Search

Major depressive disorder stands as a profound challenge in the realm of psychiatric illnesses disrupting the well-being and daily existence of affected individuals. This heterogeneous condition continues to baffle researchers due to the elusive nature of its full neurological mechanisms. This review delves into the complex landscape of major depressive disorder, exploring the diverse therapeutic avenues available, from the nuanced realms of psychotherapy to the pharmacological and non-pharmacological approaches that have been the focus of extensive research. In the relentless pursuit of relief for those afflicted, substantial efforts and resources are tirelessly channeled into the exploration of novel antidepressants and the refinement of existing therapeutic protocols. This review juxtaposes the efficiencies of existing treatments, unraveling their comparative effectiveness, and shedding light on their respective strengths and limitations. Even so, the question remains, how well are we managing the treatment of major depressive disorder, and which is the best option not only to treat this condition but also to reach full remission. Consequently, we have compiled findings on treatment selections and how efficient they are in relation to each other. The more we understand how to treat depression effectively the more we can improve the quality of life of individuals affected by this disorder. By comprehensively evaluating the diverse modalities, this review aims to guide clinicians and researchers toward evidence-based decisions, facilitating the formulation of individualized and targeted treatment protocols.

Phytocannabinoids, a diverse group of naturally occurring compounds extracted from the Cannabis plant, have attracted interest due to their potential pharmacological effects and medicinal uses. This comprehensive review presents the intricate pharmacological profiles of phytocannabinoids while exploring the diverse impacts these substances have on biological systems. From the more than one hundred cannabinoids which were identified in the Cannabis plant so far, cannabidiol (CBD) and tetrahydrocannabinol (THC) are two of the most extensively studied phytocannabinoids. CBD is a non-psychoactive compound, which exhibits potential anti-inflammatory, neuroprotective, and anxiolytic properties, making it a promising candidate for a wide array of medical conditions. THC, known for its psychoactive effects, possesses analgesic and antiemetic properties, contributing to its therapeutic potential. In addition to THC and CBD, a wide range of additional phytocannabinoids have shown intriguing pharmacological effects, including cannabichromene (CBC), cannabigerol (CBG), and cannabinol (CBN). The endocannabinoid system, made up of the enzymes involved in the production and breakdown of endocannabinoids, cannabinoid receptors (CB1 and CB2), and endogenous ligands (endocannabinoids), is essential for preserving homeostasis in several physiological processes. Beyond their effects on the endocannabinoid system, phytocannabinoids are studied for their ability to modify ion channels, neurotransmitter receptors, and anti-oxidative pathways. The complex interaction between phytocannabinoids and biological systems offers hope for novel treatment approaches and lays the groundwork for further developments in the field of cannabinoid-based medicine. This review summarizes the state of the field, points out information gaps, and emphasizes the need for more studies to fully realize the therapeutic potential of phytocannabinoids. [ABSTRACT FROM AUTHOR]

This comprehensive review explores the utilization of chiral stationary phases (CSPs) in the context of single-column simultaneous chiral–achiral high-performance liquid chromatography (HPLC) separation methods. While CSPs have traditionally been pivotal for enantioselective drug analysis, contemporary CSPs often exhibit notable chemoselective properties. Consequently, there is a discernible trend towards the development of methodologies that enable simultaneous enantio- and chemoselective separations utilizing a single CSP-based chromatographic column. This review provides an exhaustive overview of reported HPLC methods in this domain, with a focus on four major CSP types: cyclodextrin-, glycopeptide antibiotic-, protein-, and polysaccharide-based CSPs. This article delves into the diverse applications of CSPs, encompassing various chromatographic modes such as normal phase (NP), reverse phase (RP), and polar organic (PO). This review critically discusses method development, emphasizing the additional chemoselective separation mechanisms of CSPs. It also explores possibilities for method optimization and development, concluding with future perspectives on this evolving field. Despite the inherent challenges in understanding the retention mechanisms involved in chemoselective separations, this review highlights promising trends and anticipates a growing number of simultaneous enantio- and chemoselective methods in pharmaceutical analyses, pharmacokinetic studies, and environmental sample determinations. [ABSTRACT FROM AUTHOR]

