1.Bioequivalence of clavulanate potassium and amoxicillin (1:7) dispersible tablets in healthy volunteers.
Guoxin HU ; Zongshun DAI ; Lihong LONG ; Ying HAN ; Shuxian HOU ; Li WU
Journal of Huazhong University of Science and Technology (Medical Sciences) 2002;22(3):224-227
To study the bioequivalence of Clavulanate Potassium and Amoxicillin (1:7) dispersible tablets, a randomized cross-over study was conducted in 18 healthy volunteers. A single oral dose of 1,000 mg Clavulanate Potassium and Amoxicillin (1:7) dispersible tablets (Tested formulation, T) or Augmentin syrup (Reference formulation, R). Concentrations in plasma were determined with high-performance liquid chromatography. The main parameters of T were: for Clavulanate Potassium and Amoxicillin, Cmax: 2.46 +/- 1.11 micrograms/ml and 18.81 +/- 7.26 micrograms/ml, Tmax: 1.12 +/- 0.23 h and 1.30 +/- 0.34 h, AUC(0-6 h): 5.18 +/- 2.24 micrograms.h/ml and 45.09 +/- 14.53 micrograms.h/ml, t1/2: 1.43 +/- 0.44 h and 1.09 +/- 0.22 h., respectively. The relative bioavailability of T to R were 96.5 +/- 19.2% and 98.4 +/- 26.1%, respectively. Statistical analysis showed that the two formulations were bioequivalent.
Adult
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Amoxicillin-Potassium Clavulanate Combination
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pharmacokinetics
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Drug Therapy, Combination
;
pharmacokinetics
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Humans
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Male
;
Tablets
;
Therapeutic Equivalency
2.Bioequivalence of clavulanate potassium and amoxicillin (1:7) dispersible tablets in healthy volunteers.
Guoxin, HU ; Zongshun, DAI ; Lihong, LONG ; Ying, HAN ; Shuxian, HOU ; Li, WU
Journal of Huazhong University of Science and Technology (Medical Sciences) 2002;22(3):224-7
To study the bioequivalence of Clavulanate Potassium and Amoxicillin (1:7) dispersible tablets, a randomized cross-over study was conducted in 18 healthy volunteers. A single oral dose of 1,000 mg Clavulanate Potassium and Amoxicillin (1:7) dispersible tablets (Tested formulation, T) or Augmentin syrup (Reference formulation, R). Concentrations in plasma were determined with high-performance liquid chromatography. The main parameters of T were: for Clavulanate Potassium and Amoxicillin, Cmax: 2.46 +/- 1.11 micrograms/ml and 18.81 +/- 7.26 micrograms/ml, Tmax: 1.12 +/- 0.23 h and 1.30 +/- 0.34 h, AUC(0-6 h): 5.18 +/- 2.24 micrograms.h/ml and 45.09 +/- 14.53 micrograms.h/ml, t1/2: 1.43 +/- 0.44 h and 1.09 +/- 0.22 h., respectively. The relative bioavailability of T to R were 96.5 +/- 19.2% and 98.4 +/- 26.1%, respectively. Statistical analysis showed that the two formulations were bioequivalent.
Amoxicillin-Potassium Clavulanate Combination/*pharmacokinetics
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Drug Therapy, Combination/*pharmacokinetics
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Tablets
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Therapeutic Equivalency
3.Studies on accumulation of active ingredients, N, P and K in Anemarrhena asphodeloides.
Juan CHEN ; Chong-jun YANG ; Yu-hai GUO
China Journal of Chinese Materia Medica 2007;32(15):1504-1507
OBJECTIVETo study the accumulation of active ingredients, the absorption and transformation of N, P and K in Anemarrhena asphodeloides and provide basis for determination of the harvest time and fertilizing.
METHODSamples were collected in different phrases and the weight of dry matter, the content of N, P and K of different organs and the content of sarsasapogenin were determined.
RESULTAbsorption of N, P and K started by the root and rhizoma after July. At the end of August, the N and K of the aerial part transfered largely into rhizome. The content of sarsasapogenin in rhizome was the highest in early spring.
CONCLUSIONAdditional fertilizer is helpful to increase the yield in July of the second year after the transplantation. The quality is the best when harvest in early spring.
Absorption ; Anemarrhena ; metabolism ; Fertilizers ; Nitrogen ; pharmacokinetics ; Phosphorus ; pharmacokinetics ; Plant Components, Aerial ; metabolism ; Plant Roots ; metabolism ; Plants, Medicinal ; metabolism ; Potassium ; pharmacokinetics ; Rhizome ; metabolism ; Seasons ; Spirostans ; metabolism
4.In vivo targeting of ERGpotassiumchannels inmice and dogs by a positron-emitting analogue of fluoroclofilium.
Sang Wook KIM ; Seung Dae YANG ; Byung Jae AHN ; Jeong Hoon PARK ; Dong Soo LEE ; Guido GESSNER ; Stefan H HEINEMANN ; Wilhelm HERDERING ; Kook Hyun YU
Experimental & Molecular Medicine 2005;37(4):269-275
The antiarrhythmic clofilium is an efficient blocker of hERG1 potassium channels that are strongly expressed in the heart. Therefore, derivatives of clofilium that emit positrons might be useful tools for monitoring hERG1 channels in vivo. Fluoroclofilium (F-clofilium) was synthesized and its channel-blocking properties were determined for hERG1 and hEAG1 channels expressed in HEK 293 cells and in Xenopus oocytes. When applied extracellularly in the whole-cell patch-clamp configuration, F-cloflium exhibited a slower onset of block when compared with clofilium, presumably owing to its lower membrane permeability. When applied in the inside-out configuration at the intracellular membrane side, it blocked hEAG1 channels almost as efficiently as clofilium (IC50 1.37 nM and 0.83 nM, respectively). Similar results were obtained for hERG1, showing Fclofilium is a potent hERG1 and hEAG1 channel blocker once it has reached the intracellularly accessible target site at the channel. Using the 18Flabeled analog we studied the in vivo binding and distribution of F-clofilium in mice and a dog. Greatest activity was found in kidneys and bones. A small but significant enrichment of activity in the dog myocardium known for its expression of cERG1 channels allowed to depict the myocardium of a living dog by PET. Thus, F-clofilium is a useful tool for imaging hERG channels in living organisms.
