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Issue 22: June 2011
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Oral Disintegrating Tablets of Simvastatin
with F-MELTŪ
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Greetings!
In this newsletter, we introduce application of F-MELTŪ for manufacturing of oral disintegrating tablets (ODTs) of Simvastatin, a poorly water soluble drug. F-MELTŪ is a co-spray dried excipient system containing 5 pharmaceutical excipients such as carbohydrates, disintegrants and inorganic ingredients. F-MELTŪ family consists of three grades: F-MELTŪ Type M for pharmaceutical applications, F-MELTŪ Type C for pharmaceutical and nutraceutical applications and F-MELTŪ F1 for dietary supplement as well as functional food applications. This newsletter report manufacture of high quality Simvastatin ODT with F-MELTŪ Type M.
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Simvastatin, 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors (HMG-CoA reductase inhibitor) reduces cholesterol synthesis in the liver and lower intracellular cholesterol concentrations. Simvastatin is adsorbed from the gastrointestinal tract and hydrolyzed to its active β-hydroxy acid metabolite. Commercial oral Simvastatin tablets provide doses of 5 mg up to 80 mg of which not more than 7% could reach the circulation as active form. F-MELTŪ offers a new approach to produce oral Simvastatin tablets as ODTs in simple way by direct compression. This drug delivery option can improve the life cycle management of original manufacturers and could stave off competition from generic manufacturers. Simvastatin ODTs are also more convenient and friendly to users, especially children and elderly patients.
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 Table 1. Simvastatin ODT formulation with F-MELTŪ Type M |
Formulation
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Simvastatin (mg)
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5.0
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F-MELTŪ TypeM (mg)
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194.2
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Magnesium stearate (mg)
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0.8
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Total (mg)
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200
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Tablet condition: Ф 8 mm, 200 mg/Tablet, Rotary tabletting machine 15 rpm |
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Table 2. Stability Test of Simvastatin ODTs
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Tablet characteristics
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Initial
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25°C, 75% RH, Open, 1 week
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Tablet hardness (N)
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48.0
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37.2
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Compression force (kgf)
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375-395
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-
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Coefficient of variation (%, n=6)
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1.1
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ODT disintegration time ODT-101* (s)
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16.48
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14.05
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Pharmacopoeia disintegration time (s)
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13.09
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10.42
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Mouth feel
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Good
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-
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*Equipment to measure ODTs (Toyama Sangyo Co., Ltd)
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Figure1. Simvastatin Tablet Dissolution Test
Dissolution test condition: test solution, 900 mL, 0.3% polysorbate 80 37° C, paddle speed 50 rpm, detection at UV 239 nm.
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Conclusion
High quality Simvastatin ODTs with good mouth feel could be produced by simple mixing with F-MELTŪ Type M and lubricant followed by direct compression.
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F-MELTŪ is a trademark or registered trademark of Fuji Chemical Industry Co., Ltd in Japan, United States of America, Europe and/or other countries.
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The information found in this publication is presented in good faith with no guarantee or obligation as to accuracy and no assumption of liability. Users should make their own tests to determine the suitability of these products for their own particular purposes. However, because of numerous factors affecting results, Fuji Chemical Industry makes no warranty of any kind, express or implied, including those of merchantability and fitness for particular purpose other than the material conforms to its applicable current standard specifications. Statements concerning the use of the products or formulations described herein are not to be construed as recommending the infringement of any patent and seller assumes no liability for the infringement arising out of such use. | |
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 Ū2011 - Fuji Chemical Industry Co., Ltd. - All Rights Reserved
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