2.Determination of liposome/water partition coefficients of salmeterol and budesonide and study on their influencing factors.
Zhi-xuan WANG ; Ying-jie DENG ; Xiao-peng ZHANG
Acta Pharmaceutica Sinica 2006;41(4):318-322
AIMThe liposome/water partition coefficients of salmeterol and budesonide between aqueous phase and liposomes were determined and the factors that influence their partition coefficients were studied, the mechanism of interaction between the two drugs and phospholipid bilayer was elucidated.
METHODSThe liposome/water partition coefficients of the two drugs were determined by equilibrium dialysis technique. The change of the partition coefficients of the two drugs along with liposome composition and medium was also studied.
RESULTSThe partition coefficients of the two drugs decreased with the increase of cholesterol content and saturation of phospholipid used. The liposome/water partition coefficient of salmeterol increased with the increase of liposome surface negative charge, medium pH and ionic strength, while the liposome surface charge, medium pH and ionic strength had no distinct effect on the liposome/water partition coefficient of budesonide.
CONCLUSIONThe liposome/water partition coefficient of drug was affected by the type, saturation of phospholipid used in liposome preparation, the cholesterol content and surface charge of liposome, as well as the pH and ionic strength of medium also have effect on the liposome/water partition coefficient of drug. Accordingly, in order to reflect the actual partition of drug in biological membrane, the determination condition including liposome composition and medium should be similar to the biological membrane.
Albuterol ; analogs & derivatives ; chemistry ; Budesonide ; chemistry ; Cholesterol ; chemistry ; Drug Carriers ; Hydrogen-Ion Concentration ; Ions ; Liposomes ; Membranes, Artificial ; Phospholipids ; classification ; Salmeterol Xinafoate ; Water ; analysis
3.Effect of salmeterol on function of bronchi in pneumoconiosis of coal miners.
Jiu-gui HU ; Wei JIA ; Xian-wei HU ; Yong WANG
Chinese Journal of Industrial Hygiene and Occupational Diseases 2003;21(3):233-234
Adrenergic beta-Agonists
;
therapeutic use
;
Aged
;
Albuterol
;
analogs & derivatives
;
therapeutic use
;
Bronchi
;
drug effects
;
physiopathology
;
Bronchodilator Agents
;
therapeutic use
;
Coal Mining
;
Humans
;
Male
;
Middle Aged
;
Pneumoconiosis
;
drug therapy
;
physiopathology
;
Respiratory Function Tests
;
Salmeterol Xinafoate
;
Treatment Outcome
4.Efficacy and safety of tulobuterol patch versus oral salbutamol sulfate in children with mild or moderate acute attack of bronchial asthma: a comparative study.
Qian LIN ; Quan-Hua LIU ; Yi-Xiao BAO
Chinese Journal of Contemporary Pediatrics 2013;15(6):462-465
OBJECTIVETo compare tulobuterol patch and oral salbutamol sulfate in terms of efficacy and safety in children with mild or moderate acute attack of bronchial asthma.
METHODSA total of 92 children with mild and moderate acute asthmatic attack were randomly divided into salbutamol group (n=46) and tulobuterol group (n=46). Both groups received routine treatment with antihistamine, selective leukotriene receptor antagonist and glucocorticoid. In addition, the salbutamol group was given slow-release capsules of salbutamol sulfate, and the tulobuterol group was treated with tulobuterol patch. The two groups were compared with respect to symptom scores of cough, wheeze, respiratory rate, wheezing sound, three depression sign and peak expiratory flow, as well as adverse events.
RESULTSAs the treatment proceeded, symptom scores decreased in both groups; on the third day of treatment, all symptom scores except cough score showed a significant decrease in both groups (P<0.05), but the tulobuterol group had significantly lower symptom scores than the salbutamol group (P<0.05). On the fourteenth day of treatment, both groups had a significant decrease in cough score (P<0.05), but the tulobuterol group had a significantly lower cough score than the salbutamol group (P<0.05). One child developed hand trembling in the salbutamol group, while no adverse event occurred in the tulobuterol group.
