Didanosine

Selection and Characterization of Suitable Lipid Excipients for use in the Manufacture of Didanosine-Loaded Solid Lipid Nanoparticles and Nanostructured Lipid Carriers

“…1 Didanosine (DDI) is a hydrophilic nucleotide reverse transcriptase inhibitor approved by the US Food and Drug Administration for the management of advanced HIV infection in children. 2,3 DDI may be administered alone or in combination with other ARV agents as an important component of triple combination HIV treatment regimens. 4,5 A major hindrance to the use of DDI is the susceptibility of the molecule to hydrolytic cleavage in the acidic environment of the stomach, following oral administration with conventional formulations.…”

“…4,5 A major hindrance to the use of DDI is the susceptibility of the molecule to hydrolytic cleavage in the acidic environment of the stomach, following oral administration with conventional formulations. 3,6 In reality, DDI has a t 90 of less than 2 min in a solution of pH 3.0 at 37 • C. 3,7 Consequently, there is a reduction in the bioavailability and in vivo activity of the molecule. 3,6,8 In order to improve the acid stability and bioavailability of DDI, the drug is usually formulated as buffered chewable or dispersible tablets in addition to buffered or nonbuffered pediatric powders for reconstitution as an oral solution.…”

“…3,6 In reality, DDI has a t 90 of less than 2 min in a solution of pH 3.0 at 37 • C. 3,7 Consequently, there is a reduction in the bioavailability and in vivo activity of the molecule. 3,6,8 In order to improve the acid stability and bioavailability of DDI, the drug is usually formulated as buffered chewable or dispersible tablets in addition to buffered or nonbuffered pediatric powders for reconstitution as an oral solution. 3,6,8,9 The nonbuffered pediatric powders are usually mixed with antacids following reconstitution, prior to oral administration to pediatric patients.…”

Method development and validation for the analysis of didanosine using micellar electrokinetic capillary chromatography

“…Didanosine (2',3'-dideoxyinosine; ddI), a synthetic purine NRTI, is the second antiretroviral agent approved for the treatment of HIV infection [1]. Like all NRTIs, it is an inactive prodrug [2].…”

“…It can also be prepared enzymatically by the deamination of 2',3'-dideoxyadenosine [1]. The drug has a pK a of 9.12 6 0.02 and is acid labile [4,5].…”