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At least 685 records · Page 38Linked to original sources
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

Evaluation of nebulised hypertonic saline (7%) as an adjunct to physiotherapy in patients with stable bronchiectasis.

Sputum clearance is of prime importance in the management of patients with bronchiectasis. While nebulised normal isotonic saline (0.9%) (IS) has been anecdotally used to treat patients with tenacious sputum, the use of hypertonic saline (7%) (HS) could have potential muco-protective and clearance properties. 24 patients with bronchiectasis were randomised to receive four single treatment schedules in random order: (1) active cycle breathing technique (ACBT) alone, (2) nebulised terbutaline then ACBT, (3) nebulised terbutaline, nebulised IS then ACBT and (4) nebulised terbutaline, nebulised HS then ACBT. Sputum weights were significantly higher after HS than IS (P = 0.002). Ease of expectoration also differed overall (P < 0.0001) and was significantly lower with HS than with IS (P = 0.0005). Sputum viscosity differed between treatment phases, with a significant linear trend to reduced sputum viscosity with HS (P = 0.0002). These changes were associated with small but statistically significant differences in FEV1 (P = 0.043) and FVC (P = 0.011) between treatment phases. Nebulised hypertonic saline can be used safely and effectively as an adjunct to physiotherapy in selected patients. A long-term prospective trial is now indicated to determine its effectiveness on long-term infection rate, quality of life and lung function.

Aged↗
PubMed2001

Determination of ambroxol or bromhexine in pharmaceuticals by capillary isotachophoresis.

Expectorant drugs ambroxol (AX) and bromhexine (BX) were determined by capillary isotachophoresis (ITP) with conductimetric detection. The leading electrolyte (LE) was a buffer solution that contained 5 mM picolinic acid and 5 mM potassium picolinate (pH 5.2). The terminating electrolyte (TE) was 10 mM formic acid. The driving current was 80 microA (for approximately 200 s) or 50 microA (for approximately 350 s) and the detection current was 20 microA (a single analysis took about 8 min). The effective mobilities of AX and BX (evaluated with tetraethylammonium as the mobility standard) were 18.8 x 10(-9) m2 V(-1) s(-1) and 14.3 x 10(-9) m2 V(-1) s(-1) respectively. The calibration graphs relating the ITP zone length to the concentration of the analytes were rectilinear (r = 0.9993-0.9999) in the range 10 mg L(-1) (20 mg L(-1) for BX) to 200 mg l(-1) of the drug standard. The relative standard deviations (RSD) were 1.2 1.6% (n = 6) when determining 100 mg l(-1) of the analytes in pure test solutions. The method has been applied to the assay of AX or BX in seven commercial mass-produced pharmaceutical preparations. According to the validation procedure based on the standard addition technique the recoveries were 97.5-102.7% of the drug and the RSD values were 0.11-2.20% (n = 6).

Ambroxol↗
PubMedDate not supplied

In vitro rheological assessment of mucolytic activity induced by seaprose.

Proteolytic enzymes can act on the polymeric structure of the bronchial mucus, shortening the long chain of mucoproteins, DNA and other macromolecules, and thus reducing the viscosity of the mucus facilitating its expectoration. Seaprose (Flaminase, Puropharma) belongs to this class and is a proteinase from Aspergillus melleus and it is mainly used in traumatology, orthopaedics, gynaecology and pneumology. In the present study the in vitro activity of increasing concentrations (0.25, 0.5, 1%) of seaprose incubated with bronchial mucus samples (1 ml) was investigated by a rheological technique (transient test) that assesses changes in viscosity and elasticity. A dose-effect relationship between increasing concentrations of seaprose and the corresponding reductions in bronchial mucus viscosity was found. There was also a parallel reduction in elasticity after incubation with 0.5%, but an unfortunate distribution of values for 0.25 and 1% concentrations does not allow us to state whether there is a dose-effect relationship for elasticity.

Adult↗
PubMed1998

Erdosteine enhances mucociliary clearance in rats with and without airway inflammation.

Erdosteine is a new homocysteine-derived expectorant and has been reported to have many mucolytic effects. In this report, we studied the activities of erdosteine on mucociliary clearance in normal and airway-inflammation-induced rats. In normal rats, erdosteine at doses of 100-600 mg/kg significantly promoted mucociliary clearance. However, erdosteine did not change the concentrations of mucopolysaccharides in bronchoalveolar lavage fluid (BALF). In the LPS-instillated rats, the mucociliary clearance was inhibited and the number of inflammatory cells, albumin concentration, and mucopolysaccharides concentration in BALF were increased. Erdosteine at doses of 100-600 mg/kg significantly attenuated the inhibition of mucociliary clearance and the increase of inflammatory cells, however, it did not prevent the increase of albumin and mucopolysaccharides. Other mucolytic drugs which are ambroxol and S-carboxymethylcysteine, had no effect. These results indicate that erdosteine promotes the mucociliary clearance in normal and airway-inflammation-induced rats.

