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PubMed2004

Oral sustained delivery of ambroxol from in situ-gelling pectin formulations.

Gels formed in situ following oral administration of dilute aqueous solutions of pectin (1.0 and 1.5%, w/v) to rats were evaluated as vehicles for the sustained release of the expectorant drug ambroxol hydrochloride. The solutions contained calcium ions in complexed form, which on release in the acidic environment of the stomach caused gelation of the pectin. In vitro studies demonstrated diffusion-controlled release of ambroxol from the gels over a period of 6 h. A bioavailability of ambroxol of approximately 64% of that of a commercially available formulation could be achieved from gels containing an identical dose of ambroxol formed in situ in the stomachs of rats, with appreciably lower peak plasma levels and a sustained release of drug over a period of at least 6 h. The influence of added sorbitol (17%, w/v) on the rheological and drug release properties of the formulations has been examined.

Ambroxol↗
PubMed2005

Ambroxol, a Nav1.8-preferring Na(+) channel blocker, effectively suppresses pain symptoms in animal models of chronic, neuropathic and inflammatory pain.

Neuropathic pain affects many patients, and treatment today is far from being perfect. Nav1.8 Na(+) channels, which are expressed by small fibre sensory neurons, are promising targets for novel analgesics. Na(+) channel blockers used today, however, show only limited selectivity for this channel subtype, and can cause dose-limiting side effects. Recently, the secretolytic ambroxol was found to preferentially inhibit Nav1.8 channels. We used this compound as a tool to investigate whether a Nav1.8-preferring blocker can suppress symptoms of chronic, neuropathic and inflammatory pain in animal models. The drug was tested in the formalin paw model, two models of mononeuropathy, and a model of monoarthritis in rats. Ambroxol's effects were compared with those of gabapentin. Ambroxol at a dose of 1g/kg had to be administered to rats to achieve the plasma levels that are reached in clinical use (for the treatment of infant and acute respiratory distress syndrome). Ambroxol (1g/kg) was only weakly effective in models for acute pain, but effectively reduced pain symptoms in all other models; in some cases it completely reversed pain behaviour. In most cases the effects were more pronounced than those of gabapentin (at 100mg/kg). These data show that a Nav1.8-preferring Na(+) channel blocker can effectively suppress pain symptoms in a variety of models for chronic, neuropathic and inflammatory pain at plasma levels, which can be achieved in the clinic.

Ambroxol↗
PubMed2004

Bioequivalence assessment of ambroxol tablet after a single oral dose administration to healthy male volunteers.

A bioequivalence study of the ambroxol hydrochloride tablets was conducted. Twenty-four healthy male Korean volunteers received each medicine at the ambroxol hydrochloride dose of 30 mg in a 2 x 2 cross-over study. There was a 1-week washout period between the doses. Plasma concentrations of ambroxol were monitored by a high-performance liquid chromatography (HPLC) for over a period of 24h after the administration. AUC(t) (the area under the plasma concentration-time curve from time 0 to last sampling time, 24h) was calculated by the linear-log trapezoidal rule method. C(max) (maximum plasma drug concentration) and T(max) (time to reach C(max)) were compiled from the plasma concentration-time data. Analysis of variance was carried out using logarithmically transformed AUC(t) and C(max), and untransformed T(max). The geometric mean of AUC(t) was 495.8 ng ml(-1)h(-1) (test medication) and 468.3 ng ml(-1)h(-1) (reference medication). C(max) of 61.5 and 57.3 ng ml(-1) were achieved for the test and the reference medication, respectively. The point estimates and 90% confidence intervals for AUC(t) (parametric) and C(max) (parametric) were, in point estimate (90% confidence interval), 1.058 (0.989-1.134) and 1.073 (1.007-1.142), respectively, satisfying the bioequivalence criteria of the European Committee for Proprietary Medicinal Products and the US Food and Drug Administration Guidelines. The corresponding value of T(max) was 0.229 (0.015-0.444). These results indicate that the two medications of ambroxol hydrochloride are bioequivalent and, thus, may be prescribed interchangeably.

