frequently asked questions (faq)
What is the most common composition of neutral spheres used as core for active pellets?
Sugar spheres made of sucrose and corn starch represent the most important part of the neutral spheres market. The reason is that the monographs of the internationally relevant pharmacopoeias (USP/NF, EP, CP, JPE) describe explicitly this composition. This makes it easy to use these officinal excipients in a formulation.
Which are the advantages of sucrose and corn starch over other excipients?
Sucrose and corn starch are substances also commonly used as food ingredients and widely available in the necessary pharmaceutical quality. They are natural substances made from sugar beet or sugar cane and maize. Sucrose and starch are safe, non-toxic excipients. In the intestine they are digestible, and in the environment completely biodegradable. This meets the customer’s expectation for clean label products.
Sucrose is related to dental caries and diabetes, isn’t it?
Sugar spheres become part of an orally administered drug form that is swallowed (as hard gelatine capsules or matrix tablets). There is no relevant contact to the teeth. The total quantity of sucrose in the daily doses is neglectable in comparison to the carbon hydrates in the food and has no adverse effect on patients suffering from diabetes.
Any technological good reasons to make spheres from sucrose and starch?
Indeed, building-up the spheres by crystallization of sucrose enables us to manufacture mechanically very resistant particles. Attrition and breakage in the course of further processing are significantly reduced in comparison to spheres made by agglomeration of insoluble substances with the help of binding agents.
We want the spheres dissolve clearly in water…
Sucrose is easily soluble in water, but corn starch forms a cloudy suspension. When swallowed, this is completely irrelevant. However, if spheres are meant to get dissolved prior to use, we recommend the larger globuli sacchari, made solely from soluble sucrose, as alternative.
Does the hygroscopic starch interfere with water-sensitive active substances?
Definitely, no! The sugar spheres are dried in the manufacturing process to a water activity below 0.6. The residual water is bound firmly to the starch and is not available for chemical reactions. Furthermore, it would be possible to insulate the spheres’ surface prior to coating with sensitive API.
I heard about MCC spheres …
MCC is microcrystalline cellulose. There is no economic, chemical nor technological reason to use these instead of the proven sugar spheres. A saving of time in the coating process is a rumor.
Some applications need spheres made of tartaric acid?
There are formulations on the market that combine the API load on the spheres with pH lowering tartaric acid as core to improve the solubility and bioavailability of the drug substance. In this case we propose a combination of sugar spheres coated with API and sugar spheres coated with tartaric acid, combined in the same capsule.
Okay, I am nearly convinced, but the registration documents do not cover this alternative!
Let’s talk about scientific facts, not formal pseudo-problems.
What is your personal opinion about all this?
After more than 40 years of worldwide experience with sugar spheres I can honestly summarize, that there was no pellet formulation task that could not be solved with sugar spheres. Spheres of other composition were often defeated and had their specific own problems like availability, purity, stability, and others.