At CPhI 2011, a pharmaceutical networking event that was held October 25 to 27 in Frankfurt, Cargill Pharma announced pilot study results that reinforce the superior performance of Zerose™ erythritol as an orally dispersible tablet (ODT) excipient for unpalatable active ingredients.
“The results we have so far from our tests with L-ascorbic acid (Vitamin C) as the active, Zerose™ erythritol as the excipient, and C*PharmIsoMaltidex isomalt as the binder, are striking”, said Liesbeth Meeus, Pharma & Personal Care Application Centre Leader for Cargill Pharma.
The dilution potential of Zerose™ erythritol is much higher when compared to a widely used polyol under the same production conditions. With an addition of 10% to 50% of active ingredient no significant loss of tablet quality is seen. For tablets made using the other widely used polyols (in ODTs) on the other hand, a decrease of more than 75% in hardness is seen for a formulation containing 50% of active ingredient.
In tablets containing 10% Vitamin C and comparing Zerose™ erythritol to the other widely used polyol, significant variations in performance have been noted. The disintegration profile (even without the addition of a super disintegrant) is much better for Zerose™ erythritol tablets than for same formulations with the alternative excipient. As disintegration times are one of the key factors in ODTs, this can be noted as an extra benefit.
“When it comes to taste-masking, our internal taste panel was unanimous in its approval of the tablets produced containing Zerose™ erythritol”, says Liesbeth. “The tablets made with Zerose™ erythritol compared to those with the alternative polyol were received much more positively by our participants. Zerose™ erythritol has well-documented taste-masking properties relating to unpalatable compounds in food. This pilot study confirmed that the established taste-masking properties of Zerose™ erythritol as a food ingredient are just as effective with unpalatable pharma actives.
Zerose™ erythritol is zero-calorie, non-hygroscopic, non-cariogenic, has a high-level of digestive tolerance – and as this pilot study demonstrates, has unique taste-making properties. Children, older people and those on the move are particular growth areas for ODTs. Over the last three years Cargill Pharma has been developing Zerose™ erythritol as a unique pharma excipient for such tablets, announcing a new patent application for the use of Zerose™ erythritol in ODTs at last year’s CPhI.
“Our studies into the performance of Zerose™ erythritol focused on taste-masking of unpalatable actives, dilution potential and disintegration performance have been conducted to establish clear and valid comparisons with the most widely used polyol excipient for ODTs”, added Liesbeth. Cargill is now undertaking a similar pilot study with paracetamol, and will announce these results shortly.
Liesbeth Meeus concludes: “This year’s CPhI demonstrates the research and depth of application expertise which lies behind our extensive product portfolio. All of this supports Cargill’s continuing commitment to being one of the most trusted, dedicated and experienced pharma ingredient suppliers.”
Cargill Pharma’s offering is backed by international regulatory insight and a dedicated team of pharma innovators. Cargill has the capability to exploit both the distinctive capabilities of its individual ingredients and the potential synergies arising from combining ingredients in integrated systems, to meet a wider range of customer and application requirements.
Cargill is an international producer and marketer of food, agricultural, financial and industrial products and services. Founded in 1865, the privately held company employs 138,000 people in 63 countries. Cargill helps customers succeed through collaboration and innovation, and is committed to applying its global knowledge and experience to help meet economic, environmental and social challenges wherever it does business. For more information, visit www.cargill.com.
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