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1.
Int J Nanomedicine ; 17: 1549-1566, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35401001

RESUMO

Purpose: Pseudoephedrine (PSE) has rapid absorption and metabolism, which limits its pharmacologic actions. We postulated that pseudoephedrine nanoparticles (PSE-NPs) with high bioavailability could overcome this limitation. The defensive function of PSE-NPs nanoparticles against adriamycin-induced reproductive toxicity in mice was studied. Methods: We encapsulated PSE in polylactide-polyglycolide nanoparticles (PLGA-NPs) and verified their protective activity against testicular injury in vivo and in vitro. Results: We report a promising delivery system that loads PSE into PLGA-NPs and finally assembles it into a nanocomposite particle. In vitro, PSE-NPs reduced the adriamycin-induced apoptosis of GC-1 cells significantly, improved mitochondrial energy metabolism and promoted expression of the proteins related to the gonadotropin-releasing hormone (GnRh) receptor signaling pathway. In vivo, evaluation of sperm indices and histology showed that adriamycin could induce testicular toxicity. PSE-NPs significantly increased the sperm motility of mice, reduced the percent apoptosis and oxidative stress of testes, increased serum levels of GnRh, activated the GnRhR signaling pathway in testes and promoted expression of meiosis-related factors. Conclusion: In view of their safety and efficiency, these PSE-NPs have potential applications in alleviating adriamycin-induced reproductive toxicity.


Assuntos
Nanopartículas , Pseudoefedrina , Animais , Doxorrubicina/toxicidade , Hormônio Liberador de Gonadotropina , Masculino , Camundongos , Transdução de Sinais , Motilidade Espermática
2.
Sci Total Environ ; 828: 154446, 2022 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-35283119

RESUMO

The occurrence of 130 pharmaceutically active compounds (PhACs) in sediments collected from 70 sampling sites in the Odra River estuary (SW Baltic Sea) was investigated. The highest concentration levels of the compounds were found in the vicinity of effluent discharge from two main Szczecin wastewater treatment plants: "Pomorzany" and "Zdroje", and nearby the seaport and shipyard. The highest environmental risks (RQ > 1) were observed for pseudoephedrine (RQ = 14.0), clindamycin (RQ = 7.3), nalidixic acid (RQ = 3.8), carbamazepine (RQ = 1.8), fexofenadine (RQ = 1.4), propranolol (RQ = 1.1), and thiabendazole (RQ = 1.1). RQ for each compound varied depending on the sampling sites. High environmental risk was observed in 30 sampling sites for clindamycin, 22 sampling sites for pseudoephedrine, 19 sampling sites for nalidixic acid, 4 sampling sites for carbamazepine, and 3 sampling sites for fexofenadine. The medium environmental risk (0.1 < RQ < 1) was observed for 16 compounds: amisulpride, amitriptyline, amlodipine, atropine, bisoprolol, chlorpromazine, lincomycin, metoprolol, mirtazapine, moclobemide, ofloxacin, oxazepam, tiapride, tolperisone, verapamil, and xylometazoline. Due to the scarcity of toxicological data related to benthic organisms, only an approximate assessment of the environmental risk of PhACs is possible. Nevertheless, the compounds with medium and high risk should be considered as pollutants of high environmental concern whose occurrence in the environment should remain under close scrutiny.


Assuntos
Estuários , Poluentes Químicos da Água , Carbamazepina/análise , Clindamicina , Monitoramento Ambiental , Ácido Nalidíxico , Preparações Farmacêuticas , Pseudoefedrina , Medição de Risco , Rios , Poluentes Químicos da Água/análise
3.
J Sep Sci ; 45(5): 1051-1058, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34984820

RESUMO

Ephedrae Herba is one of the most commonly used herbal medicines, and it has been shown that most of the clinical efficacy for cold and asthma is exerted by its alkaloidal components. A simple and sensitive high-performance liquid chromatography method was developed using a perfluorooctyl column for the simultaneous determination of five alkaloids (norephedrine, norpseudoephedrine, ephedrine, pseudoephedrine, and methylephedrine) in Ephedrae Herba. The mobile phase comprising acetonitrile and 15 mM ammonium trifluoroacetate was used to elute the targets in isocratic elution mode. The method was validated for linearity (R2  > 0.999), repeatability, intraday and interday precision, recoveries with trueness (93.87-110.99%), limits of detection (5.35-5.76 µg/mL), and limits of quantification (20 µg/mL). The quantitative results revealed that the developed method was precise and accurate. Then it was successfully applied to determine the difference in the contents of three batches of Ephedrae Herba from three pharmaceutical companies.


