Development of Extended-Release Oral Dosage Forms of Salbutamol Sulfate Using the Hot-Melt Extrusion Manufacturing Technique.

OBJECTIVE: To fabricate and characterize extrudable polymeric matrices using a combination of ethyl cellulose (EC) and two different grades of hydroxypropyl cellulose (HPC) that can provide sustained drug release of the model drug salbutamol sulfate. SIGNIFICANCE: Implementation of the Hot-Melt Extrusion (HME) technique in the fabrication of polymeric combinations that will provide ready-to-use matrices for sustained release dosage forms. METHODS: Two formulation groups were developed; each with six formulations. The first group contained EC: HPC 370,000 ratios ranging from 55.52:13.8% to 6.9:62.46%, respectively. The second group contained EC: HPC 80,000 ranging from 59.4:10% to 9.4:60%, respectively. The release profiles were determined via in vitro studies to assess the ability of matrices to prolong salbutamol release. Solid-state characterization was also performed on the raw material and representative extrudates formulations using differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD) and polarized light microscopy (PLM). RESULTS: The first group formulations exhibited prolonged drug release profiles that accelerated progressively as the level of HPC 370,000 increased. In contrast, the second group formulations exhibited a noticeably faster release, demonstrating that HPC 80,000 can effectively accelerate drug release through enhanced matrix erosion and water penetration. DSC and XRPD revealed that the model drug remained in its stable crystalline state even after thermal processing via HME. PLM further confirmed drug crystallinity within the extrudates. CONCLUSION: EC-HPC matrices successfully demonstrated the feasibility of using HME to prepare sustained-release matrices for salbutamol sulfate with the ability to tune drug release by varying polymer grade and ratio.