Predicting the Strength of Cohesive and Adhesive Interparticle Interactions for Dry Powder Inhalation Blends of Terbutaline Sulfate with α-Lactose Monohydrate.

Grid-based systematic search methods are used to investigate molecule-molecule, molecule-surface, and surface-surface contributions to interparticle interactions in order to identify the crystal faces that most strongly affect particle behavior during powder blend formulation and delivery processes. The model system comprises terbutaline sulfate (TBS) as an active pharmaceutical ingredient (API) and α-form lactose monohydrate (LMH). A combination of systematic molecular modeling and X-ray computed tomography (XCT) is used to determine not only the adhesive and cohesive interparticle energies but, also the agglomeration behavior during manufacturing and de-agglomeration behavior during delivery after inhalation. This is achieved through a detailed examination of the balance between the adhesive and cohesive energies with the XCT results confirming the blend segregation tendencies, through the particle-particle de-agglomeration process. The results reveal that the cohesive interaction energies of TBS-TBS are higher than the adhesive energies between TBS and LMH, but that the cohesive energies of LMH-LMH are the smallest between molecule and molecule, molecule and surface, and surface and surface. This shows how systematic grid-search molecular modeling along with XCT can guide the digital formulation design of inhalation powders in order to achieve optimum aerosolization and efficacy for inhaled medicines. This will lead to faster pharmaceutical design with less variability, higher quality, and enhanced performance.

Innovative pulmonary targeting of terbutaline sulfate-laded novasomes for non-invasive tackling of asthma: statistical optimization and comparative in vitro/in vivo evaluation.

Asthma represents a globally serious non-communicable ailment with significant public health outcomes for both pediatrics and adults triggering vast morbidity and fatality in critical cases. The ß2-adrenoceptor agonist, terbutaline sulfate (TBN), is harnessed as a bronchodilator for monitoring asthma noising symptoms. Nevertheless, the hepatic first-pass metabolism correlated with TBN oral administration mitigates its clinical performance. Likewise, the regimens of inhaled TBN dosage forms restrict its exploitation. Consequently, this work is concerned with the assimilation of TBN into a novel non-phospholipid nanovesicular paradigm termed novasomes (NVS) for direct and effective TBN pulmonary targeting. TBN-NVS were tailored based on the thin film hydration method and Box-Behnken design was applied to statistically optimize the formulation variables. Also, the aerodynamic pattern of the optimal TBN-NVS was explored via cascade impaction. Moreover, comparative pharmacokinetic studies were conducted using a rat model. TBN elicited encapsulation efficiency as high as 70%. The optimized TBN-NVS formulation disclosed an average nano-size of 223.89 nm, ζ potential of -31.17 mV and a sustained drug release up to 24 h. Additionally, it manifested snowballed in vitro lung deposition behavior in cascade impactor with a fine particle fraction of 86.44%. In vivo histopathological studies verified safety of intratracheally-administered TBN-NVS. The pharmacokinetic studies divulged 3.88-fold accentuation in TBN bioavailability from the optimum TBN-NVS versus the oral TBN solution. Concisely, the results proposed that NVS are an auspicious nanovector for TBN pulmonary delivery with integral curbing of the disease owing to target specificity.

Clinical value of N-acetylcysteine combined with terbutaline sulfate in elderly patients with chronic obstructive pulmonary disease and its effect on apoptosis/anti-apoptosis mechanism.

