OBJECTIVETo investigate the correlation between dissolution in vitro and absorption in vivo of Chuanping sustained release tablets.

METHODThe ephedrine, pseudoephedrine were chosen as marker components, dissolution in vitro of Chuanping sustained release tablets in the different pH were tested by the rotating basket method and HPLC; urine drug levels were determined by HPLC and absorption fractions were calculated according to Wagner-Nelson's formula and deconvolution technique.

RESULTThe linear regressive equation between the absorption percentage in vivo F and accumulative release percentage in vitro of Chuanping sustained release tablets was established as F(ephedrine) = 1.572 5f-20. 729 (R2 = 0.974 5); F(pseudoephedrine) = 1.237f-0.147 6 (R2 = 0.959 5).

CONCLUSIONThe results suggested that there was fine correlation between the absorption percentage in vivo and the accumulative release percentage in vitro of Chuanping sustained release tablets.

Adult ; Chromatography, High Pressure Liquid ; Delayed-Action Preparations ; pharmacokinetics ; Drugs, Chinese Herbal ; administration & dosage ; pharmacokinetics ; Ephedrine ; administration & dosage ; pharmacokinetics ; Female ; Humans ; Male ; Solubility ; Tablets ; chemistry ; Young Adult

The paper is to establish a method for simultaneous determination of 5 kinds of alkaloids in ephedra and poppy which are in Kechuanning tablets. Solid-phase extraction (SPE) was adopted in pretreatment, and a UPLC method with 2 different wavelengths had been developed: 210 nm for the detection of morphine, codeine phosphate, ephedrine hydrochloride and pseudoephedrine hydrochloride, and 251 nm for papaverine hydrochloride. The column used was Acquity UPLC BEH C18 (100 mm x 2.1 mm ID, 1.7 microm) with linear gradient elution using acetonitrile and 0.1% phosphoric acid. The flow rate was 0.4 mL.min-1, and the column temperature was 30 degrees C. The linear response range was 0.375 0 - 12.50 microg.mL-1 for morphine, 0.064 32 - 2.144 microg.mL-1 for codeine phosphate, 0.030 06 - 1.002 microg.mL-1 for papaverine hydrochloride, 1.126 - 37.52 microg.mL-1 for ephedrine hydrochloride, 0.287 8 - 9.592 microg.mL-1 for pseudoephedrine hydrochloride (r = 0.999 7). The average recoveries of these compounds were 99.26%, 100.6%, 95.29%, 100.1% and 97.48%, respectively. This is a more reasonable and credible method of quality control for Kechuanning tablets.
Alkaloids ; analysis ; Chromatography, High Pressure Liquid ; Codeine ; analysis ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; isolation & purification ; Ephedra ; chemistry ; Ephedrine ; analysis ; Morphine ; analysis ; Papaver ; chemistry ; Papaverine ; analysis ; Plants, Medicinal ; chemistry ; Pseudoephedrine ; analysis ; Quality Control ; Solid Phase Extraction ; Tablets

OBJECTIVETo investigate the effects of ephedrine combined with various doses of naloxone on neural plasticity in rats after cerebral ischemia/reperfusion injury to explore the possibility of synergistic effect about ephedrine combined with naloxone, promoting the optimum ratio of neural remodeling and its molecular mechanism.

METHODA total of 192 healthy adult Sprague-Dawley rats, 220-250 g, were used to establish models of left middle cerebral artery occlusion using the suture occlusion method. Were randomly divided into 8 groups: the rats were intraperitoneally injected with 1.5 mg x kg(-1) x d(-1) ephedrine (ephedrine group), with 0.1, 0.2, 0.3 mg x kg(-1) x d(-1) naloxone (low, moderate and high doses of naloxone groups) , with 1.5 mg x kg(-1) x d(-1) ephedrine + 0.1, 0.2, 0.3 mg x kg(-1) x d(-1) naloxone (ephedrine + low, moderate and high doses of naloxone groups), and with 0.5 mL saline (model group), respectively. At 1-4 weeks following cerebral ischemia, sensorimotor integration in rats was assessed using the beam walking test, brain-derived neurotrophic factor (BDNF) expression was detected in the hippocampal CA3 area using immunohistochemistry 1-4 weeks after surgery, immunofluorescence method of detecting ischemic hemisphere hippocampal expression, The number of nerve cells apoptosis was detected using TUNEL assay.

