In vivo study of sustained-release formulations containing amoxicillin and Gelucire 64/02

Application of Hot-Melt Coating Process for Designing a Lipid Based Controlled Release Drug Delivery System for Highly Aqueous Soluble Drugs

“…4) In addition to aqueous polymers, lipids have also been used as coating materials to develop sustained and/or controlled release drug delivery systems. [5][6][7][8][9] Lipids in general have been extensively studied for their use to deliver drug in controlled/sustained release manner starting from experimental use by Shear in 1936 to deliver a carcinogen from a cholesterol based implant to induce tumours in mice 10) with many subsequent reports for its use to deliver therapeutic 11,12) and prophylactic substances. 13,14) While lipid based controlled release systems have been developed successfully for insoluble or slightly soluble drugs, development of similar system for highly aqueous soluble drugs still remains a challenging task; and due to the fact that lipids have specific physical properties and are distinctive from other commonly used excipients (like polymers), they are difficult to incorporate into formulation in quantities suitable for controlled/sustained release products.…”

“…13,14) While lipid based controlled release systems have been developed successfully for insoluble or slightly soluble drugs, development of similar system for highly aqueous soluble drugs still remains a challenging task; and due to the fact that lipids have specific physical properties and are distinctive from other commonly used excipients (like polymers), they are difficult to incorporate into formulation in quantities suitable for controlled/sustained release products. As a result, the pharmaceutical scientists have reported different ways of incorporating lipids into oral controlled/sustained release formulations like HMCP, [5][6][7][8] organic solvent coating process, 9) physical mixtures and solid dispersions of drugs and lipids, [15][16][17] melt granulation, 18,19) and lubrication. 20) When compared with HMCP, these other approaches require significantly more lipid material for similar sustained release profile, which can be a limiting factor for high dose drugs.…”