Drug Solubilizers

A range of ingredient technology for bioavailability enhancement
With more than 60% of new drugs currently in development considered poorly soluble – along with nearly half the drugs coming off patent in the next 10 years, it is increasingly important to choose ingredients that increase solubility and bioavailability of drug actives. ISP offers a variety of ingredients to assist formulators with poorly soluble drug actives.

Ingredient

Solution

Application

Plasdone® K  Povidone
Plasdone S-630 Copovidone

Matrix polymer for solid dispersions

Oral Solids

Plasdone C and K Povidones

Polymers  for crystal inhibition

Oral Liquids, Parenterals, Ophthalmics

Polyplasdone® Crospovidone

Superdisintegrant for increasing dissolution

Oral Solids

Pharmasolve® NMP
2-Pyrol

Solvent for drug solubilization

Parenterals, Ophthalmics

CAVAMAX® and CAVASOL® cyclodextrins

Inclusion complexes for solubility and stability

Oral Solids, Oral Liquids

CAVITRON® cyclodextrins

Parenterals,
Ophthalmics

Plasdone K and S-630 polymers for enhancement of drug solubility using solid dispersions
There is increasing interest in drug-polymer solid solutions and solid dispersions technology to improve the aqueous solubility and enhance the bioavailability of poorly soluble drug candidates.
Solid dispersions and solutions can be prepared via spray drying or melt extrusion. Pharmaceutically acceptable polymers are ideal to create this matrix. Proper polymer selection is critical to impede diffusion and inhibit any tendency for nucleation and crystal growth.

Polyplasdone XL-10 superdisintegrants enhances rate and extent of drug dissolution
The choice of ingredients in tablet formulation can have a significant effect on the rate and extent of drug dissolution. In a recent study, tablets with Polyplasdone XL-10 crospovidone had significantly faster drug release for 12 of 13 drugs in the recommended dissolution media compared to other tablets with other superdisintegrants.

Download recent article “Influence of superdisintegrants on the drug dissolution from oral solid-dosage froms”

Download “Polyplasdone crospovidone: The solution for poorly soluble drugs”

Cyclodextrins for preparation of drug inclusion complexes with increased drug solubility
One of the most common applications of cyclodextrins is to form inclusion complexes with poorly soluble actives to improve bioavailability. Drugs with poor bioavailability typically have low water solubility and/or tend to be highly crystalline. Cyclodextrins are water soluble and form inclusion complexes with apolar molecules of functional groups of water insoluble compounds. The resulting complex hides most of the hydrophobic functionality of the drug active in the interior cavity of the cyclodextrin while the hydrophilic hydroxyl groups on its eternal surface remain exposed to the environment. In addition to improving solubility, cyclodextrins also prevent crystallization of active ingredients by complexing individual molecules so that they can no longer assemble into a crystal lattice.

ISP offers a full range of cyclodextrins products. Let us help you select the one for your application.

Plasdone K polymers for preparation of liquid softgel fill formulations with high use
levels of drug actives

Soft gels are easy to swallow and have an elegant appearance, thus they find wide use to deliver over-the-counter (OTC) drugs. In formulation of softgels, it is often challenging to prepare a homogeneous suspensions and solutions with high levels of actives and minimize capsule size. Plasdone K polymers have been shown to enhance the solubility of actives and provide for highly concentrated solutions.

Download "Optimization of stable soft gel formulation using low molecular weight PVP 2007"

Pharmasolve NMP drug solubilizer for veterinary products
Download "Pharmasolve NMP Drug solubilizer for veterinary products"