Role of excipients in amorphous solid dispersions

Solid dispersions – a great way to increase the solubility and bioavailability of your drug

In a solid dispersion the drug is dispersed in a carrier with the system appearing to be in a solid state. Target is an increase in solubility and bioavailability. BASF offers both an comprehensive portfolio and process expertise to consult you in finding the best formulation for your poorly soluble drug using a solid dispersions.

In the following video Dr. Frank Romanski speaks about the the role of excipient selection and key characteristics in amorphous solid dispersions at the BASF Solubilization Symposium in Ludwigshafen, Germany.

Increasing number of poorly soluble drugs

The pharmaceutical industry is facing the challenge of having more and more poorly soluble drug molecules that have to be developed into dosage forms so that high and reliable drug absorption can be guaranteed on being administered to patients. Different approaches are possible to overcome solubility issues. Solid dispersions are one of them. It seeks to disperse the drug in a carrier and create a solid system that can be processed into a final dosage form.

BASF excipients for Solid Dispersions

Solubility Enhancement

Product	Description	Monograph title*/Chemical name
Soluplus®	Polymer designed for amorphous solid dispersions (ASDs), spe- cifically to increase solubility and bioavailability of poorly water soluble drugs. Ideal for hot melt extrusion and spray drying.	Polyvinyl caprolactam – polyvinyl acetate – polyethylene glycol graft copolymer
Kolliphor® RH 40	Nonionic solubilizer.	Ph.Eur.: Macrogolglycerol hydroxystearate; USP/NF: Polyoxyl 40 hydrogenated castor oil
Kolliphor® HS 15	Nonionic solubilizer.	Ph.Eur.: Macrogol 15 hydroxystearate; USP/NF: Polyoxyl 15 hydroxystearate
Kolliphor® EL	Nonionic solubilizer.	Ph.Eur.: Macrogolglycerol ricinoleate; USP/NF: Polyoxyl 35 castor oil; JPE: Polyoxyl 35 castor oil
Kolliphor® ELP	Purified Kolliphor® EL, especially for sensitive active ingredients.	Ph.Eur.: Macrogolglycerol ricinoleate 35; USP/NF: Polyoxyl 35 castor oil
Kolliphor® SLS	Ionic solubilizer and emulsifier.	Ph.Eur.: Sodium laurilsulfate; USP/NF, JP: Sodium lauryl sulfate
Kolliphor® P 188 Geismar	Polymeric solubilizer, emulsifier and plasticizer.	Ph.Eur., USP/NF: Poloxamer 188; JPE: Polyoxyethylene (160) polyoxypropylene (30) glycol
Kolliphor® P 338 Geismar	Polymeric solubilizer, emulsifier and plasticizer.	Ph.Eur., USP/NF: Poloxamer 338
Kolliphor® P 407 Geismar	Polymeric solubilizer, emulsifier and plasticizer.	Ph.Eur., USP/NF: Poloxamer 407; JPE: Polyoxyethylene (196) polyoxypropylene (67) glycol
Kolliphor® PS 20	Nonionic solubilizer, emulsifier and co-emulsifier.	Ph.Eur., USP/NF: Polysorbate 20
Kolliphor® PS 60	Nonionic solubilizer, emulsifier and co-emulsifier.	Ph.Eur., USP/NF, JPE: Polysorbate 60
Kolliphor® PS 80	Nonionic solubilizer, emulsifier and co-emulsifier.	Ph.Eur., USP/NF: Polysorbate 80
Kollidon® 12 PFKollidon® 17 PF	Endotoxin controlled – low molecular weight povidone for solubilization, stabilization and crystallization inhibition.	Ph.Eur., USP/NF, JP: Povidone
Kollidon® 25Kollidon® 30∆	Medium-molecular weight Povidone for solubilization, dispersion and oral liquid and oral semi-solid formulations crystallization inhibition.	Ph.Eur., USP/NF, JP: Povidone
Kollidon® 90 F	High-molecular weight Povidone for solubilization, dispersion and crystallization inhibition.	Ph.Eur., USP/NF, JP: Povidone

BASF excipients for Solid Dispersions

Matrices

Product	Description	Monograph title*/Chemical name
Soluplus®	Polymer designed for amorphous solid dispersions (ASDs), spe- cifically to increase solubility and bioavailability of poorly water soluble drugs. Ideal for hot melt extrusion and spray drying.	Polyvinyl caprolactam – polyvinyl acetate – polyethylene glycol graft copolymer
Kollidon® VA 64	Copolymer designed for creation of amorphous solid dispersions (ASDs) – instant release matrix, solubilizer, crystallization inhibitor. High solubility in organic solvents, high acceptability in solid oral doses. Ideal and commonly used in HME and spray drying.	Ph.Eur., USP/NF: Copovidone; JPE: Copolyvidone
Kollidon® SR	Controlled release matrix. May be blended with water soluble polymers to tailor release.	80% Polyvinyl acetate and 19% povidone, 0.8% lauryl sulfate & 0.2% silica
Kollidon® 12 PF Kollidon® 17 PF	Endotoxin controlled – low molecular weight povidone for solu- bilization, stabilization and crystallization inhibition.	Ph.Eur., USP/NF, JP: Povidone
Kollidon® 25	For instant release matrices including solubilization and crystallization inhibition.	Ph.Eur., USP/NF, JP: Povidone
Kollidon® 30∆	For instant release matrices including solubilization and crystallization inhibition. Suitable for spray drying.	Ph.Eur., USP/NF, JP: Povidone