Albumins↗
PubMed2000

Drugs affecting the respiratory system.

Differences in the disposition of drugs among exotic animals is a well-recognized hurdle when treating disease. Differences exist in pharmacokinetics, pharmacodynamics, and disease processes. This article focuses on the principles of treating respiratory tract diseases, with the recognition that not all drugs are indicated for use in all exotic species. The discussion begins with a description of respiratory physiology as it pertains to response to drugs, using the mammalian lung as a template. The role of respiratory defense mechanisms in airway protection and disease is addressed. Drugs used to treat the respiratory tract include the bronchodilators and anti-inflammatory drugs, drugs that modify respiratory secretions (e.g., mucolytics, mucokinetics, and expectorants), antitussive drugs, and decongestants. Aerosolization is an important adjuvant for respiratory therapy as long as precautions are met. Infectious diseases are among the more common respiratory diseases encountered, and the discussion includes a focus on the use of antibiotics for treating respiratory tract infections.

Administration, Inhalation↗
PubMed2003

Depressant effects of ambroxol and erdosteine on cytokine synthesis, granule enzyme release, and free radical production in rat alveolar macrophages activated by lipopolysaccharide.

The present study examined the effects of ambroxol and erdosteine, bronchial expectorants, on the cytokine synthesis, granule enzyme release, and free radical production in rat alveolar macrophages activated by lipopolysaccharide. Ambroxol and erdosteine significantly decreased the production of tumour necrosis factors-alpha, interleukin-1beta, and interleukin-6 in alveolar macrophages activated by lipopolysaccharide. These drugs significantly reduced the production of superoxide anion, hydrogen peroxide, and nitric oxide and the release of acid phosphatase and lysozyme in lipopolysaccharide-activated macrophages. Ambroxol and erdosteine showed no scavenging effect on superoxide anion and hydrogen peroxide, whereas both drugs effectively decomposed nitric oxide. The results show that ambroxol and erdosteine may inhibit the responses, including cytokine synthesis and free radical production, in rat alveolar macrophages activated by lipopolysaccharide. Unlike the production of reactive oxygen species, the inhibitory effect of ambroxol and erdosteine on the production of nitric oxide in lipopolysaccharide-activated alveolar macrophages may be accomplished by a scavenging action on the species and inhibition of the respiratory burst.

Ambroxol↗
PubMed2005

The role of airway secretions in COPD--clinical applications.

It has been established that mucus hypersecretion and decreased mucus clearance contribute to the morbidity of chronic obstructive pulmonary disease (COPD). Indeed, the classic definition of chronic bronchitis relies on determining the frequency and duration of sputum expectoration. Despite the well recognized importance of this symptom, there are few therapies routinely used to decrease the sputum production or to improve clearance. There are fewer well conducted clinical trials of existing medications and this has led many regulatory agencies, notably the Food and Drug Administration (FDA), to refuse to register these medications or approve their sale. Similarly, airway clearance devices and chest physical therapy have not been well studied in COPD. Carefully conducted studies of interventions to improve airway clearance, similar to those done in cystic fibrosis (CF), may help us to identify effective therapies and possibly novel diagnostic tests for the management of COPD.

Expectorants↗
PubMed1999

Alternative therapies for chronic bronchitis.

Alternative therapies for chronic bronchitis are therapies in which clinical efficacy is not well established. These can be broadly divided into expectorants, mucolytics, mucokinetics, antiproteases, antioxidants, and immunostimulants. Data supporting these therapies may be present in disorders clinically similar to chronic bronchitis, such as cystic fibrosis. Alternatively, these therapies may be based on clinical observations or in vitro studies that suggest a potential therapeutic benefit. Establishment of these therapies is likely to require more extensive investigation before their use is routinely recommended. Until such data is available, the clinician can only use his or her clinical judgement regarding the likely risk-benefit ratio.

Adjuvants, Immunologic↗
PubMed2000

Recent advances in alternative therapies.

