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1.
Molecules ; 26(10)2021 May 19.
Artículo en Inglés | MEDLINE | ID: mdl-34069585

RESUMEN

This study aimed to design an effective nanoparticle-based carrier for the oral delivery of fisetin (FST) with improved biopharmaceutical properties. FST-loaded nanoparticles were prepared with polyvinyl alcohol (PVA) and poly(lactic-co-glycolic acid) (PLGA) by the interfacial deposition method. A central composite design of two independent variables, the concentration of PVA and the amount of PLGA, was applied for the optimization of the preparative parameter. The responses, including average particle size, polydispersity index, encapsulation efficiency, and zeta potential, were assessed. The optimized formulation possessed a mean particle size of 187.9 nm, the polydispersity index of 0.121, encapsulation efficiency of 79.3%, and zeta potential of -29.2 mV. The morphological observation demonstrated a globular shape for particles. Differential scanning calorimetry and powder X-ray diffraction studies confirmed that the encapsulated FST was presented as the amorphous state. The dissolution test indicated a 3.06-fold increase for the accumulating concentrations, and the everted gut sac test showed a 4.9-fold gain for permeability at the duodenum region. In conclusion, the optimized FST-loaded nanoparticle formulation in this work can be developed as an efficient oral delivery system of FST to improve its biopharmaceutic properties.


Asunto(s)
Composición de Medicamentos , Flavonoles/farmacología , Nanotecnología , Rastreo Diferencial de Calorimetría , Cromatografía Líquida de Alta Presión/métodos , Diseño de Fármacos , Concentración de Iones de Hidrógeno , Mucosa Intestinal/efectos de los fármacos , Mucosa Intestinal/metabolismo , Tamaño de la Partícula , Difracción de Polvo , Reproducibilidad de los Resultados , Análisis Espectral/métodos
2.
J Sci Food Agric ; 101(12): 4934-4945, 2021 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-33543470

RESUMEN

BACKGROUND: The flower of Dendranthema morifolium Ramat Tzvel has been widely used as a nutritional health supplement worldwide. However, most of the studies have focused on the flower and the rest of the plant was neglected. Our hypothesis is that similar flavonoids may be present at different parts of D. morifolium, and the flavonoids may undergo a similar biotransformation pathway within the body. To investigate this hypothesis, an in vivo pharmacokinetic experimental model was developed to explore the comparative biotransformation of luteolin and apigenin after administration of D. morifolium extracts (10 g kg-1 , p.o.) in freely moving rats. Because luteolin and apigenin mainly underwent phase II metabolism, the metabolic enzymes of ß-glucuronidase/sulfatase or ß-glucuronidase were used to hydrolyze the plasma sample, depending on the biotransformation pathway involved. RESULTS: The results revealed that luteolin and apigenin mainly went through glucuronide and sulfate conjugations, respectively, in both the extract of flowers and the stem-and-leaf group. In addition, the area under the concentration curve (AUClast ) of luteolin glucuronides and sulfates in the group administered the stem-and-leaf extract was approximately 4.6 times higher than that of the flower extract group. The dominant products of biotransformation for apigenin were sulfates. CONCLUSION: These findings support our hypothesis that not only the flower parts of D. morifolium, but also the stem-and-leaf parts contain rich flavones, including glycosides and aglycone, and they undergo similar biotransformation pathways. © 2021 Society of Chemical Industry.


Asunto(s)
Apigenina/metabolismo , Chrysanthemum/química , Luteolina/metabolismo , Extractos Vegetales/metabolismo , Animales , Apigenina/química , Chrysanthemum/metabolismo , Flavonoides/química , Flavonoides/metabolismo , Flores/química , Hidrólisis , Luteolina/química , Estructura Molecular , Extractos Vegetales/química , Hojas de la Planta/química , Tallos de la Planta/química , Ratas , Ratas Sprague-Dawley
3.
Int J Mol Sci ; 21(7)2020 Apr 04.
Artículo en Inglés | MEDLINE | ID: mdl-32260319