CONCLUSIONSCompared with oral salbutamol sulfate, tulobuterol patch has a better therapeutic efficacy and a higher safety in children with mild or moderate acute asthmatic attack.
Acute Disease ; Administration, Oral ; Adrenergic beta-2 Receptor Agonists ; therapeutic use ; Albuterol ; administration & dosage ; adverse effects ; therapeutic use ; Asthma ; drug therapy ; Female ; Humans ; Terbutaline ; administration & dosage ; adverse effects ; analogs & derivatives ; therapeutic use
5.Comparative study on effect of acupoint heat-sensitive moxibustion and Seretide on the symptoms of bronchial asthma at chronic persistent stage.
Nan-Chang SONG ; Jin-Bao HE ; Han-Bin XU ; Ji-Feng WU
Chinese Acupuncture & Moxibustion 2012;32(7):593-596
OBJECTIVETo observe the difference in the efficacy on the symptoms of bronchial asthma at the chronic persistent stage between acupoint heat-sensitive moxibustion and western medicine with Seretide.
METHODSSixty-four cases were randomly divided into a heat-sensitive moxibustion group (32 cases) and a western medication group (32 cases). In the heat-sensitive moxibustion group, the sensitized points located between Feishu (BL 13) and Geshu (BL 17) or in the region 6-cun lateral from the 1st and the 2nd intercostal spaces of the chest were selected. The heat-sensitive moxibustion was adopted, continuously for 8 days, once per day. In the later 22 days of the 1st month, 12 treatments should be ensured. Two months later, 15 treatments should be guaranteed each month. The time of each treatment was 30 to 90 min. Totally 50 treatments were required. In the western medication group, Seretide inhaler was adopted, one inhalation each time, twice per day, for 3 months totally. The asthmatic symptoms were scored for the patients in two groups and the comparison was made between the two groups.
RESULTSAfter 3 months of treatment, the asthmatic symptom scores were all improved for the patients in the heat-sensitive moxibustion group and the western medication group as compared with those before treatment (both P < 0.05). In 6 months of follow-up visit, the asthmatic symptom scores in the heat-sensitive moxibustion group were stable, but those in the western medication group were reduced, there was significant difference between the two groups (P < 0.05).
CONCLUSIONThe acupoint heat-sensitive moxibustion effectively relieves the clinical symptoms for the patients with bronchial asthma at the chronic persistent stage. Its efficacy is similar to that of Seretide inhaler. But the long-term efficacy of the heat-sensitive moxibustion is much better.
Acupuncture Points ; Adolescent ; Adult ; Albuterol ; analogs & derivatives ; therapeutic use ; Androstadienes ; therapeutic use ; Asthma ; therapy ; Chronic Disease ; Drug Combinations ; Female ; Fluticasone-Salmeterol Drug Combination ; Humans ; Male ; Medicine, Chinese Traditional ; Middle Aged ; Moxibustion ; methods
6.Interleukin-32, not reduced by salmeterol/fluticasone propionate in smokers with chronic obstructive pulmonary disease.
Yipeng DU ; Wei WANG ; Wei YANG ; Bei HE
Chinese Medical Journal 2014;127(9):1613-1618
BACKGROUNDThe interleukin (IL)-32/tumor necrosis factor (TNF) a pathway is supposed to play a key role in the amplification of the immune response in chronic obstructive pulmonary disease (COPD) inflammation. Inhaled corticosteroids (ICS) in combination with long-acting β2-agonists (LABA) have shown airway anti-inflammatory effects in recent studies, but the mechanism is still uncertain.
