300884 Pharmacology


Write an essay about Sitagliptin.


Sitagliptin, an antihyperglycemic drug or antidiabetic drug, is used to manage the elevated enzymatic conditions associated with Type 2 Diabetic Mellitus. (Inamdar und Mhaske 2012).

Merck & Co. created this drug. They can be used in patients with T2D (Ghislieri et. al.

This drug was developed in 2006 and was approved in the United States by the Food and Drug Administration in October 2007.

Merck and Co. approved marketing of the drug on April 2, 2007, under the name Januvia (Russell-Jones et al.

Sitagliptin combined with other drugs provided positive results for patients suffering from T2D.

Janumet was the generic name for this drug. Sitagliptin and metformin were also present in the drug.

The molecular structure and chemical form of active pharmaceutical ingredients, and their physical properties

Januvia, or Sitagliptin, has a molecular structure of C16H15F6N5O. This is a pyrazine derived dipeptidyl-peptidase inhibitor (Inamdar 2012).

Sitagliptin Phosphate Monohydrate, which is an off-white hygroscopic powdery drug, is the active pharmaceutical component. It dissolves in water.

It is important to discuss the physical properties of the drug’s chiral centres, solubility, molecular mass, melting point, and molecular weight.

Russell-Jones and colleagues found that the drug has a melting point of 216 to 219 degrees Celsius. The molecular mass is 407.32g/mol. While the solubility of the drug is 179.2mg/L at 25degC.

The drug is a viscous, liquid-colored drug and is supplied to patients in a solid form.

It should also be noted that the drug’s stability can be measured if it is stored in accordance with the instructions and without any strong oxidizing agent.

The decomposition of the drug should not be performed by thermal decomposition, as it can produce toxic gases, such as carbon monoxide and carbon dioxide (Sin Mahe and Sigal 2012).

Crystallization Properties of The API

Also, when discussing the properties of crystallization, the API of this drug should be described. This includes the description of polymorphs, solvates crystallization shape behavior and process (Sin Mahe and Sigal 2012).

The crystallization process is made up of crystal salts that form monophosphate crystals.

The pharmaceutical industries currently have four versions of crystallized drugs, which are patentable and available for patients.

These salts of drug with their solvates and hydrates and polymorphic forms provide high bioavailability and reduce decomposition and hydrolysis (Ghislieri and al.

Administration Routes and Dosage Formulas with Pharmacokinetic Information

The drug should not be administered to patients suffering from type 1 diabetes. It should instead be given to patients with type 2 diabetes in tablets with strengths of 25, 50, 100, and 25 mg respectively (Sin, Mahe, Sigal 2012).

Inamdar 2012, Mhaske 2012. Moreover, oral administration is the best option as intravenous and other routes do not work well in maintaining the body’s enzymatic balance (Inamdar 2012).

Sitagliptin is a well-absorbed drug. The half-life inside the body is between 8 and 14 hours.

Russell-Jones and colleagues found that more than 80% is excreted during the excretion process. The drug also works in a dose-dependent manner.

Description of The Formulation

There are many benefits and drawbacks to the tablet dosage form.

Its oral administration has many benefits, including the ability to lower hyperglycemia.

Like other medications sitagliptin doesn’t cause weight gain so it’s safe and appropriate for type 2 diabetics (Ghislieri, et al.

Description of manufacturing steps

This is how the final pharmaceutical product is created.

Refer to

Ghislieri D. Green, A.P. Pontini M. Willies S.C. Rowles I. Frank, A. Grogan G. and Turner N.J.

Engineering an enantioselective, amine oxidase in order to synthesize pharmaceutical building blocks as well as alkaloid natural products.

Journal of the American Chemical Society. 135(29), P.10863-10869.

Mhaske A.A., 2012

International Journal of Pharmaceutical Sciences and Research. 3(9). p.3267.

DURATION-4 Study Group 2012.

Exenatide (once weekly) compared to metformin and pioglitazone in monotherapy for drug-naive type 2 diabetics (DURATION-4): A 26-week, double-blind trial.

Diabetes care, 35(2). pp. 252-258.

Sin, C.Mahe, E., Sigal, M.L. 2012

A sitagliptin patient had a drug reaction that caused eosinophilia (DRESS) and systemic symptoms.

Diabetes and metabolism, 38(6), 571-573.