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Fraction absorbed (Fa) is an important parameter to describe the absorption level of oral drugs, and an important basis for the development and optimization of the formulation process. Because it is easily confused with the concept of absolute bioavailability, it has not received enough attention from the industry. There are many complex factors affecting Fa. There are three time-related factors that directly affect the extent of Fa: the release time, the absorption time, and the residence time. The relationship between these three time-related factors determines the extent of Fa. Generally, we are more concerned about the apparent factors that affect the extent of Fa, including independent variables and covariates; The independent variables include administered dose, route, dosage form, etc. The covariates are divided into internal and external factors, and external factors include food factors, drug interactions, etc. Internal causes include age, sex, disease, etc. This paper analyzes and systematically combs how independent variables and covariates directly or indirectly affect the three time-related factors by affecting the body's physiology and internal environment, thus changing the complex process of Fa. Understanding this theoretical framework can better optimize the independent variables to reduce the impact of covariates on Fa. In addition, this paper also introduces the latest progress of prediction and evaluation of Fa, including the progress of complex dissolution device and the status of software prediction.
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Objective To evaluate the changes in the expression of hippocampal long non-coding RNAs ( lncRNAs) and bioinformatics analysis in mice with perioperative neurocognitive disorders ( PND) . Methods Thirty clean-grade male C57BL∕6 mice, aged 12-14 weeks, weighing 25-30 g, were divided into 2 groups (n=15 each) according to the random number table method: control group (group C) and PND group. The model of PND was established by performing open tibial fracture with intramedullary fixa-tion under isoflurane anesthesia in anesthetized mice. The Morris water maze test, open field test and fear conditioning test were performed at 1, 3 and 7 days postoperatively. The animals were sacrificed after the end of behavioral testing on 3 days after operation, the hippocampus was obtained, the high-throughput gene sequencing was performed to identify the differentially expressed lncRNAs, and Gene Ontology func-tional analysis and Kyoto Encyclopedia of Genes and Genomes signaling pathway analysis were used to ana-lyze the results. Results Compared with group C, the escape latency was significantly prolonged, and the percentage of time spend in the target quadrant and percentage of freezing time in the fear conditioning test were decreased at different time points after operation in group PND ( P<0. 05) . A total of 121 differential-ly expressed lncRNAs were identified, of which 69 were up-regulated and 52 were down-regulated. The Gene Ontology functional analysis showed that there were differences in various biological processes, such as synaptic transmission, cholinergic neurotransmitters, or adiponectin secretion and regulation. The KEGG signaling pathway analysis showed that there were also differences in cholinergic synapses, MAPK signaling pathway, glucagon signaling pathway, TNF signaling pathway, NOD-like receptors, Toll-like re-ceptors, chemokine signaling pathway and etc. Conclusion There are 121 differentially expressed lncR-NAs in the hippocampus of PND mice, and lncRNAs- and the target gene-related inflammatory responses, synaptic transmission, energy metabolism and etc. may be related to the pathogenesis of PND.
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Chinese materia medica is mostly taken orally. The permeability of a drug’s biofilm (e.g. cell membrane) reflects its ability of absorption and transportation in the body. It is of guiding significance to evaluate the membrane permeability of the active components of Chinese materia medica by using appropriate drug permeation model, so as to clarify, the oral absorption and transport mechanism of active ingredients, pharmacodynamic substance basis and dosage form design. The evaluation method of oral drug membrane permeability, as well as the application of various methods in Chinese medicine was summarized for reference in this review.
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Study on the pharmacodynamic material basis of Chinese materia medica (CMM) is the key and difficult points of CMM research due to its complicated components and synergistic effect of multiple pathways and multiple targets in pharmacological action. Currently, research ideas and research methods of the pharmacodynamic material basis of CMM are being constantly innovated. In this review, research ideas and progress on screening and identification of pharmacodynamic substance of CMM were summarized. It suggested that the research model of interdisciplinarity, multi-dimensional screening and evaluation should be established, in order to provide references for further and comprehensively revealing the mechanism of action of CMM and the law of compatibility, and establishing quality evaluation system of CMM.
