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1.
China Pharmacy ; (12): 2121-2127, 2023.
Article in Chinese | WPRIM | ID: wpr-987142

ABSTRACT

OBJECTIVE To explore the mechanism of Kuaisong yin in the prevention and treatment of constipation. METHODS Slow transit constipation (STC) model was established with Compound difenoxylate tablet in mice and rats. Two batches of mice were divided into blank group, model group, positive control group (Maren soft capsule, 0.64 g/kg), Kuaisong yin low-dose, medium-dose and high-dose groups (3.2, 6.4, 12.8 g/kg), with 10 mice in each group. The effect of Kuaisong yin on constipation in mice was evaluated by intestinal propulsion experiment and defecation experiment. Rats were divided into blank group, model group, positive control group (Maren soft capsule,0.36 g/kg), Kuaisong yin low-dose and high-dose groups (2.4, 4.8 g/kg), with 7 or 8 rats in each group. They were given relevant medicine once a day for 1 week. The metabonomics of serum and urine of rats were analyzed by UPLC-Q-TOF-MS/MS technology. RESULTS Compared with model group, the ink propulsion rate and 5 h defecation volume of mice in Kuaisong yin high-dose group were significantly increased (P<0.05); the first defecation time of mice in Kuaisong yin medium-dose and high-dose groups was significantly shortened, and the quality of defecation was significantly reduced within 5 h (P<0.05 or P<0.01). Serum metabonomics screened 16 compounds (such as proline, propionylcarnitine, hemolytic phosphatidylcholine, etc.) and 6 metabolic pathways (such as sphingomyelin metabolism, arginine and proline metabolism, sphingolipid biosynthesis-lactose and neolactone series). Urine metabonomics screened 20 different metabolites (such as prostaglandin A2, L-valine, phosphatidylcholine, sphingomyelin, etc.) and 8 metabolic pathways (such as valine, leucine and isoleucine biosynthesis, sphingomyelin metabolism, pyruvate metabolism, etc.). CONCLUSIONS Kuaisong yin can play a role in improving constipation by regulating different metabolites such as hemolytic phosphatidylcholine, phosphatidylcholine, prostaglandin A2, L-valine, proline, and regulating metabolic pathways such as multiple amino acid metabolism, sphingomyelin metabolism, etc.

2.
Chinese Journal of Biologicals ; (12): 158-162, 2023.
Article in Chinese | WPRIM | ID: wpr-965859

ABSTRACT

@#Objective To evaluate the pharmacodynamics of human interferon(IFN)α1b against severe acute respiratory syndrome coronavirus 2(SARS-CoV-2)Omicron strain in vitro.Methods Total four drugs human IFNα1b bulk,human IFNα1b eye drops,human IFNα1b spray and Remdesivir were detected for cytotoxicity by CCK-8 assay.The inhibitory effect of human IFNα1b on SARS-CoV-2 Omicron strains(BA.5/BA.2/BA.1)was determined by qPCR.Results Human IFNα1b bulk of the maximum concentration(1 × 107IU/mL)and Remdesivir of the maximum concentration(150 μmol/L)did not achieve half cytotoxicity to Vero cells;The median cytotoxicity concentrations(CC_(50))of human IFNα1b eye drops and human IFNα1b sprays were 29 958 and 37 550 IU/mL,respectively,showing toxicity to Vero cells.The median effective concentrations(EC_(50))of human IFNα1b against virus strains BA.1,BA.2 and BA.5 after incubation for 2 h in advance were 9.30,13.38 and 12.33 IU/mL and those of Remdesivir were 0.314 7,0.291 0 and0.300 3 μmol/L.When incubation with virus simultaneously,the EC_(50)of human IFNα1b to BA.1,BA.2 and BA.5 were19.68,10.91 and 18.84 IU/mL and those of the control drug Remdesivir were 0.320 5,0.274 4 and 0.304 1 μmol/L,respectively.Conclusion At the cell level in vitro,human IFNα1b of very low activity showed a good inhibitory effect on SARS-CoV-2 Omicron strain,which was expected to be a clinical specific drug for the treatment of SARS-CoV-2 Omicron strain infection.