RESUMEN

Andrographolide (AG), a major diterpene lactone isolated from Andrographis paniculata (Burm. f.) Nees (Acanthaceae), possesses a wide spectrum of biological activities. However, its poor water solubility and low bioavailability limit its clinical application. Therefore, this study aimed to develop a solid dispersion (SD) formulation to increase the aqueous solubility and dissolution rate of AG. Different drug-polymer ratios were used to prepare various SDs. The optimized formulation was characterized for differential scanning calorimetry, Fourier transform infrared spectroscopy, and powder X-ray diffraction. The analysis indicated that the optimized SD enhanced AG solubility and dissolution rates by changing AG crystallinity to an amorphous state. The dissolution behaviors of the optimum SD composed of an AG-polyvinylpyrrolidone K30-Kolliphor EL ratio of 1:7:1 (w/w/w) resulted in the highest accumulated dissolution (approximately 80%). Pharmacokinetic studies revealed that Cmax/dose and the AUC/dose increased by 3.7-fold and 3.0-fold, respectively, compared with AG suspension. Furthermore, pretreatment using the optimized AG-SD significantly increased the swimming time to exhaustion by 1.7-fold and decreased the plasma ammonia level by 71.5%, compared with the vehicle group. In conclusion, the optimized AG-SD formulation appeared to effectively improve its dissolution rate and oral bioavailability. Moreover, the optimized AG-SD provides a promising treatment against physical fatigue.


Asunto(s)
Diterpenos/administración & dosificación , Composición de Medicamentos/métodos , Fatiga/tratamiento farmacológico , Administración Oral , Amoníaco/sangre , Animales , Disponibilidad Biológica , Rastreo Diferencial de Calorimetría , Modelos Animales de Enfermedad , Diterpenos/farmacocinética , Fatiga/metabolismo , Masculino , Ratas , Suspensiones , Difracción de Rayos X
4.
Molecules ; 25(14)2020 Jul 08.
Artículo en Inglés | MEDLINE | ID: mdl-32650503

RESUMEN

Sesamin (SSM) is a water-insoluble compound that is easily eliminated by liver metabolism. To improve the solubility and bioavailability of SSM, this study developed and characterized a self-nanoemulsifying drug delivery system (SNEDDS) for the oral delivery of SSM and conducted pharmacokinetic assessments. Oil and surfactant materials suitable for SNEDDS preparation were selected on the basis of their saturation solubility at 37 ± 0.5 °C. The mixing ratios of excipients were determined on the basis of their dispersibility, transmittance (%), droplet sizes, and polydispersity index. An SNEDDS (F10) formulation comprising glyceryl trioctanoate, polyoxyethylene castor oil, and Tween 20 at a ratio of 10:10:80 (w/w/w) was the optimal formulation. This formulation maintained over 90% of its contents in different storage environments for 12 weeks. After the self-emulsification of SNEDDS, the SSM dispersed droplet size was 66.4 ± 31.4 nm, intestinal permeability increased by more than three-fold, relative bioavailability increased by approximately 12.9-fold, and absolute bioavailability increased from 0.3% to 4.4%. Accordingly, the developed SNEDDS formulation can preserve SSM's solubility, permeability, and bioavailability. Therefore, this SNEDDS formulation has great potential for the oral administration of SSM, which can enhance its pharmacological application value.


Asunto(s)
Dioxoles , Portadores de Fármacos , Lignanos , Nanopartículas/química , Animales , Dioxoles/química , Dioxoles/farmacocinética , Dioxoles/farmacología , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Portadores de Fármacos/farmacología , Emulsiones , Lignanos/química , Lignanos/farmacocinética , Lignanos/farmacología , Masculino , Permeabilidad , Polisorbatos/química , Ratas , Ratas Sprague-Dawley , Solubilidad
5.
Molecules ; 25(14)2020 Jul 17.
Artículo en Inglés | MEDLINE | ID: mdl-32709024

RESUMEN

Glucocorticoids are widely used anti-inflammatory drugs in clinical settings. However, they can induce skeletal muscle atrophy by reducing fiber cross-sectional area and myofibrillar protein content. Studies have proven that antioxidants can improve glucocorticoid-induced skeletal muscle atrophy. Quercetin is a potent antioxidant flavonoid widely distributed in fruits and vegetables and has shown protective effects against dexamethasone-induced skeletal muscle atrophy. In this study, we demonstrated that dexamethasone significantly inhibited cell growth and induced cell apoptosis by stimulating hydroxyl free radical production in C2C12 skeletal muscle cells. Our results evidenced that quercetin increased C2C12 skeletal cell viability and exerted antiapoptotic effects on dexamethasone-treated C2C12 cells by regulating mitochondrial membrane potential (ΔΨm) and reducing oxidative species. Quercetin can protect against dexamethasone-induced muscle atrophy by regulating the Bax/Bcl-2 ratio at the protein level and abnormal ΔΨm, which leads to the suppression of apoptosis.