Animals
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Anti-Arrhythmia Agents/pharmacokinetics/*pharmacology
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Cell Line
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Dogs
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Electrons
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Ether-A-Go-Go Potassium Channels/*antagonists & inhibitors
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Female
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Inhibitory Concentration 50
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Kidney/metabolism
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Mice
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Mice, Inbred BALB C
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Myocardium/metabolism
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*Positron-Emission Tomography
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Potassium Channel Blockers/pharmacokinetics/*pharmacology
;
Quaternary Ammonium Compounds/pharmacokinetics/pharmacology
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Research Support, Non-U.S. Gov't
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Tissue Distribution
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Xenopus
5.Na+i, K+i and Cl-i regulation of exocytosis in guinea-pig antral mucous cells.
Takashi NAKAHARI ; Shoko FUJIWARA ; Chikao SHIMAMOTO
Journal of Korean Medical Science 2000;15(Suppl):S36-S37
Effects of intracellular Na+, K+ and Cl- on Ca(2+)-regulated exocytosis activated by 10 microM acetylcholine (ACh) were studied in guinea-pig antral mucous cells which are permeabilized by nystatin treatment. Ca(2+)-regulated exocytotic events were modulated by [Na+]i, [K+]i and [Cl-]i via mediation of PTX-sensitive G proteins. Increases in [Na+]i and PTX inhibit G protein (G(Na)), which suppressed the exocytosis. Increases in [K+]i caused the exchange of G proteins (from G(Na) to G(K)) to increase, and GK evoked activation of the exocytosis and was inhibited by PTX. Increases in [Cl-]i and PTX inhibit G protein (G(Cl)), which stimulates exocytotic events. Based on these observations, the exocytosis in antral mucous cells were modulated by intracellular ions, concentration of which were increased or decreased by cell volume changes caused by Ach.
Acetylcholine/pharmacology
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Animal
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Cell Membrane Permeability/drug effects
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Exocytosis/physiology*
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Exocytosis/drug effects
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Gastric Mucosa/metabolism
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Gastric Mucosa/cytology
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Guinea Pigs
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Hypertonic Solutions/pharmacology
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Ionophores/pharmacology
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Nystatin/pharmacology
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Pertussis Toxins/pharmacology
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Potassium/pharmacokinetics*
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Pyloric Antrum/metabolism*
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Pyloric Antrum/cytology
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Sodium Chloride/pharmacokinetics*
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Vasodilator Agents/pharmacology
6.Effect of G protein in the dual regulation of opioid receptor agonist on the delayed rectified potassium channels.
Cai-ying YE ; Qing-xia LI ; Xiao-li YU ; Jing-jing QI ; Juan LI ; De-chang ZHANG
Acta Academiae Medicinae Sinicae 2003;25(3):297-300
OBJECTIVETo observe the role of G protein in the dual regulation of opioid receptor agonist on the delayed rectified potassium channels.
METHODSUsing whole-cell patch-clamp techniques applied to NG108-15 cells, investigate the effect of opioid receptor agonist on the delayed rectified potassium channels by administration of Guanosine-5'-0'-2-thiociphosphate (GDP beta S), Pertusis Toxin (PTX), Tetroacetic acid nueleoside diphosphate kinase (NDPK) and Adenosine-3' 5' cyclic monophosphate cAMP in the pipette solution.
RESULTS(1) GDP beta S could block the changes induced by both high and low concentration of (D-Pen2.5)-enkephalin (DPDPE) (P < 0.05). (2) PTX could inhibit the excitative regulation on K+ channel by high concentration of DPDPE (P < 0.05). But CTX had no effect on K+ channel caused by DPDPE. (3) UDP could block the excitative effect of K+ channel by high concentration of NDPK, while have no changes on the inhibitory effect caused by low concentration of opioid agonists. (4) cAMP took part in the regulation in high concentration of agonist administration (P < 0.05), while no changes for low concentration of agonists.
CONCLUSIONSDual changes were observed on delayed rectifier potassium channel by agonist treatment on NG108-15 cells. The excitative effect was Gi/o coupled in high concentration of agonist incubation, related to cAMP. While the inhibitory effect was possibly induced by G protein beta gamma subunit directly.
Animals ; Enkephalin, D-Penicillamine (2,5)- ; pharmacology ; GTP-Binding Proteins ; physiology ; Glioma ; metabolism ; pathology ; Guanosine Monophosphate ; analogs & derivatives ; pharmacokinetics ; Hybrid Cells ; metabolism ; pathology ; Mice ; Neuroblastoma ; metabolism ; pathology ; Patch-Clamp Techniques ; Pertussis Toxin ; pharmacology ; Potassium Channels, Inwardly Rectifying ; metabolism ; Rats ; Receptors, Opioid ; agonists ; Thionucleotides ; pharmacokinetics