Assuntos
Alcaloides , Medicamentos de Ervas Chinesas , Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas/análise , Efedrina/análise , Pseudoefedrina/análise
4.
J AOAC Int ; 105(3): 703-716, 2022 Apr 27.
Artigo em Inglês | MEDLINE | ID: mdl-35015880

RESUMO

BACKGROUND: A combination of paracetamol, pseudoephedrine, chlorpheniramine, and sodium benzoate in (Cold-Flu) 1,2,3 Syrup dosage form is specified for the treatment of common cold and flu symptoms. OBJECTIVE: The functional role of this study is to develop a novel, reliable, and selective stability-indicating reversed-phase ultra-performance liquid chromatography (RP-UPLC) method for simultaneous identification of a quaternary mixture of paracetamol, pseudoephedrine, chlorpheniramine, and sodium benzoate in (Cold-Flu) 1,2,3 Syrup dosage form. METHOD: The specific method is accomplished using an Acquity UPLC HSS T3 C18 column (2.1 mm × 100 mm), 1.8 µm particle size with pore size 100 Å, utilizing a mixture of purified water-methanol-trifluoroacetic acid (72.5:27.5:1.5, v/v) as the mobile phase at a flow rate of 0.3 mL/min. The column void volume is 1.15 min. UPLC detection is adjusted at 205 nm using a photodiode array detector. RESULTS: Calibration curves are obtained in the linearity ranges: 25-500 µg/mL for paracetamol, 10-50 µg/mL for pseudoephedrine, 0.5-5 µg/mL for chlorpheniramine, and 3-30 µg/mL for sodium benzoate with a correlation coefficient > 0.9992. The mean recovery of the developed method is tested and shows good recovery results between 99-101%; selectivity and forced degradation studies are investigated as per the International Council for Harmonisation Guidelines and no interference is detected due to degradation peaks. CONCLUSION: The proposed stability-indicating UPLC method for simultaneous determination of the three drugs, paracetamol, pseudoephedrine, and chlorpheniramine, with a preservative sodium benzoate in (Cold-Flu) 1,2,3 Syrup dosage form is successfully accomplished, developed, and validated, and can be easily used in the analysis of drugs in pure or dosage form. HIGHLIGHTS: The novelty of the current research work lies in the development of the UPLC method for simultaneous determination of a quaternary mixture of paracetamol, pseudoephedrine, chlorpheniramine, and sodium benzoate in (Cold-Flu) 1,2,3 Syrup dosage form.


Assuntos
Clorfeniramina , Resfriado Comum , Acetaminofen/análise , Clorfeniramina/análise , Cromatografia Líquida de Alta Pressão/métodos , Humanos , Pseudoefedrina/análise , Benzoato de Sódio/análise
5.
Jpn J Ophthalmol ; 66(1): 94-100, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34279747

RESUMO

PURPOSE: To quantitatively evaluate the acute effects of pseudoephedrine on the macular microvasculature using optical coherence tomography angiography (OCTA). STUDY DESIGN: Randomized placebo-controlled clinical study. METHODS: In this study, 60 right eyes of 60 healthy subjects were divided into 2 groups. The study group received 60 mg of pseudoephedrine and the control group received a placebo. All participants underwent OCTA at baseline and 1 h after oral intake. Superficial macular flow area, foveal avascular zone (FAZ), superficial macular vessel density, central foveal thickness (CFT) and subfoveal choroidal thickness (SFCT) were analyzed. RESULTS: Baseline superficial macular flow area, FAZ area, superficial macular vessel density, CFT and SFCT measurements in the study and control groups showed no significant difference (p > 0.05 for all). Oral pseudoephedrine intake caused a significant reduction in superficial macular flow area, FAZ area, superficial macular vessel density and SFCT measurements when compared with baseline (p < 0.05 for all). However, there was no significant difference in CFT after oral pseudoephedrine intake (p > 0.05). CONCLUSION: Oral pseudoephedrine intake causes a significant decrease in superficial macular blood flow and SFCT. Impairmant of macular microcirculation can be detected noninvasively and quantitavitely by OCTA.