METHODSPatients were treated in a randomized, open-labeled, parallel group clinical trial with either a combination of salmeterol xinafoate/fluticasone propionate (SF; Seretide, GlaxoSmithKline) Diskus (50/500 µg twice daily) or ipratropium bromide/salbutamol (IS; Combivent, Boehringer Ingelheim) MDI (42 µg/240 µg quartic daily) for 12 weeks. At the start and the end of treatment, induced sputum was collected and the concentration of IL-32 and TNF-α, the number of neutrophils and eosinophils were measured.
RESULTSFollowing 12 weeks of treatment, a statistically significant fall from baseline in the concentration of TNF-α in sputum (P = 0.004) was seen after treatment with SF but not with IS. However, neither treatment had significant effects on the concentration of IL-32 in sputum. There was a decrease from baseline in the number of sputum neutrophils with SF that approached statistical significance (P = 0.028) but not with IS, while the number of sputum eosinophils did not change significantly from baseline in either treatment group. There was a statistically significant decline from baseline in the quality of life as assessed by the St George's respiratory questionnaire in both the SF (P = 0.004) and IS (P = 0.030) treatment groups, but no evidence of improvement in lung function was observed in either group.
CONCLUSIONThe sputum TNF-α and neutrophils, but not IL-32 and macrophages, could be reduced by ICS/LABA treatment, suggesting that IL-32 could be involved in the corticosteroid resistance of COPD inflammation.
Adult ; Aged ; Aged, 80 and over ; Albuterol ; analogs & derivatives ; therapeutic use ; Androstadienes ; therapeutic use ; Anti-Inflammatory Agents ; therapeutic use ; Drug Combinations ; Female ; Fluticasone-Salmeterol Drug Combination ; Humans ; Interleukins ; metabolism ; Male ; Middle Aged ; Pulmonary Disease, Chronic Obstructive ; drug therapy ; metabolism
7.Efficacy on chronic obstructive pulmonary disease at stable stage treated with cutting method and western medication.
Jian-hua XU ; Bin XU ; Yan-qing DENG
Chinese Acupuncture & Moxibustion 2014;34(10):951-955
OBJECTIVETo compare the difference in clinical efficacy on chronic obstructive pulmonary disease (COPD) at stable stage in the patients among the combined therapy of cutting method and western medication (combined therapy), simple cutting method and simple western medication.
METHODSOne hundred and twenty cases of COPD were randomized into three groups, 40 cases in each one. In the cutting method group, for excessive phlegm pattern/syndrome, Feishu (BL 13), Danzhong (CV 17), Dingchuan (EX-B 1) and Yuji (LU 10) were selected as the main acupoints, and Lieque (LU 7) and Pianli (LI 6) were as the supplementary acupoints. For the pattern/syndrome of failure to consolidate kidney primary, Shenshu (BL 23), Pishu (BL 20), Guanyuan (CV 4) and Yuji (LU 10) were selected as main acupoints, and Jueyinshu (BL 14) and Zusanli (ST 36) were as the supplementary acupoint. Three acupoints were selected alternatively in each treatment and the cutting method was applied once every 10 days. Three treatments made one session. Two sessions of treatment were required. In the western medication group, salbutamol sulfate aerosol, one press (200 μg/press) was used each night, as well as salmeterol xinafoate and fluticasone propionate powder for inhalation, one inhalation each night. The treatment of 1 month made one session. Two sessions were required. In the combined therapy group, the cutting method and western medication were applied in combination. The results of clinical symptom score, lung function test, arterial blood gas analysis, degree of inflation as well as clinical efficacy were observed before and after treatment in each group.
RESULTSExcept the degree of lung inflation, the clinical symptom score, indices of lung function test, partial pressure of arterial blood gas (PaO2) and partial pressure of carbon dioxide (PaCO2) were all obviously improved after treatment as compared with those before treatment in each group (all P<0.05). They were apparently improved after treatment in the combined therapy group and the cutting method group as compared with those in the western medication group (all P<0.05). The total effective rate was 77.5% (31/40) in the combined therapy group and was 75.0% (30/40) in the cutting method group, both better than 60.0% (24/40) in the western medication group (both P<0.05).