Asunto(s)
Antioxidantes/farmacología , Músculo Esquelético/efectos de los fármacos , Atrofia Muscular/tratamiento farmacológico , Quercetina/farmacología , Antioxidantes/química , Apoptosis/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Dexametasona/toxicidad , Flavonoides/química , Flavonoides/farmacología , Glucocorticoides/química , Glucocorticoides/farmacología , Humanos , Fibras Musculares Esqueléticas/efectos de los fármacos , Músculo Esquelético/lesiones , Músculo Esquelético/metabolismo , Músculo Esquelético/patología , Atrofia Muscular/inducido químicamente , Atrofia Muscular/patología
6.
Pharm Biol ; 58(1): 545-552, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-32538243

RESUMEN

Context: Danggui Buxue Tang (DBT), one of the popular Danggui (DG) decoctions, has traditionally been used to nourish 'qi' (vital energy) and enrich 'blood' (body circulation). DBT may possess performance-enhancing effects.Objective: This work determines whether DBT can improve physical capacity and alter energy expenditure under exercise training.Materials and methods: Forty male Wistar rats were assigned to four groups: sedentary (SE), exercise training (ET), ET supplemented with 0.3 g/kg rat/d DG extract, and ET supplemented with 1.8 g/kg rat/d DBT extract. The supplementations were administered via oral gavage. During the 21-day treatment period, the exercised groups were subjected to a protocol of swimming training with a gradually increased load. Physical performance evaluation was assessed using the forelimb grip strength test and an exhaustive swimming test. Muscle glycogen contents and exercise-related biochemical parameters were analysed.Results: Both herbal supplementations remarkably increased the grip strength (DG by 49.7% and DBT by 85.7%) and prolonged the swimming time (DG by 48.4% and DBT by 72.7%) compared with SE. DBT spared a certain amount of glycogen in the muscle cells under exercise training. Regarding the regulation of fuel usage, DBT had a positive impact alongside ET on promoting aerobic glycolysis via significantly decreasing serum lactate by 31.6% and lactic dehydrogenase levels by 61.8%.Conclusions: This study found that DBT could be considered a promising sports ergogenic aid for athletic population or fitness enthusiasts. Future work focussing on isolating the bioactive components that truly provide the ergogenic effects would be of interest.


Asunto(s)
Adaptación Fisiológica/efectos de los fármacos , Adaptación Fisiológica/fisiología , Suplementos Dietéticos , Medicamentos Herbarios Chinos/farmacología , Rendimiento Físico Funcional , Natación/fisiología , Animales , Medicamentos Herbarios Chinos/aislamiento & purificación , Masculino , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Raíces de Plantas , Ratas , Ratas Wistar
7.
Biomed Chromatogr ; 31(8)2017 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-28009448

RESUMEN

Cat's claw is a large woody vine with hook-like thorns, and has been traditionally used to treat inflammatory disorders in South and Central America. In this study, a rapid, validated high-performance liquid chromatographic (HPLC) method using a silica monolithic column was developed for the simultaneous determination of oxindole alkaloids, namely rhynchophylline, pteropodine, isomitraphylline and isopteropodine, in cat's claw. The ionic liquid-based microwave-assisted extraction (ILMAE), considered as an environmentally friendly and powerful tool, was first applied in the extraction of oxindole alkaloids. To optimize the HPLC method, the stationary phases, pH values of mobile phase and flow rates were investigated. The validated HPLC method using a Monolithic RP18e column (100 × 4.6 mm) enables these analytes to be separated almost twice as fast as with a conventional particulate column (~16 vs ~30 min) with limits of quantification and detection of 0.5 and 0.15 µg/mL, respectively. The ILMAE conditions were optimized by the Taguchi orthogonal array design. In comparison with conventional water boiling extraction, ILMAE offers almost four times higher yields within an extremely short extraction time. The developed HPLC coupled with ILMAE method could be efficient and practical for rapid determination of oxindole alkaloids in cat's claw.


