Naloxone Base Formulation for Rapid Sublingual Bioavailability

The patent changes the physical-chemical parameters of naloxone by converting it from hydrochloride salt form to base form, and formulates it in non-aqueous solvents (oil-based vehicles) instead of aqueous solutions. This parameter change enables sublingual/buccal administration with rapid mucosal absorption, achieving reliable bioavailability (Cmax ≥ 1 ng/mL within 15 minutes) without being affected by nasal mucosa conditions or administration delays

The patent develops a simple, low-cost oral dosage form (lozenge, tablet, or gel) that can be administered immediately by bystanders without requiring trained medical personnel or specialized equipment. This disposable-like simplicity enables immediate administration at the scene of overdose, eliminating the 5-30 minute delay associated with professional administration of intranasal or intramuscular formulations

The patent employs inexpensive non-aqueous solvents (such as vegetable oils, mineral oils, or synthetic esters) and simple formulation techniques to create a low-cost naloxone base product. The manufacturing process avoids complex purification steps required for hydrochloride salt formulations, significantly reducing production costs while maintaining treatment effectiveness (Cmax ≥ 1 ng/mL within 15 minutes). This cost reduction makes the treatment accessible to resource-limited settings and enables broader distribution

By changing naloxone from hydrochloride salt form to base form and using non-aqueous solvents, the patent simplifies the formulation process and reduces manufacturing complexity. The base form requires less stringent purification and stability control compared to hydrochloride salt, lowering production costs while achieving equivalent or superior therapeutic effect through rapid sublingual/buccal absorption