Administration, Oral↗
PubMed2002

Ambroxol inhibits platelet-derived growth factor production in human monocytic cells.

Several growth factors, including platelet-derived growth factor (PDGF), have been implicated in the mechanism of lung and airway remodeling. We investigated the effect of ambroxol, trans-4-[(2-amino-3,5-dibromobenzyl) amino] cyclohexanol hydrochloride, on the lipopolysaccharide-induced PDGF production in human monocytic cells, THP-1. Ambroxol inhibited the lipopolysaccharide-induced PDGF-AB production via PDGF-A mRNA expression. Lipopolysaccharide activated p44/42 extracellular signal-regulated kinase (ERK), and ambroxol attenuated the lipopolysaccharide-induced p44/42 ERK activation. Furthermore, mitogen-activated protein kinase kinase (MEK)-1-specific inhibitor, 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one (PD 98059), blocked the lipopolysaccharide-induced p44/42 ERK activation and PDGF production. These findings indicate that ambroxol inhibits the lipopolysaccharide-induced PDGF production due to the suppression of p44/42 ERK activity.

Ambroxol↗
PubMed2003

Determination of ambroxol hydrochloride in pure solutions and some of its pharmaceutical preparations under batch and FIA conditions.

New ambroxol (Amb) ion selective plastic membrane electrodes of both conventional and coated graphite types based on the ion-pair of ambroxolium tetraphenylborate (Amb-TPB) ion-pair are prepared. The conventional type electrode was fully characterized in terms of membrane composition, life span, pH, ionic strength and temperature. It was applied to potentiometric determination of ambroxol in pure solutions and pharmaceutical preparations under batch and flow injection conditions. The potentiometric determination was used in the determination of ambroxol in muco syrup in four batches of different expiry dates, also the amounts of ambroxol released after 1, 8 and 16 h from the muco sustained release type (S.R.) capsules were also assayed. The selectivity of the electrode toward a large number of excipient like inorganic cations, sugars and amino acids was tested. The solubility product of the ion-pair and the formation constant of the precipitation reaction leading to the ion-pair formation were determined conductimetrically.

Ambroxol↗
PubMed2000

High performance liquid chromatographic determination of ambroxol in the presence of different preservatives in pharmaceutical formulations.

A high-performance chromatographic method is described for simultaneous determination of ambroxol in the presence of different preservatives in syrups. The method separates ambroxol from methyl- ethyl-, propyl- and butyl paraben and from other multi-component mixtures. The retention behaviour of ambroxol and parabens as a function of both pH and mobile phase composition was investigated. The eluents were monitored with a UV detector at 247 nm. Linear relationships between the amount of pharmaceutical compounds and peak heights were confirmed at the concentrations of 0.74-14.08 microg ml(-1). The high recovery (no extraction of the samples is required) and the low %RSD confirm the suitability of the proposed method for the determination of ambroxol in different pharmaceutical preparations.

Ambroxol↗
PubMed2000

Efficacy and tolerability of myrtol standardized in acute bronchitis. A multi-centre, randomised, double-blind, placebo-controlled parallel group clinical trial vs. cefuroxime and ambroxol.