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Pregnancy and childbirth are natural physiological processes for women, but most mothers, especially primipara, tend to suffer from anxiety, fear and other unhealthy psychology, accompanied by the occurrence of these bad emotions. It is a worthy concern that whether the subjective well-being of pregnant women will be affected by these bad emotions. However, there are few reports about subjective well-being of pregnant women in China. In this study, the subjective well-being′s concept, assessment tools and influencing factors of maternal subjective well-being were reviewed. The paper also described the research progress and development on the subjective well-being of pregnant women. The purpose of this paper is to provide reference for the study and practice of in China.
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Objective To investigate the effect of supine regulating on maternal fetal occiput posterior position during the delivery after epidural analgesia. Methods Totally600 cases of parturient with intravaginal posterior occipital position with 3cm voluntary labor analgesia were selected,who were born in Dalian maternity hospital from October 2015 to October 2016.The(Visual Analogue Scale/Score) VAS pain score at 15min after epidural labor analgesia was as effective as less than 3 points.They were randomly divided into the control group and the observation group by random number table method,with 300 cases in each group.The control group monitored parturient respiration, pulse, blood pressure, heart rate and fetal heart rate according to routine treatment.The control group monitored parturient respiration, pulse, blood pressure, heart rate and fetal heart rate according to routine treatment.In the observation group,except for routine treatment according to the labor process,after the opening of 5cm,the pregnant women were instructed to take the lateral prone position,so that the maternal side and the fetal side of the spinal column should be the same side. To observe the difference between the two groups in the rate of spontaneous vaginal delivery, delivery rate, cesarean section rate, fetal cardioversion rate, time of birth process and neonatal Apgar score. Results Totally 283 cases delivery through vagina and 17 cases of cesarean section in observation group,while 257 cases of vaginal delivery and 43 cases of cesarean section in the control group.The successful rate of fetal position transfer in the observation group was 74.6%(211/283) which was significantly higher than 45.9% (118/257) of the control group (Χ2=62.782, P<0.01), natural labor rate was also 87.3% (262/300) which increased significantly according to 64.7% (194/300) (Χ2=42.251, P<0.01),the rate of midwifery (7.0%, 21/300) and cesarean section (5.7%, 17/300) were significantly lower than 21.0% (63/300)and 14.3% (43/300) of the control group (Χ2=24.419, 12.519,P<0.01),the second stage of labor was(1.60±0.56)h which was significantly shortened than(2.19±0.53)h also(t=-12.589,P<0.01).In the observation group, the ratio of the posterior occipital position to the occipital transverse position after the opening of 8-10 cm and the complete dilation of the cervical were 7.4%(21/283)and 13.1%(37/283),which were also significantly increased than 3.4%(9/264),6.8%(18/264) of the control group (Χ2=4.240, 5.911, P<0.05). Conclusions Supine adjustment after the cervix dilatation larger than 5cm is more conducive to fetal rotation and to avoid the adverse complications, reduce the rate of vaginal delivery and cesarean section rate,improve the rate of natural childbirth,shorten delivery time,improve the quality of delivery.
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Etanercept has been shown to be effective for the treatment of moderate-to-severe plaque psoriasis.Since most clinical trials examined etanercept in combination with other drugs,the efficacy and safety of etanercept monotherapy for moderate-to-severe plaque psoriasis have not been well established.This prospective study enrolled 61 Chinese patients with moderate-to-severe plaque psoriasis to explore the efficacy and safety of etanercept monotherapy.These patients were treated with etanercept at a subcutaneous dose of 25 mg,twice a week,for 12 weeks.All the 61 patients completed the treatment and showed significant improvement in psoriasis area and severity index (PASI) scores.At 4,8,and 12 weeks after treatment,the response rates (PASI75) were 0％,21.31％,and 40.98％,respectively.It was concluded that etanercept monotherapy is efficacious and safe for patients with moderate-to-severe plaque psoriasis.
