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Solubility Enhancement and Emulsion Formulation

SEPPIC adresses formulator issues with solubilizers and emulsifiers

Drug formulators often face API (Active Pharmaceutical Ingredient) bioavailability issues
Solubility is one of the key factors. A rising number of therapeutic drugs currently in preclinical and clinical developments are poorly water soluble. This number is estimated at 40-70% of NCEs (New Chemical Entities (NCEs)).

Once administered, a drug must be in a solution form to be absorbed regardless of the route of administration.

Developing pharmaceutical formulations with appropriate solubility will be one of the key challenges of next years.

When solution is not the optimal option to deliver the API or when drug formulators want to develop a modified release system, they might go through emulsion vehicles thanks to use of emulsifiers.

Emulsifiers and solubilizers offered by SEPPIC enable drug formulators to manage their challenges with poorly water soluble APIs.

Solubilization

Whatever the route of administration of a drug, the formulator might have the need of a solubilizer from SEPPIC to achieve optimal solubilization.
The target is to achieve a concentrated, clear, homogenous and stable solution in order to deliver the API in an efficient way.

SEPPIC offers different ranges of solubilizers under:

  •  MONTANOX™ range: Polysorbates
  •  SEPITRAP™ range: Solubilizers in powder form for direct compression
  •  SEPICLEAR™ : The SEPPIC novel excipient
  •  SIMULSOL™: Fatty acids, fatty alcohols and castor oil derivatives


The choice of solubilizers is mainly driven by route of administration and nature of the API.

Emulsion

Drugs may be formulated with an emulsion as a vehicle to improve its bioavailability (sustained release, lipophilic or hydrophilic API solubilization, permeability...) or treatment compliance (texture).
An emulsion is a system made of at least two phases. It should be homogeneous and stable, thanks to addition of one or several emulsifiers.
Emulsifiers are used in pharmaceutical formulations to get stable emulsions to achieve the physico-chemical characteristics required for optimal delivery of API.

Depending on the emulsion type - Water in oil (W/O) or Oil in water (O/W) - emulsifiers are selected depending on their lipophilic/hydrophilic nature. They can be characterized thanks to their HLB (Hydrophilic/Lipophilic Balance) value.

SEPPIC offers different ranges of emulsifiers:

  •  MONTANE™ range: sorbitan esters
  •  MONTANOX™ range: polysorbates
  •  SIMULSOL™ range: ethoxylated fatty acids, fatty alcohols and castor oils
  •  SIMALINE WO™ : PEG 30 Dipolyhydroxystearate


Some emulsifiers may also have other functions depending on their HLB value: anti-foaming, wetting, foaming or solubilising functions.