AIMTo develop a near-infrared diffuse reflectance analysis (NIRDRA) method for rapid noninvasive quantitative determination of ambroxol hydrochloride in half-finished product particles and non-blister-packed, blistered tablets.

METHODSAll spectra were measured with a Fourier transform spectrometer equipped with a PbS and a InGaAs detector, an external integrating sphere, a rotating sample cup, and a fibre-optic probe for reflectance measurements. All samples were scanned from 12,000 cm-1 to 4,000 cm-1, and each sample spectrum was obtained as an automatic mean of 64 scans. No spectrum pre-processing method was used, and spectral regions, 4,602-4,247, 12,000-7,498 and 6,102-5,446, 12,000-5,446 cm-1 were selected to develope mathematical models by partial least square method for half-finished product particles and non-blister-packed, blistered tablets samples, respectively.

RESULTSThe optimal rank and mean square error determined for half-finished product particles and non-blister-packed, blistered tablets samples by cross validation method all was 6 and 0.306, 0.972 and 1.492, respectively, the average recovery was 100%, 100% and 102% respectively; and the RSD was 1.17%, 1.70% and 1.78% respectively.

CONCLUSIONResults showed that the NIRDRA method was rapid, simple, noninvasive and sensitive, and it can be applied to assay the content of ambroxol hydrochloride in half-finished product particles non-blister-packed and blistered tablets.

Ambroxol ; administration & dosage ; analysis ; Expectorants ; administration & dosage ; analysis ; Quality Control ; Spectroscopy, Near-Infrared ; methods ; Tablets

BACKGROUND: Fudosteine, (-)-(R)-2-amino-3-(3-hydroxypropylthio)propionic acid, is a cysteine derivative that was approved in Japan, as a new mucoactive agent. The aim of this study was to evaluate the tolerability and pharmacokinetics (PK) of fudosteine in healthy Korean subjects. METHODS: A randomized, open-label, parallel, escalating single-dose study was conducted in 16 healthy Korean male subjects. The subjects were allocated to single-dose groups of 400 or 800 mg. Serial blood samples for PK analysis were collected immediately prior and after dosing up to 24 hours, and plasma concentrations were determined by high performance liquid chromatography (HPLC). Safety profiles were evaluated by monitoring adverse events and clinical evaluations throughout the study. RESULTS: Median time to peak concentration (Tmax) of both dosing group were around 0.5 hours and half-life (t1/2) were around 3 hours. Mean peak concentration (Cmax) of 400 mg and 800 mg dosing group were 10.8 and 21.5 microg/mL and the mean area under the plasma concentration versus time curve from the dosing time to infinity (AUCinf) were 26.8 and 55.0 microg.h/mL, respectively. Mean dose-normalized Cmax were 0.0271 and 0.0269 microg/mL/mg (P=0.923), respectively and dose-normalized AUCinf were 0.0669 and 0.0688 microg.hr/mL/mg (P=0.093), respectively. Fudosteine was well tolerated without any serious adverse events or clinical laboratory abnormalities. CONCLUSION: This study showed that fudosteine has a linear PK property and is well tolerated within 800 mg in healthy Korean volunteers.
Administration, Oral ; Chromatography, Liquid ; Cysteine ; Cystine ; Expectorants ; Half-Life ; Humans ; Japan ; Male ; Plasma

This article is brief review of study on alpha-asarone after 1996. The summary mainly includes the dosage forms, pharmacokinetics, bioavailability, pharmacological effects, toxicology and clinical uses during the past ten years.
Acorus ; chemistry ; Animals ; Anisoles ; administration & dosage ; isolation & purification ; pharmacology ; Anticonvulsants ; pharmacology ; Antineoplastic Agents, Phytogenic ; pharmacology ; Expectorants ; pharmacology ; Humans ; Phytotherapy ; Plants, Medicinal ; chemistry

Adult ; Ambroxol ; administration & dosage ; therapeutic use ; Expectorants ; administration & dosage ; therapeutic use ; Female ; Glycoproteins ; therapeutic use ; Humans ; Lung ; pathology ; Lung Injury ; drug therapy ; pathology ; Male ; Paraquat ; poisoning ; Respiratory Distress Syndrome, Adult ; drug therapy ; etiology ; Retrospective Studies ; Young Adult

OBJECTIVETo observe the effect of three Chinese medical formulae (Zhifei Mixture I , Zhfei Mixture II, and Zhifei Mixture II) on main and secondary symptoms and signs of children with Totally 70 mycoplasma pneumonia in treating three types of children mycoplasma pneumonia.