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Catechol O-methyltransferase (COMT), one of the endogenous phase II metabolizing enzymes, expressed by chromosome 22. COMT catalyzes the transfer of a methyl group from common methyl donor S-adenosyl-L-methionine (AdoMet or SAM) to one of the catechol hydroxyls. COMT participates in the metabolism of many catechols in vivo, e.g. dopamine, epinephrine, noradrenaline, estradiol. Furthermore COMT also plays important roles in the metabolism of xenobiotic catechols from food and drug. COMT play a critical role in the management of catechols. Metabolism disorders of COMT can cause many diseases or an increased risk of diseases, e.g. Pakinson diseases, schizophrenia, and breast cancer. In this review, we explains the relationship of COMT and related-diseases through expounding disease caused by the COMT metabolic disorders. Finally, we hope that there will be more effective treatments for the COMT metabolism related diseases.
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<p><b>OBJECTIVE</b>To explore the effect of Scalp acupuncture on serum neuron specific enolase (NSE) and S-100β concentrations, and incidence rates of postoperative delirium (POD) and postoperative cognitive function (POCD) of elderly patients undergoing hip replacement.</p><p><b>METHODS</b>Eighty-four patients undergoing scheduled hip replacement under combined spinal-epidural anesthesia (CSEA) were assigned to the control group (group C) and the scalp acupuncture group (group S) according to random digit table, 42 cases in each group. In group S, scalp acupuncture was additionally performed according to International Standardized Scheme for Scalp Acupuncture. Scalp acupuncture was performed during the operation from the MS1 middle line of forehead [1 cun before Shenting (GV24), including Shenting (GV24)] and MS5 middle line of vertex [from Baihui (DU20) to Qianding (DU21), including Baihui (DU20) and Qianding (DU21)]. The operation time and post-operative length of stay were observed. The midazolam dosage, hemorrhage amount, fluid transfusion amount, urine amount, use rates of ephedrine and atropine during the operation were also observed and compared between the two groups. The occurrence rate of POD and POCD at post-operative day 3 (T₁), week 1 (T₂), month 3 (T₃), and month 6 (T₄) were measured. Eighteen patients were randomly selected to collect blood from internal jugular vein before anesthesia t₀), immediately after ending the surgery (t₁), 6 h after operation (t₂), 24 h after operation (t₃), and 48 h after operation (t₄), respectively. Serum levels of NSE and S-100β were correspondingly measured.</p><p><b>RESULTS</b>There was no statistical difference in the operation time, midazolam dosage used during the operation, hemorrhage amount, fluid transfusion amount, urine amount, use rates of ephedrine and atropine (P > 0.05). Compared with group C, the post-operative length of stay was shortened in group S (P < 0.05). The incidence rate of POD and that of POCD at each time point were lower in group S (P < 0.05). The expression level of NSE decreased at t₂, t3, and t₄, and the expression level of S100β also decreased at t₁, t₂, t₃, and t₄(P < 0.05). There was no statistical difference in expression levels of NSE or S100β between the two groups at other time points (P > 0.05).</p><p><b>CONCLUSION</b>Scalp acupuncture could attenuate central nervous system lesion and improve POCD of elderly patients undergoing hip replacement.</p>
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Anciano , Humanos , Puntos de Acupuntura , Terapia por Acupuntura , Artroplastia de Reemplazo de Cadera , Cognición , Tiempo de Internación , Fosfopiruvato Hidratasa , Sangre , Complicaciones Posoperatorias , Periodo Posoperatorio , Subunidad beta de la Proteína de Unión al Calcio S100 , Sangre , Cuero CabelludoRESUMEN
To study on the effects of Achyranthes bidentata on Tongsaimai pellets main active ingredients chlorogenic acid, isoliquiritin, harpagoside and glycyrrhizin in rats in vivo pharmacokinetic behaviors, a method for the simultaneous determination of chlorogenic acid, isoliquiritin, harpagoside and liquiritigenin in rat plasma was established by UPLC-MS/MS. The analysis was performed on a waters Acquity BEH C18 column (2.1 mm x 100 mm, 1.7 microm) with the mixture of acetonitrile and 0.1% formic acid/water as mobile phase, and the gradient elution at a flow rate of 0.3 mL x min(-1). The analytes were detected by tandem mass spectrometry with the electrospray ionization (ESI) source and in the multiple reaction monitoring (MRM) mode. It turned out that the analytes of Tongsaimai pellets groups C(max) and AUC(Q-infinity) values were higher than that with A. bidentata group, and the C(max) values of chlorogenic acid had significantly difference (P < 0.05), the AUC(0-infinity) values of chlorogenic acid and glycyrrhizin had significantly difference (P < 0.05); The T(max) and CL values of two groups had no significantly difference. Results showed that the established method was specific, rapid, accurate and sensitive for the studies of Tongsaimai pellets four main active ingredients in rat in vivo pharmacokinetic, and A. bidentata have varying degrees of effects on Tongsaimai pellets four main active ingredients in rat in vivo pharmacokinetic behaviors.