Asunto(s)
Alcaloides/análisis , Uña de Gato/química , Cromatografía Líquida de Alta Presión/métodos , Alcaloides Indólicos/análisis , Indoles/análisis , Compuestos de Espiro/análisis , Cromatografía Líquida de Alta Presión/economía , Cromatografía Líquida de Alta Presión/instrumentación , Líquidos Iónicos/química , Límite de Detección , Microondas , Oxindoles , Dióxido de Silicio/química
8.
Int J Mol Sci ; 18(9)2017 Aug 25.
Artículo en Inglés | MEDLINE | ID: mdl-28841149

RESUMEN

Resveratrol (RES), a natural polyphenolic compound, exerts anti-fatigue activity, but its administration is complicated by its low water solubility. To improve RES bioavailability, this study developed a self-nanoemulsifying drug delivery system (SNEDDS) for RES and evaluated its anti-fatigue activity and rat exercise performance by measuring fatigue-related parameters, namely lactate, ammonia, plasma creatinine phosphokinase, and glucose levels and the swimming time to exhaustion. Through solubility and emulsification testing, the optimized SNEDDS composed of Capryol 90, Cremophor EL, and Tween 20 was developed; the average particle size in this formulation, which had favorable self-emulsification ability, was approximately 41.3 ± 4.1 nm. Pharmacokinetic studies revealed that the oral bioavailability of the optimized RES-SNEDDS increased by 3.2-fold compared with that of the unformulated RES-solution. Pretreatment using the RES-SNEDDS before exercise accelerated the recovery of lactate after exercise; compared with the vehicle group, the plasma ammonia level in the RES-SNEDDS group significantly decreased by 65.4%, whereas the glucose level significantly increased by approximately 1.8-fold. Moreover, the swimming time to exhaustion increased by 2.1- and 1.8-fold, respectively, compared with the vehicle and RES-solution pretreatment groups. Therefore, the developed RES-SNEDDS not only enhances the oral bioavailability of RES but may also exert anti-fatigue pharmacological effect.


Asunto(s)
Sistemas de Liberación de Medicamentos , Emulsiones , Estilbenos/administración & dosificación , Administración Oral , Animales , Disponibilidad Biológica , Análisis Químico de la Sangre , Cromatografía Líquida de Alta Presión , Composición de Medicamentos , Glucógeno/metabolismo , Tamaño de la Partícula , Ratas , Resveratrol , Solubilidad , Estilbenos/química , Estilbenos/farmacocinética
9.
Molecules ; 22(11)2017 Nov 03.
Artículo en Inglés | MEDLINE | ID: mdl-29099795

RESUMEN

Hemp nut is commonly incorporated into several food preparations; however, most countries set regulations for hemp products according to their cannabinoid content. In this study, we have developed an efficient microwave-assisted extraction (MAE) method for cannabinoids (i.e., Δ9-tetrahydrocannabinol, cannabidiol, and cannabinol) in hemp nut. Optimization of the MAE procedure was conducted through single factor experiments and response surface methodology (RSM). A comparative study was also conducted to determine the differences in the extraction yields and morphology of hemp nut between MAE and reference extraction methods, namely heat reflux extraction (HRE), Soxhlet extraction (SE), supercritical fluid extraction (SFE), and ultrasound-assisted extraction (UAE). Among the independent variables in RSM, the temperature was the most significant parameter. The optimal conditions of MAE were as follows: extraction solvent of methanol, microwave power of 375 W, temperature of 109 °C, and extraction time of 30 min. Compared with reference extraction methods, MAE achieved the highest extraction yields of total cannabinoids in hemp nut (6.09 µg/g for MAE; 4.15 µg/g for HRE; 5.81 µg/g for SE; 3.61 µg/g for SFE; 3.73 µg/g for UAE) with the least solvent consumption and shortest time. Morphological observations showed that substantial cell rupturing occurred in the microstructure of hemp nut after MAE, indicating enhanced dissolution of the target compounds during the extraction process. The MAE method is thus a rapid, economic, and environmentally friendly extraction method that is both effective and practical for industrial applications.


