Titre du document / Document title

Monolithic osmotic tablet system for nifedipine delivery

Auteur(s) / Author(s)

LONGXIAO LIU ⁽¹⁾ ; KHANG G. ⁽¹⁾ ; RHEE J. M. ⁽¹⁾ ; HAI BANG LEE ⁽²⁾ ;

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

⁽¹⁾ Department of Polymer Science and Technology, Chonbuk National University, 664-14 Dukjin Dong, Dukjin Ku, Chonju 561-756, COREE, REPUBLIQUE DE
⁽²⁾ Biomaterials Laboratory, Korea Research Institute of Chemical Technology, P.O. Box 107, Yusung, Taejon 305-606, COREE, REPUBLIQUE DE

Résumé / Abstract

The monolithic osmotic tablet system, which is composed of a monolithic tablet coated with cellulose acetate (CA) membrane drilled with two orifices on both side surfaces, has been described. The influences of tablet formulation variables including molecular weight (MW) and amount of polyethylene oxide (PEO), amount of potassium chloride (KCl), and amount of rice starch as well as nifedipine loading have been investigated. The optimal tablet formulation and the osmotic-suspending co-controlled delivery mechanisms have been proposed. Orifice size and membrane variables including nature and amount of plasticizers as well as thickness on drug release have also been studied. The in vitro release profiles of the optimal system have been evaluated in various release media and different agitation rates, and compared with commercialized conventional capsule and push-pull osmotic tablet. It was found that PEO with MW of 300 000 g/mol was suitable to be thickening agent, both amount of KCl and amount of PEO had comparable and profoundly positive effects, while nifedipine loading had a strikingly negative influence on drug release. It could be found that the optimal orifice size was in the range of 0.25-1.41 mm. It has also been observed that hydrophilic plasticizer polyethylene glycol (PEG) improved drug release whereas hydrophobic plasticizer triacetin depressed drug release when they were incorporated in CA membrane. The monolithic osmotic tablet system was found to be able to deliver nifedipine at the rate of approximate zero-order up to 24 h, independent of both environmental media and agitation rate, and substantially comparable with the push-pull osmotic tablet. The monolithic osmotic tablet system was simple to be prepared as exempting from push layer and simplifying in the orifice drilling compared with the push-pull osmotic tablet. The monolithic osmotic tablet system may be used in drug controlled delivery field, especially suitable for water-insoluble drugs.

Revue / Journal Title

Journal of controlled release   ISSN 0168-3659   CODEN JCREEC 

Source / Source

2000, vol. 67, n^o2-3, pp. 309-322 (23 ref.)

Langue / Language

Anglais

Editeur / Publisher

Elsevier, Amsterdam, PAYS-BAS  (1984) (Revue)

Mots-clés anglais / English Keywords

Nifedipine ; Calcium antagonist ; Antihypertensive agent ; Pharmaceutical technology ; Dosage form ; Osmotic pump ; Coated tablet ; Drug carrier ; Release ; Active ingredient ; In vitro ; Cellulose derivatives ; Ethylene oxide polymer ; Slow release form ; Molecular weight ; Potassium Chlorine ; Rice starch ; Dihydropyridine derivatives ;

Mots-clés français / French Keywords

Nifédipine ; Antagoniste calcium ; Antihypertenseur ; Technologie pharmaceutique ; Forme pharmaceutique ; Pompe osmotique ; Comprimé enrobé ; Vecteur médicament ; Libération ; Principe actif ; In vitro ; Cellulose dérivé ; Ethylène oxyde polymère ; Forme libération lente ; Masse moléculaire ; Potassium Chlore ; Amidon riz ; Dihydropyridine dérivé ;

Mots-clés espagnols / Spanish Keywords

Nifedipino ; Antagonista calcio ; Antihipertensivo ; Tecnología farmacéutica ; Forma farmacéutica ; Bomba osmótica ; Tableta cubierta ; Vector medicamento ; Liberación ; Principio activo ; In vitro ; Celulosa derivado ; Etileno óxido polímero ; Forma liberación lente ; Masa molecular ; Potasio Cloro ; Almidón arroz ; Dihidropiridine derivado ;

Localisation / Location

INIST-CNRS, Cote INIST : 20704, 35400008874266.0170