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1.
Sensors (Basel) ; 19(2)2019 Jan 21.
Artigo em Inglês | MEDLINE | ID: mdl-30669617

RESUMO

Demand for indoor navigation systems has been rapidly increasing with regard to location-based services. As a cost-effective choice, inertial measurement unit (IMU)-based pedestrian dead reckoning (PDR) systems have been developed for years because they do not require external devices to be installed in the environment. In this paper, we propose a PDR system based on a chest-mounted IMU as a novel installation position for body-suit-type systems. Since the IMU is mounted on a part of the upper body, the framework of the zero-velocity update cannot be applied because there are no periodical moments of zero velocity. Therefore, we propose a novel regression model for estimating step lengths only with accelerations to correctly compute step displacement by using the IMU data acquired at the chest. In addition, we integrated the idea of an efficient map-matching algorithm based on particle filtering into our system to improve positioning and heading accuracy. Since our system was designed for 3D navigation, which can estimate position in a multifloor building, we used a barometer to update pedestrian altitude, and the components of our map are designed to explicitly represent building-floor information. With our complete PDR system, we were awarded second place in 10 teams for the IPIN 2018 Competition Track 2, achieving a mean error of 5.2 m after the 800 m walking event.


Assuntos
Algoritmos , Pedestres , Tórax , Calibragem , Humanos , Caminhada
2.
Eur J Drug Metab Pharmacokinet ; 41(4): 423-32, 2016 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-25698144

RESUMO

Leonurine (LE) has been found to have therapeutic efficacy in cerebral thrombosis, but its poor solubility in water leads to very low bioavailability. In this article, a leonurine O/O microemulsion (LE-ME) was prepared and investigated for its in vivo pharmacokinetic behavior and bioavailability in the mouse body using an aqueous suspension of leonurine (LE-SWW) for the control group. A simple, sensitive and specific method, HPLC-MS/MS, was developed for detection of the LE content in mouse plasma using n-benzoyl-L-arginine ethyl ester as an internal standard. The results demonstrated that the C max of LE-ME was 2.46-fold higher than that of the suspension following oral administration. The absolute bioavailability was 10.95 %, while that of the suspension was only 1.78 %. The T 1/2ß and MRT of LE-ME were 3.04- and 4.19-fold those of the suspension, respectively. In addition, following intramuscular administration of LE-ME, the absolute bioavailability was 37.45 %. The results indicated that LE-ME is a promising drug-delivery system to enhance the absorption and bioavailability of LE.


Assuntos
Emulsões/química , Emulsões/farmacocinética , Ácido Gálico/análogos & derivados , Administração Oral , Animais , Arginina/análogos & derivados , Arginina/química , Disponibilidade Biológica , Cromatografia Líquida de Alta Pressão/métodos , Sistemas de Liberação de Medicamentos/métodos , Ácido Gálico/química , Ácido Gálico/farmacocinética , Camundongos , Solubilidade , Suspensões/química , Suspensões/farmacocinética , Espectrometria de Massas em Tandem/métodos , Água/química
3.
Int J Biol Macromol ; 72: 480-6, 2015 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-25173708

RESUMO

Zein, a naturally biocompatible and biodegradable macromolecule, is widely used as plastic film material; however, the poor water solubility limits its other applications. In this study, we aimed to obtain carboxymethyl zein (CM-zein) by modifying it with sodium monochloroacetate in weakly basic environment. CM-zein showed a new FTIR peak of C-O-C bond at 1080 cm(-1), with a new signal region appearing at 4.0-4.05 ppm that assigned to the protons of the CH2 group from a carboxymethyl on (1)H NMR and a Tg of 168.0 °C by thermal analysis. Compared with the -12.3 mV of zeta potential of unmodified zein, CM-zein increased it significantly to -23.9 mV as a consequence of carboxymethylation. 5-Fluorouracil (5-FU), a model drug used in CM-zein-based tablet, was rarely detected in 0.1 mol/L HCl (pH 1.0) but it was released massively and quickly in phosphates buffer (pH 6.8) in vitro assays. The unmodified zein-based tablet illustrated much lower release level in these two fluids. Furthermore, the pharmacokinetic study of rats showed that CM-zein released 5-FU in intestine but not in stomach after dissolving. These findings indicated that CM-zein has the potential to be used for enteric preparation as a novel pH-selective biomaterial.


