid and saxagliptin and mix them uniformly according to the method of equal increase, weigh the prescribed amount of microcrystalline cellulose, lactose, cross-linked polyvinylpyrrolidone, and sodium carboxymethyl starch, and fully mix them with the mixed powder of raw materials. Add an appropriate amount of 10% starch slurry solution to make a soft material, granulate with a 20-mesh sieve, dry at 50°C for about 6 hours, sieve the granules with a 20-mesh sieve, control the water content of the granules to 2-3%, and mix the dried granules with the prescribed amount Glyceryl behenate and magnesium stearate were evenly mixed, the intermediate was tested, and pressed into 1000 tablets. Pay attention to avoiding light during the prepa...

Embodiment 3

[0039] Example 3 Preparation of Compound Vildagliptin / 5-Methyltetrahydrofolate Tablets (1000 Tablets)

[0040]

[0041]

[0042] Preparation method: the auxiliary material is a direct pressing auxiliary material, which is dried for later use. Take the prescribed amount of 5-methyltetrahydrofolate and 10 g of microcrystalline cellulose and mix uniformly according to the method of equal increase to obtain the powder mixing intermediate 1; weigh the remaining microcrystalline cellulose, lactose, and sodium carboxymethyl starch in the prescribed amount , and vildagliptin are fully mixed according to the equal increase method to obtain the mixed powder intermediate 2; the mixed powder intermediate 1 and the mixed powder intermediate 2 are mixed with the prescribed amount of magnesium stearate according to the equal increase method, Obtain the final mixed powder intermediate, detect the mixed powder intermediate, and press into 1000 pieces. Pay attention to avoiding light dur...

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PUM

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Abstract

The invention relates to dipeptidyl peptidase -4(DPP-4) inhibitor and vitamin-B pharmaceutical composition. The composition comprises effective treatment dose of DPP-4 inhibitor, one of medicinal precursor, active metabolite and salt of the DPP-4 inhibitor, effective treatment dose of one or multiple of vitamins B, and pharmaceutically acceptable carrier. The DPP-4 inhibitor is 2-200mg, and vitamins B are 0.01-50mg. The invention further relates application of the composition in the preparation of diabetes drugs. The drugs made of the composition have the effect of effectively lowering blood glucose and the effect of significantly preventing or improving diabetic angiopathy complications; accordingly the drugs are more suitable as anti-diabetic medicines.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing a dipeptidyl peptidase-4 inhibitor and B vitamins and its application, in particular to a chemical medicine composition for treating diabetes and preventing complications of diabetic vascular disease, which belongs to the field of pharmacy. Background technique [0002] Diabetes mellitus is a common endocrine and metabolic disease characterized by chronic hyperglycemia accompanied by disturbances in sugar, fat and protein metabolism caused by insufficient insulin secretion and / or action defects. According to epidemiological surveys, the prevalence of diabetes in my country is as high as 9.7%, and it is estimated that the total number of adult diabetic patients in the country is 92.4 million [Yang W, et al. Prevalence of diabetes among men and women in China. N Engl J Med.2010; 362 : 1090-1101]. In addition, according to the statistics of the International Diabetes Federation (IDF), there ...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61P3/10A61P9/00A61P9/10A61P13/12A61P17/02
Inventor 徐希平张磊陈光亮王存芳
Owner SHENZHEN AUSA PHARMA
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