BACKGROUND: The pathogenesis of chronic obstructive pulmonary disease (COPD) is complex. Our study aimed to investigate the clinical value of N-acetylcysteine (NAC) combined with terbutaline sulfate in the treatment of COPD in elderly people, and its effect on the apoptosis/anti-apoptosis mechanism. METHODS: A total of 126 elderly COPD patients in our hospital from December 2017 to June 2019 were recruited and divided into 3 groups. On the basis of conventional treatment, control group A was treated with NAC, control group B with terbutaline sulfate, and combined group with both drugs. Lung function, apoptosis/anti-apoptosis related indexes, oxidative stress indexes, COPD assessment test (CAT) score, 6-min walk distance (6MWD), blood gas indexes, and adverse reactions were measured. RESULTS: The levels of forced vital capacity (FVC), maximum mid-expiratory flow rate (MMF), peak expiratory flow (PEF), oxygenation index (OI), and blood oxygen saturation (SaO2) in 3 groups were increased after treatment, and were the highest in the combined group. The level of carbon dioxide partial pressure (PaCO2) was decreased, and was the lowest in the combined group. After 2 weeks of treatment, the 6MWD had increased in all 3 groups and was longest in the combined group. The CAT score was decreased and the extent of decrease was the highest in the combined group. After treatment, the levels of Fas receptor/apoptosis antigen 1 (Fas/APO-1), soluble Fas (sFas), malondialdehyde (MDA), and reactive oxygen species (ROS) in the three groups were decreased, and their levels were decreased most markedly in the combined group. Meanwhile, the levels of superoxide dismutase (SOD) and glutathione peroxide enzyme (GSH-PX) were increased after treatment, and their levels were the highest in the combined group. The incidence of dizziness, chest tightness, constipation, and nasal congestion in the combination group were not significantly different from the other two groups. CONCLUSIONS: The combined use of terbutaline sulfate and NAC in the treatment of elderly patients with COPD can effectively improve their lung function and blood gas status, which can strengthen athletic ability, reduce the oxidative stress response, and regulate apoptotic cytokines.

A novel nanogel loaded with chitosan decorated bilosomes for transdermal delivery of terbutaline sulfate: artificial neural network optimization, in vitro characterization and in vivo evaluation.

The objective of the present work was to formulate, optimize, and evaluate transdermal terbutaline sulfate (TBN)-loaded bilosomes (BLS) in gel, compared to conventional oral TBN solution and transdermal gel loaded with free TBN, aiming at evading the hepatic first-pass metabolism. A face-centered central composite design was adopted to observe the effects of different formulation variables on TBN-BLS, and artificial neural network (ANN) modeling was employed to optimize TBN-BLS. TBN-BLS were prepared by a thin film hydration method integrating soybean phosphatidylcholine and cholesterol as a lipid phase and sodium deoxycholate (SDC) as a surfactant with or without the coating of chitosan (CTS). After being subjected to physicochemical characterization, TBN-BLS were enrolled in a histopathological study and pharmacokinetic investigation in a rat model. The optimized TBN chitosan-coated bilosomes (TBN-CTS-BLS) were spherical vesicles (245.13 ± 10.23 nm) with adequate entrapment efficiency (65.25 ± 5.51%) and good permeation characteristics (340.11 ± 22.34 µg/cm2). The TBN-CTS-BLS gel formulation was well-tolerated with no inflammatory signs manifested upon histopathological evaluation. The pharmacokinetic study revealed that the optimized TBN-CTS-BLS formulation successively enhanced the bioavailability of TBN by about 2.33-fold and increased t1/2 to about 6.21 ± 0.24 h as compared to the oral solution. These findings support the prospect use of BLS as active and safe transdermal carrier for TBN in the treatment of asthma. Graphical Abstract.

Clinical study on the efficacy and safety of terbutaline sulfate for injection in the treatment of children with wheezing disease / 中国实用儿科杂志

OBJECTIVE: To investigate the efficacy and safety of nebulized inhalation of terbutaline sulfate for injection in the treatment of children with wheezing disease. METHODS: From December 2016 to April 2018,440 cases of lower respiratory tract infection with cough and wheezing were hospitalized for treatment in the Department of Respiratory Medicine of Children's Hospital of Soochow University,Chengdu Women's & Children's Central Hospital and Dalian Children's Hospital of Dalian Medical University. The children were selected and randomly divided into terbutaline sulfate for injection group(Group A),terbutaline sulphate solution for nebulization group(Group B)and control group(Group C). The efficacy and adverse reactions of the three groups were compared. RESULTS: The scores of wheezing symptoms in group A and group B decreased more significantly than those in group C(P<0.05). Group A and group B had a certain influence on heart rate,and the heart rate at 30 minutes and 60 minutes after nebulization was higher than that of group C. In addition to the effect on heart rate,no other adverse reactions were found in group A and group C;one patient in the group B developed arm tremor and disappeared after stopping the drug. CONCLUSION: Inhalation of terbutaline sulfate for injection in the treatment of children with wheezing disease can shorten the treatment time and effectively improve the clinical treatment effect. The clinical efficacy is comparable to that of terbutaline sulphate solution for nebulization,and it is safe and worthy of clinical application.