Assuntos
Fluoruracila/administração & dosagem , Substâncias Macromoleculares/administração & dosagem , Comprimidos/administração & dosagem , Zeína/administração & dosagem , Animais , Plásticos Biodegradáveis/síntese química , Plásticos Biodegradáveis/farmacocinética , Preparações de Ação Retardada , Composição de Medicamentos , Fluoruracila/síntese química , Fluoruracila/farmacocinética , Humanos , Concentração de Íons de Hidrogênio , Substâncias Macromoleculares/química , Substâncias Macromoleculares/farmacocinética , Ratos , Solubilidade , Comprimidos/química , Comprimidos/farmacocinética , Água , Zeína/química , Zeína/farmacocinética
4.
J Pharm Sci ; 103(4): 1075-84, 2014 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-24496859

RESUMO

The goal of this study was to develop a novel oil-body nanoemulsion (ONE) for Ginkgolide B (GB) and to conduct pharmacokinetics and pharmacodynamics evaluations. GB-ONE was prepared by O/O emulsion method. The differences in pharmacokinetics parameters and tissue distribution of rats after oral administrated with GB-ONE were investigated by liquid chromatography-tandem mass spectrometry. Changes in the ethological and pathological characterizations of the Alzheimer's disease rats after treated with GB-ONE were evaluated by Morris water maze (MWM) and pathological section, respectively. Furthermore, choline acetyltransferase (ChAT) and acetylcholinesterase (AchE) activity in hippocampus was analyzed by spectrophotometric method. The results indicated that the AUC of GB in rats' plasma was significantly improved after incorporated into ONE, and GB-ONE was significantly targeted into brain. In MWM experiment, memory improvement of rats with cognition impaired was confirmed after administrated with GB-ONE. Furthermore, GB-ONE significantly inhibited AchE activity and enhanced the activity of ChAT in the hippocampus. The overall results implicated that the novel ONE was effective for improving the drawbacks of GB and showed great potential for clinical application.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Emulsões/química , Ginkgolídeos/farmacocinética , Ginkgolídeos/uso terapêutico , Hipocampo/efeitos dos fármacos , Lactonas/farmacocinética , Lactonas/uso terapêutico , Veículos Farmacêuticos/química , Acetilcolinesterase/metabolismo , Doença de Alzheimer/metabolismo , Doença de Alzheimer/patologia , Peptídeos beta-Amiloides/metabolismo , Animais , Colina O-Acetiltransferase/metabolismo , Ginkgolídeos/administração & dosagem , Hipocampo/metabolismo , Hipocampo/patologia , Lactonas/administração & dosagem , Memória/efeitos dos fármacos , Ratos , Ratos Sprague-Dawley
5.
Pharm Dev Technol ; 19(6): 743-7, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-23978005

RESUMO

This study investigated the potential of targeted intestinal lymphatic transport of puerarin via a lipid formulation approach. Three formulations of PEG nanoemulsion, nanosuspension and an oil suspension containing puerarin were examined with the lymph-cannulated anaesthetized rat model. Plasma and lymph samples were analyzed by HPLC. Lymph triglyceride was measured using an enzymatic colorimetric technique. After 8 h, the total administered dose accumulated in the thoracic lymph duct was analyze. Nanoemulsion, nanosuspension and oil suspension was 0.065 ± 0.006%, 0.137 ± 0.018%, 0.021 ± 0.002% of the administered dose, respectively. In nanoemulsion, nanosuspension and oil suspension group, the systemic bioavailability of oral puerarin was 11%, 16% and 11% for lymph-cannulated rats, 41%, 67% and 18% for control rats. Absorption into the intestinal lymph should thus contribute to ∼30%, 51% and 7% of the systemic bioavailable puerarin. This data indicated that lipid-based nano drug formulation produced higher lymph concentrations of puerarin than oil suspension. The nanosuspension formulation may be considerable in terms of increased local concentrations in lymphoid tissue.


