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Development and evaluation of artemether taste masked rapid disintegrating tablets with improved dissolution using
Punit P Shah1, Rajashree C Mashru
1Center of Relevance and Excellence in NDDS, Pharmacy Department, The M. S. University of Baroda, G H Patel building, Donor's Plaza, Fatehgunj, Vadodara, Gujarat 390002, India. punitpshah@gmail.com
AAPS Pharmscitech
|April 24, 2008
Summary
This study successfully masked the bitter taste of artemether (ARM) using solid dispersion with glycyrrhizinate (GLY). The resulting rapid-disintegrating tablets (RDTs) offered improved dissolution and complete taste masking, enhancing patient compliance.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
Background:
- Artemether (ARM) possesses an intensely bitter taste, posing challenges for oral administration and patient compliance.
- Rapid-disintegrating tablets (RDTs) offer an alternative dosage form for improved drug delivery and patient acceptance.
Purpose of the Study:
- To mask the bitter taste of artemether (ARM).
- To formulate rapid-disintegrating tablets (RDTs) of taste-masked artemether.
- To evaluate the physicochemical properties, taste masking efficacy, and in vitro drug release of the formulated RDTs.
Main Methods:
- Taste masking was achieved through solid dispersion of ARM with mono amino glycyrrhyzinate pentahydrate (GLY) using the solvent evaporation method.
- The optimized 1:1M solid dispersion was characterized using FTIR, DSC, and XRPD.
- RDTs were formulated and evaluated for weight variation, disintegration time, hardness, friability, and in vitro drug release at pH 1.2 and 6.8.
- Taste masking was assessed using the mini-column method and gustatory sensation tests with human volunteers.
Main Results:
- XRPD indicated amorphization of ARM within the GLY solid dispersion, while FTIR and DSC showed no significant drug-carrier interactions.
- The RDT formulated with solid dispersion (RDT3) exhibited rapid disintegration (within 28 seconds) and complete taste masking.
- RDT3 demonstrated a superior dissolution profile at both pH 1.2 and 6.8 compared to RDTs prepared from pure ARM (RDT5).
- Human volunteer taste evaluation rated RDT3 as tasteless (score 0), while RDT5 received a score of 3.
Conclusions:
- Solid dispersion of artemether with glycyrrhizinate effectively masks its bitter taste.
- The developed rapid-disintegrating tablets (RDTs) provide a promising dosage form with enhanced dissolution and improved taste acceptability.
- This formulation strategy can significantly improve patient compliance for artemether therapy.
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