Effect of atomization inhalation of budesonide and terbutaline sulfate on serum levels of chemokine like factor-1 and cyclooxygenase 2 in children with bronchial asthma / 中国基层医药

Objective To investigate the effect of atomization inhalation of budesonide and terbutaline sulfate on serum levels of cyclcoxygenase 2 (COX-2) and chemokine like factor-1 (CKLF-1) in children with bronchial asthma.Methods A total of 78 children with bronchial asthma in Hangzhou Children's Hospital from April 2016 to August 2017 were selected and divided into the control group(n =39) and the study group(n =39).The control group was treated with routine treatment,and the study group was treated with budesonide and terbutaline sulfate on the basis of the control group.The treatment was continued for 7 d.After t treatment,the clinical effects,clinical symptoms improvement,hospitalization time,the serum levels of COX-2 and CKLF-1 before and after treatment,and the incidence of adverse reaction of two groups were observed.Results The total effective rate of the study group(94.87％) was higher than that of the control group (74.36％)(x2 =6.303,P ＜ 0.05).The improvement time of chest tightness,wheezing,cough and hospitalization time of the study group were shorter than those of the control group (t1 =13.054,t2 =7.365,t3 =4.944,t4 =8.342,all P ＜ 0.05).After treatment,the levels of serum COX-2 and CKLF-1 in the two groups were lower than those before treatment,which of the study group were lower than those in the control group(t1 =4.934,t2 =4.660,all P ＜0.05).There was statistically significant difference in the incidence rate of adverse reactions between the study group(12.82％) and the control group(7.69％) (x2 =0.139,P ＞ 0.05).Conclusion Atomization inhalation of budesonide and terbutaline sulfate in the treatment of children with bronchial asthma can effectively alleviate the clinical symptoms,reduce serum levels of COX-2 and CKLF-1,improve therapeutic effect,promote children's recovery and shorten the hospitalization time.Besides,the incidence rate of adverse reactions is low,and it is safe.

Clinical analysis of ipratropium bromide combined with terbutaline sulfate inhalation in the treatment of acute attack of asthma / 中国生化药物杂志

Objective To analyze the clinical efficacy of ipratropium bromide combined with terbutaline sulfate inhalation in the treatment of acute attack of asthma. Methods 100 patients with acute attack of asthma treated from March 2015 to October 2016 were selected and randomly divided into the control group and the experimental group, with 50 patients in each group. The control group received terbutaline sulfate inhalation, and the experimental group received ipratropium bromide combined with terbutaline sulfate inhalation treatment. The patients in the experimental group and the control group were treated for 7 days continuously. The therapeutic effects of the two groups were compared and analyzed. Results After the corresponding treatment, the effective rate of treatment in the experimental group (94.0%) was significantly higher than that in the control group (72.0%),the difference was statistically significant(P<0.05). The improvement time of dyspnea, rale and cough in control group was significantly longer than that in the experimental group, the difference was statistically significant(P<0.05). Conclusion Ipratropium bromide combined with terbutaline sulfate inhalation in the treatment of acute attack of asthma has better clinical efficacy and shorter clinical symptoms.

Effect of B-ultrasound combined with intravenous terbutaline sulfate for external cephalic version / 实用医学杂志

Objective To investigate the effect of ultrasound combined with intravenous terbutaline sulfate for external cephalic version and the impact of this therapy on maternal and neonatal complications.Methods 126 singleton pregnant women who were diagnosed by B-ultrasound breech pregnancy at 34-36 weeks in regular antenatal examination from January 2014 to June 2016 were randomly divided into an observation group (n =70)and a control group (n =50).The observation group was treated with intravenous drip of terbutaline sulfate after epidural anesthesia,and then received external cephalic version under B-ultrasound monitoring.The control group received traditional knee-chest position for correcting breech presentation.The success rate of breech correction,breech version rate,cesarean section rate,vaginal delivery rate,adverse reactions,postpartum hemorrhage volume,neonatal asphyxia,and neonatal birth injury were noted and compared between the two groups.Results As compared with the control group,the observation group had a higher success rate of breech correction and a higher rate of vaginal delivery while a lower rate of cesarean section,with a significant difference (x2 =20.210,8.564;P ＜0.05).The rate of postpartum hemorrhage,neonatal asphyxia,or neonatal birth injury did not differ significantly between the two groups (P ＞ 0.05).Conclusions Application of ultrasound combined with intravenous terbutaline sulfate in external cephalic version is easy to operate and has a higher success rate and greater safety,significantly reducing the rate of cesarean section and improve the success rate of vaginal delivery.

