Titre du document / Document title

Formulation and evaluation of controlled-release transdermal patches of theophylline-salbutamol sulfate

Auteur(s) / Author(s)

NARASIMHA MURTHY S. ⁽¹⁾ ; RANI Shobha ; HIREMATH R. ⁽²⁾ ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

⁽¹⁾ M. S. Ramaiah College of Pharmacy, Bangalore 560054, INDE
⁽²⁾ Al-Ameen College of Pharmacy, Hosur Road, Bangalore 560027, Karnataka, INDE

Résumé / Abstract

Transdermal formulations containing theophylline and salbutamol sulfate (SS) were formulated using hydroxypropylmethylcellulose. Theophylline was loaded by adsorption with the aid of the coadsorbate sodium chloride. The formulations were subjected to in vitro release studies, and the dose of salbutamol and theophylline was optimized to yield the desired flux. The films were uniform and 93±5.4 μm thick. The in vitro fluxes of theophylline and salbutamol sulfate from the formulation were 1.22±0.4 mg/h/cm² and 13.36±1.02 μg/h/cm². respectively. The formulation was subjected to pharmacodynamic studies in guinea pigs. The preconvulsive time (PCT) of guinea pigs increased significantly after 4 h, and the same was observed even after 24 h. Pharmacokinetic studies were carried out in healthy human volunteers. Theophylline was analyzed in saliva, and salbutamol was analyzed in the blood plasma. The T_max of the drugs was 3 h, and appreciable concentrations of the drugs above their MEC could be analyzed even after 12 h. The elimination half-life of the drugs was significantly prolonged compared to that for tablets. There were no signs of erythema or edema in the volunteers during observation for a period of 7 days.

Revue / Journal Title

Drug development and industrial pharmacy   ISSN 0363-9045 

Source / Source

2001, vol. 27, n^o10, pp. 1057-1062 (14 ref.)

Langue / Language

Anglais

Editeur / Publisher

Taylor & Francis, Colchester, ROYAUME-UNI  (1977) (Revue)

Mots-clés anglais / English Keywords

Vertebrata ; Mammalia ; Ungulata ; Artiodactyla ; Topical administration ; Pig ; Pharmacokinetics ; Xanthine derivatives ; Healthy subject ; Human ; Animal ; In vivo ; Physicochemical properties ; Active ingredient ; In vitro ; Release ; Cellulose derivatives ; Control release polymer ; Controlled release form ; Patch ; Drug carrier ; Drug combination ; Salbutamol ; Drug interaction ; Antiasthma agent ; Theophylline ; Blood ; Blood plasma ; Dosage form ; Bronchodilator ; β-Adrenergic receptor agonist ; Pharmaceutical technology ;

Mots-clés français / French Keywords

Vertebrata ; Mammalia ; Ungulata ; Artiodactyla ; Cellulose(hydroxypropyl méthyl) ; Voie externe ; Porc ; Pharmacocinétique ; Xanthine dérivé ; Individu sain ; Homme ; Animal ; In vivo ; Propriété physicochimique ; Principe actif ; In vitro ; Libération ; Cellulose dérivé ; Polymère vecteur ; Forme libération contrôlée ; Patch ; Vecteur médicament ; Association médicamenteuse ; Salbutamol ; Interaction médicamenteuse ; Antiasthmatique ; Théophylline ; Sang ; Plasma sanguin ; Forme pharmaceutique ; Bronchodilatateur ; Stimulant β-adrénergique ; Technologie pharmaceutique ;

Mots-clés espagnols / Spanish Keywords

Vertebrata ; Mammalia ; Ungulata ; Artiodactyla ; Vía externa ; Cerdo ; Farmacocinética ; Xantina derivado ; Individuo sano ; Hombre ; Animal ; In vivo ; Propiedad fisicoquímica ; Principio activo ; In vitro ; Liberación ; Celulosa derivado ; Polímero vector ; Forma liberación controlada ; Parche ; Vector medicamento ; Asociación medicamentosa ; Salbutamol ; Interacción medicamentosa ; Agente antiasma ; Teofilina ; Sangre ; Plasma sanguíneo ; Forma farmacéutica ; Broncodilatador ; Estimulante β-adrenérgico ; Tecnología farmacéutica ;

Localisation / Location

INIST-CNRS, Cote INIST : 17132, 35400010322411.0060