Assuntos
Isoflavonas/química , Isoflavonas/metabolismo , Lipídeos/química , Sistema Linfático/metabolismo , Administração Oral , Animais , Disponibilidade Biológica , Transporte Biológico , Química Farmacêutica/métodos , Emulsões/química , Emulsões/metabolismo , Absorção Intestinal , Masculino , Nanopartículas/química , Nanopartículas/metabolismo , Óleos/química , Óleos/metabolismo , Polietilenoglicóis/química , Polietilenoglicóis/metabolismo , Ratos , Ratos Sprague-Dawley , Suspensões/química , Suspensões/metabolismo , Triglicerídeos/metabolismo
6.
Zhonghua Liu Xing Bing Xue Za Zhi ; 34(10): 953-7, 2013 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-24377984

RESUMO

OBJECTIVE: To explore the characteristics related to the quality of life and the way of response among patients with anxiety disorder in Shandong province. METHODS: Case-control study was adopted, with secondary data analysis on mental disorders among adults over 18 years of age, in Shandong province. 720 patients with anxiety disorder who met the anxiety diagnostic criteria of DSM-IV, were selected from the database, according to the distributions on gender, age (±3 years of age), village or community. 720 persons without any psychiatric diagnosis were selected and served as controls, under 1 :1 paired choice. Research tools would include:General Health Questionnaire (GHQ-12),Quality of Life Questionnaire (QLQ), Simplified Coping Style Questionnaire (SCSQ), and questionnaire on general information. RESULTS: Scores of QLQ among patients with anxiety disorder were lower than that of the control group, with statistically significant difference(P < 0.01). Scores on the negative ways of coping among patients with anxiety disorder were higher than the scores of the control group, with statistically significant difference(P < 0.01). Regardless of gender, age, occupation, education, marriage, religious belief etc., results from the 'two factors anova-analysis' showed that the scores of QLQ among patients with anxiety disorder were still lower than the scores of the control group while the scores on negative coping were still higher than the scores of the control group. CONCLUSION: Patients with anxiety disorder and having poor quality of life outnumbered the ones from the control group, and using negative coping ways to cope with the stress events.


Assuntos
Transtornos de Ansiedade/psicologia , Qualidade de Vida , Adolescente , Adulto , Idoso , Transtornos de Ansiedade/epidemiologia , Estudos de Casos e Controles , China/epidemiologia , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Inquéritos e Questionários
7.
Drug Dev Ind Pharm ; 39(12): 1951-8, 2013 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-23034007

RESUMO

The aim of this study was to quantify the oral delivery systems of Tetramethylpyrazine Microemulsion (TMP ME) to heart, liver, spleen, lung, kidney and brain by comparing TMP level after oral administration at a dose of 100 mg kg(-1) with those of TMP tablet suspension (TMP SWW). This study was taken in mice to develop a suitable analytical methodology in pharmacokinetics studies and to manipulate the tissue distribution and targeting evaluation. Drug concentrations in tissues were determined at different times post-mortem. An HPLC method for separation and quantification of TMP was developed and validated by studying mice tissues. Following oral administration, TMP concentrations in different tissues were constantly detected for quite a long time and finally differed significantly from each other. The AUC rank order 3 of ME group is AUCliver > AUCbrain > AUClung > AUCspleen > AUCheart > AUCkidney, while the SWW group is AUCliver > AUClung > AUCspleen > AUCheart > AUCbrain > AUCspleen. Especially, the AUC value in brain region (AUCbrain) of ME is 6.06-fold of SWW. The drug relative overall targeting efficiency (RTE) are calculated: heart (7.49%), liver (3.54%), spleen (12.60%), lung (6.02%), kidney (2.86%) and brain (12.51%). The results from ME directly showed obvious targeting transport to the brain. These results indicated that this new family of pharmaceutical carriers can be used for the solubilization and targeted delivery of poorly soluble drugs to various pathological sites in the body.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Sistemas de Liberação de Medicamentos , Pirazinas/farmacocinética , Administração Oral , Animais , Área Sob a Curva , Transporte Biológico , Encéfalo/metabolismo , Emulsões , Camundongos , Pirazinas/administração & dosagem , Solubilidade , Fatores de Tempo , Distribuição Tecidual
8.
Sheng Wu Yi Xue Gong Cheng Xue Za Zhi ; 29(2): 307-10, 2012 Apr.
Artigo em Chinês | MEDLINE | ID: mdl-22616180