METHODSchildren with mycoplasma pneumonia were assigned to the control group (38 cases) and the treatment group (32 case). All patients were intravenously injected with Azithromycin and took Ambroxol Hydrochloride and Clenbuterol Hydrochloride Oral Solution. Those in the treatment group additionally took Zhifei Mixture I , Zhfei Mixture II, and Zhifei Mixture Ill by syndrome typing. Their main and secondary symptoms and signs were observed before and after treatment (main symptoms and signs covered fever, cough, abundant sputum, short breath, and anoxia; secondary symptoms and signs covered aversion to cold, heart rate, facial complexion, spirit, appetite, and sweating).

RESULTSSeven patients were lost in this study. Compared with before treatment in the same group, scores for main and secondary symptoms and signs decreased in the treatment group (P <0.01). The therapeutic effect on fever and cough was obviously better in the control group (P <0.01). The main and secondary symptoms and signs were more obviously improved in the treatment group than in the control group (P <0.01). Commpared with the control group, scores for main and secondary symptoms and signs decreased more in the treatment group (P <0.01). Patients' main and secondary symptoms and signs were more obviously improved (P <0.05).

CONCLUSIONSZhifei Mixture combined Western drugs could significantly improve main and secondary symptoms and signs of mycoplasma pneumonia children patients. Its efficacy was superior to that of using Western medicine alone.

Ambroxol ; administration & dosage ; therapeutic use ; Anti-Bacterial Agents ; administration & dosage ; therapeutic use ; Azithromycin ; administration & dosage ; therapeutic use ; Bronchodilator Agents ; administration & dosage ; therapeutic use ; Child ; Clenbuterol ; administration & dosage ; therapeutic use ; Drugs, Chinese Herbal ; therapeutic use ; Expectorants ; administration & dosage ; therapeutic use ; Fever ; Humans ; Pneumonia, Mycoplasma ; drug therapy ; Syndrome

Ambroxol and clenbuterol were extracted from human plasma samples by liquid-liquid extraction, ambroxol was separated on a Zorbax XDB-C18 column and detected by tandem mass spectrometry with an atmospheric pressure chemical ionization interface after oral administration of a compound preparation. Clenbuterol was separated on a Zorbax XDB-C8 column and detected by tandem mass spectrometry with an electrospray ionization interface. Diphenhydramine is used as the internal standard. The linear concentration ranges of the calibration curves for ambroxol and clenbuterol were 0.080 - 400 microg x L(-1) and 5.0 - 5 000 ng x L(-1), respectively. The lower limits of quantification were 0.080 microg x L(-1) for ambroxol and 5.0 ng x L(-1) for clenbuterol, individually. The inter-day and intra-day precision (RSD) across three validation run over the entire concentration range was below 7.5%, and the accuracy (RE) was within +/- 2.5% for both ambroxol and clenbuterol. The methods were used to determine the pharmacokinetic parameters of ambroxol and clenbuterol in human plasma after oral administration of a compound preparation containing 60 mg ambroxol hydrochloride and 40 microg clenbuterol hydrochloride. The method was proved to be highly sensitive, selective and suitable for the pharmacokinetic study of different compound preparations containing ambroxol and clenbuterol.
Administration, Oral ; Adrenergic beta-Agonists ; administration & dosage ; blood ; pharmacokinetics ; Adult ; Ambroxol ; administration & dosage ; blood ; pharmacokinetics ; Area Under Curve ; Chromatography, Liquid ; methods ; Clenbuterol ; administration & dosage ; blood ; pharmacokinetics ; Diphenhydramine ; standards ; Expectorants ; administration & dosage ; analysis ; pharmacokinetics ; Humans ; Male ; Reference Standards ; Reproducibility of Results ; Tandem Mass Spectrometry ; methods