Assuntos
Pseudoefedrina , Tomografia de Coerência Óptica , Angiofluoresceinografia , Voluntários Saudáveis , Humanos , Microcirculação , Vasos Retinianos/diagnóstico por imagem
6.
Biol Pharm Bull ; 44(11): 1781-1789, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34719654

RESUMO

Dried terrestrial stems of Ephedra sinica are known as 'Ephedra herb.' The pharmacological effects are mainly related to two major ingredients, (-)-ephedrine and (+)-pseudoephedrine (total alkaloids which are defined in Japanese Pharmacopoeia, TA). In this study, in order to aid in cultivation and breeding, the stability of TA content and stem dry weight of 46 E. sinica genets was evaluated from the first year of transplantation to the sixth year. TA content and composition ratio of these genets were stable after the second year, and dry weight was stable after the fourth year. These traits showed high inter-genet variability but low annual variability for each genet. Additionally, rank correlation coefficients of each trait among the genets were high. There was no significant correlation between these traits. Furthermore, to assess the reproducibility of these traits in clones, we evaluated TA content and dry weight of three clonal lines with high TA contents. TA content and composition ratio of the clonal lines were also stable after the second year of transplantation, and dry weight of the clonal lines was also stable after the fourth year. Moreover, TA content and composition ratio in each clonal line were comparable with those of each original genet after the second year. These results suggested that ephedrine alkaloids content and dry weight of E. sinica plants are stable, and that these traits are highly reproducible in clones. Therefore, selection breeding of E. sinica using vegetative propagation can be effective for high and stable quality of Ephedra herb.


Assuntos
Alcaloides/análise , Ephedra sinica/química , Caules de Planta/química , Efedrina/análise , Pseudoefedrina/análise , Reprodutibilidade dos Testes
7.
Molecules ; 26(22)2021 Nov 19.
Artigo em Inglês | MEDLINE | ID: mdl-34834083

RESUMO

A sensitive and reproducible liquid chromatography-tandem mass spectrometry (LC-MS/MS) system was developed and fully validated for the simultaneous determination of ephedrine and pseudoephedrine in human plasma after oral administration of the herbal prescription Ojeok-san (OJS); 2-phenylethylamine was used as the internal standard (IS). Both compounds presented a linear calibration curve (r2 ≥ 0.99) over a concentration range of 0.2-50 ng/mL. The developed method was fully validated in terms of selectivity, lower limit of quantitation, precision, accuracy, recovery, matrix effect, and stability, according to the regulatory guidelines from the U.S. Food and Drug Administration and the Korea Ministry of Food and Drug Safety. This validated method was successfully applied for the pharmacokinetic assessment of ephedrine and pseudoephedrine in 20 healthy Korean volunteers administered OJS.


Assuntos
Efedrina , Extratos Vegetais/administração & dosagem , Pseudoefedrina , Espectrometria de Massas em Tandem , Administração Oral , Cromatografia Líquida , Efedrina/administração & dosagem , Efedrina/farmacocinética , Feminino , Humanos , Masculino , Pseudoefedrina/administração & dosagem , Pseudoefedrina/farmacocinética , República da Coreia
8.
Pediatrics ; 148(5)2021 11.
Artigo em Inglês | MEDLINE | ID: mdl-34607934