RESUMO

The aim of this research was to estimate the bioactivity of nano-hydroxyapatite/poly (L-lactic acid) composites in simulated body fluid. In vitro test showed that the pH value of simulated body fluid (SBF) declined gradually and the existence of hydroxyapatite (HA) particles neutralized the acid degradation product of poly (L-lactic acid) (PLLA). Bone-like apatite deposited on the surface, and silkworm-like crystals and plate-like clusters appeared after soaking. At the same time, there were many honeycomb-like pores caused by nano-composite degraded. The results indicated that the hydroxyapatite/poly (L-lactic acid) nano-composites have good bioactivity and degradation characteristics.


Assuntos
Substitutos Ósseos/síntese química , Durapatita/química , Durapatita/síntese química , Ácido Láctico/química , Poliésteres/química , Poliésteres/síntese química , Polímeros/química , Materiais Biocompatíveis , Substitutos Ósseos/química , Microscopia Eletrônica de Varredura , Nanopartículas , Porosidade , Difração de Raios X
9.
Zhong Yao Cai ; 34(3): 455-8, 2011 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-21823467

RESUMO

OBJECTIVE: To research the disperse behavior of many Chinese medicine decoctions. METHODS: Through the analysis of the dispersible attributes of 22 kinds of Chinese medicine decoctions including Radix Salviae Miltiorrhizae by means of turbidity, ultramicroscope and TEM, we found that a lot of nanometer particles existed in these decoctions after 4000 r/min centrifugation. Based on the model of Radix Salviae Miltiorrhizae, we analyzed the influence on the loss of effective ingredients by way of centrifugation, alcohol precipitation, flocculation and salting-out edulcoration. RESULTS: The removal of infinite nanometer particles from these decoctions led to the greater loss of water-soluble and fat-soluble ingredients,and the latter accounts for the major loss. CONCLUSION: Oral liquid preparation of traditional Chinese medicine is a kind of nano-pharmaceutics with nanometer particles dispersed in the water as the carriers of effective ingredients in medicine.


Assuntos
Nanopartículas/química , Extratos Vegetais/química , Plantas Medicinais/química , Química Farmacêutica , Estabilidade de Medicamentos , Microscopia Eletrônica de Transmissão , Nanopartículas/ultraestrutura , Tamanho da Partícula , Extratos Vegetais/análise , Extratos Vegetais/isolamento & purificação , Controle de Qualidade , Salvia miltiorrhiza/química , Solubilidade , Tecnologia Farmacêutica
10.
Eur J Pharm Sci ; 42(4): 348-53, 2011 Mar 18.
Artigo em Inglês | MEDLINE | ID: mdl-21216284

RESUMO

The potential for microemulsion drug delivery systems to improve the lymphatic transport and the portal absorption of a poorly water-soluble drug, puerarin, were investigated in lymph-cannulated rats. SD rats were operated for lymph duct cannulation and were orally dosed with 3ml puerarin microemulsion (0.6mg/g, n=6). The lymph and plasma were collected over 8h and the concentrations of puerarin and triglyceride were measured. Similarly, control rats (non-lymph-cannulated, n=6) were dosed orally with puerarin microemulsion and subsequently with puerarin injection intravenously. Plasma and lymph samples were analysed by HPLC. Lymph triglyceride was measured using an enzymatic colorimetric technique. The extent of lymphatic transport via the thoracic duct was 0.06% of the dose for the animals dosed with puerarin microemulsion. The systemic bioavailability of oral puerarin co-administered with lipid was only 16% in the lymph duct-cannulated rats compared with 40% in the controls. These data clearly indicate that the lymphatic transport process contributes significantly to intestinal absorption of puerarin and subsequently to its systemic bioavailability. The results imply that the pharmaceutical scientist may use microemulsion formulations to optimize lymph-targeting drug delivery systems, by improving the extent of lymphatic transport.