Complementary and alternative medicine (CAM) is becoming more popular, and CAM remedies are used instead of, or integrated with, orthodox allopathic therapies by many patients with asthma. Although most CAM remedies may have no discernible effects when analyzed by conventional medical techniques, some double-blind controlled studies do suggest that a meaningful benefit can be obtained with acupunture and homeopathic management in asthma. Herbal medicine is more popular, despite little evidence that the vast majority of herbs for asthma have any useful effects other than a nonspecific expectorant action. Dietary adjustment may benefit a small percentage of patients with asthma, but extreme measures are very rarely indicated. Formal pyschologic approaches can help some patients by reducing anxiety. Although most CAM approaches are harmless, the lack of benefit of many remedies and the potential harm from some of them must be recognized.

Acupuncture Therapy↗
PubMed1988

Effects of iodinated glycerol on thyroid function studies in elderly nursing home residents.

Iodinated glycerol is used as a mucolytic expectorant in the treatment of respiratory disorders. Iodine can inhibit the biosynthesis of thyroid hormone and induce hypothyroidism, particularly in patients with a history of thyroid disease. Such effects have not been reported in individuals without known thyroid disease who are being treated with organically bound iodine in the form of iodinated glycerol. In the course of a thyroid screening program for nursing home residents, eight subjects were identified who were being treated with iodinated glycerol. Five of these were found to have thyrotropin elevations; one showed a low serum thyroxine level and a decreased free thyroxine index. None of these residents had a history of thyroid disease. Abnormalities of thyroid function improved or resolved after discontinuation of therapy. Elderly nursing home residents without known thyroid disease are at risk of thyroid suppression when given iodinated glycerol.

Aged↗
PubMed1987

Benylin dependence, metabolic acidosis and hyperglycaemia.

We describe a patient who had consumed large quantities of a proprietary cough mixture containing diphenhydramine, ammonium chloride and sodium citrate (Benylin expectorant) daily for several months and subsequently presented with confusion, marked metabolic acidosis and non-ketotic hyperglycaemia.

Acidosis↗
PubMed2003

Genetic distinction of radix adenophorae from its adulterants by the DNA sequence of 5S-rRNA spacer domains.

Radix Adenophorae (Shashen), a traditional Chinese medicine commonly used as an antitussive and expectorant, is derived from roots of Adenophora stricta Miq. and Adenophora tetraphylla (Thunb.) Fisch. Twelve species and varieties of Adenophora and Glehnia, however, could act as substitutes or adulterants of Radix Adenophorae on the commercial markets in South East Asia, and roots of Adenophora hunanensis Nannf. and Glihnia littoralis F. Schmidt ex Miq. are the most common examples. The authentic identification of dried roots of A. stricta and A. tetraphylla, however, is difficult on the basis of appearance and morphology. A molecular genetic approach was developed here to identify the species of Radix Adenophorae. The 5S-rRNA spacer domains (approximately 250 bp) were amplified by the polymerase chain reaction (PCR) from genomic DNAs isolated from A. stricta, A. tetraphylla, A. hunanensis and G. littoralis, and subsequently, the nucleotide sequences were determined. Diversity in DNA sequence and restriction enzyme mapping among various species were found in their 5S-rRNA spacer domains, which could serve as markers for authentic identification of Radix Adenophorae.

Antitussive Agents↗
PubMed1980

Tracheobronchial function in health and disease. Effect of mucolytic substances.

The effect of mucolytic and expectorant substances on ciliary beat frequency, mucus transport velocity and mucus production, was investigated in normal and bronchitic rats. The results showed that: (i) N-acetylcysteine and S-carboxymethylcysteine were mildly cilioexcitatory at low and ciliodepressive at higher concentrations in both normal and bronchitic rats. A similar pattern was seen in mucus transport velocity. (ii) Bisolvon enhanced all aspects of mucociliary activity in both groups of animals. Sobrepin was less effective than Bisolvon and more effective than Tachoquilin. (iii) Geleomyrtol, Ozothin and prostaglandin E1 were all cilioexcitatory in rats with bronchitis. Mucus transport velocity was similarly stimulated by both Geleomyrtol and Ozothin. (iv) Ammonium chloride and potassium iodide enhanced mucociliary activity in normal and bronchitic rats. (v) All substances stimulated mucus production, however, the most potent was prostaglandin E1. The mechanisms for increased mucociliary activity involve inter alia the probable cleaving of disulfide bridges, decreased mucosal swelling, altered rheological characteristics and stimulation of adenylate cyclase.

Animals↗
PubMed1996

Short-term recombinant human DNase in bronchiectasis. Effect on clinical state and in vitro sputum transportability.