CONCLUSIONThe simple cutting method based on syndrome differentiation and the combined therapy with western medication achieve the superior efficacy on COPD at stable stage as compared with the simple western medication. The effect mechanism is possibly related to the improvement of bronchial airway function through constant acupoint stimulation.
Acupuncture Points ; Acupuncture Therapy ; Aged ; Albuterol ; administration & dosage ; analogs & derivatives ; Androstadienes ; administration & dosage ; Combined Modality Therapy ; Female ; Fluticasone ; Humans ; Lung ; physiopathology ; Male ; Middle Aged ; Pulmonary Disease, Chronic Obstructive ; drug therapy ; physiopathology ; therapy ; Salmeterol Xinafoate ; Treatment Outcome
8.Observation on the effects of the treatment of sillicosis merger asthma.
Xian-hui WU ; Cuang CAI ; Jian-pu XU ; Chu-hui RU ; Fei HE
Chinese Journal of Industrial Hygiene and Occupational Diseases 2013;31(5):386-388
OBJECTIVETo investigate Salmeterol/Fluticasone Propionate and Totropiumi treatment of Sillicosis merger Asthma.
METHODS30 patients with Sillicosis merger Asthma were randomly divided into group Salmeterol/Fluticasone Propionate( Single group) ( n=14) and group Salmeterol/Fluticasone Propionate and Totropiumi (Joint group) ( n= 16), patient in single group were only given Salmeterol/Fluticasone Propionate (50 f.Lg Bid) inhaling,and those in Joint group were given Salmeterol/Fluticasone Propionate (50 f.Lg Bid) and Totropiumi ( 18 f.Lg Qd) inhaling. The treatment was last for 6 months.Before the treatment,evaluation of the two groups of Sillicosis installment,determination their foungation lung function and ACT score .. After the cause of treatment, lung function FEV10/FVC(% ), FEV10 pred%, FEV10(ml), ACT score, the incidence of side effects of two groups were compared and analyzed.
RESULTThe two groups before the treatment of lung fuction and ACT score had no statistically significant difference. The two groups after treatment of lung fuction FEV10/FVC (% ),FEV10 pred%, ACT score obviously higher than before treatment (P<0.05), Joint group in FEV1/FVC(% ), ACT score significantly higher than in Single group (?<0.05), Joint group acute attack times(0.98±0.79)/time lower than Single group (2.10 ± 0.81 )/time (t=3.86,P<0.05). There were no significant side effect in two groups.
CONCLUSIONSalmeterol/Fluticasone Propionate or the combination of Salmeterol/Fluticasone Propionate and Totropiumi can improve lung function and clinical symptoms of patients with Sillicosis merger Asthma. It is also better that the combination of Salmeterol/Fluticasone Propionate and Totropiumi obviously improve clinical symptoms of patients and reduice acute attack times.
Administration, Inhalation ; Adult ; Albuterol ; analogs & derivatives ; therapeutic use ; Androstadienes ; therapeutic use ; Asthma ; complications ; drug therapy ; Drug Combinations ; Female ; Fluticasone-Salmeterol Drug Combination ; Humans ; Male ; Middle Aged ; Silicosis ; complications ; drug therapy ; Treatment Outcome
9.Comparative observation on therapeutic effect of chronic persistent bronchial asthma treated with heat-sensitive moxibustion and medication.
Chao LIANG ; Tang-Fa ZHANG ; Kun YANG
Chinese Acupuncture & Moxibustion 2010;30(11):886-890
OBJECTIVETo probe a better therapy for chronic persistent asthma.
METHODSThirty-six cases of chronic persistent asthma were randomly divided into a beat-sensitive moxibustion group (17 cases) and a western medication group (19 cases). In heat-sensitive moxibustion group, the sensitization points between Feishu (BL 13) and Geshu (BL 17) were selected with heat-sensitive moxibustion; in western medication group, Seretide inhalant was applied. The patients of both groups were continuously treated for 3 months and the therapeutic effects were evaluated by clinical symptom scores and pulmonary ventilation function test.
