(Current Challenges and Updates in Pharmacy Education and Research)

Formulation variables effect on gelation temperature of Nefopam hydrochloride intranasal in situ gel

Not scheduled

20m

كلية الصيدلة

Live presentation Conference Track Four

Speaker

Mr Ammar Alabdly (University of Baghdad / College of Pharmacy)

Description

Abstract
Nefopam (N.F.) HCl is a non-narcotic centrally-acting, non-opioid benzoxazocine analgesic to relieve acute and chronic pain. It exhibits low bioavailability (about 36%) due to its first-pass degradation in the liver and shows several common side effects related to peripheral action of N.F. HCl, such anticholinergic side effects include urinary retention, dry mouth, and nausea.
Intranasal administration has been used as a new route for targeting active brain sites and enhancing the bioavailability of N.F. HCl bypassing hepatic metabolism. In order to create an optimal intranasal formula, Preformulation studies were executed on N.F. HCl and excipients to be used as an in situ gel system.
Preformulation studies include: Identification tests are carried out to ensure the purity of materials ( drug and polymers), and Solubility study focusing on N.F. HCl solubility in Simulated nasal fluid, compatibility studies with the in situ gel polymers (FTIR), and an initial screening test on the preparation of the best combination of polymers for in situ gel administration of N.F. HCl.
In situ gel of N.F. HCl was prepared by the cold method using different concentrations of Poloxamer 407 as thermosensitive polymer, Poloxamer 188 as gelling temperature modifier, and HPMC K4M, Carbapol 934, Hyaluronic acid, and Methylcellulose as a mucoadhesive polymer.
The results show that identification tests are superimposed with references, solubility study shows that N.F. HCl is suitable to be administered intranasally; Compatability studies reveal incompatibility of Nefopam HCl with HPMC K4M and Carbapol 934; meanwhile, no interaction with Methylcellulose and Hyaluronic acid.
In conclusion, the obtained results revealed the incredible ability of the produced N.F. HCl intranasal in situ gel is intended to enhance drug bioavailability bypassing the metabolizing effect of the liver that N.F. HCl is facing when given orally.