Increased bioavailability of propranolol in rats by retaining thermally gelling liquid suppositories in the rectum

Mucoadhesive liquid suppositories were prepared by adding mucoadhesive polymers (0.6%) to a formulation of thermally gelling suppositories that contained poloxamer 407 (15%), poloxamer 188 (15%) and propranolol HCl (2%). Hydroxypropylcellulose (HPC), polyvinylpyrrolidone (PVP), carbopol, polycarboph...

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Bibliographic Details
Published in:Journal of controlled release 1999-05, Vol.59 (2), p.163-172
Main Authors: Ryu, Jei-Man, Chung, Suk-Jae, Lee, Min-Hwa, Kim, Chong-Kook, Chang-Koo Shim
Format: Article
Language:English
Subjects:
Adhesiveness
Adrenergic beta-Antagonists - pharmacokinetics
Animals
Antiarythmic agents
Bioavailability
Biological and medical sciences
Biological Availability
Cardiovascular system
Chromatography, High Pressure Liquid
Gelation
Gels - chemistry
General pharmacology
In Vitro Techniques
Irritants - pharmacology
Liquid suppositories
Male
Medical sciences
Mucoadhesion
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Poloxamer
Poloxamer - chemistry
Polycarbophil
Polymers - chemistry
Propranolol
Propranolol - pharmacokinetics
Rats
Rats, Sprague-Dawley
Rectum - physiology
Sodium alginate
Suppositories - pharmacokinetics
Temperature
Thermally gelling
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Summary:Mucoadhesive liquid suppositories were prepared by adding mucoadhesive polymers (0.6%) to a formulation of thermally gelling suppositories that contained poloxamer 407 (15%), poloxamer 188 (15%) and propranolol HCl (2%). Hydroxypropylcellulose (HPC), polyvinylpyrrolidone (PVP), carbopol, polycarbophil and sodium alginate were examined as mucoadhesive polymers. The characteristics of the suppositories differed depending on the choice of mucoadhesive polymer. For example, the gelation temperature was between 30 and 36°C, the mucoadhesive force was between 430 and 5800 dyne/cm 2, the apparent first-order release rate constant in phosphate buffer, pH 6.8, was between 0.399 and 0.271 h −1, the migration distance of the suppository in the rectum 4 h after administration was between 1 and 5 cm, and the bioavailability of propranolol was between 60.9 and 84.7%. Rectal bioavailability increased as the mucoadhesive force increased ( r=0.984, p
ISSN:0168-3659
1873-4995
DOI:10.1016/S0168-3659(98)00189-8