RESUMO

BACKGROUND AND OBJECTIVES: In 2008, over-the-counter cough and cold medications (CCMs) underwent labeling changes in response to safety concerns, including fatalities, reported in children exposed to CCMs. The objective of this study is to describe fatalities associated with exposures to CCMs in children <12 years old that were detected by a safety surveillance system from 2008 to 2016. METHODS: Fatalities in children <12 years old that occurred between 2008 and 2016 associated with oral exposure to one or more CCMs were identified by the Pediatric Cough and Cold Safety Surveillance System. An expert panel reviewed all cases to determine the causal relationship between the exposure and death, if the intent of exposure was therapeutic, and if the dose was supratherapeutic. Other contributing factors related to the child's death were also identified as part of a root cause analysis. RESULTS: Of the 180 eligible fatalities captured during the study period, 40 were judged by the expert panel to be either related or potentially related to the CCM. Of these, the majority (n = 24; 60.0%) occurred in children <2 years old and involved nontherapeutic intent (n = 22; 55.0%). The most frequently involved index ingredient was diphenhydramine (n = 28; 70.0%). In 6 cases (n = 6; 15.0%), the CCM was administered to murder the child. In another 7 cases (n = 7; 17.5%), death followed the intentional use of the CCM to sedate the child. CONCLUSIONS: Pediatric fatalities associated with CCMs occurred primarily in young children after deliberate medication administration with nontherapeutic intent by a caregiver.


Assuntos
Antitussígenos/envenenamento , Medicamentos sem Prescrição/envenenamento , Antitussígenos/administração & dosagem , Bromofeniramina/envenenamento , Criança , Pré-Escolar , Clorfeniramina/envenenamento , Dextrometorfano/envenenamento , Difenidramina/administração & dosagem , Difenidramina/envenenamento , Doxilamina/envenenamento , Rotulagem de Medicamentos , Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos/mortalidade , Feminino , Guaifenesina/envenenamento , Homicídio/estatística & dados numéricos , Humanos , Lactente , Masculino , Medicamentos sem Prescrição/administração & dosagem , Fenilefrina/envenenamento , Pseudoefedrina/envenenamento
9.
Phytother Res ; 35(10): 5847-5860, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34472141

RESUMO

The coronavirus disease 2019 has infected over 150 million people worldwide and led to over 3 million deaths. Severe acute respiratory syndrome (SARS)-CoV-2 lineages B.1.1.7, B.1.617, B.1.351, and P.1 were reported to have higher infection rates than that of wild one. These mutations were noticed to happen in the receptor-binding domain of spike protein (S-RBD), especially mutations N501Y, E484Q, E484K, K417N, K417T, and L452R. Currently, there is still no specific medicine against the virus; moreover, cytokine storm is also a dangerous factor for severe infected patients. In this study, potential S-RBD-targeted active monomers from traditional Chinese medicine Ephedra sinica Stapf (ephedra) were discovered by virtual screening. NanoBiT assay was performed to confirm blocking activities of the screened compounds against the interaction between SARS-CoV-2 S-RBD and angiotensin-converting enzyme 2 (ACE2). We further analyzed the blocking effect of the active compounds on the interactions of mutated S-RBD and ACE2 by computational studies. Moreover, antiinflammatory activities were evaluated using qRT-PCR, enzyme-linked immune sorbent assay, and Western blot analysis. As a result, pseudoephedrine (MHJ-17) and its derivative (MHJ-11) were found as efficient inhibitors disrupting the interactions between ACE2 and both wild and mutated S-RBDs. In addition, they also have antiinflammatory activities, which can be potential drug candidates or lead compounds for further study.


Assuntos
COVID-19 , Pseudoefedrina , Humanos , Ligação Proteica , SARS-CoV-2 , Glicoproteína da Espícula de Coronavírus/metabolismo
10.
Yakugaku Zasshi ; 141(8): 1041-1048, 2021.
Artigo em Japonês | MEDLINE | ID: mdl-34334549

RESUMO

Some controlled substances, such as stimulants and narcotics, have asymmetric carbons in their molecules. Because the enantiomers do not always show the same pharmacological effects, and there are substances with different controls due to differences in their stereochemistry, a simple and unambiguous method for assessment of the composition of enantiomers is necessary. In this study, to develop a simple and rapid stereoscopic identification method for methamphetamine and its raw materials (ephedrine and pseudoephedrine), the 1H-NMR method was studied using three commercially available chiral solvating agents (CSAs); 1,1'-bi(2-naphthol)(BINOL), 2,2,2-trifluoro-1-(9-anthryl)ethanol (TFAE) and α-methoxy-α-(trifluoromethyl)phenylacetic acid (MTPA). In addition, the accuracy of the optical purity, which was measured using samples mixed with enantiomers in various ratios, was investigated. The NMR peaks of the enantiomers were separated by adding (R)- or (S)-form of BINOL, TFAE or MTPA to the chloroform-d solution of methamphetamine, ephedrine or pseudoephedrine. A sufficient discrimination of enantiomers was obtained by adding about 10 equal amounts of each CSA to the solutions. With regard to the optical purity, it was possible to determine accurately the mixing of small amounts of enantiomers of about 5% even if the NMR peaks did not reach the baseline separation, when impurity peaks do not overlap. This method will be one of the useful techniques for the rapid and simple discrimination of enantiomers of illegal methamphetamine and its raw materials.


