Excipients for Dry Forms

Diluent-binders for direct compression

Direct compression is a process that is becoming increasingly more important. Compared with wet granulation, direct compression requires less industrial equipment and allows productivity to be improved. Excipients for direct compression, known as diluent-binders, need to have good flowability, excellent compressibility and a specific particle size distribution to ensure uniform mixing.

Roquette proposes a remarkable varied range of such diluent-binders suitable for the formulation of all types of tablets:

Starches or starch compounds for swallowable / dispersible tablets.

They include some of Roquette’s newest developments:

• STARLAC® : an innovative lactose-starch compound with unique tabletting properties
• LYCATAB® C: a multifunctional starch excipient for capsules and tablets
• LYCATAB® Mineral: a directly compressible excipient easy to use in mineral supplements

Direct compression maltodextrins for robust and suckable tablets with excellent smooth texture

Polyols with their outstanding combination of chemical stability and great tasting and sugar free properties:

• NEOSORB® sorbitol powder with its characteristic sweet and cool taste is ideally suited for oral medication such as suckable tablets
• PEARLITOL® SD and DC mannitol, a comprehensive range of granulated mannitol, with particular use in challenging or unstable formulations and appropriate for all types of tablets including chewable / oral dispersible or effervescent tablets

Diluents and binders for wet granulation

Wet granulation, a traditional manufacturing process, is still widely used. It is often required when the pharmaceutical form contains a high level of active ingredients.

Granules obtained by wet granulation are characterised by a uniform particle size distribution with few fine particles allowing a uniform filling of capsules, sachets or compression matrices, and giving very good compression profiles while maintaining low tablet disintegration time.

Diluents

Diluents are inert powders acting as fillers in the formulation of tablets, capsules and powders for sachets. Roquette offers a range of both water-soluble or water-insoluble diluents that also have a disintegration function:

The starches or partially pregelatinised starches are traditional excipients, among the most used and trusted insoluble excipients in the world, having the added function of disintegration aid:

• Maize starch B and extra White maize starch B
• Wheat starch TB
• Potato starch B
• LYCATAB® C partially pregelatinised starch

The large range of soluble diluents include maltodextrins, dried glucose syrups, dextrose -monohydrate and anhydrous-, and the highly functional polyols appreciated for their physicochemical stability, organoleptic properties (sweetening power, cooling effect) and sugar-free, dietary benefits:

• NEOSORB® sorbitol powder
• PEARLITOL® mannitol powder (crystalline, granulated)
• SweetPearl maltitol powder
• XYLISORB® xylitol powder

Binders

Wet granulation can be achieved through different processes, the wetting and granulation having a marked impact on the quality of the final granules. Roquette has specifically developed pharmaceutical binders with different degrees of water solubility or dispersibility:

• LYCATAB® PGS, a pregelatinised dispersible starch, ideally used in dry blends
• LYCATAB® DSH, a water-soluble maltodextrin binder suitable for preparation of granulation solutions or use in dry blends

Disintegrants and superdisintegrants

Disintegrants and superdisintegrants are used in tablets and capsules to ensure that these compacts are rapidly broken down into the primary particles to facilitate the dissolution or release of the active ingredients.

ROQUETTE has developed a versatile range of standard disintegration excipients ranging from the traditional native starches to the innovative multifunctional starch compound STARLAC®, and the partially pregelatinized starch LYCATAB® C, and has extended its offer of superdisintegrant, GLYCOLYS® sodium starch glycolate, with three unique grades of this market reference product to meet specific formulation needs:

• GLYCOLYS®
• GLYCOLYS® LV
• GLYCOLYS® Low PH

Excipients for molecular encapsulation

The formation of molecular inclusion complexes with cyclodextrins has become an accepted formulation strategy to improve the solubility or stability of active ingredients and can also be used to improve the taste of bitter or unpleasant drugs.

Roquette has pioneered the development of betacyclodextrin technology leading to a full range of KLEPTOSE® betacyclodextrins, with different powder properties, chemical substitution or solubility profile to suit modern formulation needs:

• KLEPTOSE®, native betacyclodextrins
• KLEPTOSE® HPBCD, hydroxypropyl betacyclodextrins
• CRYSMEB, methyl betacyclodextrin*

* under development

Carrier for freeze-drying or lyophilisation

Freeze-dried products exhibit porous and brittle structures that are highly water sensitive.

The chemical nature of PEARLITOL® mannitol (crystalline, granulated), as well as its remarkable non-hygroscopic crystalline structure, makes it the excipient of choice for freeze drying formulation.

Excipients for hard coating

Hard Coating is the traditional method of covering tablets. It is mainly used to mask unpleasant odours and tastes or to protect actives against light.

Roquette’s SweetPearl maltitol powder has become the reference standard for sugar-free hard coating around the world. SWEETPEARL® maltitol successfully replaces sugar, and allows to achieve faster coating time while offering dietary benefits: sugar-free, low-caloric, non-cariogenic and suitable for diabetics.