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Animales , Masculino , Ratas , Achyranthes , Química , Chalcona , Sangre , Farmacocinética , Ácido Clorogénico , Sangre , Farmacocinética , Medicamentos Herbarios Chinos , Farmacocinética , Glucósidos , Sangre , Farmacocinética , Glicósidos , Sangre , Farmacocinética , Ácido Glicirrínico , Farmacocinética , Interacciones de Hierba-Droga , Piranos , Sangre , Farmacocinética , Ratas Sprague-Dawley , Espectrometría de Masas en TándemRESUMEN
To explore a new method to identify Moutan Cortex to guarantee its safe use, internal transcribed spacer 2 (ITS2) sequence was used to identify Moutan Cortex and its adulterants. DNA was extracted and target fragments were amplified. Sequences were analyzed and assembled by CodonCode Aligner V3.7.1. Genetic distances were computed and phylogenetic tree was constructed based on kimura 2-parameter (K2P) model by MEGA 5.0. The length of the 20 ITS2 sequences of Moutan Cortex from nine different places is 227 bp, and no variation site was detected. The maximum inter-specificK2P distance of Moutan Cortex is 0, the minimum intra-specific K2P distance is 0.041, the average intra-specific K2P distance is 0.222. According to NJ analysis, Moutan Cortex from different places can get together as one branch with bootstrap support values 99%, which indicates Moutan Cortex can be easily distinguished from its adulterants. Using ITS2 sequence can accurately identify Moutan Cortex and its adulterants, it is an effective supplementary to traditional identification methods.
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Secuencia de Bases , China , Código de Barras del ADN Taxonómico , Métodos , ADN de Plantas , Genética , ADN Espaciador Ribosómico , Genética , Contaminación de Medicamentos , Medicamentos Herbarios Chinos , Química , Clasificación , Datos de Secuencia Molecular , Paeonia , Clasificación , Genética , Filogenia , Control de CalidadRESUMEN
Drug-loading micro-particles are a targeted, positioned and controlled-release drug delivery carrier with a wide application prospect. Various micro-carrier drug delivery systems have their own advantages in promoting absorption, improving stability, targeting and controlled release. Accordingly, it is of far-reaching significance for the studies on micro carrier drug delivery systems to build oral traditional Chinese medicine (TCM) compound micro-carrier drug delivery systems with effective TCM components and effective fractions. This article introduces several features and advantages of oral micro-carrier drug delivery systems, and summarizes their application in the field of TCMs.
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Animales , Humanos , Administración Oral , Portadores de Fármacos , Química , Sistemas de Liberación de Medicamentos , Métodos , Medicamentos Herbarios Chinos , QuímicaRESUMEN
This study is to investigate the effects of concentration, intestinal section, pH, paracellular route, substrate/inhibitor of enzyme (CYP3A) and proteins (P-gp, MRP2, SGL1) on the absorption of forsythoside A. The absorption of three concentrations (2.6, 5.2, and 10.4 microg x mL(-1)) of forsythoside A in different intestinal segments was studied with phenol red as the marker by rat circulation in situ. The results showed that the residue of forsythoside A with different concentrations had little significant difference from that obtained after perfusing via duodenum, jejunum, ileum and colon, which indicated that the absorption of forsythoside A was passive diffusion and had no difference in different segments of rat intestine. The residue of forsythoside A increased to 466.160 and 463.429 microg respectively when cyclosporine (4 microg x mL(-1)) or midazolam (50 micromol x L(-1)) was added to the circulation fluid, which showed significant difference compared to the control group (P < 0.05). Moreover, the residue of forsythoside A showed a tendency of increase with the increase of cyclosporine or midazolam. When digoxin (50 micromol x L(-1)) or EDTA (10 microg x mL(-1)) was added to the circulation fluid, the residue of forsythoside A decreased to 325.110 and 369.888 microg respectively, which showed significant difference as compared to the control group (P < 0.05). Besides, the residue of forsythoside A showed a tendency of reduction with the increase of digoxin or EDTA. However, there is no significant change in the absorption of forsythoside A when the different concentrations of mannitol were added to the circulation fluid. The results above indicated that the absorption of forsythoside A was mainly passive diffusion and involved paracellular route at the same time. In addition, the substrates of P-gp or CYP3A had dose-dependent effect on the absorption of forsythoside A.
