title: Substitution of didanosine sachets by chewable tablets: a pharmacokinetic study in patients with AIDS.
abstract: We have conducted a pharmacokinetic study of didanosine (ddI), formulated in sachets and in tablets, in patients with acquired immune deficiency syndrome (AIDS). Fifteen subjects received 250 or 167 mg of ddI twice daily as the sachet formulation and used this for at least 1 month. Subsequently, the patients were converted to receive ddI chewable/dispersible tablets (250-mg sachets to 200-mg tablets; 167-mg sachets to 125-mg tablets). Four subjects withdrew because of clinical deterioration or adverse effects. Serial blood samples were collected for pharmacokinetic monitoring during the use of the sachets and after 1 month of use of the tablets. No statistically significant differences were found in the maximum plasma concentration (Cmax), the time to reach Cmax (tmax), the area under the plasma concentration-time curve (AUC), or the terminal elimination half-life (t1/2) between the two formulations. Patients who received low-dose ddI (sachets, 167 mg; tablets, 125 mg) displayed lower plasma concentrations than did the patients receiving high-dose ddI (sachets, 250 mg; tablets, 200 mg), despite an equal weight-normalized dose of ddI in these two groups.
authors.affiliation: Department of Pharmacy, Slotervaart Hospital, Amsterdam, The Netherlands.
authors.forename: D
authors.initials: D
authors.lastname: Burger
authors.forename: P
authors.initials: P
authors.lastname: Meenhorst
authors.forename: J
authors.initials: J
authors.lastname: Mulder
authors.forename: J
authors.initials: J
authors.lastname: Henrichs
authors.forename: J
authors.initials: J
authors.lastname: Frissen
authors.forename: F
authors.initials: F
authors.lastname: Kroon
authors.forename: C
authors.initials: C
authors.lastname: ten Napel
authors.forename: K
authors.initials: K
authors.lastname: Koks
authors.forename: A
authors.initials: A
authors.lastname: Bult
authors.forename: J
authors.initials: J
authors.lastname: Beijnen
mesh_terms: D000042:Absorption; D000163:Acquired Immunodeficiency Syndrome / Q000188:drug therapy / Q000378:metabolism*; D000284:Administration, Oral; D000328:Adult; D000998:Antiviral Agents / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use; D001682:Biological Availability; D016049:Didanosine / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use; D005260:Female; D006207:Half-Life; D006801:Humans; D008297:Male; D008875:Middle Aged; D011208:Powders; D013607:Tablets; D013810:Therapeutic Equivalency
chemical_list: D000998:Antiviral Agents; D011208:Powders; D013607:Tablets; D016049:Didanosine