Assuntos
Sistemas de Liberação de Medicamentos/métodos , Isoflavonas , Sistema Linfático/metabolismo , Ducto Torácico/metabolismo , Administração Oral , Animais , Disponibilidade Biológica , Transporte Biológico , Cateterismo , Química Farmacêutica , Emulsões/administração & dosagem , Injeções Intravenosas , Absorção Intestinal , Isoflavonas/administração & dosagem , Isoflavonas/sangue , Isoflavonas/farmacocinética , Masculino , Ratos , Ratos Sprague-Dawley , Triglicerídeos/sangue
11.
AAPS PharmSciTech ; 12(1): 172-6, 2011 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-21184205

RESUMO

A unique polymer-based sustained-release implant drug delivery system was prepared by using biocompatible and biodegradable Zein as the skeleton material. After preparing Zein colloids, the Zein-loaded implant rods were formulated by injection molding followed by evaporating the solvent, and being coated with poly(lactic-co-glycolic) acid (PLGA) solution. Drug release kinetics was examined by using Fluorouracil (5-FU) as model drug. Nearly zero-order release was achieved for the model drugs for a period of 0-25 days when the implants were incubated in distilled water at 37 °C. And then the degradation kinetics of the rods in vivo and in vitro were evaluated, which indicated that Zein could be absorbed by body and has good degradation property. The effects of different ratios of Zein/5-FU and the rods' diameter on drug release were studied, respectively. The plasma concentration of 5-FU in the implants were determined by HPLC after implanting a single dose of the implants in rats. All data were subsequently processed by using the computer program 3P97, and the values were showed as follows: the area under the plasma concentration-time curve (AUC) value was 321.88 (µg/ml) × day, and the mean residence time (MRT) value was 23.05 days. The sustained-release implants of Zein/5-FU were successfully formulated. The uniqueness of the article is that Zein has been used as a skeleton material in implant delivery system for the first time and zero-order release kinetics has been obtained successfully.


Assuntos
Implantes de Medicamento , Excipientes/química , Excipientes/farmacocinética , Fluoruracila/farmacocinética , Zeína/química , Zeína/farmacocinética , Animais , Biotransformação , Preparações de Ação Retardada , Composição de Medicamentos , Feminino , Fluoruracila/química , Fluoruracila/farmacologia , Masculino , Ratos , Ratos Sprague-Dawley
12.
Zhongguo Zhong Yao Za Zhi ; 35(20): 2674-8, 2010 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-21246816

RESUMO

OBJECTIVE: To investigate the mechanisms of the oil-in-oil nanoemulsions transport through the gastrointestinal tract and the transport efficiency changed with its different particle size in the lymphatic channels. METHOD: The behavior of nanoemulsions in vivo and their absorption via lymph after oral administration was investigated, with the transport efficiency and absorption pathway of nanoemulsions clarified by lymph duct cannulation in rats. RESULT: It suggested about 36.8% of puerarin nanoemulsions was transported into systematic circulation via lymph. Nanoparticles with different size absorbed by the lymphatic channels varied as the degree of transportion. CONCLUSION: The degree of absorption and particle transport is inversely proportional to the size.