Asunto(s)
Cannabinoides/química , Cannabinoides/aislamiento & purificación , Cannabis/química , Nueces/química , Extractos Vegetales/química , Fraccionamiento Químico , Microondas , Propiedades de Superficie , Temperatura
11.
Molecules ; 21(10)2016 Oct 16.
Artículo en Inglés | MEDLINE | ID: mdl-27754467

RESUMEN

An analytical method entailing high-performance liquid chromatography coupled with electrochemical detection was developed for determining forsythiaside (FTS) in rat plasma. Rat plasma samples were prepared through efficient trichloroacetic acid deproteination. FTS and the internal standard were chromatographically separated on a reversed-phase core-shell silica C18 column (100 mm × 2.1 mm, i.d. 2.6 µm), with a mobile phase consisting of an acetonitrile-0.05-M phosphate solution (11.8:88.2, v/v), at a flow rate of 400 µL/min. The calibration curve, with r² > 0.999, was linear in the 20-1000 ng/mL range. The intra- and interday precision were less than 9.0%, and the accuracy ranged from 94.5% to 106.5% for FTS. The results indicated that the newly developed HPLC-EC method is more sensitive than previous reported methods using UV detection, and this new analytical method is applied successfully for the pharmacokinetic study of FTS. The hydrogel delivery system can efficiently improve bioavailability and mean residual time for FTS, as evidenced by the 2.5- and 6.3-fold increase of the area under the curve and the extension of the half-life, respectively.


Asunto(s)
Antiinfecciosos/farmacocinética , Cromatografía Líquida de Alta Presión/métodos , Técnicas Electroquímicas/métodos , Glicósidos/farmacocinética , Plasma/química , Animales , Antiinfecciosos/administración & dosificación , Disponibilidad Biológica , Glicósidos/administración & dosificación , Semivida , Hidrogel de Polietilenoglicol-Dimetacrilato/química , Masculino , Extractos Vegetales/administración & dosificación , Extractos Vegetales/farmacocinética , Ratas
12.
Molecules ; 21(6)2016 Jun 01.
Artículo en Inglés | MEDLINE | ID: mdl-27258243

RESUMEN

This study aimed to examine the efficacy of epirubicin-loaded gelatin hydrogel (EPI-H) in the treatment of superficial urothelium carcinoma. Hydrogel was prepared by Schiff base-crosslinking of gelatin with glutaraldehyde. EPI-H exhibited high entrapment efficiency (59.87% ± 0.51%). EPI-H also increased epirubicin accumulation in AY-27 cells when compared with the effect of aqueous solutions of epirubicin (EPI-AQ); respective epirubicin-positive cell counts were 69.0% ± 7.6% and 38.3% ± 5.8%. EPI-H also exhibited greater cytotoxicity against AY-27 cells than that of EPI-AQ; IC50 values were 13.1 ± 1.1 and 7.5 ± 0.3 µg/mL, respectively. Cystometrograms showed that EPI-H reduced peak micturition, threshold pressures, and micturition duration, and that it increased bladder compliance more so than EPI-AQ. EPI-H enhanced epirubicin penetration into basal cells of urothelium in vivo, whereas EPI-AQ did so only to the umbrella cells. EPI-H inhibited tumor growth upon intravesical instillation to tumor-bearing bladder of F344 rats, inducing higher levels of caspase-3 expression than that observed with EPI-AQ treatment; the number of caspase-3 positive cells in treated urothelium carcinoma was 13.9% ± 4.0% (EPI-AQ) and 34.1% ± 1.0%, (EPI-H). EPI-H has value as an improved means to administer epirubicin in intravesical instillation treatments for bladder cancer.


Asunto(s)
Antibióticos Antineoplásicos/administración & dosificación , Sistemas de Liberación de Medicamentos , Epirrubicina/administración & dosificación , Hidrogel de Polietilenoglicol-Dimetacrilato , Administración Intravesical , Animales , Antibióticos Antineoplásicos/farmacología , Apoptosis/efectos de los fármacos , Caspasa 3/metabolismo , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Modelos Animales de Enfermedad , Portadores de Fármacos/química , Epirrubicina/farmacología , Epitelio/efectos de los fármacos , Epitelio/metabolismo , Epitelio/patología , Hidrogel de Polietilenoglicol-Dimetacrilato/química , Permeabilidad , Ratas , Transducción de Señal/efectos de los fármacos , Neoplasias de la Vejiga Urinaria/tratamiento farmacológico , Neoplasias de la Vejiga Urinaria/metabolismo , Neoplasias de la Vejiga Urinaria/patología , Ensayos Antitumor por Modelo de Xenoinjerto
13.
Biomed Chromatogr ; 28(3): 439-45, 2014 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-24122787