3.
China Pharmacy ; (12): 429-432, 2023.
Article in Chinese | WPRIM | ID: wpr-962486

ABSTRACT

OBJECTIVE To compare anti-ischemic stroke (IS) effect of different extraction parts from Gastrodia elata, and to provide reference for screening the anti-IS effective parts of G. elata. METHODS G. elata was extracted and separated by ethanol reflux extraction and ethyl acetate extraction. The rat model of diffuse cerebral thrombosis was induced by internal carotid artery injection of arachidonic acid (AA); the anti-IS effect of G. elata powder, ethanol extract of G. elata, residue of ethanol extract of G. elata, ethyl acetate extract of G. elata, residue of ethyl acetate extract of G. elata, gastrodin and aspirin (positive control drug) were investigated with the content of Evans blue (EB) in the ischemic brain tissue as index. RESULTS Compared with model group, aspirin, ethanol extract of G. elata and ethyl acetate extract of G. elata could significantly decrease the content of EB in the ischemic brain tissue of model rats (P<0.05). G. elata powder had the tendency to reduce the content of EB in the ischemic brain tissue of model rats, without statistical significance (P>0.05). The residue of ethanol extract of G. elata, residue of ethyl acetate extract of G. elata and gastrodin had little effect on the content of EB in the ischemic brain tissue of model rats. CONCLUSIONS Both ethanol extract of G. elata and ethyl acetate extract of G. elata have anti-IS effects, which are stronger than that of G. elata powder.

4.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 323-332, 2023.
Article in English | WPRIM | ID: wpr-982704

ABSTRACT

Pharmacodynamics material basis and effective mechanisms are the two main issues to decipher the mechnisms of action of Traditional Chinese medicines (TCMs) for the treatment of diseases. TCMs, in "multi-component, multi-target, multi-pathway" paradigm, show satisfactory clinical results in complex diseases. New ideas and methods are urgently needed to explain the complex interactions between TCMs and diseases. Network pharmacology (NP) provides a novel paradigm to uncover and visualize the underlying interaction networks of TCMs against multifactorial diseases. The development and application of NP has promoted the safety, efficacy, and mechanism investigations of TCMs, which then reinforces the credibility and popularity of TCMs. The current organ-centricity of medicine and the "one disease-one target-one drug" dogma obstruct the understanding of complex diseases and the development of effective drugs. Therefore, more attentions should be paid to shift from "phenotype and symptom" to "endotype and cause" in understanding and redefining current diseases. In the past two decades, with the advent of advanced and intelligent technologies (such as metabolomics, proteomics, transcriptomics, single-cell omics, and artificial intelligence), NP has been improved and deeply implemented, and presented its great value and potential as the next drug-discovery paradigm. NP is developed to cure causal mechanisms instead of treating symptoms. This review briefly summarizes the recent research progress on NP application in TCMs for efficacy research, mechanism elucidation, target prediction, safety evaluation, drug repurposing, and drug design.


Subject(s)
Drugs, Chinese Herbal/pharmacology , Network Pharmacology , Artificial Intelligence , Medicine, Chinese Traditional , Metabolomics
5.
Braz. J. Pharm. Sci. (Online) ; 59: e22982, 2023. tab, graf
Article in English | LILACS-Express | LILACS | ID: biblio-1520311

ABSTRACT

Abstract Sepsis is described as a life-threatening organ dysfunction caused by a host's response to infection, leading to an unbalance in body homeostasis. It is one of the leading causes of death in developed countries. Considering that in critically ill patients, such as those with sepsis, plasma concentrations do not necessarily reflect tissue concentrations, one way to assess tissue concentrations is through the microdialysis technique, which allows direct measurements of free drug at the site of action. This review was carried out after searching the Pubmed, Scielo and Web of Science databases, using the following descriptors: (microdialysis AND (sepsis OR septic shock OR severe sepsis OR septicemia)) OR (microdialysis AND (sepsis OR septic shock OR severe sepsis) OR septicemia) AND (antimicrobial OR antibiotic OR antifungal)). The physiological changes generated by sepsis may imply changes in pharmacokinetic parameters, such as in clearance, which may be reduced in these patients and in volume of distribution, which presents an expansion, mainly due to edema. Both events contribute to a high inter- individual variability in tissue penetration of antimicrobials which is generally observed in patients with sepsis.