UNLABELLED: Myrtol standardized (Gelomyrtol forte) is a phytotherapeutic extract (distillate) consisting mainly of three monoterpenes: (+)alpha-pinene, d-limonene and 1,8-cineole. OBJECTIVE: This study describes and compares the efficacy, safety and tolerability of a 2-week treatment with myrtol stand. (4 x 300 mg, day 1-14), cefuroxime (CAS 55268-75-2) (2 x 250 mg daily for day 1-6), ambroxol (CAS 18683-91-5) (3 x 30 mg for day 1-3, 2 x 30 mg for days 4-14) and matched placebo in acute bronchitis. PATIENTS: 676 male and female outpatients, aged > or = 18 years, with acute bronchitis of recent onset (within last 5 days), with an FEV1 > 75% of the normal EGKS-value and without evidence or suspicion of chronic pulmonary disease or any further confounding illness were included in the study. INTERVENTION: Patients were randomly assigned to a 2-week treatment course with either myrtol stand. (N = 170), cefuroxime (N = 171), ambroxol (N = 163) or placebo (N = 172) in a double-blind, placebo-matched, parallel-group fashion. Evaluations were at baseline (visit 1), after 1 and 2 weeks of treatment (visits 2 and 3) and at 2 weeks after conclusion of the treatments (visit 4). CRITERIA: Responder- and non-responder rates (primary), signs (abnormal auscultation), symptoms (daily diary data on nightly cough, coughing fits during the day, sputum consistence and general well-being; visit data on bronchial hyperreactivity and absence/presence of associated symptoms), FEV1, overall efficacy, absence of relapse, safety and tolerability (adverse events, laboratory screens, vital signs and physical examination). Criteria were evaluated for the intention-to-treat data-set (ITT) and the 'efficacy evaluable' sample (EAP), i.e. excluding patients with missing values (incl. discontinued non-responders and drop-outs for other reasons) at the time of assessment. RESULTS: The signs and symptoms of acute bronchitis regressed readily in all treatment groups, but regression was slower and less complete in the patients treated with placebo. In patients treated with placebo, the acute bronchitis was considered to have deteriorated to such an extent that discontinuation was indicated ('non-responder') in 36 patients (ITT: 20.9%, 95% CI: 15.1 to 27.8% and EAP: 21.3%, CI: 15.4 to 28.3%) after 1 week (visit 2) and in 19 further patients (ITT: 11.0%, CI: 6.8 to 16.7%; EAP: 14.8%, CI: 9.2 to 22.2%) after 1 further week (visit 3). In contrast, in the group of patients treated with myrtol stand. the non-responder rates at visits 2 and 3 were only 5.3% (ITT, CI: 2.4 to 9.8%; EAP: 5.4%, CI: 2.5 to 10.0%) and 1.2% (ITT, CI: 0.1 to 4.2%; EAP: 1.3%, CI: 0.2 to 4.7%); the responder rates at visit 2 were statistically significantly higher (p < 0.001) for myrtol stand. (ITT: 92.9%, CI: 88.0 to 96.3) compared to placebo (ITT: 77.3%, CI: 70.3 to 83.4), and similar to those for cefuroxime (ITT: 92.4%, CI: 87.4 to 95.9) and ambroxol (ITT: 89.6%, CI: 83.8 to 93.8%). The superiority of the active treatments vs. placebo with little difference among the treatments was confirmed for all further criteria of evaluation. There was no evidence of bronchoconstriction or relapse in any treatment group for the patients continuing treatment (i.e. for those who were not discontinued because of non-response). The treatments were safe and comparably well tolerated. CONCLUSION: Compared to placebo, treatment with myrtol stand. was well tolerated but evidently superior in terms of efficacy, resulting in a more rapid and more complete recovery; although well comparable with the other active treatments, myrtol stand. tended to be superior to cefuroxime and ambroxol for several ancillary criteria. Myrtol stand. is a well-evidenced alternative to antibiotics for acute bronchitis without specified infective agent, without the risk to promote the development of bacterial resistance.

Acute Disease↗
PubMed1991

Ambroxol inhibits Na+ absorption by canine airway epithelial cells in culture.

To study the effect of ambroxol on ion transport functions of airway mucosa, we measured bioelectric properties of canine cultured tracheal epithelium under short-circuit conditions in-vitro. Addition of ambroxol to the submucosal but not to the mucosal solution in an Ussing chamber decreased short-circuit current, transepithelial potential difference and cell conductance. The ambroxol-induced decrease in short-circuit current was not affected by bumetanide or diphenylamine-2-carboxylate, but it was abolished by pretreatment of cells with amiloride. These results suggest that ambroxol may selectively inhibit Na+ absorption by airway epithelium, thereby increasing water composition in airway surface fluid and reducing mucus viscosity.

