How to improve the effectiveness of Active pharmaceutical ingredients

Did you know that 80% of APIs are not water soluble? This is a major concern for pharmaceutical formulators who sometimes encounter difficulties in producing effective medicines. To answer this challenge, Lauriane Carrier, Eastman's product manager, is happy to introduce a brand new innovative excipient: BioSustane SAIB NF.

Laurianne Carrier, product manager for Eastman at Safic-Alcan :

Our customers frequently develop products that require excipients in order to meet the challenges of increasingly complex formulations. Indeed most of APIs are insoluble in water.
But despite the huge offer of APIs today and the huge investments in the development of new molecules or in biotechs, the offer of innovative excipients is quite rare. 
Safic Alcan, as a privileged partner of major players in the manufacture of excipients, is responding to this challenge by proposing a new excipient from our partner Eastman.
This new excipient is called BioSustane SAIB NF, a fully substituted sucrose molecule containing acetate and isobutyrate esters (2:6 ratio).

Sucrose long chain fatty acid esters (SE) have been widely used for a long time in the food and cosmetic industries and their application in various pharmaceutical fields has recently attracted great interest. They are natural and biodegradable excipients whose emulsifying and solubilizing behaviors are well known. 
BioSustane SAIB NF can be used to improve drug solublization and absorption in the GI tract , as well as displaying utility in  in controlled release systems and amorphous solid dispersions.
Although the scientific literature is starting to grow, we note that materials such as BioSustane SAIB NF have a large potential for development. 

BioSustane SAIB NF is a viscous and very hydrophobic material, this makes it an excellent solvent for poorly water-soluble APIs, i.e., Class II and IV APIs (representing 80% of APIs).
In addition it also confers a sustained release functionality that is remarkable for all types of APIs :

• In the case of BCS Class II and IV APIs (i.e. hydrophobic and often very crystalline), BioSustane SAIB NF dissolves the APIs and in presence of a surfactant these APIs will diffuse out of the matrix. The chart below shows delivery of 80-90% of a Class IV drug (aprepitant) within one hour.

• In the case of BCS Class I and III APIs, BioSustane SAIB NF traps by encapsulating the active ingredient in a matrix from which the API diffuses over time.

BioSustane SAIB NF is heated to 70 – 80°C and the API is added with agitation to be dissolved. Higher temperature can be used depending on the temperature stability of the API.  Alternatively, the BioSustane SAIB NF is heated to 70 – 80°C and a small amount of suitable solvent is added, typically 5-10% ethanol based on weight of the BioSustane SAIB NF.  After wet granulation of the API/ BioSustane SAIB NF solution with usual tableting components, the resulting powder is tableted or put into capsules.   
For a BCS Class IV drug (aprepritant) we can for example advise the following formulation :

We are at your disposal to discuss together the most appropriate formulation according to your constraints.

It's really formulation dependent. 
For example, we have formulations of Diclofenac Sodium that have reasonable sustained release (80-100% in 6-8 hours) that use 8-16% BioSustane SAIB NF in the tablet formulation, and some formulations using Ephedrine as a pseudo-opioid with BioSustane SAIB NF content of 16-30%. 
Again, we are at your disposal to go into the details of the formulations.

It can be used for oral, parenteral and even topical forms.

• BioSustane SAIB NF does not crystallize and remains amorphous at room temperature when ingested and absorbed by the tissues, which greatly facilitates the consistent rate of drug delivery.
• BioSustane SAIB NF is not a polymer and does not coagulate or precipitate when in contact with body fluids.
• BioSustane SAIB NF has mucoadhesive properties which makes it an interesting excipient for very specific formulations

In fact, a webinar has been done, which was a nice success and projects in Europe have been launched, this webinar is available on request.
We hope that we will see many more projects from now on.