RESUMEN

An ultra-performance liquid chromatography with tandem mass spectrometry (UPLC-MS/MS) method was developed and validated to concurrently determine rhynchophylline and hirsutine in rat plasma. The sample preparation of rat plasma was achieved by alkalization and liquid-liquid extraction. The mass transition of precursor ion → product ion pairs were monitored at m/z 385.2 → 160.0 for rhynchophylline, m/z 369.3 → 144.0 for hirsutine and m/z 414.0 → 220.0 for noscapine (internal standard). This method revealed linear relationships from 2.5 to 50 ng/mL (r(2) > 0.997) for rhynchophylline and from 2.5 to 50 ng/mL (r(2) > 0.998) for hirsutine. The limit of quantification values for rhynchophylline and hirsutine in rat plasma were both 2.5 ng/mL. Intra-day and inter-day precisions were within 10.6% and 12.5%, respectively, for rhynchophylline and hirsutine, and the accuracy (bias) was <10%. Liquid-liquid extraction of rat plasma samples resulted in insignificant matrix effect, and the extraction recoveries were >83.6% for rhynchophylline, 73.4% for hirsutine and 90.7% for the internal standard. This method was applied successfully to a pharmacokinetic study of rhynchophylline and hirsutine in rats after oral administration.


Asunto(s)
Alcaloides/sangre , Cromatografía Líquida de Alta Presión/métodos , Alcaloides Indólicos/sangre , Extractos Vegetales/administración & dosificación , Espectrometría de Masas en Tándem/métodos , Uncaria/química , Administración Oral , Alcaloides/química , Alcaloides/farmacocinética , Animales , Alcaloides Indólicos/química , Alcaloides Indólicos/farmacocinética , Modelos Lineales , Masculino , Oxindoles , Extractos Vegetales/química , Ratas , Ratas Sprague-Dawley , Reproducibilidad de los Resultados , Sensibilidad y Especificidad
14.
Biomed Chromatogr ; 28(5): 630-6, 2014 May.
Artículo en Inglés | MEDLINE | ID: mdl-24264996

RESUMEN

Epimedin C, an ingredient of Herba Epimedii, has potential for treatment of cardiovascular disease and bone loss. However, there is still no sensitive analytical method to monitor epimedin C in biological samples. The goal of this study was to develop a sensitive and reliable method based on a LC-MS/MS for evaluating the pharmacokinetics of epimedin C after administration of Herba Epimedii in rat. Electrospray ionization in positive-ion mode and multiple reaction monitoring were used to identify and quantitate active components. Analytes were separated by a reverse-phase C18 column. Liquid-liquid extraction using ethyl acetate, evaporation and reconstitution was used to plasma sample preparation. Mass transition of precursor ion → product ion pairs were monitored at m/z 823.4 → 313.1 for epimedin C and m/z 237.1 → 178.9 for carbamazepine (internal standard). A calibration curve gave good linearity (r > 0.999) over the concentration range 2.5-500 ng/mL. Pharmacokinetic data demonstrated that there was rapid distribution and slow elimination after epimedin C administration (1 mg/kg, i.v.). Oral bioavailabilities of epimedin C in the pure compound and in the Herba Epimedii were around 0.58% and 0.13%, respectively. The result suggests that other herbal ingredients of Herba Epimedii may suppress the oral bioavailability of epimedin C.