We report a double blind placebo-controlled phase II study of the efficacy and safety of nebulized recombinant human DNase (rhDNase) administered for 14 d to adults with bronchiectasis not caused by cystic fibrosis. All were in a stable clinical state at the commencement of the study, and they received (1) rhDNase 2.5 mg twice daily, (2) rhDNase once daily, or (3) placebo (excipient only) inhalation. The outcome measures were spirometry, subjective quality of life/dyspnea, and safety. We also measured the ciliary transportability of the sputum expectorated before and after the treatment period, using the mucus-depleted bovine trachea. The drug was well tolerated, but it produced no significant change in any of the outcome variables or in sputum transportability. When the drug was incubated with bronchiectatic sputum in vitro, a fall in transportability was observed. We discuss possible explanations for the lack of a measurable benefit from rhDNase in this study population, which appears to contrast with the improvements shown in cystic fibrosis using studies of similar design.

Administration, Inhalation↗
PubMed1997

Rheology of cystic fibrosis sputum after in vitro treatment with hypertonic saline alone and in combination with recombinant human deoxyribonuclease I.

Treatment with recombinant human deoxyribonuclease I (rhDNase) is currently used as therapy for cystic fibrosis (CF) lung disease. Hypertonic saline (HS) acts as an expectorant promoting mucus secretion and augmenting the volume of sputum. We evaluated the individual and combined effects of HS and rhDNase in vitro on the viscoelasticity of CF sputum. Sputum samples were collected from nine CF patients to use for in vitro testing. Aliquots of CF sputum (0.20 to 0.40 g) were subjected to the following protocols: (1) negative control sample without any treatment; (2) positive control sample, adding 10% volume of normal saline (0.9% NaCl); (3) application of hypertonic saline (HS-3% NaCl); (4) combining approximately 100 nM concentration of rhDNase with protocols 2 and 3. The samples in protocols 2 through 4 were incubated for 30 min at 37 degrees C. For each protocol, CF sputum was analyzed at baseline and at 30 min for spinnability by filancemeter and viscoelasticity by magnetic microrheometry. Spinnability decreased for the sputum samples that were treated with rhDNase, in combination with either HS or normal saline. Treatment with HS alone and combined treatment with rhDNase and HS decreased log G* (the principal viscoelasticity index) to the same degree. Saline alone and rhDNase in normal saline both increased the predicted cough clearability of the sputum; however, the combined treatment with rhDNase and hypertonic saline had the best overall effect on cough clearability. The change in predicted mucociliary clearability, although greatest after HS, was not significant. These in vitro results suggest that combined treatment with rhDNase and HS should be evaluated further as a potential mucotropic approach to augment the clearance of purulent sputum in CF lung disease.

Adolescent↗
PubMed1991

Hyperthyroidism induced by iodinated glycerol.

We report a case of iodide-induced thyrotoxicosis after the use of iodinated glycerol (Organidin) for the symptomatic treatment of chronic obstructive pulmonary disease. In patients with severe chronic obstructive pulmonary disease, symptoms of hyperthyroidism may be overlooked. Hyperthyroidism may be induced by any iodinated expectorant, especially in patients with preexisting thyroid disease.

Aged↗
PubMed1980

Clinical indications for and effects of bland, mucolytic, and antimicrobial aerosols.

The clinical usefulness of bland, mucolytic, and antimicrobial aerosols in the management of obstructive airway disease or bronchopulmonary infections was critically reviewed at th last Conference on th Scientific Basis of Respiratory Therapy in 1974. From the information available at that time, it was cocluded that there was little scientific basis for these therapeutic modalities. It was also suggested that the value of aerosol therapy should be evaluated by objective tests. The relatively few studies reported during the last 5 years have not generated new data in support of such aerosol therapy. Three criteria have been used to assess the efficacy of bland and mucolytic aerosols: respiratory function, mucociliary function, and subjective symptoms. Although respiratory and mucociliary function have generally been found to remain unaltered or to deteriorate after administration of bland or mucolytic aerosols, some investigators have observed facilitated expectoration or improved cough efficiency. The effectiveness of antimicrobial aerosols is more difficult to evaluate, and their value in patients with bacterial or fungal pulmonary infections remains to be demonstrated. Considering the cost and potential hazards of aerosol therapy, its use should be restricted to forms of aerosols whos clinical value has been objectively demonstrated; a reassessment of the literature suggests that bland and currently used mucolytic and antimicrobial aerosols do not meet this requirement.

Adult↗