Clinical analysis of ipratropium bromide combined with terbutaline sulfate inhalation in the treatment of acute attack of asthma / 中国生化药物杂志

Objective To analyze the clinical efficacy of ipratropium bromide combined with terbutaline sulfate inhalation in the treatment of acute attack of asthma. Methods 100 patients with acute attack of asthma treated from March 2015 to October 2016 were selected and randomly divided into the control group and the experimental group, with 50 patients in each group. The control group received terbutaline sulfate inhalation, and the experimental group received ipratropium bromide combined with terbutaline sulfate inhalation treatment. The patients in the experimental group and the control group were treated for 7 days continuously. The therapeutic effects of the two groups were compared and analyzed. Results After the corresponding treatment, the effective rate of treatment in the experimental group (94.0%) was significantly higher than that in the control group (72.0%),the difference was statistically significant(P<0.05). The improvement time of dyspnea, rale and cough in control group was significantly longer than that in the experimental group, the difference was statistically significant(P<0.05). Conclusion Ipratropium bromide combined with terbutaline sulfate inhalation in the treatment of acute attack of asthma has better clinical efficacy and shorter clinical symptoms.

HPLC determination of terbutaline sulfate impurity I / 中国药学杂志

OBJECTIVE: To establish a qualitative and quantitative HPLC method for the determination of impurity Iin tebutaline sulfate. METHODS: The Kromasil C18 column(4.6 mm×150 mm,5 μm) was used as the analysis column;buffer solution [dissolving 4.23 g of sodium hexanesulfonate in 770 mL of 0.050 mol·L-1 ammonium formate solution (pH 3)]-methanol (77:23) was used as the mobile phase. The flow rate was 1.0 mL·min-1, the column temperature was maitained at 30℃, the detection wavelength was set at 276 nm,and the injectiong volume was 20 μL. Area normalization method with correction factor was used for the quantitative analysis of the impurity I. RESULTS: Under the separation condition, the impurity I was completely separated from the principal components. The calibration curve showed good linearity in the concentration range of 0.10-579 μg·mL-1(r=1.000 0). The correction factor was 3.6. CONCLUSION: The area normalization method with correction factor developed in the paper can be used for the qualitative and quantitative analysis of the impurity Iin terbutaline sulfate, which can not only solve the problem of the availability of impurity reference standards, but also reflect the actual contents of impurity. The method provides an efficient and convenient method for quality control of terbutaline sulfate.

Therapeutic Effects of Magnesium Sulfate Combined with Budesonide and Terbutaline Sulfate Inhalation for the Treatment of Bronchiolitis / 昆明医科大学学报

Objective To observe the clinical efficacy of magnesium sulfate inhalation combined with budesonide and terbutaline sulfate nebulizer for the treatment of bronchiolitis.Methods Sixty children with bronchiolitis were randomly divided into observation group and control group with 30 cases in each group.Children in the control group received routine treatment and the observation group were inhaled with magnesium sulfate combining budesonide and terbutaline sulfate.Curative effects were evaluated in the aspects of the clinical symptoms,serum inflammatory factors and overall clinical efficacy.Results The symptoms in children including asthma,shortness of breath,coughing,wheezing and lung auscultation were significantly alleviated within a shorter period of time than that in the control group (P＜0.05).The serum levels of TNF-u,IL-6,IL-8 and TIgE were significantly reduced in both groups after the treatment (P＜0.05).But in the observation group,the alleviation of the symptoms was significantly greater than that in the control group (P＜0.05).The overall effective rate in the observation group and the control group was 93.3％ and 70.0％ respectively (P＜0.001).Conclusion The clinical efficacy of inhaling magnesium sulfate with budesonide and terbutaline sulfate to treat bronchiolitis is satisfactory and worth clinical application.