Absorption↗
PubMed1999

Effects of ambroxol on spontaneous or stimulated generation of reactive oxygen species by bronchoalveolar lavage cells harvested from patients with or without chronic obstructive pulmonary diseases.

We examined the effects of ambroxol on spontaneous or stimulated generation of reactive oxygen species (ROS) by bronchoalveolar lavage (BAL) cells prepared from 6 patients with chronic obstructive pulmonary disease (COPD) and age-matched control subjects without COPD. The ROS produced by BAL cells were measured by the lucigenin-dependent chemiluminescence method. The application of ambroxol into culture media containing BAL cells inhibited spontaneous and stimulated generation of ROS by BAL cells harvested from COPD patients and control subjects in an ambroxol concentration-dependent manner. These results indicate that ambroxol may be a candidate agent for reducing oxidant stresses of airways in COPD.

Aged↗
PubMed1981

Lung compliance and alveolar expansion in the artificially ventilated premature newborn rabbit after maternal treatment with ambroxol.

Premature newborn rabbits were delivered on day 27 of gestation, with or without antenatal treatment with ambroxol (50 mg/kg/day in maternal injections, on days 24-26). The animals were tracheostomized, kept in body plethysmographs at 35 degrees C, and ventilated artificially for 10 min with 100% oxygen, insufflation pressure 30 cm H2O, frequency 40/min, and varying inspiration time (20, 40, 60, or 80%). Lung-thorax compliance increased with inspiration time in both ambroxol-treated animals and controls, but there was no difference in compliance between treated and non-treated litters. Alveolar expansion, evaluated morphometrically in histological sections, was enhanced in ambroxol-treated animals ventilated with prolonged inspiration phase (60 or 80%); such a difference was not found in the on-treated group. This suggests that antenatal treatment with ambroxol might have a stimulating effect on the synthesis and/or release of factors improving alveolar stability in the premature lung.

Ambroxol↗
PubMed1987

Pharmacodynamic mechanism and therapeutic activity of ambroxol in animal experiments.

The mucokinetic activity of ambroxol was demonstrated as an increase in mucus or particle transport rate on the frog palate and in guinea pig tracheas. To clarify the mechanism we examined the influence of the drug on the ciliary beat frequency (CBF) of isolated cells from guinea pig tracheas. Ambroxol significantly stimulated the CBF up to 10.8%, salbutamol up to 19.5%. The effect of ambroxol on CBF certainly contributes to, but does not explain the more pronounced increase in transport rate. Thus a stimulation of the mucociliary transport rate by the other major pharmacodynamic mechanisms, secretagogue activity and stimulation of pulmonary surfactant, has to be considered. The therapeutic activity of ambroxol in models of the infant and adult respiratory distress syndrome and of the chronic bronchitic syndrome is reviewed.

Albuterol↗
PubMed1987

Multicenter study on the treatment of secretory otitis media with ambroxol. Importance of a surface-tension-lowering substance.

Animal studies showed the presence of a surfactant substance in the Eustachian tube. On the premise that alteration of surfactant-like substance might cause pathology of the middle ear in man, a multicenter (24 ENT hospitals) double-blind trial versus placebo was carried out in 435 adults and children with secretory otitis media. Treatment was ambroxol, a drug that changes the bronchial secretions and promotes surfactant synthesis. The dosage regimen was as follows: adults--one 30-mg tablet of ambroxol 3 times/day; children--9 mg of ambroxol syrup, 4 times daily. The treatment lasted 15 days. The clinical signs and symptoms (hypoacusis, conduction deafness) and the otoscopic and rhinoscopic findings of treated patients improved. The differences in these parameters between patients given ambroxol and the controls were statistically significant (p less than 0.05). The symptomatological amelioration was supported by improvement in tympanometric findings and hearing threshold. Drug tolerance was excellent.

