Profiles of Drug Substances, Excipients, and related Methodology

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Betaxolol is a relatively cardioselective β-adrenoceptor blocking drug, with no partial agonist (intrinsic sympathomimetic) activity and weak membrane-stabilizing (local anesthetic) activity. Betaxolol selectively and competitively binds to and blocks beta-1 (β1) adrenergic receptors in the heart, thereby decreasing cardiac contractility and rate. This leads to a reduction in cardiac output and lowers blood pressure. When applied topically in the eye, this agent reduces aqueous humor secretion and lowers the intraocular pressure (IOP)...

The present study describes a comprehensive profile of Bisoprolol including detailed nomenclature; formulae, elemental analysis, appearance, its uses, applications, and methods for the preparation are outlined. The profile contains physicochemical properties of Bisoprolol including pKa value, solubility, X-ray powder diffraction, and methods of analysis (including compendial, electrochemical, spectroscopic, chromatographic and capillary electrophoresis). The study also covers thermal analysis such as differential scanning calorimetry and thermogravimetry of Bisoprolol...

This present review described the validation method of in-vitro bioassay for its application in herbal drug research. Seven sequencing steps that can be taken for performing a valid bioassay include: literature survey, sample stability evaluation, Biosystem performance testing, Sample performance evaluation, determination of 50% effective concentration or cytotoxic concentrations, selective index evaluation, and determination of accurate relative potency of sample. Detailed methods and acceptance criteria for each step are described herein...

Irbesartan, (2-butyl-3-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-1,3-diazaspiro[4.4]non-1-en-4-one), is a member of non-peptide angiotensin II receptor antagonists used worldwide in the treatment of hypertension and diabetic nephropathy in hypertensive patients with type 2 diabetes, elevated serum creatinine, and proteinuria. Irbesartan can be used alone or in combination with other antihypertensive agents (e.g., hydrochlorothiazide). These combination products are indicated for hypertension in patients with uncontrolled hypertension with monotherapy or first line in patients not expected to be well controlled with monotherapy...

Rabeprazole belongs to the class of anti-secretory drugs, with benzimidazoles substitution. These drugs induce gastric acid secretion through precise inhibition of the enzyme H+ /K+ -ATPase (acid or proton pump). This effect helps to treat and prevent conditions in which gastric acid directly aggravates symptoms such as duodenal and gastric ulcers. This chapter includes a comprehensive review of rabeprazole in terms of nomenclature, its physical-chemical properties, methods of preparation and ADME profiles...

Darunavir: (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-4-{[(4-aminophenyl)sulfonyl] (isobutyl)amino}-3-hydroxy-1-phenyl-2-butanyl]carbamate is a synthetic non-peptide protease inhibitor. On June 2006, it was first approved by the Food and Drug administration (FDA) for treatment of resistant type-1 of the human immunodeficiency virus (HIV). In July 2016, the FDA expanded the approval for use of darunavir in pregnant women with HIV infection. Darunavir prevents the replication of HIV virus by inhibiting the catalytic activity of the HIV-1 protease enzyme, and selectively inhibits the cleavage of HIV encoded Gag-Pol polyproteins in virus-infected cells, which prevents the formation of mature infectious virus particles...

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)...

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...

Carbetapentane citrate, a non-opioid centrally-acting antitussive drug, is a common treatment for cough associated with other diseases such as common cold and respiratory tract infections. Its mode of action is very close to that of atropine; since it acts at the level of the peripheral parasympathetic nerve endings. The drug reaches its maximum plasma concentration (Cmax ) 2h after administration, and it has a plasma half-life of 2.3h in case of oral administration. Due to its clinical importance, there are many analytical methods in the literature for carbetapentane determination...

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...

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...

Isotretinoin is chemically named as: (2Z, 4E, 6E, 8E)-3,7-Dimethyl-9-(2,6,6-trimethylcyclohex-1-enyl)nona-2,4,6,8-tetraenoic acid. It is an orally active retinoic acid derivative for the treatment of severe refractory nodulocystic acne. It acts primarily by reducing sebaceous gland size and sebum production, and as a result alters skin surface lipid composition. Using isotretinoin for 1-2mg/kg/day for 3-4 months produces 60%-95% clearance of inflammatory lesions in patients with acne. Doses as low as 0.1mg/kg/day have also proven successful in the clearance of lesions...

Azilsartan is used for treatment of the high blood pressure (hypertension). Reducing high blood pressure enables avoid strokes, heart attacks and problems of kidneys. Azilsartan comes under the name angiotensin receptor blocker (ARBs) as a class of drugs. It acts by relaxing blood vessels to make it easier for blood to flow. Azilsartan Medoxomil's a comprehensive profile containing the description, formulae, Elemental Analysis, Uses and application. Furthermore, methods and schemes are outlined for the preparation of the drug substance...

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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...

Pharmaceutical preparations may contain a single ingredient or multi-ingredients as well as excipients. In multicomponent systems, specific analytical methods are required to determine the concentrations of individual components in the presence of interfering substances. Ultraviolet and visible spectrometric methods have widely been developed for the analysis of drugs in mixtures and pharmaceutical preparations. These methods are based on ultraviolet and visible multicomponent analysis and chemometrics (multivariate data analysis)...

Topiramate, 2,3:4,5-di-O-isopropylidene-β-d-fructopyranose sulfamate, is a potent antiepileptic drug with a broad spectrum of activity. It is effective in both partial and generalized seizures. Topiramate was also found to have significant efficacy in migraine prevention with considerable reductions in the frequency of migraine headaches. The most common adverse events, which may accompany the use of topiramate, are paresthesia, fatigue, decreased appetite, nausea, diarrhea, weight decrease and taste perversion...

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...

Sucrose octaacetate (SOA) is a United States National Formulary (NF) monograph compendial material (U.S. Pharmacopeia, 2008), and, as shown in Fig. 1, has eight acetate groups attached to a sucrose moiety. It is a natural product that has been extracted from the seeds of Annona cornifolia (Lima et al., 2011). It is nontoxic (Sigma-Aldrich, 2016) and has a number of uses based on its bitter taste. For example, sugar is rendered too bitter is eat at a concentration of 0.06% (w/w) SOA (Mann et al., 1992). SOA can form 255 different possible isomers and degradation products, all of which have a very low molar absorptivity...