6.
Journal of Pharmaceutical Practice ; (6): 416-421, 2023.
Article in Chinese | WPRIM | ID: wpr-978480

ABSTRACT

Objective To explore the pharmacokinetic properties of curcumin nano emulsion and its pharmacodynamic effects on hyperlipidemia in rats. Methods The method for determination of curcumin was established by HPLC-MS. The pharmacokinetics characteristics of curcumin nano emulsion oral administration system were investigated. SD rats were used as model animals to establish hyperlipidemia animal models, and the pharmacodynamic effects of curcumin nano emulsion on hyperlipidemia induced by high fat diet was preliminarily investigated. Results The results of pharmacokinetic studies in vivo showed that the relative bioavailability of curcumin nano emulsion was 313.47% with bulk drug group as the reference preparation. The relative bioavailability of curcumin nano emulsion was 279.52 % with tablets as reference preparation. Cmax of curcumin nano emulsion group was 201.48 % of that of bulk drug group and 193.02 % of that of tablet group, and had higher MRT value (183.52 % of that of bulk drug group and 154.21 % of that of tablet group) than bulk drug group and tablet group. Pharmacodynamics research results showed that curcumin nano emulsion oral administration system could significantly reduce the levels of triglyceride and LDL-c in serum of model rats, and relieve liver lipid deposition and liver injury caused by high-fat diet in model animals. Conclusion The oral administration system of curcumin nano emulsion could effectively improve the bioavailability of curcumin, which has a good hypolipidemic effect. It also could control the weight gain of hyperlipidemia rats and improve the changes of liver coefficient caused by lipid metabolism disorder.

7.
China Pharmacy ; (12): 1661-1664, 2023.
Article in Chinese | WPRIM | ID: wpr-977861

ABSTRACT

Meropenem is the first choice for the treatment of multi-drug-resistant bacterial infections, which has been widely used in clinical practice. However, the physiological and pathological characteristics of special populations have a significant impact on the pharmacokinetics/pharmacodynamics (PK/PD) parameters of meropenem, so it is necessary to develop individualized drug administration plan according to the characteristics of patients in clinical application. Therefore, this paper summarizes PK/PD characteristics and application of meropenem in special population, and recommends the dosage of meropenem as follows: 10-40 mg/kg, q8 h for children; 1 g, q8-12 h for elderly patients; 0.75 g, q8 h for the patients with renal insufficiency who received continuous veno-venous hemofiltration and continuous veno-venous hemodialysis; 1 g, q8 h prolonged infusion until 3 hours or 2 g, q8 h for patients with hyperrenal function; 1 g, q8 h after 2 g loading dose for patients with cirrhosis.

8.
JOURNAL OF RARE DISEASES ; (4): 414-419, 2023.
Article in English | WPRIM | ID: wpr-1004968

ABSTRACT

The research and development of somatostatin analogues is a hot area in endocrinology and metabolism. The first generation octreotide, lanreotide and the second generation pareotide have been approved to be effective for the treatment of neuroendocrine tumors such as acromegaly. However, paltusotine, a somatostatin receptor ligand, is a novel non-peptide small molecule drug which can be administered orally and inhibits excessive secretion of growth hormone and insulin-like growth factor 1. This review summarizes the research progress of the pharmacokinetics, pharmacodynamics, clinical efficacy, telerability, and safety of paltusotine.

9.
Acta Pharmaceutica Sinica ; (12): 3655-3668, 2023.
Article in Chinese | WPRIM | ID: wpr-1004656

ABSTRACT

Atopic dermatitis (AD) is a chronic, relapsing, inflammatory dermatosis with a variety of clinical manifestations and difficult to cure. Currently, many AD drug candidates have entered the research and development pipeline. In order to provide technical specifications for the clinical development of AD drugs, the Center for Drug Evaluation of National Medical Products Administration released the "Technical Guidelines for Clinical Trials of Drugs for AD Treatment" (Draft for Comments) in November 2022. Non-clinical pharmacodynamics evaluation is an important research before the drug enters clinical trials. Oxazolone (OXA)- and 2,4-dinitro-fluorobenzene (DNFB)-induced models are the most popular classical hapten-induced AD murine models, but variations of modeling are existing in the methods from different studies, including sensitization sites, haptens' dosages, the period of challenges, and the skin lesions severity evaluation as well. In this study, the investigation of OXA- and DNFB-induced AD murine models with various conditions of modeling was performed to compare the characteristics of hapten-induced AD murine models in the pathological process and severity according to the appearance of AD patients, and the guidance of pharmacodynamics evaluation of AD-therapeutic drugs in clinical trials as well, which may provide a proposal for AD treatment drug candidates in the non-clinical pharmacodynamics evaluation. All animal experiments were approved by the Animal Care & Welfare Committee of Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College (approval No.: 00007782 and 00007784).