Adult↗
PubMed1989

Ambroxol inhibits airway hyperresponsiveness induced by ozone in dogs.

To follow up previous observations that airway hyperresponsiveness induced by ozone is linked to airway inflammation and particularly to the release of arachidonic acid metabolites, we investigated the effect of ambroxol (a mucoactive and surfactant-stimulating drug that has recently been discovered to inhibit the release of arachidonic acid from cell membrane phospholipids) on airway hyperresponsiveness and bronchoalveolar neutrophilia induced by ozone in dogs. One group of 5 dogs was studied before treatment with nebulized saline and then after exposure to ozone (3 ppm, 1 h); another group of 6 dogs was studied before treatment with ambroxol (100 breaths of a 1% solution) and after exposure to ozone. On each occasion, we measured airway responsiveness to acetylcholine and counted the number of cells in bronchoalveolar lavage fluid. When the dogs were given the saline placebo, ozone induced a marked increase in airway responsiveness to acetylcholine and a marked influx of neutrophils in the airways. When the dogs were given ambroxol, ozone induced the same increase in the number of neutrophils in bronchoalveolar lavage, but did not increase the degree of airway responsiveness to acetylcholine. We conclude that ambroxol inhibits ozone-induced airway hyperresponsiveness in dogs, probably by inhibiting the formation and release of oxygenation products of arachidonic acid from neutrophils.

Acetylcholine↗
PubMed1986

[Effects of ambroxol on pulmonary surfactant--analysis of the fatty acid composition of phosphatidylcholine in the sputum and normal respiratory tract fluid in rabbits].

The mechanism of action of secretagogic expectorants (ex., ambroxol) has not been clarified. Recently, attention has been directed to the relationship of their action to pulmonary surfactants. In the present study, the fatty acid (FA) composition of phosphatidylcholine (PC), which is the main physiological surfactant, was investigated using sputum, respiratory tract fluid, mucin-like substance, lung washings and lung tissue of rabbits. Effects of ambroxol (20 mg/kg, i.s.) on several parameters such as output volume, FA contents of PC, protein content and viscosity of respiratory tract fluid of rabbits were also investigated. In respiratory tract fluid, lung washings and mucin-like substance of rabbits, saturated FA, especially C16:0, were predominant components of PC; while in sputum and lung tissue of rabbits and respiratory tract fluid of hens, unsaturated FA, especially C18:1 and C18:2, were more predominant components in comparison with those in the above specimens. Ambroxol significantly increased the contents of C16:0, saturated FA and total FA of PC, and it also increased protein content with an increase in the viscosity of respiratory tract fluid. These results suggest that in the respiratory tract fluid of rabbits, PCs are pulmonary surfactants, and the increasing secretion of pulmonary surfactant is likely to be involved in the expectorant action of ambroxol.

Ambroxol↗
PubMed2000

[Prophylaxis against ventilator-induced lung injury by Ambroxol].

OBJECTIVE: To investigate the protective effect of Ambroxol on ventilator induced lung injury (VILI) of rats. METHODS: 30 healthy SD rats were randomly divided into three groups: group A was served as control group (n = 10, V(T) 8 ml/kg), group B received large V(T) ventilation (n = 10, V(T) 40 ml/kg), group C received large V(T) ventilation with pre-treatment of IP ambroxol. The contents of protein, TNF-alpha, IL1-beta, IL-8 in BALF and MDA, SOD, GSH levels in the homogenate of the rat lungs were assayed respectively. Total white blood cells in BALF were counted; The severities of lung injury of the three groups were assessed under a light microscope. RESULTS: The albumin and total protein contents in BALF were significantly higher group A than in groups B and C. A large quantity of WBCs infiltration were found in BALF of group B, while the amount of WBCs were decreased in group C. TNF-alpha, IL-1beta and IL-8 level in BALF of group B were 101.6 pmol.L(-1).mg(-1) Pr +/- 37.4 pmol.L(-1).mg(-1) Pr, 0.47 microgram.L(-1).mg(-1) Pr +/- 0.14 microgram.L(-1).mg(-1) Pr and 2.02 microgram.L(-1).mg(-1) Pr +/- 0.49 microgram.L(-1).mg(-1) Pr, respectively. MDA, one of the parameters reflecting the extent of oxidative reaction, were produced profoundly in the lungs of group B, but the local levels of SOD, which reflects the ability of antioxidation, were decreased significantly in group B. There existed significant differences of the above parameters between group B and group A. Ambroxol could significantly decrease the locally produced TNF-alpha and inhibit the oxidative reactions, and increase the locally antioxidative potency. Severe acute lung injuries were detected in group A by histological examination and the extent of injury was much lighter in group C than in group B. CONCLUSION: Locally increased inflammatory cytokines formation and the imbalanced oxidative/antioxidative reaction play important roles in the pathogenesis of VILI. Ambroxol has an obvious protective effect on VILI through its antioxidant/anti-inflammation potent.

