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Palatable reconstitutable dry suspension of artemether for flexible pediatric dosing using cyclodextrin inclusion
Punit P Shah1, Rajashree C Mashru
1Pharmacy Department, Center of Relevance and Excellence in NDDS, The Maharaja Sayajirao University of Baroda, Fatehgunj, Vadodara, Gujarat, India. punitpshah@gmail.com
Pharmaceutical Development and Technology
|June 22, 2012
Summary
This study developed a stable, palatable artemether (ARM) pediatric formulation using beta-cyclodextrin (CD) inclusion complexation. The optimized formulation effectively masked bitterness and improved drug release.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Formulation Development
Background:
- Artemether (ARM) is a crucial antimalarial drug, but its bitter taste poses challenges for pediatric adherence.
- Improving the palatability and bioavailability of ARM is essential for effective pediatric treatment.
Purpose of the Study:
- To investigate the inclusion complexation of artemether with beta-cyclodextrin (CD) to mask bitterness.
- To enhance drug release and develop a stable, palatable pediatric formulation of ARM.
- To evaluate the physicochemical properties and in vitro performance of the developed formulation.
Main Methods:
- Inclusion complexation using physical mixture and kneaded systems.
- Characterization via FTIR, DSC, XRPD, and SEM to confirm complex formation.
- Evaluation of reconstitutable dry suspension properties (flowability, redispersibility, pH).
- In vitro drug release studies at pH 1.2 and 6.8.
- Gustatory sensation tests for bitterness evaluation.
Main Results:
- FTIR, DSC, and XRPD confirmed successful inclusion complexation between ARM and CD.
- Both physical mixture and kneaded systems showed improved in vitro drug release.
- The optimized 1:20M physical mixture resulted in a reconstitutable dry suspension (DS4) with complete bitter taste masking.
- DS4 exhibited good flowability and redispersibility, with a taste score of 0 in human volunteers.
Conclusions:
- Beta-cyclodextrin inclusion complexation is an effective strategy for masking artemether's bitterness.
- The developed reconstitutable dry suspension provides a stable, palatable, and effective dosage form for pediatric use.
- This formulation offers improved drug release and adherence for pediatric malaria treatment.
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