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Nateglinide: A comprehensive profile.

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.

Degradation of fenamates.

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 d

Ponatinib: A comprehensive drug profile.

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, (

Duvelisib: A comprehensive profile.

Duvelisib (DUV) is chemically named as (S)-3-(1-((9H-Purin-6-yl)amino)ethyl)-8-chloro-2-phenylisoquinolin-1(2H)-one. It is a novel drug with a small molecular weight and characterized by dual phosphoinositide-3-kinase (PI3K)- and PI3K-inhibitory activity. The Food and Drug Administration (FDA) recently approved DUV for the management of small lymphocytic lymphoma (SLL) and relapsed or refractory chronic lymphocytic leukemia (CLL) in adult patients. DUV is marketed under the brand name of Copiktra® (Verastem, Inc., Needham, MA, USA). This chapter provides a critical extensive review of the lite

Betaxolol: A comprehensive profile.

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). In addition, betaxolol prevents the release of renin, a ho

Irbesartan (a comprehensive profile).

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

Isotretinoin.

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. Encouraging results have

Thiouracil: Comprehensive profile.

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 i

Cinacalcet Hydrochloride.

Cinacalcet hydrochloride is a calcimimetic agent that increases the sensitivity to the extracellular calcium of the calcium-sensing receptors of the parathyroid gland which regulates parathyroid hormone secretion. This comprehensive profile on cinacalcet hydrochloride starts with a description: nomenclature, formulae, chemical structure, elemental composition, and appearance. The uses and applications of the drug are included. The methods of preparation of cinacalcet hydrochloride are described and their respective schemes are outlined. The physical characterization of the drug is: ionization

Azithromycin.

Azithromycin is an azalide, a subclass of macrolide antibiotics. It is derived from erythromycin, with a methyl-substituted nitrogen atom incorporated into the lactone ring, thus making the lactone ring 15-membered. It prevents bacteria from growing by interfering with their protein synthesis. It binds to the 50S subunit of the bacterial ribosome and thus inhibits translation of mRNA. Azithromycin is used to treat or prevent certain bacterial infections, most often those causing middle ear infections, strep throat, pneumonia, typhoid, bronchitis, and sinusitis. In recent years, it has been use

Carvedilol.

Carvedilol ((2RS)-1-(9H-carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]propan-2-ol), a β1-, β2-, and α1-adrenoreceptor blocker drug with antioxidant and antiproliferative effects, is indicated for treatment of hypertension, stable angina pectoris, and congestive heart failure. A profile of this drug substance is provided in this chapter and includes physical characteristics of Carvedilol (e.g., UV-vis, IR, NMR, and mass spectra). Details regarding the stability of Carvedilol in the solid state and solution phase are presented and methods of analysis (compendial and literature) are summa

Paroxetine hydrochloride.

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

Buclizine.

A comprehensive profile on buclizine hydrochloride, the piperazine derivative which is a sedating antihistamine with antimuscarinic and moderate sedative action and used mainly for its antiemetic effect in the prevention of motion sickness and migraine, is prepared. This profile contains the following sections: description, uses and applications, methods of preparation, physical characteristics, methods of analysis and stability. The physical characteristics section includes solubility, melting range, X-ray powder diffraction pattern, ultraviolet/visible spectroscopy, infrared spectroscopy, pr

[Biological activity and antitumor effect of long-acting recombinant human interleukin-2 drug].

OBJECTIVE: To investigate the biological activity and antitumor effect of pegylated recombinant human interleukin 2 (PEG-rhIL-2) obtained by site-specific conjugation of polyethylene glycol (PEG) with non-natural amino acids, and to explore its antitumor mechanism. METHODS: The binding activities of PEG-rhIL-2 at three different sites (T41, Y45, and V91) to human interleukin 2 receptors α (IL-2Rα) and β (IL-2Rβ) and were detected by surface plasmon resonance (SPR) technology. Western blot was used to detect the levels of the Janus kinase-signal transducer and activator of transcription 5 (JAK

Dry powder inhalers of gentamicin and leucine: formulation parameters, aerosol performance and in vitro toxicity on CuFi1 cells.