RESULTBWT, BDNF, TUNEL assay results showed three doses of naloxone group had no significant effect, the effects increased together with the quantitative ephedrine, and had the amount-effect relationship, in which ephedrine + high dose of naloxone group the recovery of movement was fastest, BDNF expression in the best and ischemic apoptosis in the hippocampus at least, ischemic injury to the minimum, speed up the process of neural remodeling.

CONCLUSIONThe ephedrine and ephedrine + naloxone groups were accelerated motor function recovery rate in rat after cerebral ischemia, and the promotion of neural remodeling is closely related to the expression of BDNF, inhibit apoptosis in ischemic area, and with the increase of naloxone amount of additives, its role more clearly, the mechanism may be related to the dose of naloxone can significantly inhibit the ischemic area of apoptosis in early cerebral ischemia, so had the positive synergy effect with ephedrine to speed up the formation of neural remodeling.

Animals ; Apoptosis ; drug effects ; Brain Ischemia ; drug therapy ; genetics ; metabolism ; physiopathology ; Brain-Derived Neurotrophic Factor ; genetics ; metabolism ; Disease Models, Animal ; Ephedrine ; administration & dosage ; Female ; Hippocampus ; drug effects ; metabolism ; physiopathology ; Humans ; Male ; Naloxone ; administration & dosage ; Neuronal Plasticity ; drug effects ; Random Allocation ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo establish a method to evaluate the in vitro release of Zhike Pingchuan sustained-release tablets.

METHODThe ephedrine, pseudoephedrine, scopolamine were chosen as marker components components, and the chromatographic conditions were chosen according to the separation of baseline and theoretical plate number for determining the marker in vitro release of Zhike Pingchuan sustained-release tablets; through the dissolution curves of the three active components, the release behavior was judged as well-balanced release or not.

RESULTCompared with conventional tablets, the Zhike Pingchuan sustained-release tablets had a well-balanced behavior in 10 h.

CONCLUSIONThe maker components of Zhike Pingchuan sustained-release tablets and two chromatographic conditions, which were used to determine the dissolution of the sustained-release tablets, could be chosen as evaluation methods for the in vitro release of Zhike Pingchuan sustained-release tablets.

Administration, Oral ; Chemistry, Pharmaceutical ; Chromatography, High Pressure Liquid ; Delayed-Action Preparations ; chemistry ; Drug Carriers ; Drug Compounding ; Drug Stability ; Ephedrine ; chemistry ; Hardness ; Hydrogen-Ion Concentration ; Kinetics ; Pharmaceutical Preparations ; chemistry ; Solubility ; Spectrophotometry, Ultraviolet ; Tablets ; chemistry

We designed a randomized, double-blinded study to determine the efficacy and safety of 0.5 mg/kg intravenous ephedrine for the prevention of hypotension during spinal anesthesia for cesarean delivery. Patients were randomly allocated into two groups: ephedrine group (n=21) and control group (n=21). Intravenous preload of 15 mL/kg lactated Ringer's solution was given. Shortly after the spinal injection, ephedrine 0.5 mg/kg or saline was injected intravenous for 60 sec. The mean of highest and lowest heart rate in the ephedrine group was higher than those of control group (P<0.05). There were significant lower incidences of hypotension and nausea and vomiting in the ephedrine group compared with the control group (8 [38.1%] vs. 18 [85.7%]); (4 [19%] vs. 12 [57.1%], respectively) (P<0.05). The first rescue ephedrine time in the ephedrine group was significantly longer (14.9+/-7.1 min vs. 7.9+/-5.4 min) than that of the control group (P<0.05). Neonatal outcome were similar between the study groups. These findings suggest, the prophylactic bolus dose of 0.5 mg/kg intravenous ephedrine given at the time of intrathecal block after a crystalloid fluid preload, plus rescue boluses reduce the incidence of hypotension.
Adult ; *Anesthesia, Spinal/adverse effects ; Blood Pressure/drug effects ; *Cesarean Section ; Ephedrine/administration & dosage/*therapeutic use ; Female ; Heart Rate/drug effects ; Humans ; Hypotension/chemically induced/prevention & control ; Injections, Intravenous ; Postoperative Nausea and Vomiting/prevention & control ; Pregnancy ; Vasoconstrictor Agents/administration & dosage/*therapeutic use