Assuntos
Isoflavonas/farmacocinética , Absorção , Animais , Transporte Biológico , Emulsões , Feminino , Isoflavonas/administração & dosagem , Linfa/metabolismo , Masculino , Nanopartículas , Tamanho da Partícula , Ratos , Ratos Sprague-Dawley
13.
Yao Xue Xue Bao ; 44(7): 798-802, 2009 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-19806923

RESUMO

The best absorption location of puerarin microemulsion-in-oil in intestine parva of rat and pharmacokinetic characteristics, and the pathway of absorption and conveying of puerarin microemulsion were studied. In situ rat perfusion method was used to investigate the intestinal absorption of puerarin. Through the changes of drug concentration in blocked and unblocked lymphs, to determine the pathway of absorption and conveying. Puerarin microemulsion-in-oil can be absorbed in any part of intestine, and the K(a), P(app) of every part is ileum > duodenum > jejunum > colon, and the K(a), P(app) of ileum is significantly larger than that of others. The absorption rate of different concentrations is not significantly different (P > 0.05). The puerarin transited by gastrointestinal tract, about 36.8% is absorbed by the lymphatic channels to enter the systemic circulation and 63.2% is absorbed by the non-lymphatic channels. The best part of intestine to absorb puerarin microemulsion is ileum, and it is passive transport. The pathway of conveying is lymphoid and non-lymphoid transit.


Assuntos
Absorção Intestinal , Isoflavonas/farmacocinética , Absorção , Animais , Colo/metabolismo , Duodeno/metabolismo , Íleo/metabolismo , Isoflavonas/administração & dosagem , Jejuno/metabolismo , Nanoestruturas , Tamanho da Partícula , Ratos , Ratos Sprague-Dawley
14.
Drug Dev Ind Pharm ; 35(2): 138-44, 2009 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-19040180

RESUMO

The main purpose of this study was to prepare puerarin microemulsion system to improve oral bioavailability of puerarin. The microemulsion formulations were prepared using soybean oil, soybean lecithin/ethyl lactate (1:1), and 1,2-propanediol/water. The presence of microemulsion regions were investigated by pseudo-ternary phase diagrams. The droplet size of microemulsion was characterized by photo-correlation spectroscopy. In vivo pharmacokinetic study was conducted in mice, and the results indicated that AUC(0-->infinity) was 15.82-fold higher than that of puerarin suspension upon oral administration. Particles of puerarin microemulsion were round and homogeneous. Puerarin microemulsion also showed good stability. These studies showed that microemulsion system of puerarin might be promising vehicles for the peroral delivery of puerarin.


Assuntos
Sistemas de Liberação de Medicamentos/métodos , Isoflavonas/administração & dosagem , Isoflavonas/farmacocinética , Vasodilatadores/administração & dosagem , Vasodilatadores/farmacocinética , Administração Oral , Animais , Área Sob a Curva , Disponibilidade Biológica , Química Farmacêutica , Cromatografia Líquida de Alta Pressão , Composição de Medicamentos , Estabilidade de Medicamentos , Emulsões , Isoflavonas/química , Medicina Tradicional Chinesa , Camundongos , Microscopia Eletrônica de Transmissão , Tamanho da Partícula , Veículos Farmacêuticos/metabolismo , Solubilidade , Tensoativos/química , Vasodilatadores/química
15.
Yao Xue Xue Bao ; 43(5): 490-4, 2008 May.
Artigo em Chinês | MEDLINE | ID: mdl-18717336

RESUMO

To search for potential antitumor drugs with potent efficiency and low toxicity, a novel 1,4,7-triazacyclodecane and its platinum (II) complex were synthesized. These compounds were characterized by elemental analysis, IR, 1H NMR, 13C NMR, MS spectra, thermoanalysis and conductivity measurement. Antitumor activity study indicated these compounds had strong antitumor activity in vitro to some extent. Inhibition of human liver tumor of CA was examined by antitumor rate and growth rate, complex C showed inhibition activity on transplanting-tumor growth of CA, 12 mg x kg(-1) was as potent as cisplatin, its ID50 was 853.6 mg x kg(-1).


Assuntos
Antineoplásicos , Neoplasias Hepáticas/patologia , Compostos Organoplatínicos/síntese química , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Humanos , Concentração Inibidora 50 , Masculino , Camundongos , Transplante de Neoplasias , Compostos Organoplatínicos/química , Compostos Organoplatínicos/farmacologia , Distribuição Aleatória
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