PURPOSE: This study aims to investigate the additive effect of the Hedera helix (HH) and Rhizoma coptidis (RC) extracts mixture on antitussive and expectorant activities in animals. MATERIALS AND METHODS: The expectorant assay was performed with phenol red secretion in mice trachea. Mice or guinea pigs were randomly divided into groups of 8 each, including negative and positive control groups. After gastric administration of the test extracts in mice, 2.5% phenol red solution (0.2 mL) was intraperitoneally injected. Trachea was dissected and optical density of tracheal secretion was measured. After gastric administration of the test extracts in guinea pigs, the antitussive activities were assessed using a citric acid-induced cough measurement. RESULTS: The extracts of HH and RC significantly increased tracheal secretion and inhibited cough. The mixture of HH and RC extracts in a 1:1 concentration at a dose of 200 mg/kg showed a more potent effect on phenol red secretion (25.25+/-3.14) and cough inhibition (61.25+/-5.36) than the individual use of each extracts [phenol red secretion; HH 13.39+/-4.22 (p=0.000), RC 20.78+/-2.50 (p=0.010), cough inhibition; HH 9.89+/-4.14 (p=0.010), RC 30.25+/-7.69 (p=0.000)]. A 3:1 ratio mixture of HH to RC demonstrated an optimal expectorant effect (p<0.001), and this mixture showed expectorant and antitussive effects in a dose-dependent manner. CONCLUSION: This study provides evidence for antitussive and expectorant effect of a 3:1 mixture of HH and RC, which may be a useful therapeutic option for respiratory diseases.
Animals ; Antitussive Agents/*administration & dosage/pharmacology/therapeutic use ; *Behavior, Addictive ; Cough/*drug therapy ; Drugs, Chinese Herbal/*administration & dosage/pharmacology/therapeutic use ; Ethanol ; Expectorants/*administration & dosage/pharmacology/therapeutic use ; Guinea Pigs ; Hedera/*chemistry/metabolism ; Male ; Mice ; Phytotherapy ; Plant Extracts/*pharmacology ; Plant Roots/chemistry ; Trachea/drug effects/metabolism

OBJECTIVETo observe the antitussive, expectorant and antiashmatic effects of the extract from Citrus grandist var. tomentosa.

METHODThe cough models induced by ammonia liquor in mice and citric acid in guines pigs were used to observe the antitussive effects. The methods of phenel red execretion in mice and phlegm displacement of rats were used to investigate the expectorant effects. Bronchial asthma model induced by histamine-acetylcholine in guinea pigs was used to observe the antiasthmatic effects.

RESULTThe extract from the title plant could inhibit the cough induced by ammonia in mice, decrease the frequency of cough induced by citric acid in guineas pig and prolong the latent period of cough. The extract also could obviously increase phenol red output of trachea in mice, promote expectoration in rats and prolong the latent period of asthma induced by histamine-acetylcholine in guinea pigs.

CONCLUSIONThe extract from C. grandis var. tomenfosa has significant antitussive, expectorant and antiasthmatic effects.

Acetylcholine ; Ammonia ; Animals ; Anti-Asthmatic Agents ; administration & dosage ; isolation & purification ; therapeutic use ; Antitussive Agents ; administration & dosage ; isolation & purification ; therapeutic use ; Asthma ; chemically induced ; drug therapy ; Citric Acid ; Citrus ; chemistry ; Cough ; chemically induced ; drug therapy ; Dose-Response Relationship, Drug ; Drugs, Chinese Herbal ; administration & dosage ; isolation & purification ; therapeutic use ; Expectorants ; administration & dosage ; isolation & purification ; therapeutic use ; Female ; Fruit ; chemistry ; Guinea Pigs ; Histamine ; Male ; Mice ; Phytotherapy ; Plants, Medicinal ; chemistry ; Rats ; Rats, Sprague-Dawley