Assuntos
Controle de Medicamentos e Entorpecentes/métodos , Éteres , Drogas Ilícitas/química , Drogas Ilícitas/isolamento & purificação , Espectroscopia de Ressonância Magnética/métodos , Metanfetamina/química , Metanfetamina/isolamento & purificação , Naftóis , Fenilacetatos , Clorofórmio/química , Efedrina/química , Éteres/química , Naftóis/química , Fenilacetatos/química , Pseudoefedrina/química , Solventes , Estereoisomerismo
12.
Int J Mol Sci ; 22(10)2021 May 13.
Artigo em Inglês | MEDLINE | ID: mdl-34067981

RESUMO

Pseudoephedrine (PSE) is a drug with a long history of medical use; it is helpful in treating symptoms of the common cold and flu, sinusitis, asthma, and bronchitis. Due to its central nervous system (CNS) stimulant properties and structural similarity to amphetamine, it is also used for non-medical purposes. The substance is taken as an appetite reducer, an agent which eliminates drowsiness and fatigue, to improve concentration and as a doping agent. Due to its easier availability, it is sometimes used as a substitute for amphetamine or methamphetamine. Pseudoephedrine is also a substrate (precursor) used in the production of these drugs. Time will tell whether legal restrictions on the sale of this drug will reduce the scale of the problem associated with its misuse.


Assuntos
Broncodilatadores/uso terapêutico , Metanfetamina/efeitos adversos , Pseudoefedrina/uso terapêutico , Medição de Risco/métodos , Transtornos Relacionados ao Uso de Substâncias/prevenção & controle , Humanos , Metanfetamina/química , Transtornos Relacionados ao Uso de Substâncias/etiologia
13.
Spectrochim Acta A Mol Biomol Spectrosc ; 260: 119943, 2021 Nov 05.
Artigo em Inglês | MEDLINE | ID: mdl-34030038

RESUMO

A comparative study of successive spectrophotometric resolution technique for the simultaneous determination of a challengeable quaternary mixture of Chlorpheniramine maleate (CPM), Pseudoephedrine hydrochloride (PSE), Ibuprofen (IBU) and Caffeine (CAF) is presented, without preliminary physical separation steps. Several successive steps were applied on built-in spectrophotometer software utilizing zero and/or derivative and/or ratio spectra of the studied components. These methods, namely, Dual amplitude difference (DAD) as a novel method, Constant multiplication coupled with spectrum subtraction method (CM-SS), Factorized first derivative coupled with derivative transformation method (FD1 -DT) and Derivative ratio method (DD1). The calibration graphs are linear over the concentration range of 10.0-80.0 µg/mL,150.0-900.0 µg/mL, 200.0-1400.0 µg/mL and 3.0-30.0 µg/mL for CPM, PSE, IBU and CAF, respectively. The specificity of suggested methods was studied via laboratory prepared (diverse ratios) mixtures and were successfully applied for Antiflu® capsules' analysis. Moreover, sample enrichment via In Silico (via software of spectrophotometer) and In Lab (via spiking with pure sample) techniques was elected for a pharmaceutical dosage form analysis comprising CPM and PSE as minor components. Accuracy, precision and specificity were between the valid limits. Validation steps were done in accordance with the ICH guidelines. Moreover, statistical comparison was carried out between the obtained and reported results for pure powder form and no significant difference appeared.