Vildagliptin (VIL) is a dipeptidyl peptidase-4 inhibitor used in the treatment of type 2 diabetes mellitus; in therapy, it is available as the enantiomerically pure S-VIL, the other enantiomer R-VIL being considered as an enantiomeric impurity. A systematic screening of 16 cyclodextrin (CD) derivatives as chiral selectors was performed at three pH levels using phosphate (pH 2.5, pH 7.0) and acetate (pH 4.5) buffers. Method optimization employed an experimental design approach, systematically investigating the effect of buffer and CD concentration, buffer pH, capillary temperature, and applied voltage on the chiral resolution and analysis time. The method's analytical performance was thoroughly assessed and subsequently employed for determining the enantiomeric purity of VIL in a pharmaceutical formulation. The properties of the inclusion complexes, such as stoichiometry and atomic level intermolecular host–guest interactions were studied by NMR measurements and molecular modeling. Native α-CD at acidic pH has demonstrated its exceptional suitability for the separation of VIL enantiomers with a favorable migration order (R-VIL followed by S-VIL). The optimized analytical conditions (75 mM acetate buffer, pH 4.5, containing 50 mM α-CD, 18 kV applied voltage, and 15 °C capillary temperature) provided a baseline separation of VIL enantiomers within 9 min. The developed method represents a cost-effective alternative to the enantiomeric impurity control of VIL. Symmetry is often a fundamental aspect of molecular structures and interactions, and our detailed analysis of the chiral recognition process contributes to the understanding of symmetry-related aspects in molecular systems. This developed method not only offers a cost-effective alternative for the enantiomeric impurity control of VIL but also provides valuable information regarding the mechanism of the chiral recognition process, aligning with the broader themes of symmetry in molecular sciences. [ABSTRACT FROM AUTHOR]

Analytical Quality by Design principles using the design of experiments were applied for the development of a capillary electrophoresis method for the determination of enantiomeric purity and chemically related impurities of tamsulosin. From initial scouting experiments, a dual cyclodextrin (CD) system composed of sulfated β‐CD and carboxymethyl‐α‐CD was selected as the chiral selector. A fractional factorial resolution V+ design was used for the identification of the critical process parameters, while a face‐centered central composite design and Monte Carlo simulations were employed for final optimization and defining the design space of the method. The experimental conditions of the working point were: 30 mM sodium phosphate buffer, pH 3.0, containing 40 mg/mL sulfated β‐CD and 7 mg/mL carboxymethyl‐α‐CD, capillary temperature 18°C, applied voltage ‐23 kV. Following the assessment of robustness by applying a Plackett‐Burman design, the method was validated according to the International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use guideline Q2(R1). The method allowed the quantification of the chiral impurity and three other related impurities at the 0.1 % level with acceptable accuracy and precision. [ABSTRACT FROM AUTHOR]

Five-membered heterocycles are essential structural components in various antibacterial drugs; the physicochemical properties of a five-membered heterocycle can play a crucial role in determining the biological activity of an antibacterial drug. These properties can affect the drug's activity spectrum, potency, and pharmacokinetic and toxicological properties. Using scientific databases, we identified and discussed the antibacterials used in therapy, containing five-membered heterocycles in their molecular structure. The identified five-membered heterocycles used in antibacterial design contain one to four heteroatoms (nitrogen, oxygen, and sulfur). Antibacterials containing five-membered heterocycles were discussed, highlighting the biological properties imprinted by the targeted heterocycle. In some antibacterials, heterocycles with five atoms are pharmacophores responsible for their specific antibacterial activity. As pharmacophores, these heterocycles help design new medicinal molecules, improving their potency and selectivity and comprehending the structure-activity relationship of antibiotics. Unfortunately, particular heterocycles can also affect the drug's potential toxicity. The review extensively presents the most successful five-atom heterocycles used to design antibacterial essential medicines. Understanding and optimizing the intrinsic characteristics of a five-membered heterocycle can help the development of antibacterial drugs with improved activity, pharmacokinetic profile, and safety. [ABSTRACT FROM AUTHOR]

