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3.
Pharmacol Res ; 22(5): 611-7, 1990.
Article in English | MEDLINE | ID: mdl-2277801

ABSTRACT

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.


Subject(s)
Aspergillus/enzymology , Endopeptidases/pharmacology , Expectorants/pharmacology , Peptide Hydrolases/pharmacology , Serine Endopeptidases , Adult , Aged , Dose-Response Relationship, Drug , Elasticity , Female , Humans , In Vitro Techniques , Male , Middle Aged , Mucus/drug effects , Viscosity
4.
Arzneimittelforschung ; 40(8): 938-41, 1990 Aug.
Article in English | MEDLINE | ID: mdl-2242088

ABSTRACT

The topical tolerability of an intranasal salmon calcitonin spray preparation, of the excipients alone and of sodium taurocholate has been studied by assessment of the mucociliary transport velocity (MTV) on the frog's palate. The rate of mucus transport was investigated in 3 groups of animals (Rana esculenta; 6 frogs per group) in basal conditions and after a challenge with a salmon calcitonin intranasal spray preparation, with the excipients and with sodium taurocholate, respectively. The salmon calcitonin intranasal spray preparation and the excipients did not affect the mucociliary transport velocity on the frog's palate. On the contrary, sodium taurocholate produced severe impairments in the mucociliary transport velocity and histological lesions of the epithelial layer of the frog's palate. The comparison among the mean values of the mucociliary transport velocity before and after treatments showed a significant difference between controls and sodium taurocholate groups (p less than 0.05) as well as among the groups treated with sodium taurocholate versus salmon calcitonin and versus the excipients alone of the calcitonin preparation (p less than 0.05). These findings provide evidence that the salmon calcitonin intranasal spray preparation tested in the present ex vivo model does not affect the mucociliary transport velocity in the frog's palate, while this is markedly affected by sodium taurocholate. The use of sodium taurocholate as a promoter of absorption in intranasal preparations should thus be reconsidered.


Subject(s)
Calcitonin/toxicity , Mucociliary Clearance/drug effects , Administration, Topical , Animals , Calcitonin/administration & dosage , Calcitonin/pharmacology , In Vitro Techniques , Palate/anatomy & histology , Palate/metabolism , Rana esculenta , Taurocholic Acid/pharmacology
5.
Respiration ; 57(6): 353-8, 1990.
Article in English | MEDLINE | ID: mdl-2099568

ABSTRACT

The rheological behavior and clearance of bronchial mucus samples collected by protected expectoration from 24 out-patients with simple chronic bronchitis were investigated before, at the end of a short period of treatment (4 days) with a single oral dose of 2.7 g (sachet) of carbocysteine-lysine (evening meal), and on the 4th and 8th days after the end of treatment versus placebo. In the group treated with carbocysteine-lysine, there were significant reductions in viscosity (-67, -48, -62%) and increases in mucociliary transport (+41, +31, +34%) at the three times mentioned. The most striking finding was that the improvements were still present 8 days after cessation of treatment. The elasticity parameter was not affected in any statistically significant way (-10, -24, +65%). These findings suggest the presence of some type of 'post-mucoactive' effect.


Subject(s)
Bronchitis/metabolism , Carbocysteine/pharmacokinetics , Mucus/metabolism , Adult , Aged , Chronic Disease , Female , Humans , Male , Middle Aged , Mucociliary Clearance , Random Allocation , Rheology , Viscosity
6.
Int J Clin Pharmacol Res ; 9(1): 77-83, 1989.
Article in English | MEDLINE | ID: mdl-2707929

ABSTRACT

Nesosteine, a new agent shown to improve physical characteristics of bronchial mucus in animal models, has been studied in chronic bronchitic patients to confirm its effect on viscoelasticity of bronchial secretions. Sputum was collected from hypersecretory bronchitic patients in a stable condition before and after seven days of treatment with nesosteine (900 mg/day) or a placebo. At the end of treatment a significant (p less than 0.05) decrease was found in the viscosity in the nesosteine group: on the contrary, a slight, non-significant increase in viscosity was observed in the mucus samples of the placebo group. The improvement in rheological characteristics of the bronchial mucus in the patients treated with nesosteine was associated with an increase in mucus transport rate (mucociliary clearance) observed in the same samples. The findings indicate that nesosteine reduces mucus viscosity in chronic bronchitic patients and that this change induces also an improvement in mucociliary clearance.


Subject(s)
Bronchitis/drug therapy , Expectorants/therapeutic use , Mucociliary Clearance , Mucus/metabolism , Rheology , Thiazoles/therapeutic use , Humans , Molecular Structure
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