Binding studies of terbutaline sulfate to calf thymus DNA using multispectroscopic and molecular docking techniques.

The interaction of terbutaline sulfate (TS) with calf thymus DNA (ctDNA) were investigated by fluorescence quenching, UV-vis absorption, viscosity measurements, ionic strength effect, DNA melting experiments and molecular docking. The binding constants (Ka) of TS to ctDNA were determined as 4.92×10(4), 1.26×10(4) and 1.16×10(4) L mol(-1) at 17, 27 and 37 °C, respectively. Stern-Volmer plots suggested that the quenching of fluorescence of TS by ctDNA was a static quenching. The absorption spectra of TS with ctDNA revealed a slight blue shift and hyperchromic effect. The relative viscosity ctDNA was hardly changed by TS, and melting temperature varied slightly. For the system of TS-ctDNA, the intensity of fluorescence decreased with the increase of ionic strength. Also, the Ka for TS-double stranded DNA (dsDNA) was clearly weaker than that for TS-single stranded DNA (ssDNA). All these results revealed that the binding mode of TS with ctDNA should be groove binding. The enthalpy change and entropy change suggested that van der Waals force or hydrogen bonds was a main binding force between TS and ctDNA. Furthermore, the quantum yield of TS was measured by comparing with the standard solution. Based on the Förster energy transference theory (FRET), the binding distance between the acceptor and donor was calculated. Molecular docking showed that TS was a minor groove binder of ctDNA and preferentially bound to A-T rich regions.

Effects of terbutaline sulfate on pulmonary fluid transport in preterm rats / 临床儿科杂志

Objectives To investigate the effect and mechanism of terbutaline sulfate on pulmonary fluid transport in pre-mature rats. Methods Pregnant rats were randomly divided into 5 groups (control group, premature group, low-dose terbutaline group, high-dose terbutaline group and dexamethasone group). Drugs were administered by gavage after rats were fertilized for 16 days and continued for 3 days. Premature rats were taken out from the 19 days pregnant rats, and mature rats were delivered on the due day. Lungs were collected, and the ratio of pulmonary wet weight to dry weight (W/D), Na+, K+-ATP ase activity and concentration of cyclic adenosine monophosphate (cAMP) were measured in lungs. Results The W/D rate, Na+,K+-ATPase acti-vity and cAMP concentration in lungs had significant difference among different groups (P<0.01). The W/D rate was highest in premature group and lowest in the control group. It was lower in the high-dose terbutaline group than in the low-dose terbutaline group and the dexamethasone group (P<0.05). The Na+,K+-ATPase activity was lowest in premature group and highest in high-dose terbutaline group. It was higher in dexamethasone group, low-dose terbutaline group, and high-dose terbutaline group than in premature group, and it was higher in high-dsoe terbutaline group than in low-dose terbutaline group and dexamethasone group (P<0.05). The cAMP levle was lowest in premature group and highest in high-dose terbutaline group. It was higher in dexamethasone group, low-dose terbutaline group, high-dose terbutaline group than in premature group, and it was higher in high-dose terbutaline group than in low-dose terbutaline group and dexamethasone group (P<0.05). Conclusions Terbutaline sulfate facilitates lung fluid transport in premature rats, leading to reduce the W/D rate in terbutaline-treated group. We speculate that this effect is related to the increased cAMP level and Na+, K+-ATPase activity in lung tissue.

Preparation and characterization of a sustained release buccoadhesive system for delivery of terbutaline sulfate.

Terbutaline sulfate exhibits extensive first pass metabolism and a short elimination half life which makes frequent oral administration of the drug inevitable. A novel buccoadhesive controlled delivery system of the drug can easily overcome the problem. A two-layered core tablet composed of a fast release layer made of mannitol, lactose, PEG and the drug attached to a sustained release layer composed of drug, varying ratios of HPMC, Carbomer 934 (CP), and lactose capped with a buccoadhesive cup coated with an impermeable backing layer was developed. Buccoadhesive cup initially optimized for bioadhesion strength using HPMC and CP with various ratios. Drug transport through buccal membrane indicated a high permeability coefficient (0.00105 cm/sec). All tablets were acceptable with regard to drug contents, thickness, weight variations, hardness and drug content uniformity. The CP:HPMC 2:1 mixture showed the best mucoadhesion properties and was selected as excipient for the cup layer. Swelling index was higher for formulations containing greater amount of lactose and lower percentage of polymers. Fast release layer released its entire content within 15 min while sustained release layer lasted for 12 h. Drug release controlled by a combination of diffusion and chain relaxation mechanism.