Acne vulgaris stands out as the most prevalent skin disorder among teenagers and young adults, causing physical discomfort and considerable economic and psychological burdens on individuals and society. A wide range of topical and systemic therapies are available in acne treatment. Chemical peeling is a skin resurfacing technique designed to rebuild healthy skin using exfoliating substances, a simple and affordable process with various dermatological uses. Chemical peels, classified as superficial, medium, and deep, have been utilized for acne vulgaris and multiple other skin issues. In these chemical peels, a diverse range of chemical substances is employed, each with its unique mode of action. Among these, α-hydroxy and β-hydroxy acids have gathered attention for their efficacy in reducing acne lesions and enhancing overall skin appearance. Acids, such as salicylic acid, glycolic acid, or lactic acid, are commonly used in chemical peels due to their exfoliating and sebum-regulating properties. Despite the widespread use of these acids, there exists a lack of consensus regarding the most effective acid type and concentration for treating acne-prone skin. This review aims to bridge this knowledge gap by evaluating the effectiveness and safety of various organic acids used in chemical peels specifically for acne-prone skin. The findings of this comprehensive bibliographic review indicate that organic acid-based chemical peels represent effective and safe treatment options for individuals with acne-prone skin. Their adaptability sets these treatments apart; the choice of organic acid can be tailored to meet individual patient needs and tolerability levels. This personalized approach ensures that patients receive optimal care while minimizing the risks associated with the treatment. As research in this field progresses, it is anticipated that a more nuanced understanding of the ideal acid type and concentration will emerge, further enhancing the efficacy and safety of chemical peels for acne-prone skin. [ABSTRACT FROM AUTHOR]

A rapid, simple and sensitive capillary zone electrophoresis method was developed for the simultaneous determination of amlodipine besylate and telmisartan, in fixed-dose combinations, through the utilization of a UV photodiode array detector. Electrophoretic parameters such as buffer concentration and pH, system temperature, applied voltage and injection parameters, were optimized in order to improve the efficiency of the separation. The best results were obtained when employing fused silica capillary (48 cm length X 50 μm ID) and 50 mM phosphate buffer electrolyte at pH 4.50, + 25 kV applied voltage, as well as 25°C system temperature. The separation was achieved in approximately 3 minutes, with a resolution of 4.90, while the order of migration was amlodipine followed by telmisartan. The analytical performance of the method was verified with regard to linearity, precision and robustness. In addition, the limit of detection and the quantification were calculated.

A rapid and simple capillary electrophoresis method has been developed for the simultaneous determination of six extensively used cephalosporin antibiotics (cefaclor, cefadroxil, cefalexin, cefuroxim, ceftazidim, ceftriaxon). The determination of cephalosporins was performed at a pH 6.8, using a 25 mM phospate - 25 mM borate mixed buffer, + 25 kV voltage at a temperature of 25 °C. We achieved a baseline separation in approximately 10 minutes. The separation resolution was increased by addition of an anionic surfactant, 50 mM sodium dodecyl sulfate, to the buffer solution. The proposed separation was evaluated on the basis of detection and quantification limits, effective electrophoretic mobility and relative standard deviation for migration times and peak areas.

Cannabinoids, terpenophenolic chemicals found only in cannabis, are primarily responsible for cannabis pharmacologic effects; nearly 150 distinct cannabinoids have been identified thus far. Among these, the main psychoactive molecule, tetrahydrocannabinol (THC), and the non-psychoactive counterpart, cannabidiol (CBD) are distinguishable. In the past decade, a CBD-containing pharmaceutical preparation was approved by Food and Drug Administration (FDA) for the treatment of drug-resistant epileptic seizures in children, and research trials for a variety of additional medical conditions for which CBD has been suggested as a therapy are being conducted. Additionally, the number of "CBD-containing" dietary supplements, largely available online, is increasing rapidly. Consequently, the necessity for the development of qualitative and quantitative methodologies for the analysis of the bioactive components of Cannabis is rising because of the increase in the production of therapeutic cannabis products. One of the analytical methods with good potential in cannabinoids analysis is capillary electrophoresis (CE). It has advantages related to high separation efficiency, relatively short analysis time, and the small consumption of analytes and reagents which generates relatively lower operational costs than other methods. This review focuses on the use of CE techniques to examine biological matrices and plant materials for the presence of cannabinoids and other bioactive compounds found in cannabis. The advantages, drawbacks, and applicability of the various electromigration approaches are also assessed. The article provides an overview of the "state of the art" and the latest trends in CE-based methods for the determination of cannabinoids. [ABSTRACT FROM AUTHOR]