10.
Chinese Journal of Biologicals ; (12): 742-750, 2023.
Article in Chinese | WPRIM | ID: wpr-996459

ABSTRACT

@#The Coronavirus Disease 2019(COVID-19) pandemic is having a dramatic impact on human health,lives,and the global economy. The development of a safe and efficacious vaccine is the most effective intervention to protect the population from the disease and limit the spread of the virus. Based on the current guidelines and research progress of severe acute respiratory symptom coronavirus 2(SARS-CoV-2) vaccines in various countries,this review summarized the research progress on non-clinical safety evaluation of SARS-CoV-2 vaccines by referring to the guidelines and relevant literatures over the world,in order to provide a reference for non-clinical research of SARS-CoV-2 vaccines.

11.
Medicina (B.Aires) ; 82(5): 752-759, Oct. 2022. graf
Article in Spanish | LILACS-Express | LILACS | ID: biblio-1405732

ABSTRACT

Resumen La insulina aspártica de acción rápida es una formulación más rápida de la insulina aspártica convencional, a la que se adicionan nicotinamida y L-arginina para lograr una absorción más rápida en el tejido celular subcutáneo. Estudios farmacocinéticos y farmacodinámicos demostraron un desplazamiento de las curvas de concentración sérica de insulina/tiempo hacia la izquierda en comparación con la formulación conven cional. Su perfil de eficacia se destaca en términos del control de la glucemia posprandial temprana. Además, la insulina aspártica de acción rápida aporta flexibilidad al tratamiento, ya que puede aplicarse al momento de la comida, inmediatamente antes o hasta 20 minutos después, lo que constituye una ventaja en cuanto a calidad de vida en los pacientes con diabetes en tratamiento con insulina prandial, especialmente en poblaciones como los niños, las embarazadas o los ancianos. El patrón de seguridad y tolerabilidad es comparable al de la insulina aspártica convencional.


Abstract Fast acting aspart insulin is a faster-acting formulation of aspart insulin, having nicotinamide and L-arginine added to the molecule, in order to achieve a faster absorption through the subcutaneous cellular tissue. Pharmacokinetic and pharmacodynamic studies showed a left-shifted mean serum concentration-time profile compared to the conventional formulation. Its efficacy profile is highlighted in terms of early postprandial glycemic control. In addition, fast acting aspart insulin allows a more flexible treatment schedule, as it may be administrated at mealtime, immediately before or up to 20 minutes after; this schedule represents an advantage regarding quality of life in patients with diabetes treated with prandial insulin, especially in populations such as children, pregnant women or elderly subjects. The safety and tolerability profiles are comparable to conventional aspart insulin.

12.
Rev. cuba. hematol. inmunol. hemoter ; 38(2): e1583, abr.-jun. 2022. graf
Article in Spanish | LILACS, CUMED | ID: biblio-1408455

ABSTRACT

Introducción: Los linfomas no Hodgkin indolentes se destacan por el reto que suponen desde el punto de vista terapéutico. La introducción de la terapia con rituximab, un anticuerpo monoclonal que se une al antígeno CD20 de la membrana de los linfocitos B, revolucionó los tratamientos hasta ese momento y abrió el camino para el desarrollo de otros anticuerpos monoclonales anti-CD20. Objetivo: Describir las características generales de los linfomas no Hodgkin indolentes y de los anticuerpos monoclonales anti-CD20, así como el rol de la terapia anti-CD20 en dichas enfermedades. Métodos: Se realizó una revisión de la literatura publicada en los últimos 20 años, disponible en los repositorios: Scielo, Scopus, Pubmed/Medline, ScienceDirect y Mediagraphic. Se emplearon para elaborar este manuscrito 35 documentos, de ellos 80 por ciento correspondieron a los últimos 5 años. Conclusiones: La sólida evidencia científica, acumulada durante las últimas dos décadas, respalda el uso clínico de los anticuerpos monoclonales anti-CD20 en el tratamiento de los linfomas no Hodgkin indolentes. El uso efectivo de estos fármacos como agentes únicos o combinados con quimioterapia demuestran su versatilidad terapéutica(AU)