Ambroxol↗
PubMed2005

Effect of ambroxol, spirulina and vitamin-E in naphthalene induced cataract in female rats.

Anticataract activity of Ambroxol, Spirulina and Vitamin E was examined using the naphthalene cataract model. Adult female albino rats of Wistar strain weighing between 180 and 220 grams were taken and divided into eight groups. Group I received light liquid paraffin 5 ml/kg/ day p.o. for 6 weeks. Group II received naphthalene solution 0.5 gm/kg/ day p.o. for first three days and 1 gm/kg/day p.o. thereafter for six weeks. Group III received Ambroxol suspension in 0.5% carboxy methyl cellulose (CMC) at the dose of 100 mg/kg/day p.o. alongwith naphthalene. Group IV received Spirulina in distilled water at the dose of 1500 mg/kg/ day p.o. alongwith naphthalene. Group V received Vitamin E emulsion at the dose of 50 mg/kg/day p.o. alongwith naphthalene. Group VI received Ambroxol alone at the dose of 100 mg/kg/day p.o. Group VII received Spirulina alone at the dose of 1500 mg/kg/day p.o. Group VIII received vitamin E alone at the dose of 50 mg/kg/day p.o. Lens glutathione, soluble protein and water content profiles revealed the preventive role of Ambroxol, Spirulina and Vitamin E in naphthalene-induced cataract in female rats.

Ambroxol↗
PubMed1991

[The effect of ambroxol on peroxidative processes in dog lung mitochondria].

The influence of Ambroxol on the Fe3+ (ADP) dihydroxyfumarate-induced peroxidation of mitochondrial lipids in dog lung was investigated. It was shown that changes in mitochondrial lipid composition include great decrease in phosphatidylcholine and phosphatidylethanolamine content, with concomitant increase in lysophosphoglyceride content. Addition of Ambroxol (5 mM and 10 mM) to the incubation medium decreases these changes in dose-dependent manner. The malondialdehyde production was greatly reduced in the presence of Ambroxol. The mode of Ambroxol action was comparable to that of other free radical scavengers.

Ambroxol↗
PubMed1986

Normalization of bronchial exocrine pathology after endobronchial treatment with ambroxol.

A clinical study was performed on nine adult in-patients suffering from chronic intercrisis bronchopneumopathy, to evaluate whether a local endobronchial treatment with ambroxol could be effective in stabilizing the secretory activity of bronchial glands modified by phlogistic injury. The patients underwent bronchoscopic examination and deep biopsy, before and after treatment with local medication of ambroxol every other day for 30 days. In addition to morphometric measurements, detailed histochemical examinations were performed on the secretion of mucous acinic and glandular excretory ducts. The trial proved that the treatment with ambroxol stimulates serous acini, restoring normal production of sulphomucins and also of mucous acini, increasing the metabolic activities of acid glycoproteins and proportionally curtailing the excessive synthesis of glycoproteins. Ambroxol can therefore be considered a mucoregulating drug.

Adult↗