OBJECTIVETo compare the cutaneous permeation of Kechuan acupoint patch and power, and evaluate the possibility of dosage form reform of Kechuan recipe.

METHODTake the Eugend and Ephedrine as the indexes, HPLC was employed to determine their contents, the pond with Franz diffusion were used to measured the cutaneous.

RESULTThe permeation of Patch matched with Higuchi Equation. Take Eugend as the index, the permeation rate of total of Patch is 2.319 and 1.738 times of the powder, and 1.784 and 1.215 times of the powder with the Ephedrineas as index.

CONCLUSIONThe permeation rate of Kechuan acupoint patch was more rapid than the powder. Moreover, the total quantity of permeation of patch was also more than the powder.

Acupuncture Points ; Administration, Cutaneous ; Animals ; Anti-Asthmatic Agents ; administration & dosage ; pharmacokinetics ; Chromatography, High Pressure Liquid ; Drug Combinations ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; pharmacokinetics ; Ephedrine ; administration & dosage ; pharmacokinetics ; Eugenol ; administration & dosage ; pharmacokinetics ; In Vitro Techniques ; Permeability ; Plants, Medicinal ; chemistry ; Powders ; Rabbits ; Skin ; metabolism ; Skin Absorption

A cardiovascular collapse, due to preoperatively administered intravenous vitamin K (phytonadione), was experienced in a 59-year-old woman who was scheduled to undergo a left upper lung lobectomy. The patient developed sudden facial flushing, an upper torso rash, dyspnea, palpitation, and severe hypotension about 2 min after the intravenous administration of approximately 2 mg of vitamin K. Immediate hydration and an injection of 20 mg ephedrine restored her blood pressure to the preoperative level within 5 min. The patient recovered without any sequelae, but the operation was postponed. The patient's symptoms seemed to be due to an anaphylactoid reaction or anaphylaxis following the intravenous administration of vitamin K. This case report suggests that physicians should carefully review the indications of vitamin K prior to administration, even at low doses.
Administration, Intravenous ; Anaphylaxis ; Blood Pressure ; Dyspnea ; Ephedrine ; Exanthema ; Female ; Flushing ; Humans ; Hypotension ; Lung ; Middle Aged ; Torso ; Vitamin K ; Vitamins*

OBJECTIVETo compare the solubilities of ephedrine and d-pseudo-ephdrine in the compound of traditional Chinese drugs--Maxing Shigan decoction with and without ultramicro-pulverizations using a RP-HPLC procedure.

METHODThe analytical column was a YMC ODS-C18(4.6 mm x 150 mm,4 microm). A mixture of water-acetonitrile-sodium dodecyl sulfate-phosphorous acid (650:350:5:1) was used as the mobile phase at flow rate of 1.5 mL x min(-1). The column temperature was 50 degrees C and the wavelength was 210 nm.

RESULTIn this way, ephedrine and d-pseudo-ephedrine of the compound samples can be separated well and showed significant differences before and after the ultramicro-pulverizations.

CONCLUSIONFor the Maxing Shigan decoction, the dissolution rates and solubilites of ephedrine and d-pseudo-ephedrine ultramicro-pulverization were greatly improved.

Calcium Sulfate ; chemistry ; Drug Combinations ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; isolation & purification ; Ephedra ; chemistry ; Ephedrine ; analysis ; chemistry ; Glycyrrhiza uralensis ; chemistry ; Particle Size ; Plants, Medicinal ; chemistry ; Powders ; Prunus ; chemistry ; Solubility ; Technology, Pharmaceutical ; methods

AIMTo develop and validate a liquid chromatography-tandem mass spectrometric (LC/MS/MS) method for the simultaneous quantification of ephedrine and chlorpheniramine in human plasma after oral administration of a compound preparation.