RESULTSAfter treatment, the effective rate of 88.2% (15/17) in heat-sensitive moxibustion group was superior to that of 47.4% (9/19) in western medication group (P < 0.05); the clinical symptom scores and pulmonary ventilation function were obviously improved in the two groups, and the heat-sensitive moxibustion group was superior to the western medication group (all P < 0.05).
CONCLUSIONFor chronic persistent bronchial asthma, heat-sensitive moxibustion can improve the clinical symptoms and the pulmonary ventilation function, and it is better than Seretide inhalant.
Adolescent ; Adult ; Aged ; Albuterol ; analogs & derivatives ; therapeutic use ; Androstadienes ; therapeutic use ; Asthma ; drug therapy ; physiopathology ; therapy ; Chronic Disease ; therapy ; Drug Combinations ; Female ; Fluticasone-Salmeterol Drug Combination ; Humans ; Lung ; physiopathology ; Male ; Middle Aged ; Moxibustion ; Pulmonary Ventilation ; Treatment Outcome ; Young Adult
10.Salmeterol/fluticasone treatment reduces circulating C-reactive protein level in patients with stable chronic obstructive pulmonary disease.
Yong-Jiang TANG ; Ke WANG ; Tao YUAN ; Ting QIU ; Jun XIAO ; Qun YI ; Yu-Lin FENG
Chinese Medical Journal 2010;123(13):1652-1657
BACKGROUNDEvidence suggests that systemic inflammation may play an important role in the progression and morbidity of chronic obstructive pulmonary disease. It remains controversial whether inhaled corticosteroid in combination with a long-acting beta(2)-adrenoceptor agonist can attenuate systemic inflammation. We evaluated the effect of salmeterol/fluticasone propionate on circulating C-reactive protein level in stable chronic obstructive pulmonary disease patients.
METHODSAn open-label clinical trial was conducted to recruit 122 outpatients with stable moderate-to-severe chronic obstructive pulmonary disease from department of respiratory medicine in two teaching hospitals between June 2007 and March 2008. Patients were randomized into two groups (1:1) to receive either the combination of 50 microg salmeterol and 500 microg fluticasone twice daily (n = 61), or the combination of 206 microg albuterol and 36 microg ipratropium q.i.d (n = 61) over 6 months. Circulating C-reactive protein concentrations were measured before randomization and during the follow-up. The efficacy of treatment was also assessed by spirometry, as well as health status and dyspnea score at baseline and after 6-month treatment.
RESULTSBaseline characteristics of two groups were similar. Compared with ipratropium/albuterol, the combination of salmeterol/fluticasone significantly reduced circulating level of C-reactive protein (-1.73 vs. 0.08 mg/L, respectively, P < 0.05) after 6-month treatment. Forced expiratory volume in one second (FEV(1)) and health status also improved significantly in salmeterol/fluticasone group compared with ipratropium/albuterol. Salmeterol/fluticasone treatment subjects who had a decrease of circulating C-reactive protein level had a significant improvement in FEV(1) and St George's Respiratory Questionnaire total scores compared with those who did not (185 vs. 83 ml and -5.71 vs. -1.79 units, respectively, both P < 0.01).
CONCLUSIONSalmeterol/fluticasone treatment reduced circulating C-reactive protein concentration in clinically stable moderate-to-severe chronic obstructive pulmonary disease patients after 6-month treatment.
Albuterol ; analogs & derivatives ; therapeutic use ; Androstadienes ; therapeutic use ; C-Reactive Protein ; metabolism ; Female ; Fluticasone ; Humans ; Male ; Middle Aged ; Pulmonary Disease, Chronic Obstructive ; drug therapy ; metabolism ; Salmeterol Xinafoate ; Treatment Outcome