Transbuccal tablets of carbamazepine: formulation, release and absorption pattern

Giannola Li; De Caro V; Giandalia G; Siragusa Mg; D'Angelo M; Lo Muzio L; Campisi G

Risultato della ricerca: Article

23 Citazioni (Scopus)

Abstract

Tranbsuccal drug administration is an attractive method, as it has several advantages especially with respect to peroral delivery. Here we report: i) the aptitude of carbamazepine (CBZ) to penetrate porcine buccal mucosa and reconstituted human oral (RHO) epithelium; ii) three different tablet formulations for transbuccal administration; iii) the drug release rate from tablets. CBZ permeation through the buccal mucosa was investigated by using two different bi-compartmental open models: Franz cells for porcine buccal mucosa and Transwell diffusion cells system for RHO epithelium. Results, expressed as drug flux (Js) and permeability coefficients (Kp), indicated that CBZ well penetrates the membrane and arrives in the acceptor phase. Js and Kp resulted 7x10(-2) mg/cm2h and 0.23 cm/h for in vitro experiments and 1.81 x 10(-2) mg/cm2h and 4.57 x 10(-2) cm/h for ex vivo experiments. The flux is extensively affected by the membrane thickness. The CBZ release from three different formulations of tablets, prepared with loaded microspheres, loaded matrices, and conventional compressed physical mixture of components was studied. Using the new formulated "non-conventional" tablets prolonged drug release was obtained. Loaded matrix tablets discharged CBZ faster than microsphere tablets (17% and 12% in about 2.5 h respectively). Results indicate the possibility of administering CBZ on buccal mucosa.
Lingua originaleEnglish
pagine (da-a)21-31
Numero di pagine11
RivistaInternational Journal of Immunopathology and Pharmacology
Volume18
Stato di pubblicazionePublished - 2005

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Carbamazepine
Tablets
Mouth Mucosa
Microspheres
Swine
Epithelium
Membranes
Pharmaceutical Preparations
Permeability

All Science Journal Classification (ASJC) codes

  • Immunology and Allergy
  • Pharmacology
  • Immunology

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Giannola Li; De Caro V; Giandalia G; Siragusa Mg; D'Angelo M; Lo Muzio L; Campisi G (2005). Transbuccal tablets of carbamazepine: formulation, release and absorption pattern. International Journal of Immunopathology and Pharmacology, 18, 21-31.

Transbuccal tablets of carbamazepine: formulation, release and absorption pattern. / Giannola Li; De Caro V; Giandalia G; Siragusa Mg; D'Angelo M; Lo Muzio L; Campisi G.

In: International Journal of Immunopathology and Pharmacology, Vol. 18, 2005, pag. 21-31.

Risultato della ricerca: Article

Giannola Li; De Caro V; Giandalia G; Siragusa Mg; D'Angelo M; Lo Muzio L; Campisi G 2005, 'Transbuccal tablets of carbamazepine: formulation, release and absorption pattern', International Journal of Immunopathology and Pharmacology, vol. 18, pagg. 21-31.
Giannola Li; De Caro V; Giandalia G; Siragusa Mg; D'Angelo M; Lo Muzio L; Campisi G. Transbuccal tablets of carbamazepine: formulation, release and absorption pattern. International Journal of Immunopathology and Pharmacology. 2005;18:21-31.
Giannola Li; De Caro V; Giandalia G; Siragusa Mg; D'Angelo M; Lo Muzio L; Campisi G. / Transbuccal tablets of carbamazepine: formulation, release and absorption pattern. In: International Journal of Immunopathology and Pharmacology. 2005 ; Vol. 18. pagg. 21-31.
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abstract = "Tranbsuccal drug administration is an attractive method, as it has several advantages especially with respect to peroral delivery. Here we report: i) the aptitude of carbamazepine (CBZ) to penetrate porcine buccal mucosa and reconstituted human oral (RHO) epithelium; ii) three different tablet formulations for transbuccal administration; iii) the drug release rate from tablets. CBZ permeation through the buccal mucosa was investigated by using two different bi-compartmental open models: Franz cells for porcine buccal mucosa and Transwell diffusion cells system for RHO epithelium. Results, expressed as drug flux (Js) and permeability coefficients (Kp), indicated that CBZ well penetrates the membrane and arrives in the acceptor phase. Js and Kp resulted 7x10(-2) mg/cm2h and 0.23 cm/h for in vitro experiments and 1.81 x 10(-2) mg/cm2h and 4.57 x 10(-2) cm/h for ex vivo experiments. The flux is extensively affected by the membrane thickness. The CBZ release from three different formulations of tablets, prepared with loaded microspheres, loaded matrices, and conventional compressed physical mixture of components was studied. Using the new formulated {"}non-conventional{"} tablets prolonged drug release was obtained. Loaded matrix tablets discharged CBZ faster than microsphere tablets (17{\%} and 12{\%} in about 2.5 h respectively). Results indicate the possibility of administering CBZ on buccal mucosa.",
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AU - Giannola Li; De Caro V; Giandalia G; Siragusa Mg; D'Angelo M; Lo Muzio L; Campisi G

AU - Giannola, Libero Italo

AU - De Caro, Viviana

AU - Campisi, Giuseppina

AU - Giandalia, Giulia

AU - Siragusa, Maria Gabriella

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AB - Tranbsuccal drug administration is an attractive method, as it has several advantages especially with respect to peroral delivery. Here we report: i) the aptitude of carbamazepine (CBZ) to penetrate porcine buccal mucosa and reconstituted human oral (RHO) epithelium; ii) three different tablet formulations for transbuccal administration; iii) the drug release rate from tablets. CBZ permeation through the buccal mucosa was investigated by using two different bi-compartmental open models: Franz cells for porcine buccal mucosa and Transwell diffusion cells system for RHO epithelium. Results, expressed as drug flux (Js) and permeability coefficients (Kp), indicated that CBZ well penetrates the membrane and arrives in the acceptor phase. Js and Kp resulted 7x10(-2) mg/cm2h and 0.23 cm/h for in vitro experiments and 1.81 x 10(-2) mg/cm2h and 4.57 x 10(-2) cm/h for ex vivo experiments. The flux is extensively affected by the membrane thickness. The CBZ release from three different formulations of tablets, prepared with loaded microspheres, loaded matrices, and conventional compressed physical mixture of components was studied. Using the new formulated "non-conventional" tablets prolonged drug release was obtained. Loaded matrix tablets discharged CBZ faster than microsphere tablets (17% and 12% in about 2.5 h respectively). Results indicate the possibility of administering CBZ on buccal mucosa.

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