Capillary electrophoresis (CE) is a potent method for analyzing chiral substances and is commonly used in the enantioseparation and chiral purity control of pharmaceuticals from different matrices. The adoption of Quality by Design (QbD) concepts in analytical method development, optimization and validation is a widespread trend observed in various analytical approaches including chiral CE. The application of Analytical QbD (AQbD) leads to the development of analytical methods based on sound science combined with risk management, and to a well understood process clarifying the influence of method parameters on the analytical output. The Design of Experiments (DoE) method employing chemometric tools is an essential part of QbD-based method development, allowing for the simultaneous evaluation of experimental parameters as well as their interaction. In 2022 the International Council for Harmonization (ICH) released two draft guidelines (ICH Q14 and ICH Q2(R2)) that are intended to encourage more robust analytical procedures. The ICH Q14 guideline intends to harmonize the scientific approaches for analytical procedures' development, while the Q2(R2) document covers the validation principles for the use of analytical procedures including the recent applications that require multivariate statistical analyses. The aim of this review is to provide an overview of the new prospects for chiral CE method development applied for the enantiomeric purity control of pharmaceuticals using AQbD principles. The review also provides an overview of recent research (2012–2022) on the applicability of CE methods in chiral drug impurity profiling. [ABSTRACT FROM AUTHOR]

Mexiletine (MXL) is a class IB antiarrhythmic agent, acting as a non-selective voltage-gated sodium channel blocker, used in therapy as a racemic mixture R,S-MXL hydrochloride. The aim of the current study was the development of a new, fast, and efficient method for the chiral separation of MXL enantiomers using capillary electrophoresis (CE) and cyclodextrins (CDs) as chiral selectors (CSs). After an initial CS screening, using several neutral and charged CDs, at four pH levels, heptakis-2,3,6-tri-O-methyl-β-CD (TM-β-CD), a neutral derivatized CD, was chosen as the optimum CS for the enantioseparation. For method optimization, an initial screening fractional factorial design was applied to identify the most significant parameters, followed by a face-centered central composite design to establish the optimal separation conditions. The best results were obtained by applying the following optimized electrophoretic conditions: 60 mM phosphate buffer, pH 5.0, 50 mM TM-β-CD, temperature 20 °C, applied voltage 30 kV, hydrodynamic injection 50 mbar/s. MXL enantiomers were baseline separated with a resolution of 1.52 during a migration time of under 5 min; S-MXL was the first migrating enantiomer. The method's analytical performance was verified in terms of precision, linearity, accuracy, and robustness (applying a Plackett–Burman design). The developed method was applied for the determination of MXL enantiomers in pharmaceuticals. A computer modeling of the MXL-CD complexes was applied to characterize host–guest chiral recognition. [ABSTRACT FROM AUTHOR]

Orodispersible tablets (ODTs) are pharmaceutical formulations used to obtain fast therapeutic effects, usually recommended for geriatric and pediatric patients due to their improved compliance, bioavailability, ease of administration, and good palatability. This study aimed to develop ODTs with cannabidiol (CBD) phytocannabinoid extracted from Cannabis sativa used in the treatment of Lennox–Gastaut and Dravet syndromes. The tablets were obtained using an eccentric tableting machine and 9 mm punches. To develop CBD ODTs, the following parameters were varied: the Poloxamer 407 concentration (0 and 10%), the type of co-processed excipient (Prosolv® ODT G2—PODTG2 and Prosolv® EasyTab sp—PETsp), and the type of superdisintegrant (Croscarmellose—CCS, and Soy Polysaccharides—Emcosoy®—EMCS), resulting in eleven formulations (O1–O11). The following dependent parameters were evaluated: friability, disintegration time, crushing strength, and the CBD dissolution at 1, 3, 5, 10, 15, and 30 min. The dependent parameters were verified according to European Pharmacopoeia (Ph. Eur.) requirements. All the tablets obtained were in accordance with quality requirements in terms of friability (less than 1%), and disintegration time (less than 180 s). The crushing strength was between 19 N and 80 N. Regarding the dissolution test, only four formulations exhibited an amount of CBD released higher than 80% at 30 min. Taking into consideration the results obtained and using the Modde 13.1 software, an optimal formulation was developed (O12), which respected the quality criteria chosen (friability 0.23%, crushing strength of 37 N, a disintegration time of 27 s, and the target amount of CBD released in 30 min of 99.3 ± 6%). [ABSTRACT FROM AUTHOR]