Stability-Indicating RP-HPLC Method for the Simultaneous Estimation of Doxofylline and Terbutalinesulphate in Pharmaceutical Formulations.

An isocratic, stability-indicating, reversed-phase high-performance liquid chromatography (RP-HPLC) method was developed for the quantitative determination of doxofylline and terbutaline sulphate, used for the treatment of respiratory problems. The chromatographic separation was achieved on a Zorbax-SB Phenyl 250 × 4.6mm × 5 µm column with the mobile phase consisting of a mixture of 25 mM ammonium acetate (pH 5.0) : acetonitrile (85:15 %v/v) at a flow rate of 1.0 ml/min. The eluate was monitored at 274 nm using a PDA detector. Forced degradation studies were performed on the bulk sample of doxofylline and terbutaline sulphate using acid (0.1N HCl), base (0.1N NaOH), oxidation (10% hydrogen peroxide), photolytic, and thermal degradation conditions. Good resolution was observed between the degradants and analytes. Degradation products resulting from the stress studies did not interfere with the detection of doxofylline and terbutaline sulphate, thus the assay is stability-indicating. The method has the requisite accuracy, selectivity, sensitivity, and precision for the simultaneous estimation of doxofylline and terbutaline sulphate in bulk and pharmaceutical dosage forms. The limit of quantitation and limit of detection were found to be 1.16 µg/ml and 0.38 µg/ml for doxofylline, 2.08 µg/ml and 0.62 µg/ml for terbutaline sulphate, respectively.

Stability-indicating HPLC Method for Simultaneous Determination of Terbutaline Sulphate, Bromhexine Hydrochloride and Guaifenesin.

The aim of the present study was the development and subsequent validation of a simple, precise and stability-indicating reversed phase HPLC method for the simultaneous determination of guaifenesin, terbutaline sulphate and bromhexine hydrochloride in the presence of their potential impurities in a single run. The photolytic as well as hydrolytic impurities were detected as 3,5-dihydroxybenzoic acid, 3,5-dihydroxybenzaldehyde, 1-(3,5-dihydroxyphenyl)-2-[(1,1-dimethylethyl) amino]-ethanone from terbutaline, 2-methoxyphenol and an unknown impurity identified as (2RS)-3-(2-hydroxyphenoxy)-propane-1,2-diol from guaifenesin. The chromatographic separation of all the three active components and their impurities was achieved on Wakosil II column, using phosphate buffer (pH 3.0) and acetonitrile as mobile phase which was delivered initially in the ratio of 80:20 (v/v) for 18 min, then changed to 60:40 (v/v) for next 12 min, and finally equilibrated back to 80:20 (v/v) for 10 min. Other HPLC parameters were: Flow rate at 1.0 ml/min, detection wavelengths 248 and 280 nm, injection volume 10 µl. The calibration graphs plotted with five concentrations of each component were linear with a regression coefficient R(2) >0.9999. The limit of detection and limit of quantitation were estimated for all the five impurities. The established method was then validated for linearity, precision, accuracy, and specificity and demonstrated to be applicable to the determination of the active ingredients in commercial and model cough syrup. No interference from the formulation excipients was observed. These results suggest that this LC method can be used for the determination of multiple active ingredients and their impurities in a cough and cold syrup.

A validated HPTLC method for determination of terbutaline sulfate in biological samples: Application to pharmacokinetic study.

