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Formulation development of allopurinol suppositories and injectables.
1Department of Pharmacy, Kaoshiung Veterans General Hospital, Kaoshiung, Taiwan, R.O.C.
Drug Development and Industrial Pharmacy
|December 22, 1999
Summary
Injectable and suppository allopurinol formulations were developed. Allopurinol stability in a dimethyl sulfoxide and propylene glycol cosolvent system showed first-order degradation, while suppository release rates were influenced by polyethylene glycol ratios and sodium lauryl sulfate.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Formulation Development
Background:
- Allopurinol is a medication used to treat gout and hyperuricemia.
- Developing alternative dosage forms for allopurinol can improve patient compliance and therapeutic outcomes.
- Investigating the stability and release characteristics of novel allopurinol formulations is crucial for clinical application.
Purpose of the Study:
- To formulate and characterize injectable and suppository dosage forms of allopurinol.
- To assess the stability of allopurinol in a cosolvent system for injectable formulations.
- To evaluate the in vitro release profiles of allopurinol suppositories with varying polyethylene glycol bases.
Main Methods:
- Injectable formulation: Dissolving allopurinol in a 50/50 (v/v) dimethyl sulfoxide (DMSO) and propylene glycol cosolvent system.
- Stability study: Accelerated storage conditions to determine degradation kinetics and activation energy.
- Suppository formulation: Incorporating allopurinol into polyethylene glycol (PEG) mixtures of different molecular weights.
- In vitro release testing: USP 23 paddle method at 100 rpm in pH 7.4 buffer for suppositories.
Main Results:
- Allopurinol in the DMSO/propylene glycol cosolvent system exhibited first-order degradation kinetics with an activation energy of 24.3 kcal/mol.
- Suppository formulations with PEG 1500/PEG 4000 at weight ratios from 2.5/10 to 10/2.5 showed similar allopurinol release rates.
- The addition of sodium lauryl sulfate significantly reduced the release rate of allopurinol from suppositories.
Conclusions:
- Stable injectable and effective suppository formulations of allopurinol were successfully developed.
- The choice of polyethylene glycol base and excipients like sodium lauryl sulfate critically impacts allopurinol release from suppositories.
- Further studies are recommended to establish an in vitro/in vivo correlation for these novel allopurinol dosage forms.