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Pharmaceutical composition containing dozagliptin and sitagliptin and preparation method thereof

A composition and compound technology, applied in the pharmaceutical composition containing dozagliliptin and sitagliptin and its preparation, improving the field of drug combination for type II diabetes, capable of solving the problem of metformin's large toxic and side effects and reducing drug effects Insufficient effect and long-term effect of drugs, etc., to avoid toxic and side effects, improve β-cell function, and improve drug efficacy

Active Publication Date: 2021-12-07
HAINAN ZHONGJI MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when sitagliptin phosphate is used alone due to the limitations of the existing preparation process, the disintegration rate is relatively slow, and the long-term effect of the drug is insufficient, resulting in a short duration of action of the drug in the human body, thereby shortening the interval between medications. In order to achieve the purpose of controlling blood sugar, repeated administration within a certain period of time, this indirectly reduces the effect of the drug
[0005] Although the compound drug improves the above situation, it will also introduce the toxic and side effects of the drug compounded with it, such as the compound drug of sitagliptin and metformin, Although metformin is mixed with sitagliptin to improve the effect of the drug, the side effects of metformin are relatively large, which reduces the safety of the drug

Method used

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  • Pharmaceutical composition containing dozagliptin and sitagliptin and preparation method thereof
  • Pharmaceutical composition containing dozagliptin and sitagliptin and preparation method thereof
  • Pharmaceutical composition containing dozagliptin and sitagliptin and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 A preparation method of pharmaceutical composition X1 containing dozagliliptin and sitagliptin

[0033] The present embodiment provides a preparation method of pharmaceutical composition X1 containing dozagliliptin and sitagliptin, which comprises the following steps:

[0034] S1. Synthesis of dozaglietin

[0035] T1, take by weighing the compound shown in 157g formula SM1 and the compound shown in 249g formula SM2 respectively and join in 500ml dichloromethane and mix uniformly, add 100g anhydrous magnesium sulfate, stir 5min, add 570g HATU (1.5eq) and 318g sodium carbonate ( 3eq), after mixing evenly, heat to 40°C and keep warm for reaction, react for 4h, use TLC to monitor the progress of the reaction during the reaction, until the fluorescent spots of the compounds shown in formula SM1 and formula SM2 on the silica gel plate disappear, that is, the end of the reaction, the reaction After finishing, filter and rinse filter cake with 300ml ethyl acetate, co...

Embodiment 2～6

[0042] Examples 2-6 Preparation methods of pharmaceutical compositions X2-X6 containing dozagliliptin and sitagliptin

[0043] The present Examples 2-6 provide the preparation method of pharmaceutical compositions X2-X6 containing dozagliliptin and sitagliptin, the preparation method is basically the same as that of Example 1, the only difference is that some process parameters are different, the specific process The parameters are shown in Table 1.

[0044] Table 1: Preparation process table of pharmaceutical compositions X2-X6 containing dozaglietin and sitagliptin

[0045]

[0046] Other processing parameters are all identical with embodiment 1.

experiment example 1

[0047] Experimental example 1 repeated administration test

[0048] Randomly select 18 mice with similar physical signs, good health and half male and half male for repeated administration test, randomly divide 18 half male and half male mice into three groups, the first group is fed with a single sitagliptin Hypoglycemic drugs, the second group fed the pharmaceutical composition of sitagliptin and metformin, and the third group fed the pharmaceutical composition X3 containing dozaglietin and sitagliptin prepared in Example 3;

[0049] Three groups of experiments were administered orally. At the beginning of the test, the dosage was administered at a daily rate of 2 mg / kg. After 3 weeks, the dosage was increased, and the dosage was changed to 10 mg / kg. After feeding again for 3 weeks, the improvement The dosage of the drug is 50mg / kg, and the feeding is continued for 3 weeks. The dosage of no adverse reactions in the test is 10mg / kg. Calculated according to the daily recommend...

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Abstract

The invention discloses a pharmaceutical composition containing dozagliptin and sitagliptin and a preparation method thereof. The pharmaceutical composition containing the dozagliptin and the sitagliptin is prepared by mixing the autonomously synthesized dozagliptin with the sitagliptin, a disintegrating agent and a dispersing agent, tabletting, sterilizing and the like. The pharmaceutical composition containing the dozagliptin and the sitagliptin, provided by the invention, has a remarkable pharmaceutical effect of reducing blood sugar, is high in stability and free from toxic and side effects, and reduces the probability of hypoglycemia of a patient in a taking process. The preparation method is suitable for preparing the pharmaceutical composition containing the dozagliptin and the sitagliptin, and is used for safely and effectively reducing the blood sugar concentration of patients with type II diabetes.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and relates to a drug combination for improving type II diabetes, in particular to a drug composition containing dozagliliptin and sitagliptin and a preparation method thereof. Background technique [0002] Type II diabetes mellitus (diabetes mellitus type 2, T2DM), formerly known as noninsulin-dependent diabetes mellitus (NIDDM) or adult-onset diabetes (adult-onsetdiabetes), is a chronic metabolic disease, mostly between 35 and 40 After the age of onset, accounting for more than 90% of diabetic patients. Patients are characterized by hyperglycemia, relative lack of insulin, and insulin resistance. Common symptoms are polydipsia, frequent urination, unexplained weight loss, and may include eating too much, tiredness, or soreness. Long-term complications of high blood sugar include heart disease, stroke, diabetic retinopathy, which can lead to blindness, kidney failure, and even poor blood flow to ...

Claims

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Application Information

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IPC IPC(8): A61K31/4985A61K31/4155C07D403/12A61P3/10
CPCA61K31/4985A61K31/4155C07D403/12A61P3/10C07B2200/07A61K2300/00
Inventor 章燕杨贵方肖文礼
Owner HAINAN ZHONGJI MEDICAL TECH
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