Introduction: Indolent non-Hodgkin's lymphomas are notable for the challenge they pose from a therapeutic point of view. The introduction of rituximab, a monoclonal antibody that binds to the CD20 antigen of the B-lymphocyte membrane, revolutionized treatments up to that time and opened the way for the development of other anti-CD20 monoclonal antibodies. Objective: To describe the general characteristics of indolent non-Hodgkin's lymphomas and anti-CD20 monoclonal antibodies, as well as the role of anti-CD20 therapy in these diseases. Methods: A review of the literature published in the last 20 years, available in the repositories: Scielo, Scopus, Pubmed/Medline, Science Direct and Mediagraphic, was performed. Thirty-five papers were used to prepare this manuscript, 80 percent of which corresponded to the last 5 years. Conclusions: Strong scientific evidence, accumulated over the last two decades, supports the clinical use of anti-CD20 monoclonal antibodies in the treatment of indolent non-Hodgkin's lymphomas. The effective use of these drugs as single agents or in combination with chemotherapy demonstrates their therapeutic versatility(AU)


Subject(s)
Humans , Male , Female , Antigens, CD20/therapeutic use , Rituximab , Antibodies, Monoclonal/therapeutic use , Pharmaceutical Preparations
13.
Braz. J. Pharm. Sci. (Online) ; 58: e19321, 2022. tab, graf
Article in English | LILACS-Express | LILACS | ID: biblio-1420424

ABSTRACT

Abstract To investigate the pharmacokinetics and pharmacodynamics of Astragali Radix-Corni Fructus herb-pair in kidney-yin deficiency model, which was made by continuously oral gavage of thyroxine. A simple and rapid LC-MS/MS method was developed and validated for the determination of loganin and morroniside in rat plasma and used for the pharmacokinetics study. The kidney-yin deficiency significantly changed the AUC(0-∞), Cmax and CLz/F of loganin and morroniside. The T1/2z of morroniside increased significantly in the kidney-yin deficiency rats. For the pharmacodynamics study, the liver index, kidney index, and ALT, TBIL, UREA, CREA level in the kidney-yin deficiency mice were examined. The herb-pair had been proved to be effective for the treatment of kidney-yin deficiency by affecting the liver, kidney, ALT, UREA and CREA, which showed positively correlated with the dose. The pharmacokinetics and pharmacodynamics studies in the pathological status could offer more valuable information for the future application of Astragali Radix-Corni Fructus herb-pair.

14.
China Pharmacy ; (12): 1782-1786, 2022.
Article in Chinese | WPRIM | ID: wpr-934965

ABSTRACT

Augmented renal clearance (ARC)refers to the significant enhancement of patients ’renal function ,which is manifested by the significant increase of glomerular filtration rate ,which increases the clearance of drugs ,and the effective blood drug concentration cannot be achieved under the conventional dose. The efficacy of antibiotics is closely related to the concentration. The influence of renal dysfunction on drug metabolism is an important factor that clinicians should consider when determining the dosage. This article reviews the definition ,risk factors ,occurrence mechanism ,evaluation methods of ARC ,as well as its impact on the pharmacokinetics/pharmacodynamics of antibiotics and administration methods. It is found that ARC widely exists in critically ill patients ,and the risk factors include age (≤50 years old ),brain trauma ,sepsis,multiple trauma , etc. When using antibiotics in ARC patients ,the therapeutic effect of drugs can be improved by increasing the dosage ,prolonging the duration of administration and increasing the frequency of administration. However ,in order to prevent adverse reactions caused by high concentration accumulation of drugs ,it is recommended to try to combine treatment drug monitoring.

15.
Chinese Pediatric Emergency Medicine ; (12): 246-249, 2022.
Article in Chinese | WPRIM | ID: wpr-930840

ABSTRACT

Pharmacokinetics/pharmacodynamics study fully considers the relationship among pathogens, hosts and drugs, which reflects the relationship between bactericidal effects and adverse drug reactions and the change of drug concentrations, which is of much value to the rational use of antimicrobial agents and delaying antimicrobial resistance.This review discussed design and optimization of dosing regimens for anti-infective therapy base on theory of pharmacokinetics/pharmacodynamics.

