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

A comprehensive profile of piroxicam including the nomenclatures, formulae, elemental composition, appearance, uses and applications. The methods which were utilized for the preparation of the drug substance and their respective schemes are outlined. The physical characteristics of the drug including the ionization constant, solubility, x-ray powder diffraction pattern, differential scanning calorimetry, thermal behavior and spectroscopic studies are described. The methods which were used for the analysis of the drug substance in bulk drug and/or in pharmaceutical formulations including the compendial, spectrophotometric, electrochemical and the chromatographic methods are reported. The stability, toxicity, pharmacokinetics, bioavailability, drug evaluation, comparison, in addition to compiled reviews on the drug substance are involved. Finally, more than four hundred and fifty references are listed at the end of this profile.

Emtricitabine (Emtriva, FTC) is an antiviral medicine which decreases the body's amount of HIV. Emtricitabine on of Anti-HIV drugs slow down or protect the immune system against damage and reduce the risk of diseases related to developing of AIDS. Emtricitabine use also for treatment of hepatitis B virus. Emtricitabine is a drug class known as nucleoside reversing transcriptase inhibitors (NRTIs). In view of Emtricitabine's clinical significance, a thorough review of the physical and pharmaceutical characteristics and details of the multiple analytical techniques used to test the drug in pharmaceutical and biological systems was conducted. The methods investigated include identification test, Spectroscopy, chromatography, electrochemicals, and Thermal. Beside the analytical profile, the degradation and stability of Emtricitabine, its pharmacology and pharmacokinetics, Pharmaceutical Applications, Mechanism of Action, dosage forms and dose, ADME profile, and interactions have been debated.

Erlotinib (OSI-774), marketed by Genentech as Tarceva®, is anticancer drug approved by US-FDA for the treatment of Non-Small Cell Lung Cancer (NSCLC) and Pancreatic Cancer. Erlotinib inhibited epidermal growth factor receptor (EGFR) that blocks tumor cell division, produces cell cycle arrest, and initiates programmed cell death in EGFR-overexpressing human tumor cells. This study presents a comprehensive profile of erlotinib, including detailed nomenclature, formula, elemental analysis, methods of preparation, physico-chemical characteristics, and methods of analysis (including spectroscopic, electrochemical, and chromatographic methods of analysis). Spectroscopic and spectrometric analyses include UV/vis spectroscopy, vibrational spectroscopy, nuclear magnetic resonance spectrometry ((1)H and (13)C NMR), and mass spectrometry. Chromatographic methods of analyses include thin layer chromatography, and high-performance liquid chromatography. Pharmacology of erlotinib including pharmacodynamics, mechanism of action, pharmacokinetics and drug-drug interactions were also presented. An appropriate table and figures were attached to each of the above mentioned sections along with total of 48 references.

Meloxicam, an oxicam derivative: 4-Hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2- benzothiazine-3-carboxamide 1,1-dioxide, is a nonsteroidal anti-inflammatory drug (NSAID). It is a selective inhibitor of cyclooxygenase-2 (COX-2). It is used in the management of rheumatoid arthritis, acute exacerbations of osteoarthritis, ankylosing spondylitis and juvenile idiopathic arthritis. It is given in a single oral dose of 7.5mg, increased if necessary to a maximum of 15mg daily (7.5mg in the elderly). It may also be given by rectal suppository in doses similar to those used orally. The reported side effects of meloxicam are similar to those of nonsteroidal anti-inflammatory drugs (NSAIDs), such as abdominal pain, anemia, and edema. There is also an increased risk of serious gastrointestinal (GI) adverse events, including ulceration and bleeding. This profile is prepared to discuss and explain physical characteristics, Proprietary and nonproprietary names of meloxicam. It also includes methods of preparation, thermal and spectral behavior, methods of analysis, pharmacokinetics, metabolism, excretion and pharmacology.

Developments in the field of pharmaceutical cocrystals have been documented in the form of chronological review articles, and the present review encompasses articles published during 2012, 2013, and 2014. Appropriate publications were drawn from the major physical, crystallographic, and pharmaceutical journals, being sorted according to the identity of the drug substance involved. This information is contained in tabular form, where the primary sorting has been by compound name and year of publication. For each entry, the table also contains the bibliographic citation to the paper, a complete list of the authors, and the title of the paper.

Thiouracil, 2-sulfanylidene-1H-pyrimidin-4-one, has been used as anti-thyroid, coronary vasodilator, and in congestive heart failure. It was found to cause agranulocytosis and it is suspected to be teratogenic and carcinogenic. Owing to its high frequency of adverse reactions, especially agranulocytosis, its use was abandoned in favor of other, less toxic drugs, such as propylthiouracil and methimazole. Thiouracil refers both to a specific molecule consisting of a sulfated uracil and a family of molecules based upon the structure. An important member of this family is propylthiouracil, which is a thiourea antithyroid drug that acts by blocking the production of thyroid hormones; it also inhibits the peripheral deiodination of thyroxine to tri-iodothyronine. This profile is prepared to discuss and explain physical and chemical properties, proprietary and nonproprietary names of thiouracil and propylthiouracil. It also includes uses and applications, methods of preparation, thermal and spectral behavior and methods of analysis. In addition, metabolism, excretion and pharmacology of propylthiouracil are also discussed.

Paclitaxel is the first microtubule-stabilizing agent identified and considered to be the most significant advance in chemotherapy of the past two decades. It is considered one of the most widely used antineoplastic agents with broad activity in several cancers including breast cancer, endometrial cancer, non-small-cell lung cancer, bladder cancer, and cervical carcinoma. It is also used for treating AIDS-related Kaposi sarcoma as a second line treatment. This comprehensive profile of paclitaxel gives overview of nomenclature, formulae, elemental analysis, appearance, application and uses. In addition, mechanism of action and resistance, different dosage forms and methods of drug preparation are elaborated. Moreover, the physicochemical properties involving X-ray powder diffraction pattern, drug solubility, melting point, differential scanning calorimetry, and stability were summarized. Furthermore, method of drug analysis including compendial, spectrophotometric, and chromatographic was discussed.

Sorafenib (BAY-43-9006), marketed by Bayer as Nexavar® (USA), is anticancer drug approved by US-FDA for the treatment of unresectable hepatocellular carcinoma and advanced renal cell carcinoma. Sorafenib inhibited tumor growth and angiogenesis through targeting both the RAF/MEK/ERK pathway and receptor tyrosine kinases. This study presents a comprehensive profile of sorafenib, including detailed nomenclature, formula, elemental analysis, methods of preparation, physico-chemical characteristics, and methods of analysis (including spectroscopic, electrochemical, and chromatographic methods of analysis). Spectroscopic and spectrometric analyses include UV/vis spectroscopy, vibrational spectroscopy, nuclear magnetic resonance spectrometry ((1)H and (13)C NMR), and mass spectrometry. Chromatographic methods of analyses include thin layer chromatography and high-performance liquid chromatography. Only few stability indicating methods were found for quantification of sorafenib after exposing tablet dosage form to various stress conditions such as hydrolysis, oxidation, thermal stress, photo and UV light. However, none of these described methods were made to separate and quantify the degradation products. Pharmacology studies including pharmacodynamics, mechanism of action, pharmacokinetics and drug-drug interactions were also presented. An appropriate table and figures were attached to each of the above mentioned sections along with total of 55 references.