Chirality is becoming an essential issue in modern pharmaceutical research as regulatory agencies emphasize the safety and efficiency of enantiomers in drug development. The development of efficient and reliable chiral separation methods became a necessity in the last 30 years, and capillary electrophoresis (CE), due to its relatively low costs and "green" features, is attracting increased attention. Cyclodextrin (CD) and their derivatives are the most frequently used chiral selectors (CSs) in CE, however, the use of antibiotics as CSs represents an interesting alternative. Various classes of antibiotics (aminoglycosides, ansamycins, glycopeptides, lincosamides, macrolides, tetracyclines) have been used more or less successfully for the enantio-separation of pharmaceuticals. Antibiotics offer the possibility of a multitude of potential interactions (electrostatic, inclusion, hydrogen bonding, etc.) due to their chemical diversity, allowing the enantio-separation of analytes with a wide range of structural characteristics. This article aims to review the application of various classes of antibiotics in the CE enantio-separation of pharmaceuticals. Antibiotic physiochemical characteristics, variables impacting enantio-separation, advantages, and disadvantages when certain antibiotics are used as CSs in CE are also explored. [ABSTRACT FROM AUTHOR]

A novel, validated, reversed-phase (RP), chiral high performance liquid chromatography (HPLC) method was developed for the enantiopurity control analysis of naproxen, a frequently used non-steroidal anti-inflammatory agent using polysaccharide-type chiral stationary phase (CSP). In the screening phase of method development, seven columns were tested in polar organic (PO) mode using mobile phases consisting of 0.1% acetic acid in methanol, ethanol, 2-propanol, and acetonitrile. Enantiorecognition was observed only in five cases. The best enantioseparation was observed on a Lux Amylose-1 column with 0.1% (v/v) acetic acid in ethanol with a resolution (Rs) of 1.24. The enantiomer elution order was unfavorable, as the distomer eluted after the eutomer. When the ethanolic mobile phase was supplemented with water, enantiomer elution order reversal was observed, indicating a difference in the enantiorecognition mechanism upon switching from PO to RP mode. Furthermore, by changing ethanol to methanol, not only lower backpressure, but also higher resolution was obtained. Subsequent method optimization was performed using a face-centered central composite design (FCCD) to achieve higher chiral resolution in a shorter analysis time. Optimized parameters offering baseline separation were as follows: Lux Amylose-1 stationary phase, thermostated at 40 °C, and a mobile phase consisting of methanol:water:acetic acid 85:15:0.1 (v/v/v), delivered with 0.65 mL/min flow rate. Using these optimized parameters, a Rs = 3.21 ± 0.03 was achieved within seven minutes. The optimized method was validated according to the ICH guidelines and successfully applied for the analysis of different pharmaceutical preparations, such as film-coated tablets and gel, as well as fixed-dose combination tablets, containing both naproxen and esomeprazole. [ABSTRACT FROM AUTHOR]

Photochemical degradation of drugs can lead to degradation products with potential toxic or allergizing effects for the human body. A significant amount of work has been carried out over the past few decades to clarify the molecular mechanism of photosensitizing processes observed after the administration of certain drugs and exposure to light. There is a close relation between the photosensitizer effect of a drug and its chemical structure. Compounds possessing certain moieties and functional groups in their molecular structure, like aromatic chromophore systems or photo-dissociable bonds that can form free radicals, and consequently are susceptible to have light-induced adverse effects. Photoionization, photodissociation, photoaddition and photoisomerization are the main chemical processes, which can occur during the photochemical decomposition of a pharmaceutical compound. The current study is a short review describing photochemical degradation of certain pharmaceuticals, presenting specific examples from various pharmaceutical classes for the different types of decomposition mechanisms. In vivo methods and clinical tests available for the investigation of photosensitizing reactions are also discussed. [ABSTRACT FROM AUTHOR]

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Venlafaxine (VFX) is a serotonin and norepinephrine reuptake inhibitor chiral drug used in therapy as an antidepressant in the form of a racemate consisting of R‐ and S‐VFX. The two enantiomers of VFX exhibit different pharmacological activities: R‐VFX inhibits both norepinephrine and serotonin synaptic reuptake, whereas S‐VFX inhibits only the serotonin one. R‐ and S‐VFX are metabolized in the liver to the respective R‐ and S‐O‐desmethylvenlafaxine (ODVFX), R‐ and S‐N‐desmethylvenlafaxine (NDVFX), and R‐ and S‐N,O‐didesmethylvenlafaxine (NODVFX). The pharmacological profile of ODVFX is close to that of VFX, whereas the other two chiral metabolites (NDVFX and NODVFX) have lower affinity for the receptor sites. The pharmacokinetics of the VFX enantiomers appear stereoselective, including the metabolism process. In the past 20 years, several studies describing the enantioselective analysis of R‐ and S‐VFX in pharmaceutical formulations and its chiral metabolites in biological matrices were published. These methods encompass liquid chromatography coupled with UV detection, mass spectrometry, or tandem mass spectrometry, and capillary electrophoresis. This paper reviews the published methods used for the determination of the individual enantiomers of VFX and its chiral metabolites in different matrices. [ABSTRACT FROM AUTHOR]

