Sitagliptin Phosphate Monohydrate API code MK-0431 was approved by FDA in October 2006 for the treatment of type 2 diabetes. Clinical trials show that it is very effective in treating type 2 diabetes. As a new type of hypoglycemic raw material, it not only has the advantages of blood sugar dependence and moderate hypoglycemic effect, but also increases insulin secretion without hypoglycemia and effectively relieves hunger. In the application investigation, it also has no side effects such as nausea, vomiting, edema and weight gain.
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Item |
Specification | Results | |
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Appearance |
White or light yellow fine powder |
conform |
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Identification |
The IR spectrum of samle is consistent with that of the reference |
conform |
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The retention time of the major peak of product corresponds to that of the standard |
conform |
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Solubility |
Very Slight solube in water;solube in alkali-OH Soln ;Almost insolube in ethanol,acetone,Ether,chloroform |
conform |
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Melting Point |
274°-280° |
140.9° |
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Water Content |
NMT10.0% |
0.5% |
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PH |
2.6-3.0 |
2.9 |
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Particle size |
100% through 65mesh, No leass that 60% through 80 mesh |
conform |
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Density |
0.35-0.60g/ml |
conform |
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Heavy Metal |
NMT 10 ppm |
5ppm |
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Arsenic |
NMT 1.0 ppm |
0.5ppm |
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Lead |
NMT1.5 ppm |
0.8ppm |
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Cadmium |
NMT0.5ppm |
0.1ppm |
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Mercury |
NMT1.56ppm |
1.0ppm |
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Loss on Drying |
NMT1.0% |
0.5% |
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Pyridoxine HCL |
NMT 0.50% |
0.1% |
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Residual solveb=nts |
Methylbenzene |
NMT 890 ppm |
550ppm |
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Ethanol |
NMT 5000ppm |
1000ppm |
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N-Butyl alcohol |
NMT 5000ppm |
1000ppm |
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Assay(dried substance) |
98.0%-102.0.% |
99.0% |
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Microbiological Tests |
Total Plate Count |
NMT1000CFU/g |
conform |
| Conclusion | Conform with enterprise specification . | ||
What is the pharmacological action of sitagliptin phosphate monohydrate?
DPP-4 (also known as CD26) is an enzyme expressed on the surface of T cells and plays an important role in immune regulation. In addition to degrading incretin, DPP-4 can also hydrolyze various bioactive peptides, including growth hormone releasing hormone, neuropeptide Y, pituitary adenylate cyclase activating peptide, and gastrin releasing peptide. Among them, glucagon like peptide-1 has a very short half-life in plasma (t ₁/₂ ≈ 1 minute) and is easily degraded by DPP-4. Based on this mechanism, pharmaceutical raw materials development for the intestinal insulinotropic system mainly focuses on the following two directions:
1： It is the development of peptide analogs that are not easily degraded by DPP-4 and can activate GLP-1 receptors, such as the 2005 FDA approved Exenatide. It can simulate the physiological effects of GLP-1 while avoiding rapid degradation by DPP-4.
2： We are developing DPP-4 inhibitors, represented by sitagliptin. Research has shown that Sitagliptin phosphate monohydrate API 98% purity can enhance the activity and levels of endogenous GLP-1 and glucose dependent insulinotropic peptides by selectively inhibiting DPP-4. Due to its blood glucose dependent insulin secretion promoting effect, it can significantly reduce the risk of hypoglycemia caused by traditional hypoglycemic raw powders. Meanwhile, it exhibits high selectivity towards DPP-4 (with a selectivity ratio of approximately 2600:1 for DPP-8/DPP-9), making it less susceptible to adverse reactions caused by inhibition of DPP-8/DPP-9. In addition, its effect of increasing GLP-1 levels is relatively mild, which helps to avoid gastrointestinal side effects such as nausea and vomiting caused by excessive GLP-1.
What are the advantages and disadvantages of Sitagliptin phosphate monohydrate API compared with other DPP-4 inhibitors (such as saxagliptin)?