The high hygroscopicity of gentamicin (G) as raw material hampers the production of respirable particles during aerosol generation and prevents its direct use as powder for inhalation in patients suffering from cystic fibrosis (CF). Therefore, this research aimed to design a new dry powder formulation of G studying dispersibility properties of an aminoacid, L-leucine (leu), and appropriate process conditions. Spray-dried powders were characterized as to water uptake, particle size distribution, morphology and stability, in correlation with process parameters. Aerodynamic properties were analyz

Moxifloxacin-Gelrite in situ ophthalmic gelling system against photodynamic therapy for treatment of bacterial corneal inflammation.

In this study, six in situ gelling formulations based on Gelrite were prepared and evaluated for the retained ophthalmic delivery of Moxifloxacin (Mox). The effectiveness of the best developed formula G5 was compared with photodynamic therapy (PDT), the recent expanding approach for the treatment of ophthalmologic disorders after the assessment of optimum photodynamic inactivation parameters that permit efficient pathogens eradication. It was found that, Staphylococcus aureus (S. aureus) (Gram-positive) was more susceptible to effective lethal photosensitization that reaches 93.5% reduction in

Comparison of different methods for preparation of a stable riccardin D formulation via nano-technology.

Riccardin D is a new compound extracted from liverwort Marchantia polymorpha L. It has been proved to be useful in antifungal therapy and reversing the resistance of Candida albicans against fluconazole. However, the poor solubility leads to the poor bioavailability and limits its development. In this study, nanocrystals were prepared in the evaporative precipitation into aqueous solution (EPAS) and the microfluidisation process. The characterizations of nanocrystals were compared by transmission electron microscope, size distribution, and zeta potential. In the EPAS method, the drug was disso

The efficacy and safety of bufadienolides-loaded nanostructured lipid carriers.

Bufadienolides-loaded nanostructured lipid carriers (BU-NLC) were prepared for parenteral application using glyceryl monostearate as solid core, medium-chain triglyceride and oleic acid as liquid lipid material, and Lipoid E-80, sodium deoxycholate and pluronic F68 as stabilizers. In this study, the in vitro cytotoxicity, pharmacokinetics, biodistribution, antitumor efficacy and safety of BU-NLC were evaluated. Against human astrocytoma cell line (U87-MG) and human gastric carcinoma cell line (HGC-27) BU-NLC exhibited cytotoxicity that was similar to that of the free drug, and superior to that

Aqueous hydrocortisone mouthwash solution: clinical evaluation.

Patients often experience difficulties in applying topical steroids in orabase to the oral mucosa, particularly when large areas need to be covered. An aqueous hydrocortisone mouthwash solution has been developed, one that was anticipated to be more acceptable to patients. The solution contains hydrocortisone (0.3% w/v) in a 4.5% (w/v) 2-hydroxypropyl-beta-cyclodextrin solution. Hydroxypropylmethylcellulose (0.5% w/v) was used to increase the viscosity of the solution and to promote the hydrocortisonecyclodextrin complex. One hundred and two patients with aphthous ulceration, lichen planus, an

Оптимизированная внутриназальная доставка сегестерона ацетатата в мозг с использованием наноэмульсии и микроэмульсии.

Segesteron aцетат (SA) является селективным и мощным агонистом рецептора прогестерона с потенциальным применением в лечении неврологических заболеваний, таких, как множественный склероз и инсульт. В этом исследовании микроэмульсия (МЭ) и three Наноэмульсии (NEs) с целевой концентрацией SA 0.48 Мг/г были разработаны для интраназального администрирования и подробно описаны в отношении их физико-химических свойств, устойчивости, антимикробной активности и безопасности (на первичных кортикальных клетках, тесте на яйцеклетки Hen/s, модели MucilAirTM и на крысах). Измерялись уровни плазмы и SA мозга

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… Validation Selectivity with respect to excipients of the formulation composition was determined by analyzing properly diluted blank samples of the different ME and NE in the mobile phase. … Thus, increasing the excipients-to-drug proportion in the ME, or even its replacement by the SMEDDS form, is expected to better solubilize SA and prevent its precipitation. …