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Capping Prevention - High dose tablets
Ceolus™ KG
Formulations with poorly compactible or high-dose APIs have the higher possibility of capping. Conventional MCC grades have insufficient compactibility, and the inherent capping can result in high tablet friability. By using a highly compactible MCC, the tablet's binding ability is increased and capping can be suppressed.
Challenges
Key words
Capping prevention - Large tablets
Ceolus™ KG
For formulations with poorly compactible APIs or high-dose APIs, achieving the target tablet hardness and tablet friability along with capping prevention is essential. Especially large tablets tend to have higher friability, which makes achieving targets difficult. However, by using a highly compactible MCC, the tablet's binding ability is increased, and the desired tablet hardness and tablet friability are realized and capping prevention is made possible.
Challenges
Key words
Capping prevention - Small tablets
Ceolus™ UF
For formulations with poorly compactible or high-dose APIs, when high compression force is used to achieve the desired tablet hardness, the possibility of capping becomes higher. By using a highly compactible MCC, the tablet's binding ability is increased and capping is suppressed even under high compression force. This enables the achievement of the desired tablet hardness.
Challenges
Key words
Capping prevention - Extra addition of MCC
Ceolus™ KG
In tableting poorly compactible granules, achieving the desired tablet hardness requires high compression force, which increases the possibility of capping. An extra addition of a small amount of highly compactible MCC increases the tablet's binding ability and capping can be suppressed.
Challenges
Key words
Improvement of tablet friability - High-dose tablets
Ceolus™ KG
High-dose formulations by direct compression limits space for excipients, and tableting issues such as capping, sticking and tablet friability are predicted. These issues could be solved with a small amount of a highly compactible MCC.
Challenges
Key words
Improvement of tablet friability - High-dose tablets
Ceolus™ KG
High-dose formulations by direct compression limits space for excipients, and tableting issues such as capping, sticking and tablet friability are predicted. These issues could be solved with a small amount of a highly compactible MCC.
Challenges
Key words
Improvement of tablet hardness - Roller compaction
Ceolus™ KG
Roller compaction is one of the methods used for formulations with moisture sensitive APIs, but sometimes slag granules have insufficient compactibility. An extra addition of a highly compactible MCC improves compactibility of roller compacted granules and reduces tablet friability.
Challenges
Key words
Improvement of tablet friability for film coating
Ceolus™ KG
Regarding tablet film coating, the airborne powder inside the coating machine can penetrate the film layer, potentially affecting tablet dissolution. By using a highly compactible MCC, the tablet's binding ability is increased and tablet friability is reduced, leading to reduced impact on the film layer and tablet dissolution.
Challenges
Key words
MUPS tablets
Ceolus™ KG
In the development of MUPS tablets, damage to film-coated granules, low compactibility of granules during tableting or API segregation would be major concerns. A highly compactible MCC Ceolus KG™ could solve the issue of granule damage and insufficient tablet hardness by reducing compression force in tableting. Also, granule segregation could be prevented by combination of a fibrous particle MCC Ceolus KG™ and a large particle MCC (e.g., PH-200).
Challenges
Key words
Tablet size reduction
Ceolus™ UF
Multivitamins and multiple-API-combination formulations often have large dose of active ingredients, and the choice of direct compression method can lead to large tablet size due to a large amount of binders required. By using a MCC with balance of compactibility and flowability at smaller additive amount compared to conventional MCCs, even with direct compression method, tablet size can be reduced while maintaining the same level of tablet weight variance and tablet friability as conventional MCCs.
Challenges
Key words
Tablet size reduction
Ceolus™ UF
Direct compression of poorly compactible and flowable APIs may require more excipients which can improve tablet properties, and those excipients increase tablet size. MCC with balance of compactibility and flowability requires less amount of excipients, and may contribute to tablet size reduction without hampering mixed powder flowability and tensile strength of tablets.
Challenges
Key words
Tablet size reduction
Ceolus™ UF
Direct compression of poorly compactible APIs at high dose may require more excipients which can improve tablet properties, and those excipients increase tablet size. MCC with balance of compactibility and flowability requires less amount of excipients, and may contribute to tablet size reduction without hampering mixed powder flowability and tensile strength of tablets.
