Formulation development of allopurinol suppositories and injectables.
Allopurinol was formulated into injectable and suppository dosage forms. The injectable formulation was prepared by dissolving allopurinol in a cosolvent system consisting of dimethyl sulfoxide (DMSO) and propylene glycol (v/v = 50/50). The stability of allopurinol in the cosolvent system was studied under accelerated storage conditions, and results indicate first-order degradation kinetics with an activation energy of 24.3 kcal/mol. The development of suppository dosage forms was performed by formulating allopurinol with polyethylene glycol (PEG) mixtures of different molecular weights. In vitro release profiles of suppositories formulated with different polyethylene bases were obtained in the pH 7.4 buffer solution using the USP 23 paddle method at 100 rpm. Results indicate that the release rate of the suppository formulations containing PEG 1500/PEG 4000 at the ratio (w/w) of 2.5/10 to 10/2.5 appeared to be similar. However, the addition of sodium lauryl sulfate in the suppository decreased the release rate of allopurinol significantly. A future study to establish in vitro/in vivo correlation (iv/ivc) is suggested.
Lee
D K
DK
Department of Pharmacy, Kaoshiung Veterans General Hospital, Kaoshiung, Taiwan, R.O.C.
Wang
D P
DP
D000493:Allopurinol / Q000008:administration & dosage* / Q000737:chemistry; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000737:chemistry; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002851:Chromatography, High Pressure Liquid; D004339:Drug Compounding; D004355:Drug Stability; D007267:Injections; D019999:Pharmaceutical Solutions; D012997:Solvents; D013488:Suppositories; D013696:Temperature
D000964:Antimetabolites, Antineoplastic; D019999:Pharmaceutical Solutions; D012997:Solvents; D013488:Suppositories; D000493:Allopurinol