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

Aripiprazole is an atypical antipsychotic drug which belongs to the benzisoxazole derivatives. Aripiprazole is available in many salts and polymorphs forms. X-ray diffraction, IR spectroscopy, and DSC could be used for differentiating the polymorphs of aripiprazole. Some instrumental methods of analysis such as UV spectrophotometer, HPTLC, HPLC, and CE can be applied for analyzing aripiprazole and its impurities. Chromatography methods that have an MS/MS detector is the method of choice for analyzing aripiprazole and its metabolites. Bioavailability studies of the polymorphs of aripiprazole and their pharmaceutical preparations are very important to optimize the formulations of the dosage forms.

A profile of the analgesic tramadol hydrochloride ((1RS,2RS)-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol hydrochloride) is provided in this chapter and includes a summary of the physical characteristics known for this drug substance (e.g., UV/vis, IR, NMR, and mass spectra). Details regarding the stability of tramadol hydrochloride in the solid state and solution-phase are presented and methods of analysis (compendial and literature) are summarized. Furthermore, an account of biological properties and a description of the chemical synthesis of tramadol hydrochloride are given.

This chapter is a review on physical and chemical properties, methods of preparation, analysis, as well as pharmacodynamics and pharmacokinetics of Alendronate sodium (4-amino-1-hydroxybutane-1,1-diphosphonic acid sodium salt), a bone metabolism regulator, indicated for the treatment of excessive bone resorption and osteoporosis.

The polymorphic (crystal systems for which a substance can exist in structures defined by different unit cells, and where each of the forms has the same elemental composition) and solvatomorphic (systems where the crystal structures of the substance are defined by different unit cells, but where these unit cells differ in their elemental composition through the inclusion of one or molecules of solvent) landscape of paroxetine hydrochloride have been critically evaluated in order to learn how many authentic crystal forms have actually been discovered. After a survey of the patent and open literature, it was determined that paroxetine hydrochloride has been crystallized in four genuine nonsolvated polymorphic forms and in four fully characterized solvatomorphic forms.

Sucralose is a nonnutritive, zero-calorie artificial sweetener. It is a chlorinated sugar substitute that is about 600 times as sweet as sucrose. It is produced from sucrose when three chlorine atoms replace three hydroxyl groups. It is consumed as tablets (Blendy) by diabetic and obese patients. It is also used as an excipient in drug manufacturing. Unlike other artificial sweeteners, it is stable when heated and can, therefore, be used in baked and fried foods. The FDA approved sucralose in 1998. This review presents a comprehensive profile for sucralose including physical, analytical, and ADME profiles and methods of its synthesis. Spectral data for X-ray powder diffraction and DSC of sucralose are recorded and presented. The authors also recorded FT-IR, (1)H- and (13)C NMR, and ESI-MS spectra. Interpretation with detailed spectral assignments is provided. The analytical profile of sucralose covered the compendial methods, spectroscopic, and different chromatographic analytical techniques. The ADME profile covered all absorption, distribution, metabolism, and elimination data in addition to pharmacokinetics and pharmacological effects of sucralose. Some nutritional aspects for sucralose in obesity and diabetes are also presented. Both chemical and microbiological synthesis schemes for sucralose are reviewed and included.

Paroxetine hydrochloride (3S-trans)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)-piperidine hydrochloride (or (-)-(3S,4R)-(4-(p-fluorophenyl)-3-[[3,4-(methylenedioxy)-phenoxy]methyl]piperidine hydrochloride), a phenylpiperidine derivative, is a selective serotonin reuptake inhibitor. Paroxetine is indicated for the treatment of depression, generalized anxiety disorder, obsessive-compulsive disorder, panic disorder, posttraumatic stress disorder, and social anxiety disorder. The physicochemical properties, spectroscopic data (1D and 2D NMR, UV, FT-IR, MS, PXRD), stability, methods of preparation and chromatographic methods of analysis of pharmaceutical, and biological samples of paroxetine are documented in this review. Pharmacokinetics, metabolism, and pharmacological effects are also discussed.