Challenges
Key words
Orally disintegrating tablets (ODT)
Ceolus™ KG
ODT formulations require many challenging properties: rapid tablet disintegration, sufficient tablet hardness, low tablet friability and good mouth feel. A highly compactible MCC can reduce the MCC load while maintaining rapid tablet disintegration, sufficient tablet hardness and low tablet friability. The low MCC load also may potentially contribute to better mouth feel.
Challenges
Key words
Pressure-sensitive API
Ceolus™ KG
APIs are subjected to energies such as compression force or heat during tableting process, which leads to instability and increased number of related substances/compounds generation during storage. Using a highly compactible MCC with lower compression force lowers the energies to which APIs are exposed, which can supress API instability and improve storage stability.
Challenges
Key words
Oily-active-ingredients tablets
Ceolus™ KG
When oily active ingredients are absorbed into powders and tableted, in addition to securing sufficient tablet hardness and friability, oil bleeding during tableting becomes a problem. Compared to conventional MCCs, a long-particle MCC with higher compactibility and higher oil absorption capacity reduces oil bleeding due to less compression force and facilitates tableting of oily active ingredients.
Challenges
Key words
HPC replacement
Ceolus™ KG
HPC is very well known as an excellent binder for tablets, however it is not one of the cheapest ingredients. Using a highly compactible MCC instead of HPC will eliminate the need of using disintegrants and will still obtain the similar level of tablet hardness at very low loading just as HPC. This will result in a more cost effective approach in tablet formulation. In addition, using a MCC, a plant-derived ingredient may contribute to clean label.
Challenges
Key words
Balance of tablet hardness and tablet disintegration - High shear granulation
Ceolus™ UF
In high shear granulation, the granulation time affects the compactibility, disintegration and dissolution properties of granules. In particular, longer granulation time tends to deteriorate the compactibility, disintegration or dissolution properties. Ceolus™ UF grade is a round and porous MCC and its high swellability can reduce adverse effects of high shear granulation on tablet hardness, disintegration and dissolution.
Challenges
Key words
Control of disintegration and dissolution
Ceolus™ KG Ceolus™ UF
In the development of generic drugs, changing the grade of MCC can be an option to match the disintegration and dissolution profile with the original drug. Due to the different particle morphology compared to conventional MCCs, our MCCs Ceolus™ KG tends to slow dissolution and Ceolus™ UF tends to accelerate dissolution.
Challenges
Key words
Improvement of API content uniformity
Ceolus™ UF
API segregation is one of typical challenges in direct compression of low dose API formulations. A porous MCC particle forms an ordered mixture by API adhesion on its surface. The ordered mixture mitigates API segregation risk and provides better API content uniformity compared to conventional MCCs.
Challenges
Key words
Prevention of hardness decline due to over-lubrication
Ceolus™ UF
Lubricant mixing is a process which requires great care in tablet manufacturing. Excessive addition or mixing of lubricants may cause deterioration of tablet hardness. A porous MCC particle adsorbs lubricant on its surface and reduces negative effect on tablet hardness. It may simplify the mixing method and shorten the process.
Challenges
Key words
Design space study
Ceolus™ UF
Ceolus™ UF can be used to enable poorly compactible formulation, to solve tableting issues including over-lubrication and to enable high speed tableting . In this data, we visualized and compared the applicable range of Ceolus™ UF-702 and conventional MCC grade PH-102 as a design space study, using Acetaminophen as a model of low compactible API. In comparison with PH-102, Ceolus™ UF-702 has a wider design space and is useful for highly robust formulation design.
Challenges
Key words
Improvement of tablet weight variance under high speed tableting
Ceolus™ UF
In direct compression of formulation with poorly flowable APIs, increasing the tableting speed tends to cause tablet weight variance. A high flowable MCC may improve flowability of mixed powder, prevent tablet weight variance, and increase tableting speed.