Asunto(s)
Cromatografía Líquida de Alta Presión/métodos , Medicamentos Herbarios Chinos/farmacocinética , Flavonoides/farmacocinética , Espectrometría de Masas en Tándem/métodos , Administración Oral , Animales , Disponibilidad Biológica , Medicamentos Herbarios Chinos/administración & dosificación , Medicamentos Herbarios Chinos/química , Flavonoides/administración & dosificación , Masculino , Ratas , Ratas Sprague-Dawley
15.
Drug Test Anal ; 2024 Apr 23.
Artículo en Inglés | MEDLINE | ID: mdl-38653500

RESUMEN

To prevent athletes from unintentional doping, the anti-doping authorities in Taiwan have launched several sports-prohibited substances inquiry services since 2008. This study aimed to enhance the prevention of sports-prohibited substance misuse by analyzing data collected from major nationwide service systems, enabling the identification of trends in athletes' exposure to drugs and prohibited substances. The study collected over 30,000 data points from three major national anti-doping inquiry systems, spanning from 2008 to 2022. The information of the users consulted products, prohibited substances, and sports disciplines in the data were calculated and categorized. The usage of inquiry systems has shown an increasing trend from 2008 to 2022. Athletes comprised the majority of users (> 40%), significantly outnumbering other user groups (all below 20%). Among the inquiries, Western medicine accounted for the highest percentage (up to 79.6%), and it also contained the majority of the prohibited substances. Interestingly, traditional Chinese medicines had a higher chance (35.9%) of containing prohibited substances, as indicated by the mobile application. The prohibited substances mainly belonged to class S6 stimulants and S9 glucocorticoids. Among the daily medicinal products and nutritional supplements encountered by sports personnel, approximately 30% of them were found to contain prohibited substances. Future educational efforts should focus on raising awareness about traditional Chinese medicines and drugs for the common cold, ADHD, and pain relief, as well as their regulation, to prevent the misuse of prohibited substances.

16.
Molecules ; 18(6): 7323-35, 2013 Jun 21.
Artículo en Inglés | MEDLINE | ID: mdl-23792897

RESUMEN

Epimedium sagittatum (Sieb. et Zucc.) Maxim is one of the herbs used to treat erectile dysfunction in Traditional Chinese Medicine. Sildenafil is a phosphodiesterase 5 inhibitor used to treat erectile dysfunction in Western Medicine. This study evaluates the herbal-drug interaction of Epimedium sagittatum extract on the pharmacokinetics of sildenafil in rats by ultra-performance liquid chromatography. The rat plasma was sampled from each anesthetized rat after pretreatment with 3-days Epimedium sagittatum extract (1/2 g/kg/day) and intravenous injection with sildenafil (10/30 mg/kg). The pharmacokinetic data demonstrate that the area under the concentration-time curve (AUC) of sildenafil (10 mg/kg) was significantly decreased in groups that received a high dose of Epimedium sagittatum extract. In conclusion, the study demonstrates that there was significant herb-drug interaction of Epimedium sagittatum extract on the pharmacokinetics of sildenafil at low and high daily doses, suggesting co-administration use of Epimedium sagittatum extract and sildenafil in clinical practice should be prevented due to possible herb-drug interactions.


Asunto(s)
Medicamentos Herbarios Chinos/administración & dosificación , Epimedium/química , Interacciones de Hierba-Droga , Inhibidores de Fosfodiesterasa 5/farmacocinética , Piperazinas/farmacocinética , Extractos Vegetales/administración & dosificación , Extractos Vegetales/química , Sulfonas/farmacocinética , Administración Oral , Animales , Masculino , Inhibidores de Fosfodiesterasa 5/administración & dosificación , Inhibidores de Fosfodiesterasa 5/química , Piperazinas/administración & dosificación , Piperazinas/química , Purinas/administración & dosificación , Purinas/química , Purinas/farmacocinética , Ratas , Citrato de Sildenafil , Sulfonas/administración & dosificación , Sulfonas/química
17.
Pharmaceutics ; 15(2)2023 Feb 01.
Artículo en Inglés | MEDLINE | ID: mdl-36839810

RESUMEN

Carotenoids, including carotenes and xanthophylls, have been identified as bioactive ingredients in foods and are considered to possess health-promoting effects. From a biopharmaceutical perspective, several physicochemical characteristics, such as scanty water solubility, restricted dissolution, and susceptibility to oxidation may influence their oral bioavailability and eventually, their effectiveness. In this review, we have summarized various formulation approaches that deal with the modification of crystalline status for carotenoids, which may improve their physicochemical properties, oral absorption, and biological effects. The mechanisms involving crystalline alteration and the typical methods for examining crystalline states in the pharmaceutical field have been included, and representative formulation approaches are introduced to unriddle the mechanisms and effects more clearly.