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Animales , Masculino , Ratas , Colon , Metabolismo , Ciclosporina , Farmacología , Digoxina , Farmacología , Relación Dosis-Respuesta a Droga , Duodeno , Metabolismo , Ácido Edético , Farmacología , Glicósidos , Farmacocinética , Concentración de Iones de Hidrógeno , Íleon , Metabolismo , Absorción Intestinal , Yeyuno , Metabolismo , Manitol , Farmacología , Midazolam , Farmacología , Ratas Sprague-DawleyRESUMEN
Objective To investigate the regulation effect of bispectral index (BIS) on the depth of total intravenous anesthesia (TI-VA) by comparing with regulating the depth of anesthesia according to the changes of hemodynamics. Methods 60 ASA Ⅰ～Ⅱ patients undergoing laparoscopic cholecystectomy (LC) were randomly assigned into controlled group (group C) and trial group (group T) ,with 30 patients in each group, according to the rules of regulating the titration of propofol during TIVA. The target of group C was to keep SBP/DBP 100 ～ 140mmHg/60 ～ 89mmHg and that of group T was to keep BIS 40 ～ 60 during anesthesia. The measure indexes included SBP/DBP, HR, BIS, total dosis of Propofol, time to extubate, time to leave operating room and OAA/S (observer's assessment of alert-ness/sedation). After operation, we evaluated whether awareness during surgery happens. Results As compared with group C, there were higher SBP/DBP and BIS in group T after induction of anesthesia, during aeroperitonia, immediately after finishing operation and just before extubating endotracheal catheter, but less dosis of propofol and less time of extubation and leaving operating room in group T. The differences had significance (P <0.01). There were no significant differences in the changes of HR between two groups (P >0.05) and no awareness during surgery happened in both groups. Conclusion TIVA regulated by BIS during LC can decrease the dosis of propofol, accelerate the recovery from anesthesia and avoid extremely deep anesthesia and awareness during surgery.
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<p><b>OBJECTIVE</b>To screen enhancer-like sequences from vaccinia virus genome, to construct an expression vector harboring prokaryotic enhancer-like sequence and study the effect of interferon gene expression.</p><p><b>METHODS</b>Enhancer-like element from vaccinia virus genome was obtained by using the chloramphenicol acetyl-transferase cat gene as reporter gene. An expression vector harboring prokaryotic enhancer-like sequence VV1 from vaccinia virus was constructed. Interferon was expressed and assayed.</p><p><b>RESULTS</b>Eighteen enhancing sequences were found. From them two enhancer-like sequences with distance and orientation independence property were screened and named VV1 and VV16 respectively. Quantification test showed that the direct and reverse orientation of VV1 could increase the activity of beta-galactosidase with 10.9 and 3.8 times and those of VV16 could increase by 9.0 times and 4.1 times respectively. The enhancing activity of the element was on transcription level. An expression vector harboring prokaryotic enhancer-like sequence VV1 was constructed. Using this vector the antiviral activity of interferon alpha-2b was increased by 2.6 times in comparison with the original expression plasmid.</p><p><b>CONCLUSION</b>Two enhancer-like sequences were screened from vaccinia virus genome. Interferon gene was highly expressed by using an expression vector harboring enhancer-like sequences.</p>