Design and evaluation of sustained-release and buccal adhesive propranolol hydrochloride tablets

Taylan B., Capan Y., Guven O., Kes S., Hincal A.

JOURNAL OF CONTROLLED RELEASE, cilt.38, sa.1, ss.11-20, 1996 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 38 Sayı: 1
  • Basım Tarihi: 1996
  • Doi Numarası: 10.1016/0168-3659(95)00094-1
  • Dergi Adı: JOURNAL OF CONTROLLED RELEASE
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.11-20
  • Anahtar Kelimeler: propranolol, buccal adhesive, sustained-release tablet, interpolymer complex, human clinical study, LONG-ACTING PROPRANOLOL, ABSORPTION, BIOAVAILABILITY, PLASMA, BIOADHESIVE
  • Lokman Hekim Üniversitesi Adresli: Hayır

Özet

The release of propranolol hydrochloride incorporated into sustained-release and buccal adhesive tablets was studied in vitro. The formulation containing 20% hydroxypropyl methylcellulose (HPMC) yielded good sustained-release matrix tablets. Buccal adhesive controlled-release tablets were prepared by compression of HPMC with polycarbophil (PAA), which served as the bioactive adhesive compound. The release behaviour of buccal adhesive tablets was found to be non-Fickian. The adhesion force was significantly affected by the mixing ratio of HPMC and PAA in the tablet and the weakest adhesion force was observed at the ratio of 1:1 (HPMC:PAA). Interpolymer complex formation was confirmed between HPMC and PAA in acidic medium by turbidity, viscosity and FT-IR measurements. The kinetics of sustained-release and buccal adhesive tablets of propranolol were examined in nine healthy volunteers. Conventional propranolol (Dideral(R)) was also studied for comparison purposes. As compared to conventional propranolol (40 mg), a single dose of 20% HPMC (160 mg) produced a smoother plasma level profile, with lower and delayed peak times. Dose corrected AUG(0-8) values were greater after Dideral(R) than after 20% HPMC (168.7 +/- 80.3 vs 97.3 +/- 36.1 ng h ml(-1) p < 0.05). The buccal delivery of propranolol caused ulceration and serious irritation that took weeks to heal, There was no significant difference (p > 0.05) in the AUG(0-4) values between 20% HPMC and buccal adhesive tablets.