Profiles of drug substances, excipients, and related methodology最新文献

This chapter presents an overall account of cyclodextrins (CDs) with a brief description of the history, classification, and properties of these macromolecules. CDs act as complexing agents for drugs to form CD-drug inclusion complexes by various techniques. These complexes lead to the modification of the physicochemical properties of drugs to make them more soluble, chemically, and photochemically stable, and less toxic. It focuses in detail on various pharmaceutical uses of CDs and their derived forms in drug solubility, bioavailability, drug stability, drug delivery, and drug safety which have been specifically highlighted. The role of CDs and derivatives as excipients in the drug formulation of solid dosage forms, parenteral dosage forms, and anticancer drugs has been emphasized. Some other applications of CDs in cosmetics, environmental protection, food technology, and analytical methods have been described.

Linagliptin (LINA) is the first dipeptidyl peptidase IV (DPP-IV) inhibitor that could be administered orally to control hyperglycemia. It is indicated for controlling adult blood sugar levels that are diagnosed with diabetes mellitus type II. The current chapter provides a complete review of LINA including nomenclature, physiochemical characteristics, synthesis, and thermal analysis. Additionally, different analytical techniques used for quantitative and qualitative determination of LINA are presented.

Sofosbuvir, a nucleotide analogue, is an antiviral medication that belongs to the class of direct-acting antivirals (DAAs). It is primarily used in the treatment of chronic hepatitis C virus (HCV) infections. Sofosbuvir works by inhibiting the replication of HCV, disrupting its ability to produce RNA and effectively reducing the viral load in the body. This chapter offers a comprehensive examination of sofosbuvir, including its nomenclature, physiochemical attributes, synthesis, and thermal analysis. Furthermore, it presents various analytical methods employed for both spectrophotometric and chromatographic assessments of sofosbuvir in different matrices.

Nateglinide belongs to the meglitinide class of insulin secretagogues. It is used as an oral hypoglycemic agent for the treatment of type 2 diabetes mellitus. Nateglinide is an amino acid derivative of D-phenylalanine that binds to the ATP-sensitive potassium channels in pancreatic beta cells and stimulates the secretion of insulin. In this chapter, various aspects of Nateglinide are discussed. This includes methods used for its synthesis, physicochemical properties, and different techniques employed to determine its structure, such as elemental analysis, IR, UV, (¹H and ¹³C) NMR, MS, and XRD. Additionally, the chapter covers a literature review of various methods of analysis of Nateglinide, such as X-ray powder diffraction pattern analysis, differential scanning calorimetry, spectrophotometric, chromatographic, capillary electrophoresis and immunoassay methods. Moreover, the pharmacology of the title drug including pharmacokinetics, pharmacodynamics, mechanism of action, drug-drug and drug-food interactions are also reviewed.

Fenamates are the most crucial non-steroidal anti-inflammatory drugs (NSAIDs) used to treat pain-related diseases. The clinically prescribed drugs of the fenamate group include mefenamic acid, tolfenamic acid, meclofenamic acid, flufenamic acid, and niflumic acid. Due to their widespread use, all these drugs are considered as the most common water and sewerage pollutants. Studies have been performed to remove these contaminants from water sources by various forced degradation procedures, but the number of studies in this area is limited. In this chapter, an effort has been made to review the degradation of multiple fenamates in different systems and the factors affecting the degradation rates with the proposed degradation pathways.

This comprehensive drug profile provides a detailed exploration of Dronedarone, an antiarrhythmic medication used for regulating irregular heartbeats. This chapter covers various aspects of Dronedarone, including its nomenclature, formulae, physical characteristics, methods of preparation, and analytical methods. The nomenclature section presents the IUPAC and nonproprietary names of Dronedarone, along with its proprietary names. The empirical formula, molecular weight, and CAS number are provided for both Dronedarone and its hydrochloride salt. The document also explores the physical characteristics, including color, form, and optical activity, as well as the melting point, solubility, and spectroscopic analysis. Stability, clinical applications, pharmacology, mechanism of action, and pharmacokinetics are discussed.

Ponatinib is a prescription medication used to treat a rare form of blood cancer called Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) and chronic myeloid leukemia (CML) that is resistant to other treatments. It belongs to a class of drugs called tyrosine kinase inhibitors, which work by blocking abnormal proteins that promote the growth of cancer cells. In this chapter, the synthesis methods and physicochemical properties of ponatinib were reviewed, besides the characterization of the ponatinib structure using different techniques such as elemental analysis, IR, UV, (¹H and ¹³C) NMR, MS, and XRD. Furthermore, the compendial method for analysis of ponatinib was not found, while the literature review of a non-compendial method for analysis of ponatinib, such as spectroscopic, chromatographic, and immunoassay methods, was covered. Moreover, pharmacology and biochemistry were surveyed in the pharmacokinetic and pharmacodynamic studies.

Deferasirox is an iron-chelating drug developed by Novartis company for treatment of diseases accompanied by chronic iron overload; such as β-thalassemia or sickle cell diseases. Owing to its advantages such as high affinity, specificity and wide therapeutic window, it is considered as first line treatment. The current chapter describes the physicochemical characteristics, mode of action, pharmacokinetics, therapeutic applications and synthetic methods for deferasirox. Moreover, it includes Fourier transform infrared spectrometry (FTIR) and nuclear magnetic resonance spectroscopy (NMR) analysis for its functional groups. In addition, the selected analytical methods are summarized to aid the analysts in their routine analysis of deferasirox.

Regorafenib is a small molecule tyrosine kinase inhibitor administered orally drug, act by inhibiting the activity of the VEGF receptors. It is used for the treatment of patients with metastatic colorectal cancer (CRC), advanced gastrointestinal stromal tumors, and hepatocellular carcinoma. This comprehensive profile on regorafenib includes an original data as well as data collected from the literature on Profiles of Methods of Drug Synthesis, different Physical Drug Profiles, Drug Analytical methods and Pharmacological profile (ADME). This chapter is divided into five main sections: General Description of the drug, Physical Characteristics, Methods of Preparation, Methods of Analysis, Pharmacology and List of References. These main sections are further divided to many sub-titles to cover most aspect of the drug in the light of the available literature. Among these sub-titles are the formulae, Elemental Analysis, physical characteristics which include constant of ionization, solubility, X-ray powder diffraction pattern, TGA, thermal conduct and spectroscopic and stability. Additionally, analytical techniques including Electrochemical, Spectrophotometric and chromatographic methods, ADME profiles and pharmacological effects were also discussed. Furthermore, methods and schemes are outlined for the preparation of the drug substance.