Assuntos
Laboratórios , Pseudoefedrina , Simulação por Computador , Ibuprofeno , Reprodutibilidade dos Testes , Espectrofotometria
14.
Rev Endocr Metab Disord ; 22(4): 1013-1025, 2021 12.
Artigo em Inglês | MEDLINE | ID: mdl-33945051

RESUMO

Obesity is a major public health problem worldwide. Only relatively few treatment options are, at present, available for the management of obese patients. Furthermore, treatment of obesity is affected by the widespread misuse of drugs and food supplements. Ephedra sinica is an old medicinal herb, commonly used in the treatment of respiratory tract diseases. Ephedra species contain several alkaloids, including pseudoephedrine, notably endowed with indirect sympathomimetic pharmacodynamic properties. The anorexigenic effect of pseudoephedrine is attributable primarily to the inhibition of neurons located in the hypothalamic paraventricular nucleus (PVN), mediating satiety stimuli. Pseudoephedrine influences lipolysis and thermogenesis through interaction with ß3 adrenergic receptors and reduces fat accumulation through down-regulation of transcription factors related to lipogenesis. However, its use is associated with adverse events that involve to a large extent the cardiovascular and the central nervous system. Adverse events of pseudoephedrine also affect the eye, the intestine, and the skin, and, of relevance, sudden cardiovascular death related to dietary supplements containing Ephedra alkaloids has also been reported. In light of the limited availability of clinical data on pseudoephedrine in obesity, along with its significantly unbalanced risk/benefit profile, as well as of the psychophysical susceptibility of obese patients, it appears reasonable to preclude the prescription of pseudoephedrine in obese patients of any order and degree.


Assuntos
Alcaloides , Ephedra sinica , Efedrina/efeitos adversos , Humanos , Obesidade/induzido quimicamente , Obesidade/tratamento farmacológico , Pseudoefedrina/uso terapêutico
15.
Ann Allergy Asthma Immunol ; 127(3): 342-348.e2, 2021 09.
Artigo em Inglês | MEDLINE | ID: mdl-34000435

RESUMO

BACKGROUND: Although it is known that oral antihistamine-pseudoephedrine combination tablets have a faster onset than intranasal corticosteroid sprays in the treatment of allergic rhinitis after the first dose, the magnitude of change has not been measured in a comparative manner. Furthermore, the sensation of sprayed liquid in the nose may lead patients to mistakenly believe that intranasal steroid sprays work instantly. OBJECTIVE: To evaluate, numerically, nasal airflow changes provided by a single dose of loratadine-pseudoephedrine tablet (LP) and fluticasone propionate nasal spray (FP) in participants experiencing allergic rhinitis symptoms, including nasal congestion. METHODS: This single-center, double-blinded, placebo-controlled, crossover study evaluated objective nasal airflow changes in patients with a documented sensitivity to ragweed pollen. Participants were randomized to receive 1 of 4 treatment sequences, and their peak nasal inspiratory flow (PNIF) was measured in a span of 4 hours after pollen exposure in an environmental exposure unit. RESULTS: Average change in PNIF was 31% with LP in the course of the study, significantly greater than with placebo and FP (12% and 15%, respectively; P < .001). Nevertheless, FP did not produce a significant change compared with its placebo. At hour one post-dose, LP had a clinically significant 31% increase in PNIF, whereas FP only yielded an 8.6% increase (P < .001). Measurable nasal airflow improvements are associated with the opening of nasal passages, allowing congested patients to breathe more freely. CONCLUSION: A single dose of LP quickly and significantly (P < .001) improved nasal airflow after ragweed pollen challenge in an environmental exposure unit. Comparatively, FP did not display this same benefit. TRIAL REGISTRATION: ClinicalTrials.gov Identifier: NCT03443843.


Assuntos
Antialérgicos/administração & dosagem , Fluticasona/administração & dosagem , Loratadina/administração & dosagem , Descongestionantes Nasais/administração & dosagem , Pseudoefedrina/administração & dosagem , Rinite Alérgica/tratamento farmacológico , Administração Intranasal , Adulto , Antialérgicos/efeitos adversos , Estudos Cross-Over , Método Duplo-Cego , Combinação de Medicamentos , Feminino , Fluticasona/efeitos adversos , Humanos , Loratadina/efeitos adversos , Masculino , Pessoa de Meia-Idade , Cavidade Nasal/fisiologia , Descongestionantes Nasais/efeitos adversos , Sprays Nasais , Pseudoefedrina/efeitos adversos , Fenômenos Fisiológicos Respiratórios , Rinite Alérgica/fisiopatologia , Comprimidos , Adulto Jovem
16.
Int J Biol Macromol ; 182: 1248-1258, 2021 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-33992650

