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Issue 22: June 2011

Greetings!

In this newsletter, we introduce application of F-MELT for manufacturing of oral disintegrating tablets
(ODTs) of Simvastatin, a poorly water soluble drug. F-MELT is a co-spray dried excipient system
containing 5 pharmaceutical excipients such as carbohydrates, disintegrants and inorganic ingredients.
F-MELT family consists of three grades: F-MELT Type M for pharmaceutical applications,
F-MELT Type C for pharmaceutical and nutraceutical applications and F-MELT F1 for dietary
supplement as well as functional food applications. This newsletter report manufacture of high quality
Simvastatin ODT with F-MELT Type M.

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 -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-MELT 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.

Table 1. Simvastatin ODT formulation with F-MELT Type M


Formulation
Simvastatin (mg) 5.0
F-MELT TypeM (mg) 194.2
Magnesium stearate (mg) 0.8
Total (mg) 200
Tablet condition: 8 mm, 200 mg/Tablet, Rotary tabletting machine
15 rpm

Table 2. Stability Test of Simvastatin ODTs


Tablet characteristics Initial 25C, 75% RH, Open, 1 week
Tablet hardness (N) 48.0 37.2
Compression force (kgf) 375-395 -
Coefficient of variation (%, n=6) 1.1
ODT disintegration time ODT-101* (s) 16.48 14.05
Pharmacopoeia disintegration time (s) 13.09 10.42
Mouth feel Good -
*Equipment to measure ODTs (Toyama Sangyo Co., Ltd)
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.

Conclusion
High quality Simvastatin ODTs with good mouth feel could be produced by simple mixing with F-MELT
Type M and lubricant followed by direct compression.

F-MELT 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.

2011 - Fuji Chemical Industry Co., Ltd. - All Rights Reserved


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