Duloxetine (DLX) is a widely used antidepressant drug belonging to the class of selective serotonin and norepinephrine reuptake inhibitors (SNRIs); its efficacy has been demonstrated in the treatment of not only major depressive disorders but also diabetic neuropathic pain, generalized anxiety disorder, fibromyalgia or stress urinary incontinence. It is a chiral substance and is used in therapy in the form of the enantiopure S‐DLX, which is twice as active as R‐DLX. Several methods have been published for the achiral and chiral determination of DLX in pharmaceuticals, biological materials and environmental samples, the majority using liquid chromatography and capillary electrophoresis coupled with different detection techniques (UV detection, fluorescence, mass spectrometry). The aim of the current review is to provide a systematic survey of the analytical techniques used for the determination of DLX from different matrices. [ABSTRACT FROM AUTHOR]

Objective: Pharmaceutical serialization is a process in the pharmaceutical industry that offers a secure solution to track and authenticate drugs in the distribution chain. The unique recognition number for every drug unit helps to identify and combat counterfeit products. This paper aims to highlight the advantages of serialization implementation as an innovative tool to combat globally the counterfeiting drugs phenomenon. Methods: Worldwide a considerable effort was focused on enhancing medicines identification. Analytical methods, development of the new lab equipment, digital solutions, and blockchain technology are the new directions for the future. Also, legislation needs to be correlated at the international level between the pharmaceutical industry, distribution, and pharmacies. Results: A good collaboration between responsible entities should be implemented to protect public health and to promote patients' access to safe medicines. A directive implemented on European Union focused on fake drugs, Global Monitoring and Surveillance System launched by the World Health Organization, or the international campaign "Fight the Fakes" are remarkable examples. Conclusions: An efficient joint effort between the pharmaceutical industry and law enforcement is required. Counterfeit medicines are a worldwide threat to public health and demand a unitary pharmaceutical serialization system to be implemented as an ideal solution. [ABSTRACT FROM AUTHOR]

Citalopram (CIT) is a frequently used modern antidepressant that inhibits selectively serotonin reuptake in the brain. It has a chiral center in its structure and is used in therapy as both racemic mixture and pure enantiomer as its pharmacological effect is almost entirely associated with S‐CIT. The aim of this study was the development of a simple and rapid capillary electrophoresis (CE) method for the separation and quantification of CIT enantiomers. To establish the optimum chiral selector, several native and derivatized, neutral, and ionized cyclodextrins (CDs) were examined at different pH levels. An experimental design strategy was adopted for method optimization; a fractional factorial design was applied for screening purposes to identify significant experimental factors followed by a face‐centered central composite design used for optimization purposes. Computational modeling was used to obtain information on the interaction energy and the geometry of the complexes to aid in the understanding of chiral separation mechanism. The best results were obtained when using a 25‐mM phosphate buffer at pH 7.0, 3‐mM CM‐β‐CD as chiral selector, 17.5°C temperature, 15‐kV voltage, and 50 mbar/s hydrodynamic injection. The separation time was fast, below 3 min, and the migration order was S‐CIT followed by R‐CIT. The analytical performance of the method was verified in terms of precision, linearity, accuracy, sensibility, and robustness, and the method was applied for the determination of CIT enantiomers from pharmaceutical preparations. [ABSTRACT FROM AUTHOR]

Chemical peel is a dermato-cosmetic procedure used to destroy and remove, in a controlled manner and under the supervision of the specialists, the degraded parts of the skin, in order to allow acceleration of the skin regeneration process. Based on their depth of skin penetration chemical peels are classified into superficial, medium and deep peels. The substances used in the chemical peels differ from each other depending on the effective action depth. Different peel agents with an appropriate peel depth should be selected based on the problem to be treated, considering also the nature of skin pathology. To achieve the best results other factors, such as skin type and characteristics, region to be treated, safety issues, healing time, and patient adherence, should also be considered. The present review focuses on the particularities of the substances used in various peel types, highlighting recent advances in chemical peel technology and explaining suggested application of certain substances in different peel types. [ABSTRACT FROM AUTHOR]