18.
Drug Test Anal ; 2023 Sep 27.
Artículo en Inglés | MEDLINE | ID: mdl-37753668

RESUMEN

Chlorphenesin is a legitimate preservative commonly used in cosmetics. It shares one urinary metabolite of 4-chlorophenoxyacetic acid with meclofenoxate, a prohibited stimulant in sports. Recently, there have been cases where athletes using chlorphenesin-containing products were falsely identified as users of meclofenoxate. This study developed and validated a liquid chromatography method with diode-array detection to determine the chlorphenesin content in 61 selected personal care products with various functions (e.g., facial care, body cleansing, sun protection, make-up, hairstyling, perfume, and oral cleaning). The analytical method demonstrated fit-for-purpose quantitation and provided good linearity, precision, accuracy, and recovery for analyzing different cosmetic matrices. Among the 27 cosmetics labeled with chlorphenesin, the chlorphenesin concentrations ranged from 0.10 to 2.67 mg/g, with three products showing no detection. None of the products exceeded the maximum limit of 3 mg/g (0.3%) set by regulatory authorities. Among the 34 cosmetics not labeled with chlorphenesin, none of them contained chlorphenesin. This study confirmed the absence of undeclared chlorphenesin in the selected cosmetics, supporting the correctness of chlorphenesin labeling in cosmetics sold in Taiwan. Further investigations studying urinary excretion patterns after different types, doses, frequencies, and sites of cosmetics applications could contribute to strengthen current testing approaches in anti-doping.

19.
Pharmaceutics ; 14(3)2022 Mar 14.
Artículo en Inglés | MEDLINE | ID: mdl-35336010

RESUMEN

The aim of this study was to develop a nanoparticle formulation made of poly (vinyl pyrrolidone) (PVP) and poly (lactic-co-glycolic) acid (PLGA) for the oral delivery of ß-carotene (BC). The hybrid nanoparticles were prepared by the interfacial deposition method, and the physicochemical properties of this formulation were characterized in terms of its morphology, particle size, size distribution, encapsulation efficiency, dissolution, intestinal permeability, and in vivo pharmacokinetics. Our results demonstrated that BC-loaded nanoformulation and PLGA nanoparticles (PNP) significantly enhanced a release 6.1 times higher than BC suspension. The fortification of PVP into PLGA nanoparticles, named PLGA-PVP hybrid nanoparticles (PPNP), significantly reduced the particle size, as well as led to an increase 1.9 times higher in the in vitro release of BC, compared with PNP. For the ex vivo intestinal permeability assessment, PNP and PPNP-K15 significantly enhanced the intestinal permeability by 2.7 and 6.5 times at the jejunum, and 2.3 and 4.5 times at the ileum, when compared with unformulated BC. According to the pharmacokinetic study, the optimized hybrid formulation significantly increased the peak plasma concentration (Cmax) and the area under the curve (AUC0-t), and the oral relative bioavailability showed a five-fold enhancement compared with that of the BC suspension. Our results indicate that the hybrid nanoparticulate delivery system is an efficient strategy for the oral delivery of BC.

20.
Materials (Basel) ; 15(16)2022 Aug 20.
Artículo en Inglés | MEDLINE | ID: mdl-36013884

RESUMEN

This study has developed an environmentally friendly, simple, and economical process by utilizing seaweed as a carbon precursor to prepare a hierarchical porous carbon for the application of a supercapacitor. In the carbonization process, the design of experiment (DOE) technology is used to obtain the optimal preparatory conditions with the best electrochemical properties for the electrode materials of supercapacitors. Without using strong acid and alkali solution of the green process, NaCl is used as the pore structure proppant of seaweed (SW) for carbonization to obtain hierarchical porous carbon material to improve the pore size distribution and surface area of the material. In the experiment of SW activation, the interaction between factors has been explored by the response surface methodology (RSM) and Box-Behnken design, and the optimal conditions are found. The activated carbon with the specific surface area of 603.7 m2 g-1 and its capacitance reaching 110.8 F g-1 is successfully prepared. At a current density of 1 A g-1, the material still retains 95.4% of the initial capacitance after 10,000 cycles of stability testing. The hierarchical porous carbon material prepared by the design of experiment planning this green process has better energy storage properties than supercapacitors made of traditional carbon materials.

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