Faster formulation at CPhI by Colorcon

Being showcased at this year’s CPhI Worldwide, Colorcon’s StarTab has been designed to simplify the tablet formulation process. Here, gain an exclusive look into StarTab’s manufacturing benefits and be sure to visit Colorcon's stand (102B70).

Simpler Formulation to Speed Your Product to Market

Pharmaceutical manufacturers prefer excipients that are easy to use, functional and provide benefits for the drug product while maintaining safety and efficacy. Colorcon’s Starch 1500, partially pregelatinised starch has been proven in-use in the marketplace for over 40 years, with the company’s manufacturing facility in Indianapolis, USA, producing millions of kilos of starch excipient products every year that subsequently go into billions of tablets and capsules used around the world.

Choosing the Right Excipient

Through the addition of innovative products, the starch product line enables the formulator to reduce the number of excipients needed, thereby lowering costs and complexity. StarCap, superior flow maize starch product has been developed specifically for high speed capsule filling. Whilst the latest addition, StarTab, directly compressible starch, brings superior compaction properties and simplifies formulation development for tablets.

Starch 1500 has a proven track record and is trusted for performance and versatility. In addition to its effectiveness for low dose drugs to promote content uniformity, it helps stabilise moisture sensitive drugs. It has no known active pharmaceutical ingredient (API) incompatibilities and meets global regulatory requirements.

Active Pharmaceutical Ingredient (API) Compatibility

Unwarranted moisture sorption by either APIs or excipients can result in unstable oral solid formulations. In solid oral dose development, API compatibility will drive the selection of the excipient, which in turn determines the necessary manufacturing process; with an impact on long term production costs and resulting profitability.

Through inclusion of starch excipients to preferred excipient lists, pharmaceutical companies have realised the benefits of using these most effective ingredients that do not contain reactive species for possible incompatibility.

Stabilising Moisture Sensitive Drugs

The stability of moisture-sensitive products depends on many factors including choice of excipients used in the formulation and their concentration. Although careful control of the manufacturing environment and the use of protective (and often expensive) packaging can reduce the exposure of a drug, to improve the stability of the final dosage form it is advisable to select excipients that have low water activity.

Excipients that possess low water activity, such as pregelatinised starch, are preferred in the development of moisture sensitive formulations because they can protect actives from hydrolytic degradation by tightly binding moisture on storage. One common misconception surrounding choice of materials is the level of excipient moisture content. In reality, water activity, not absolute moisture content, is the trigger for unwanted reactions.

Loss on drying (LOD) or total moisture content of pharmaceutical products can include both bound (e.g. water of hydration) and free water. It is the free water that is responsible for degradation of moisture sensitive materials resulting in poor stability profiles. Starch 1500 has a relatively high moisture content ranging from 6-14% LOD, while its low free water content means that water activity is equal to, or lower than, other excipients of lower moisture content (see Figure 1).

Multiple studies have been performed showing that the low water activity of Starch 1500, and now StarTab, improves product stability and reduces formation of degradants on moisture sensitive actives.

Moisture barrier coatings with low water permeability, such as Opadry PVA-based film coating systems, applied to a final dosage form can further improve the stability of water-sensitive drugs on storage. The moisture uptake of the core during aqueous film coating processes is minimised through correct selection of process parameters such as drying step (pre-warming the tablets), airflow, inlet air temperature and spray rate.

Blend Homogeneity for Low Dose Drugs

Achieving blend homogeneity is an important criterion for formulating micronised drugs, as they tend to segregate during blending due to their increased surface area and particle agglomeration. Blending of micronised low-dose drugs may be challenging and cause content uniformity issues and physical instability.

The choice of filler in a formulation, for a low-dose micronised drug, may assist uniform dispersibility of the drug throughout the blend with no segregation during compression. Fillers with irregular surface characteristics (such as Starch 1500) may provide favourable adsorption for micronised particles and behave as a carrier, rendering content uniformity.

The potency of both new and currently used drugs necessitates doses as low as 0.025 mg. During the development and manufacturing of a low dose tablet, content uniformity is the principal technical challenge. Starch 1500, and now StarTab, directly compressible starch improves formulation flow properties, resulting in good tablet weight uniformity which is demanded for high-speed direct compression.

Innovation

The many advantages and application successes of Starch 1500 have been built on through the development of two new products.

StarCap – Superior Flow Maize Starch

StarCap is an inert excipient with a unique particle morphology that provides free flow and ensures good compactibility.  Ensuring weight uniformity and enhancing powder flow are essential for effective capsule filling operation. StarCap demonstrates smooth operation on high-speed production scale, continuous movement, dosator encapsulation equipment at 100,000 capsules per hour. In a case study, capsules were filled, and weight measurements taken every minute, for 30 minutes. Low weight variation demonstrates that StarCap is highly applicable for high-speed capsule filling operations.

StarTab – Directly Compressible Starch

Recently launched, StarTab is designed especially for direct compression to simplify tablet formulation and process, providing excellent flow and superior compressibility; resulting tablets have low friability, ideal for film coating and packaging.

StarTab alone provides excellent tablet hardness and very low disintegration time compared to other directly compressible excipients. Formulation is simpler by removing the addition of flow aid, compression aid and disintegrant; and by limiting the number of ingredients, there is less potential for interactions with the API.

With just one main material needed for the direct compression process, the formulator can think “Less is More”.......less complexity, more efficiency.

Colorcon continues to innovate with specialty excipients and film coating systems, providing pharmaceutical manufacturers with improved convenience marked by speed and efficiency, cost savings and dependable performance.