16.
Chinese Journal of Experimental Traditional Medical Formulae ; (24): 123-130, 2022.
Article in Chinese | WPRIM | ID: wpr-940395

ABSTRACT

ObjectiveTo explore the pharmacodynamic ingredients of Zhenqi Fuzheng granules (ZFG) for immunomodulatory through spectrum-effect relationship analysis, which provides experimental basis for improving the quality standard of ZFG. MethodEighteen batches of ZFG from six manufacturers were collected for analysis. The fingerprints were established by high performance liquid chromatography (HPLC). Acetonitrile (A)-0.1% formic acid aqueous solution (B) were adopted as the mobile phase with gradient elution (0-15 min, 5%A; 15-23 min, 5%-8%A; 23-30 min, 8%-11%A; 30-45 min, 11%-18%A; 45-60 min, 18%-21%A; 60-67 min, 21%-23%A; 67-90 min, 23%-37%A), the detection wavelength was 220 nm. Chemometric analysis such as similarity analysis and hierarchical cluster analysis (HCA) were subsequently used to analyze the similarities and chemical differences among these samples. A cyclophosphamide-induced immunodeficiency mouse model was used to evaluate the immune-enhancing effects of the products from different manufacturers. The spectrum-effect relationship between HPLC fingerprints and the immunomodulatory effects was examined using Spearman bivariate correlation analysis. HPLC coupled with mass spectrometry (HPLC-MSn) was used to identify the spectrum-effect related peaks with electrospray ionization, positive and negative ion modes, and scanning range of m/z 100-1 500. ResultThe HPLC fingerprint of ZFG was established, and twenty peaks with good resolution were selected as common peaks. The results of quality analysis and pharmacodynamic test showed there were significant differences in both ingredients content and immune-enhancing effects of ZFG from different manufacturers. Through spectrum-effect relationship study, twelve peaks were screened as bioactive ingredients peaks. Thereafter, eight peaks among them were subsequently identified by HPLC-MSn. They were salidroside (peak 2), echinacoside (peak 5), calycosin-7-glucoside (peak 6), isomer of specnuezhenide (peak 7), isonuezhenide (peak 9), calycosin (peak 11), nuezhenide G13 or oleonuezhenide (peak 14), and formononetin (peak 18), respectively. ConclusionThere are differences in quality and efficacy of ZFG produced by different manufacturers. Through spectrum-effect relationship analysis, the medicinal ingredients of ZFG for immune-enhancing effects are screened, which can provide reference for the improvement of its quality standard.

17.
Acta Pharmaceutica Sinica ; (12): 2153-2157, 2022.
Article in Chinese | WPRIM | ID: wpr-936573

ABSTRACT

This study is to establish and validation in vivo models of moxifloxacin based on the theory of physiologically based pharmacokinetics (PBPK), and then to predict the distribution of moxifloxacin in human venous return and organ such as lung, spleen and so on. The efficacy of moxifloxacin and its pharmaceutical preparations were quantified by comparing the pharmacokinetic parameters with the minimum inhibitory concentration of related pathogenic bacterium. The results showed that the anti-infection efficacy of pharmaceutical moxifloxacin preparation in the corresponding organs was basically the same. The PBPK model of moxifloxacin preparations can be more accurately described the pharmacokinetic of anti-infective drugs in human, it is suitable for the efficacy evaluation of anti-infective drugs and provides a strong basis for the corresponding scientific research and scientific supervision.

18.
Japanese Journal of Drug Informatics ; : 189-196, 2022.
Article in Japanese | WPRIM | ID: wpr-924598

ABSTRACT

Objective: To evaluate the editing of “ Goodman & Gilman’s The Pharmacological Basis of Therapeutics ”, which is well known as a resource for the te aching of pharmacology.Methods: The text has been edited 13 times between 1941, when it was first published, and 2018, the latest (13th) edition. We examined and compared the transition of each of the editions and their content.Results: In fact, one of the editors was awarded the Nobel Prize in Physiology or Medicine in 1994. Moreover, from the first edition of this text, the term “pharmacodynamics” was applied to the usage of medicine useful. As the four important basic principles in drug therapy of the book are continuously edited, it is used in School of Medicine for the teaching of pharmacology and is highly regarded.Conclusions: This book is high-quality one edited with the latest information and shares new drug in the field of pharmacology. We should surely recognize the usefulness of this resource.

