Abstract
Formulation and In-Vitro, Ex-Vivo, and In-Vivo Evaluation of Mucoadhesive Buccal Tablets Containing Labetalol Hydrochloride for Enhancement of Systemic Bioavailability
Highlights
Delivery of drugs in the oral cavity can be classified according to site of application into local, buccal and sublingual delivery
The buccal route is preferred over the oral route for drugs that suffer from acid decomposition in the stomach or that are highly http://aprh.journals.ekb.eg/ 15
Labetalol hydrochloride was kindly received from Al Debeiky Pharma (DBK) Pharmaceutical Co
Summary
Delivery of drugs in the oral cavity can be classified according to site of application into local, buccal and sublingual delivery. The drug is nearly completely absorbed from the gastrointestinal (GI) tract, but in the liver and/or GI mucosa, the drug undergoes significant first-pass metabolism It is characterized by a short biological halflife of [2,3,4,5] hours and it undergoes significant presystemic metabolism resulting in low bioavailability 25% 12. It has a low molecular weight (364.9 g/mol) and a favorable partition coefficient (7.08) 11 so it is small and lipophilic enough to pass through buccal mucosa. This study aimed to formulate and characterize mucoadhesive buccal tablets containing labetalol hydrochloride using different combinations of mucoadhesive polymers in order to enhance the systemic bioavailability. The characterization processes included physical, in-vitro, ex-vivo, and in-vivo evaluation
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