A direct HPLC method was developed for the enantioseparation of pantoprazole using macrocyclic glycopeptide‐based chiral stationary phases, along with various methods to determine the elution order without isolation of the individual enantiomers. In the preliminary screening, four macrocyclic glycopeptide‐based chiral stationary phases containing vancomycin (Chirobiotic V), ristocetin A (Chirobiotic R), teicoplanin (Chirobiotic T), and teicoplanin‐aglycone (Chirobiotic TAG) were screened in polar organic and reversed‐phase mode. Best results were achieved by using Chirobiotic TAG column and a methanol‐water mixture as mobile phase. Further method optimization was performed using a face‐centered central composite design to achieve the highest chiral resolution. Optimized parameters, offering baseline separation (resolution = 1.91 ± 0.03) were as follows: Chirobiotic TAG stationary phase, thermostated at 10°C, mobile phase consisting of methanol/20mM ammonium acetate 60:40 v/v, and 0.6 mL/min flow rate. Enantiomer elution order was determined using HPLC hyphenated with circular dichroism (CD) spectroscopy detection. The online CD signals of the separated pantoprazole enantiomers at selected wavelengths were compared with the structurally analogous esomeprazole enantiomer. For further verification, the inline rapid, multiscan CD signals were compared with the quantum chemically calculated CD spectra. Furthermore, docking calculations were used to investigate the enantiorecognition at molecular level. The molecular docking shows that the R‐enantiomer binds stronger to the chiral selector than its antipode, which is in accordance with the determined elution order on the column—S‐ followed by the R‐isomer. Thus, combined methods, HPLC‐CD and theoretical calculations, are highly efficient in predicting the elution order of enantiomers. [ABSTRACT FROM AUTHOR]

Citalopram (CIT) is a highly selective serotonin reuptake inhibitor (SSRI) frequently used in the treatment of major depressive disorders. It has a chiral centre in its structure and is used in therapy both as a racemic mixture (R,S‐CIT) and a pure enantiomer (S‐CIT). The differences between the pharmacokinetic and pharmacological profiles of the two enantiomers are well established. Consequently, the development of new efficient chiral analysis methods for their enantiomeric separation is a topic of great actuality. CIT metabolism is stereoselective as it is metabolized in chiral active metabolites, which retain considerable SSRI activity and contribute to the pharmacological effect. Chiral analytical methods are employed for the determination of enantiomeric ratio in pharmaceutical preparations and for monitoring the enantiomer levels in biological samples for therapeutic and toxicologic purposes. The current study reviews the published literature for the chiral analysis of CIT and its metabolites based on chromatographic and electrophoretic methods coupled with UV, fluorescence and mass spectrometry detectors. [ABSTRACT FROM AUTHOR]

The treatment of obesity includes along with lifestyle modification, pharmacological therapy. Until now there are only few drugs approved by FDA for the treatment of obesity, therefore physicians often prescribe off-label drugs. In this article we review tolerability, side effects and contraindication of both on-label and off-label drugs used in obesity treatment. Currently there are 5 approved drugs for long-term use (phentermine/topiramate, bupropion/naltrexone, orlistat, lorcaserin and liraglutide) and 4 approved drugs for short-term use (phentermine, diethylpropion, benzphetamin, phendimetrizine). On-label therapy is generally well tolerated, with specific contraindication for each drug. On the other side, off-label therapy can be considered safe only for drugs that have already long-term safety data (metformin, phentermine). For other drugs (pramlintide, zonisamide, GLP-1 agonists) off-label prescribing should be limited to clinical trials due to their unknown adverse effect profile. [ABSTRACT FROM AUTHOR]