RESUMO

There is a continued global effort to prevent the spread of prescription drug abuse. In particular, chemical structure of pseudoephedrine hydrochloride (PSE), an over-the-counter medication, is very similar to that of methamphetamine (MET). The aim of this study was to develop abuse-deterrent formulations (ADF) of PSE by using thermal modified starch (TMR). PSE is a water-soluble drug, but it is intended to inhibit extraction from the extraction medium in excess tablets. Starch-based formulations were successfully developed using cross-linking agent and lipid. The extraction (%) of PSE from TMR7-L5 formulation (equivalent to 5 tablets) were 75.3% in DW, 2.7% in ethyl alcohol, and 63.0% in 40% ethyl alcohol (v/v) at 60 °C for 30 min. Moreover, TMR7-L5 formulation delayed drug release compared to the commercial product in in vitro release. In conclusion, the development of ADFs using a starch-based formulation shows novelty and has potential to prevent drug abuse.


Assuntos
Metanfetamina/química , Pseudoefedrina/química , Amido/química
17.
Molecules ; 26(6)2021 Mar 13.
Artigo em Inglês | MEDLINE | ID: mdl-33805790

RESUMO

A highly specific and sensitive proton nuclear magnetic resonance (1H-NMR) method has been developed for the quantification of ephedrine alkaloid derivatives in Ephedra herbal commercial prescriptions. At the region of δ 4.0 to 5.0 ppm in the 1H NMR spectrum, the characteristic signals are separated well from each other, and six analogues in total, methylephedrine (ME), ephedrine (EP), norephedrine (NE), norpseudoephedrine (NP), pseudoephedrine (PE), and methylpseudoephedrine (MP) could be identified. The quantities of these compounds are calculated by the relative ratio of the integral values of the target peak for each compound to the known concentrations of the internal standard anthracene. The present method allows for a rapid and simple quantification of ephedrine alkaloid derivatives in Ephedra-related commercial prescriptions without any preliminary purification steps and standard compounds, and accordingly it can be a powerful tool to verify different Ephedra species. In comparison to conventional chromatographic methods, the advantages of this method include the fact that no standard compounds are required, the quantification can be directly performed on the crude extracts, a better selectivity for various ephedrine alkaloid derivatives, and the fact that a very significant time-gain may be achieved.


Assuntos
Alcaloides/análise , Ephedra/química , Efedrina/análogos & derivados , Efedrina/análise , Ephedra/classificação , Estudos de Viabilidade , Humanos , Limite de Detecção , Espectroscopia de Ressonância Magnética/métodos , Espectroscopia de Ressonância Magnética/estatística & dados numéricos , Medicina Tradicional Chinesa , Fenilpropanolamina/análise , Preparações de Plantas/química , Pseudoefedrina/análise , Especificidade da Espécie
18.
Biosens Bioelectron ; 180: 113109, 2021 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-33677356

RESUMO

Here, we present a new family of hierarchical porous hybrid materials as an innovative tool for ultrasensitive and selective sensing of enantiomeric drugs in complex biosamples via chiral surface-enhanced Raman spectroscopy (SERS). Hierarchical porous hybrid films were prepared by the combination of mesoporous plasmonic Au films and microporous homochiral metal-organic frameworks (HMOFs). The proposed hierarchical porous substrates enable extremely low limit of detection values (10-12 M) for pseudoephedrine in undiluted blood plasma due to dual enhancement mechanisms (physical enhancement by the mesoporous Au nanostructures and chemical enhancement by HMOF), chemical recognition by HMOF, and a discriminant function for bio-samples containing large biomolecules, such as blood components. We demonstrate the effect of each component (mesoporous Au and microporous AlaZnCl (HMOF)) on the analytical performance for sensing. The growth of AlaZnCl leads to an increase in the SERS signal (by around 17 times), while the use of mesoporous Au leads to an increase in the signal (by up to 40%). In the presence of a complex biomatrix (blood serum or plasma), the hybrid hierarchical porous substrate provides control over the transport of the molecules inside the pores and prevents blood protein infiltration, provoking competition with existing plasmonic materials at the limit of detection and enantioselectivity in the presence of a multicomponent biomatrix.