Sitagliptin phosphate monohydrate API and saxagliptin are both DPP-4 inhibitors, and their hypoglycemic effects are generally equivalent, but there are differences in pharmacokinetics, pharmacology interaction and safety. The specific comparison is as follows:
| Contrast dimension | Sitagliptin Phosphate Monohydrate | Saxagliptin |
| pharmacokinetics | Half life is about 12.4 hours, once a day, unaffected by food. | The half-life is about 2.5 hours, but the active metabolites have a long-lasting effect. They are also administered once a day and are not affected by food. |
| Metabolic pathway | About 79% is excreted by the kidney in prototype, and the dose of renal insufficiency needs to be adjusted according to eGFR. | Mainly metabolized by liver CYP3A4/5 enzymes, patients with renal insufficiency (eGFR<45) need to reduce their dosage. |
| Medical interactions | There is less interaction between pharmaceutical raw materials, and the combination with common hypoglycemic raw materials is safer. | When used in combination with potent CYP3A4 inhibitors (such as ketoconazole), dosage should be reduced; Combined use with inducers such as rifampicin may reduce efficacy. |
| Security focus | Low risk of hypoglycemia, common side effects include hypersensitivity reactions, elevated liver enzymes, upper respiratory tract infections, etc. | The risk of hypoglycemia increases when combined with insulin or sulfonylureas; There are studies suggesting that it may be slightly associated with an increased risk of heart failure. |
| Applicable Population | The interaction between medicine raw materials is minimal, making it suitable for patients who require the combination of multiple pharmaceutical raw materials. | Be cautious when using it in combination with certain potent inhibitors; Individuals with a history of heart failure or high risk should be evaluated with caution. |
What are the adverse reactions of Sitagliptin phosphate monohydrate API?
Sitagliptin phosphate monohydrate API has good overall tolerance, and common adverse reactions include nasopharyngitis, headache, dizziness, abdominal discomfort, constipation, diarrhea, and rash, which are usually mild and mostly self limiting. However, caution should be exercised against rare but serious risks such as hypoglycemia (especially when combined with insulin or sulfonylurea raw materials), acute pancreatitis, acute kidney injury, liver dysfunction, interstitial pneumonia, intestinal obstruction, rhabdomyolysis, thrombocytopenia, bullous pemphigoid, and allergic reactions (including angioedema, Stevens Johnson syndrome, etc.). The Sitagliptin posphate monohydrate powder is mainly excreted through the kidneys. For patients with moderate to severe renal insufficiency, the dosage should be adjusted according to the creatinine clearance rate to prevent medicine accumulation. It is forbidden for people allergic to this product, type 1 diabetes patients and diabetes ketoacidosis patients. Women in pregnancy and lactation should weigh the advantages and disadvantages before using it
A variety of shipping methods for you to choose
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Transportation Time |
Shipping method |
Cargo weight requirements |
Advantage |
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3-7 days |
DHL,Germany DHL,Germany DPD, |
Suitable for under 50kg. |
We have warehouses in Germany and California, USA, |
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7-15 days |
By Air |
Suitable for more than 50kg. |
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15-60 days |
By Sea |
Suitable for more than 500kg. |
Our strengths:
Our company has passed FDA and ISO19001 quality management system certification. And we have internal cooperation agreements with multiple factories and laboratories in China,Our company can provide Sitagliptin Phosphate Monohydrate API Powder etc. at a more favorable price. If you are interested, please leave a message.
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FAQ:
Q1. How to store?
It is recommended to store it sealed, away from light, and moisture at 2-8 ° C. Under dry and sealed conditions, Sitagliptin phosphate monohydrate solid powder can usually be stably stored for several years. The solution should be used as soon as possible after preparation, or frozen at -20 ° C or -80 ° C after packaging.
Q2. What is its stability?
Sitagliptin phosphate monohydrate API Powder is stable under conventional storage conditions. Its solution is stable under acidic and neutral conditions, but it degrades over time under alkaline conditions. Therefore, strong alkaline environments should be avoided during the production and analysis of formulations.
Q3. What are its main impurities?
Impurities are mainly divided into two categories:
Process impurities: intermediates or by-products generated during the synthesis process.
Degradation impurities: oxidation or hydrolysis products produced under light, high temperature, or acid-base conditions.
Various known impurities are listed in the pharmacopoeia and require qualitative and quantitative control through methods such as HPLC
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