Capillary zone electrophoresis (CZE) could be a useful technique for the quantification of active substances from transdermal therapeutic systems (TTSs). TTSs are pharmaceutical forms in development that may release one or more active substances with some significant advantages as increased compliance to treatment, avoidance of first hepatic passage and low manufacturing costs. A simple, reliable, efficient, and lowcost CZE method was developed and validated for the simultaneous determination of levofloxacin (fluoroquinolone) and meloxicam (non-steroidal anti-inflammatory) from TTSs. The selected experimental parameters were 50 mM borax (pH 9.3) as background electrolyte, +25 kV applied voltage, 50 mbar/5 seconds hydrodynamic injection and 40°C temperature, using an uncoated fused-silica capillary with (51 cm total length/43 cm effective length, 50 µm i.d.). CZE experiments were performed in less than four minutes with a resolution of 7.79 at a wavelength of 335 nm. Validation of the method presented good linearity data, precision (RDS% < 1 for migration times and RDS% < 2 for peaks area) and sensitivity (LOD 3.43 and 16.05 µg·mL-1, LOQ 10.38 and 54.55 µg·mL-1 for levofloxacin and meloxicam, respectively). Recovery of the active substances ranged between 85.14% and 96.38%. Our developed CZE method proved its applicability for analysis of the two substances from TTSs. [ABSTRACT FROM AUTHOR]

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Through doping, we understand the use by athletes of substances prohibited by the antidoping agencies in order to gain a competitive advantage. Since sport plays an important role in physical and mental education and in promoting international understanding and cooperation, the widespread use of doping products and methods has consequences not only on health of the athletes, but also upon the image of sport. Thus, doping in sports is forbidden for both ethical and medical reasons. Narcotics and analgesics, anabolic steroids, hormones, selective androgen receptor modulators are among the most frequently utilized substances. Although antidoping controls are becoming more rigorous, doping and, very importantly, masking doping methods are also advancing, and these are usually one step ahead of doping detection techniques. Depending on the sport practiced and the physical attributes it requires, the athletes will look for one or more of the following benefits of doping: recovering from an injury, increasing body recovery capacity after training, increasing muscle mass and strength, decreasing fat tissue, increasing endurance. Finally, when we look once again at a doping scandal, amazed at how much animosity against those caught can exist; the question is: is it really such a disaster as presented by the media or a silent truth under our eyes, but which many of us have refused to accept? [ABSTRACT FROM AUTHOR]

Objective: Miconazole, an imidazole antifungal derivative, is a very hydrophobic compound, a major drawback in obtaining topical pharmaceutical formulations with optimal bioavailability. Cyclodextrins (CDs) may increase local drug delivery by enhancing the drug release and/or permeation. The aim of the study is the characterization of inclusion complexes between miconazole and different CD derivatives. Methods: Several CD derivatives were tested in the experiments. The binary systems between miconazole and different CDs were prepared in 1:1 molar ratios by physical-mixture and kneading methods. Differential scanning calorimetry (DSC) and Fourier transformed-infrared spectroscopy (FT-IR) methods were used to characterize solid state interactions between miconazole and CDs in their binary systems. Results: The FT-IR analysis suggests the formation of a new solid phase, indicating a molecular interaction between the components. The DSC analysis sustains the hypothesis of formation of partial inclusion complexes between miconazole nitrate and CD. Conclusion: The thermic behaviour of the complexes depends both on the preparation method and the composition of the products. [ABSTRACT FROM AUTHOR]

To describe the chemical structure and characterize physico-chemical properties of organometallic complexes it is necessary to use a complex set of analysis methods. Thus, this review has been compiled as a relevant guide which includes the most commonly used methods of analysis in the study of silver complexes with antibacterial quinolones, compounds with promising biological potential. This selection of analysis methods puts on balance the obtained data and the accessibility of the experimental approach. The steps to follow in order to obtain reliable structural information about organometallic complexes of silver, particularly the silver complexes of antibacterial quinolones, are established and presented in the review. [ABSTRACT FROM AUTHOR]

Fluoxetine is a widely used antidepressant belonging to the selective serotonin reuptake inhibitor class; it is used in the treatment of major depression, obsessive compulsive, premenstrual dysphoric, panic and post-traumatic stress disorders. Fluoxetine is an optical active pharmaceutical substance, which is used as a racemate in therapy, but stereospecific interactions associated with the serotonin-reuptake carrier, for both the parent drug and its active metabolite, norfluoxetine, have been described in the literature. Therefore, the stereoselective analysis of fluoxetine and norfluoxetine is important in order to characterize the pharmacokinetic and pharmacodynamic profile of the analytes. Several chromatographic and electrophoretic methods have been published in the literature for the chiral discrimination of fluoxetine enantiomers from different matrices. The purpose of the current review is to provide a systematic survey of the analytical techniques used for the chiral determination of fluoxetine and norfluoxetine covering a period of ~25 years. [ABSTRACT FROM AUTHOR]