19.
China Pharmacy ; (12): 699-705, 2022.
Article in Chinese | WPRIM | ID: wpr-923005

ABSTRACT

OBJECTIVE To study th e pharmacodynamics and pha rmacokinetics of Qinglian ningxin capsule in rats with ischemic arrhythmia. METHODS Totally 30 male SD rats were randomly divided into blank control group ,model control group , Qinglian ningxin capsule group (4.00 g/kg),Artemisia annua group(1.43 g/kg),Coptis chinensis group(0.42 g/kg),with 6 rats in each group. Administration groups were given relevant medicine intragastrically ;model control group and blank control group were given normal saline intragastrically ,once a day ,for consecutive 7 days. After last medication ,except for blank control group,other groups were given Posterior pituitary injection via tail vein (1 u/kg) to induce ischemic arrhythmia model. electrocardiogram changes of rats in each group were recorded. Another 36 rats were randomly divided into Qinglian ningxin capsule model group and Qinglian ningxin capsule control group (4.00 g/kg),A. annua model group and A. annua control group (1.43 g/kg),C. chinensis model group and C. chinensis control group (0.42 g/kg). After the rats in each model group were injected with Posterior pituitary injection (1 u/kg)via tail vein ,administration groups were given relevant drugs intragastrically , and control groups were given constant volume of normal saline intragastrically. Blood was taken from the orbit at different time points(0,0.25,0.75,1,2,4,6,8,12 and 24 h). The concentrations of berberine hydrochloride and artemisinin in plasma were determined by HPLC ,and the pharmacokinetic parameters were calculated by WinNonlin 7.0 software. RESULTS Compared with the model control groups ,Qinglian ningxin capsule could significantly improve the heart rate slowing of rats and redu ced the prolongation of PR interval and QT interval significantly ,and the effects were generally better than those of A. annua group and C. chinensis group(P<0.05). Compared with A. annua control group and C. chinensis control group ,cmax,AUC0-t and AUC 0-∞ of berberine hydrochloride and artemisinin were increased significantly in Qinglian ningxin capsule control group,while CL was decreased significantly ;t1/2z of artemisinin was prolonged significantly (P<0.05). Compared with Qinglian ningxin capsule control group ,cmax(except artemisinin ),AUC0-t,AUC0-∞,MRT0-t and MRT 0-∞(except artemisinin )of berberine hydrochloride and artemisinin were increased significantly in Qinglian ningxin capsule model group ,while CL was decreased significantly(P<0.05). CONCLUSIONS Qinglian ningxin capsule could significantly improve ischemic arrhythmia better than A. annua and C. chinensis ,and can improve the absorption of berberine hydrochloride and artemisinin in model rats and slow down their elimination.

20.
Chinese Journal of Biotechnology ; (12): 990-1003, 2022.
Article in Chinese | WPRIM | ID: wpr-927758

ABSTRACT

Antimicrobial resistance is one of the critical public health issues in the world. There is an urgent need to develop effective broad-spectrum antibiotics to treat the infection of multi-drug resistant Gram-negative bacilli. Cefiderocol, developed by the Shionogi Inc. in Japan, is a new type of iron carrier cephalosporin antibiotics, which overcomes the drug resistance of Gram-negative bacilli due to the down-regulation of outer membrane pore protein and the up-regulation of efflux pump, and has good stability to serine- and metallo-carbapenemases. This drug has a broad spectrum and strong antibacterial activity against carbapenem-resistant Enterobacteriaceae (CRE), Pseudomonas aeruginosa, Acinetobacter baumannii, and Stenotrophomonas maltophilia. Cefiderocol can be used to treat complex urinary tract infections (including pyelonephritis), hospital-acquired pneumonia, and ventilator-associated pneumonia. By summarizing the chemical structure, antibacterial mechanism, in vitro antibacterial activity, pharmacokinetics, pharmacodynamics, and clinical treatment of cefiderocol, this review shows the application potential of cefiderocol as a new iron carrier cephalosporin in the treatment of multi-drug resistant Gram-negative bacilli infections.


Subject(s)
Cephalosporins/therapeutic use , Gram-Negative Bacteria , Microbial Sensitivity Tests , Siderophores/pharmacology
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