Challenges
Key words
Improvement of tablet weight variance under high speed tableting
Ceolus™ UF
In direct compression of formulation with poorly flowable APIs, increasing the tableting speed tends to cause tablet weight variance. A high flowable MCC may improve flowability of mixed powder, prevent tablet weight variance, and increase tableting speed.
Challenges
Key words
Improvement of tablet weight variance under high speed tableting
Ceolus™ UF
In direct compression of formulation with poorly flowable APIs, increasing the tableting speed tends to cause tablet weight variance. A high flowable MCC may improve flowability of mixed powder, prevent tablet weight variance, and increase tableting speed.
Challenges
Key words
Improvement of tablet weight variance under high speed tableting
Ceolus™ UF
In direct compression of formulation with poorly flowable APIs, increasing the tableting speed tends to cause tablet weight variance. A high flowable MCC may improve flowability of mixed powder, prevent tablet weight variance, and increase tableting speed.
Challenges
Key words
MCC sphere for controlled release formulations
Celphere™
Film coating with MCC spheres causes less agglomeration than with sugar spheres regardless of the film coating conditions such as spray rate because of their moderate water absorption capacity without dissolving. Also, film coating with MCC spheres causes less damage to core particles than with sugar spheres because of their high mechanical strength. These results suggest MCC spheres facilitates precise dissolution profile of controlled release formulations.
Challenges
Key words
MCC sphere for controlled release formulations
Celphere™
In the case of film coating with sugar spheres, core particles dissolve in water and the granules become unstable. It indicates negative impact on dissolution profile would be assumed due to external shear stress such as the gastrointestinal tract. On the other hand, film coated granules with MCC spheres are more robust against external shear stress, and maintain stable dissolution profile because of insoluble property of MCC.
Challenges
Key words
Reduction of agglomeration in coating process
Celphere™
Drug layering with MCC spheres causes less agglomeration than with sugar spheres regardless of the drug layering conditions such as spray rate because of their moderate water absorption capacity without dissolving. This result suggests that the use of MCC sphere improves productivity.
Challenges
Key words
Reduction of agglomeration in coating process
Celphere™
Drug layering with MCC spheres causes less agglomeration than with sugar spheres regardless of the drug layering conditions such as spray rate because of their moderate water absorption capacity without dissolving. This result suggests that the use of MCC sphere improves productivity.
Challenges
Key words
Reduction of agglomeration in coating process
Celphere™
Film coating with MCC spheres causes less agglomeration than with sugar spheres regardless of the film coating conditions such as spray rate because of their moderate water absorption capacity without dissolving. This result suggests that the use of MCC sphere improves productivity.
Challenges
Key words
Reworking on tablets - Direct compression
Ceolus™ KG
In the rework process, adding Hydroxypropyl Cellulose ("HPC") to the formulation is the preferred route to salvage such failed batches from becoming expensive waste. Adding a highly compactible MCC to formulation instead of HPC keeps tablet friability low, prevents capping without slowing down disintegration. If the hardness deficiency can be solved by using MCC instead of HPC, the cost increase by changing the label can be avoided.
Challenges
Key words
Reworking on tablets - Extra addition of MCC
Ceolus™ KG
In the rework process, adding Hydroxypropyl Cellulose ("HPC") to the granulating powder blend before tableting is the preferred route to salvage such failed batches from becoming expensive waste. Adding a highly compactible MCC to granules prior to tableting imparts a much higher compressibility and revents tablet defects such as capping.
Challenges
Key words
Continuous manufacturing - Wet granulation
Ceolus™ KG
Pharmaceutical manufacturers have explored introducing continuous manufacturing from the perspective of cutting the facility space needed for processes and omitting scale-up studies with the aim of shortening the drug development period. We studied the applicability of Ceolus™ in a continuous manufacturing system, Granuformer® Gf-2050 developed by the Freund Corporation. Ceolus™ grades tested in this study could be granulated to the target granule size by adjusting the added volume of water, and the tablet properties also met the practical target values. Of these grades, KG-1000 was the optimum Ceolus™ grade with its high-water absorption rate in a continuous manufacturing system by Freund.
Challenges
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