Assuntos
Técnicas Biossensoriais , Nanopartículas Metálicas , Ouro , Plasma , Pseudoefedrina , Estereoisomerismo
19.
Inflammopharmacology ; 29(3): 673-682, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-33772383

RESUMO

Pseudoephedrine (substituted phenethylamine) is well known as psychotic and bronchodilator. Numerous studies on phenethylamine derivatives indicated that these agents have the potential to abolish inflammatory responses in the non-biological and biological systems. These facts provided the basis to conduct a study on pseudoephedrine to explore its therapeutics in Complete Freund's Adjuvant (CFA)-induced arthritis. Furthermore, existing treatment approaches for RA associated with limited effect on chronic immunological models. Real-time polymerase chain reaction (q-PCR) was performed to execute the expression of pro and anti-inflammatory cytokines in treated and non-treated arthritic rats. These findings were further co investigate by histological observations. The paw volume, paw diameter, weight variations and arthritic score were determined at specific days throughout the experiment of 28 days. Pseudoephedrine at all doses significantly (p < 0.001) suppressed the expression of PGE2, TNF-α, IL-1ß and IL-6. Moreover, pseudoephedrine (20 and 40 mg/kg) caused significant augmentation of IL-4 and IL-10. Similarly, the drug expressed a significant anti-arthritic effect by reducing the paw volume, paw diameter and arthritic score. Similarly, it also reverts the reduction in body weight of arthritic rats at all above-mentioned doses. These findings supported the anti-arthritic potential of pseudoephedrine and recommended it for clinical trials.


Assuntos
Antirreumáticos/uso terapêutico , Artrite Experimental/tratamento farmacológico , Citocinas/antagonistas & inibidores , Pseudoefedrina/uso terapêutico , Fator de Necrose Tumoral alfa/antagonistas & inibidores , Animais , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Antirreumáticos/química , Antirreumáticos/farmacologia , Artrite Experimental/metabolismo , Artrite Experimental/patologia , Citocinas/metabolismo , Relação Dose-Resposta a Droga , Regulação para Baixo/efeitos dos fármacos , Regulação para Baixo/fisiologia , Adjuvante de Freund , Interleucina-10/agonistas , Interleucina-10/metabolismo , Interleucina-1beta/antagonistas & inibidores , Interleucina-1beta/metabolismo , Interleucina-4/agonistas , Interleucina-4/metabolismo , Interleucina-6/antagonistas & inibidores , Interleucina-6/metabolismo , Fenetilaminas/química , Fenetilaminas/farmacologia , Fenetilaminas/uso terapêutico , Pseudoefedrina/química , Pseudoefedrina/farmacologia , Ratos , Ratos Sprague-Dawley , Fator de Necrose Tumoral alfa/metabolismo
20.
J Nat Med ; 75(3): 707-716, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-33599897

RESUMO

A discriminant LC/MS quantitative analysis of ephedrine (EP) and pseudoephedrine (PEP) in Ephedrae herba was performed. Aerial parts of three Ephedra species were separated into internodes and extracted using Finger Masher with minimum loss. The contents of EP and PEP were measured by LC/MS/MS using the multiple reaction monitoring (MRM) method. Their contents in old-year branches were lower than those current-year branches and tended to be higher in the middle part than in the tip of each branch. The content ratio of EP and PEP was reversed in some branches depending on their extent of growth. In E. sinica, the contents were low at the first internode closest to the central main stem at each branch. The contents drastically increased from the second internode and were highest at the third internode. There was a strong correlation between the internode distance and alkaloid (EP + PEP) contents. The distribution of alkaloids in one internode was examined and the results showed that the part closest to the node had the lowest contents.


Assuntos
Ephedra/química , Efedrina/análise , Pseudoefedrina/análise , Alcaloides/análise , Cromatografia Líquida , Medicamentos de Ervas Chinesas/análise , Ephedra/classificação , Caules de Planta/química , Espectrometria de Massas em Tandem
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