New excipients & actives

Large and medium sized pharmaceutical industries have to diversify their innovation strategies so as to respond to their clients’ expectations for novelty, efficiency, and health benefits, cost controls, and for maintaining their growth and profitability.

Priority goes to excipients and drug delivery

The new pharmacology won’t be enough to respond to all of these objectives. Other components of medicine preparation, excipients and drug delivery technology are going to take more and more space during the global innovation cycle of pharmaceutical developments.

The paradox of innovation in a tightly regulated industry

This excipients sector and the drug delivery technology must respect highly strict requirements in terms of security of the developed products. These deeply rooted requirements demand the carrying out over several years of toxicological and clinical tests that have an uncertain outcome as to getting regulatory approval of any new chemical substance, no matter how promising it may appear. Such regulation limits the practical development of new chemical entities, even though the innovation is indispensable.

Development of the Carbohydrates chemistry

Carbohydrate derived products (starch, glucose polymers and their by-products) are taking an increasing role among new chemical ingredients used in new formulas and in medicines administration technology.

In this context, carbohydrates chemistry and Roquette’s know-how in the field of excipients and drug delivery have a good part to play in the innovating dynamics of the pharmaceutical, neutraceutical, and in the healthcare and personal care sectors.

The Roquette Research and Development department is present in the following fields:
 

• Molecular encapsulation of active principles slightly soluble in cyclodextrines
• Use of carbohydrates as osmotic agents for a new generation
• Multi-functional composed excipients and written up in several pharmacopoeia 
• Film forming compositions

Molecular encapsulation in cyclodextrin (carbohydrates)

Roquette's R&D department has participated in the development of cyclical modified carbohydrates, such as hydroxypropyl-bêta-cyclodextrins as an activation platform for active low solubility principles. Know-how as far as analytical characterization, preparation competences, reliable, innovating production technology are many of the assets at the disposal of ROQUETTE’s R&D department in making carbohydrates chemistry an accessible and efficient technology.

Marketed throughout the world, this technology has a varied range of products for both oral and injectable preparations. Its immediate value is in pioneering preparations with difficult active principles.

A new generation of carbohydrates used as osmotic agents

Osmotic agents are used in the treatment of various clinical pathologies (notably intra-peritoneal dialysis) and plasma substitutes in intensive care units, oral rehydration preparations and for special nutritional purposes.

Roquette’s R&D department has a definite know-how in these domains. It possesses intellectual property protection, in particular for the carbohydrates profiles adapted to such applications.

The glucose polymers, prepared from natural or hybrid starch hydrolysis (enzymatic or acid) consist of glucose and glucose polymers with a large saccharine distribution. Their degradation by digestive enzymes brings their reduction in “limit dextrins”, then through different enzymatic systems in single units of physiological glucose.

The kinetics of these different enzymatic degradations is connected to the structure or to the original carbohydrate polymer process.

Roquette’s R&D department studies soluble and highly branched glucose polymers, which could confer, thanks to the controlled model of branched carbohydrate, a level of control over the metabolism or degradation of the carbohydrate polymer. Such a metabolic control can be used, in the long run, to generate special osmotic profiles and allow to access modulation in biodegradable matrixes.

Composed multi-functional excipients and registered in several pharmacopoeia

It has been well known for a long time that carbohydrates are precious ingredients in pharmaceutical preparations. Their physical and chemical properties are used for dilution, disintegration, linking, modulating the viscosity or matrix formation.

Roquette’s R&D department has acknowledged the value of these unique and unitary functionalities. It is now engaged in the developmental process of synergic compounds in which several carbohydrates, either chemical or structural, are brought together to release new properties.

This is the case, for example, of affordable carbohydrate compositions that have both good dilution properties as well as disintegration ones. These carbohydrates compositions enhance the fluidity and compression capacity of the preparation. The presence of rich amylose grains of starch assures on its side an efficient disintegration.

The development process of the new compounds brings about an innovation of very useful functionalities for the pharmaceutical preparations sector, while conserving a satisfactory regulatory status.

Film forming compositions

The carbohydrate polymers have the advantage of being connected to the biodiversity of starch sources. The continuing research made by Roquette’s R&D department on new natural sources of starch reveal inherent properties transformable into beneficial properties for clients, patients, or consumers.

Its recent research has permitted the discovery of a special starch, rich in amylose that possesses exceptional film forming compositions

This innovative polymer carbohydrate film forming compositions constitutes another technological platform accessible to pharmaceutical and nutraceutical applications as well as health and personal care.