Terbutaline sulfate (TBS) was assayed in biological samples by validated HPTLC method. Densitometric analysis of TBS was carried out at 366 nm on precoated TLC aluminum plates with silica gel 60F254 as a stationary phase and chloroform-methanol (9.0:1.0, v/v) as a mobile phase. TBS was well resolved at RF 0.34 ± 0.02. In all matrices, the calibration curve appeared linear (r (2) â©¾ 0.9943) in the tested range of 100-1000 ng spot(-1) with a limit of quantification of 18.35 ng spot(-1). Drug recovery from biological fluids averaged ⩾95.92%. In both matrices, rapid degradation of drug favored and the T 0.5 of drug ranged from 9.92 to 12.41 h at 4 °C and from 6.31 to 9.13 h at 20 °C. Frozen at -20 °C, this drug was stable for at least 2 months (without losses >10%). The maximum plasma concentration (Cpmax) was found to be 5875.03 ± 114 ng mL(-1), which is significantly higher than the maximum saliva concentration (Csmax, 1501.69 ± 96 ng mL(-1)). Therefore, the validated method could be used to carry out pharmacokinetic studies of the TBS from novel drug delivery systems.

Determination of Terbutaline Sulfate and Its Combination with β_2 Adrenergic Receptor in Erythrocyte Membrane by High Performance Liquid Chromatography / 分析化学

A high performance liquid chromatographic method with hypersil C_(18) column, 0.020 mol/L potassium dihydrogen phosphate solution(which contains 0.25% triethylamine, pH 5.1)-methanol(20∶ 80, V/V) as mobile phase and fluorescence detection with 280 nm as excitation wavelength and 320 nm as emission wavelength has been developed for the determination of terbutaline sulfate and propranolol hydrochloride in Erythrocyte suspensions. Erythrocyte surface receptor oscillating reacted 1 h with terbutaline in 37 ℃ water bath. Free terbutaline and propranolol were separated from the membrane receptor-binding complex through 1500 r/min centrifugal in 5 min. The linear range was 0.010-3.000 mg/L in Alsever's solutions and the correlation coefficients were 0.9999 and 0.9998. The relative standard deviations(RSDs) of terbutaline and propranolol were 0.8% and 1.2%, respectively. The limits of detection(LODs) of both were 1.00 and 3.00 mg/L. This simple, safety and sensitive method was suitable for the determination of terbutaline and propranolol in erythrocyte suspensions and for the study of receptor-ligand binding.

Determination of Terbutaline Sulfate Based on the Enhancement Chemiluminescence of Ag Nanoparticles in Luminol-Potassium Ferricyanide Chemiluminescence System / 分析化学

It was found that Ag nanoparticles (NPs) could enhance the chemiluminescence (CL) intensity of luminol- potassium ferricyanide system. On the basis of enhancement effect,a flow injection method was developed for the determination of terbutaline sulfate. The structure and shape of Ag NPs were characterized by transmission electron microscopy. The UV-Vis absorption spectra and chemiluminescence spectra suggested that new luminophor was not formed after Ag NPs introducing in luminol-potassium ferricyanide chemiluminescence system. A possible mechanism of Ag NPs strengthening on luminol-potassium ferricyanide CL reaction was also discussed. The effect of concentration of luminol,potassium ferricyanide,sodium hydroxide and Ag NPs on CL reaction was investigated respectively. In the optimum conditions,the linear range was 1.0×10~(-9) -2.0 ×10~(-5) g/L(r =0.9935) and the detection limit was 1×10~(-10) g/L. The relative standard deviation (RSD) was 3.6% for 1. 0 ×10~(-6) g/L terbutaline sulfate (n = 11 ). The recommended method has been successfully applied to the determination of terbutaline sulfate tablets and the recovery was between 98. 5% - 102. 5% ,moreover the results were almost identical with the same results of Pharmacopoeia method.

Effect of Inhalation of Salmeterol Xinafoate and Fluticasone Propionate Powder in Acute Onset of Children with Asthma / 实用儿科临床杂志

Objective To observe influence of salmeterol xinafoate and fluticasone propionate powder applied in asthmatic exacerbated period on relieving efficacy of a fast-acting beta2-agonist.Methods Eighty-nine children with asthma in exacerbated period were randomly assigned into two groups.Thirty-nine cases in treatment group inhaled salmeterol xinafoate and fluticasone propionate powder, compared with 50 cases in control group treated with budesonide aerosol. Two groups were all given Bricanyl aerolised inhalation in same way at meanwhile.Results The improvement of peak expinatory flow in two groups was evident. The disappearing time of main symptoms and signs, the duration of staying in hospital of two groups were no difference (all P