METHODSThe analytes and the internal standard, diphenhydramine, were isolated from plasma by protein precipitation with methanol, then chromatographied on a Zorbax SB-C18 column (150 mm x 4.6 mm ID) using a mobile phase consisted of methanol-water-formic acid (80: 20: 0.5, v/v), at a flow rate of 0.5 mL x min(-1). A tandem mass spectrometer equipped with electrospray ionization source was used as detector and was operated in the positive ion mode. Selected reaction monitoring (SRM) using the precursor to produce ion combinations of m/z 166-->115, m/z 275-->230 and m/z 256-->167 were used to quantify ephedrine, chlorpheniramine and the internal standard, respectively. Results The linear concentration ranges of the calibration curves for ephedrine and chlorpheniramine were 0.50 - 200 microg x L(-1) and 0.050 - 20.0 microg x L(-1), respectively. The lower limits of quantification were 0. 50 microg x L(-1) for ephedrine and 0.050 microg x L(-1) for chlorpheniramine, individually. The intra- and inter-day relative standard deviation (RSD) across three validation runs over the entire concentration range was less than 9.3% for both ephedrine and chlorpheniramine. The inter-day accuracy (RE) was within +/- 3.4% for the analytes. Each sample was chromatographied within 3.3 min. The method was successfully used in pharmacokinetics study of ephedrine and chlorpheniramine in human plasma after oral administration of a compound preparation containing 5 mg ephedrine hydrochloride, 1 mg chlorpheniramine maleate, 50 mg phenytoin, 12.5 mg theophylline, 12.5 mg theobromine and 7.5 mg caffeine. No interaction among the six components was observed on their pharmacokinetic parameters.

CONCLUSIONThe method was proved to be highly sensitive, selective, and suitable for pharmacokinetics investigations of different compound preparations containing low dosage of both ephedrine and chlorpheniramine.

Administration, Oral ; Area Under Curve ; Chlorpheniramine ; administration & dosage ; blood ; pharmacokinetics ; Chromatography, Liquid ; methods ; Drug Combinations ; Ephedrine ; administration & dosage ; blood ; pharmacokinetics ; Humans ; Male ; Spectrometry, Mass, Electrospray Ionization ; methods

OBJECTIVETo develop a GC-MS method for the determination of pseudo-ephedrine in human plasma and study the mutative rules of the pharmacokinetic parameters of the pseudo-ephedrine in different compositions.

METHODOrthogonal design was used to determine 8 compositions from Mahuang decoction (MHD). The healthy volunteers were divided into groups in random, each group including 8 men. After taking the medicine orally, vena blood would be taken out at different time. Determining pseudo-ephedrine in plasma and plotting the concentration-time curve, the pharmacokinetic parameters of each composition were calculated by WinNonlin 4.0.1. The statistical analysis of the pharmacokinetic parameters was proceeded by SPSS 10.0.

RESULTAll concentration-time curves were adequately modeled by one compartment, first order absorption model, no lag time. Some parameters of pseudo-ephedrine showed significant variance (P < 0.05) in different compositions. The statistic results showed interactions between drugs in MHD (P < 0.05).

CONCLUSIONThe other herbs erds of MHD have some certain extent effects to the pharmacokinetic parameters of pseudo-ephedrine in the dominant drug.

Administration, Oral ; Adult ; Area Under Curve ; Cinnamomum ; chemistry ; Drug Combinations ; Drug Interactions ; Drugs, Chinese Herbal ; administration & dosage ; isolation & purification ; pharmacokinetics ; Ephedra ; chemistry ; Ephedrine ; isolation & purification ; pharmacokinetics ; Glycyrrhiza uralensis ; chemistry ; Humans ; Male ; Plants, Medicinal ; chemistry ; Prunus ; chemistry ; Random Allocation