EXCIPIENTS FOR ENHANCING DRUG SOLUBILITY

Many techniques have been devised to enhance the absorption of poorly soluble medications. A straightforward and efficient approach involves the use of excipients to accelerate drug dissolution. Common excipients that facilitate this process include…

Disintegration agent

Make tablet “disintegrant” quickly into smaller particles.
Increase the surface area of the API with the dissolution medium.
Some common super disintegrants: croscarmellose sodium, sodium starch glycolate, crospovidone.

Excipients adjust pH

Allows drug molecules stay in an ionic state, making them more soluble.
Organic acids: citric acid, Tartaric acid and carbonic acid are used to increase absorption of weakly alkaline drugs.

Complexing with cyclodextrin (CD):

Forms a complex with a hydrophobic cavity capable of containing hydrophobic active ingredients with a hydrophilic surface.
Used in many dosage forms: ODT, effervescent tablets, modified release tablets and researched to improve the solubility of carbamazepine, eslicarbazepine,…

Solid dispersion system

Disperse amorphous solid active ingredients in polymer carrier materials (PVP, HMPC, CMC, chitosan, etc.).
The amorphous form has higher solubility than the crystalline form.

Surfactants:

Increases the permeability of the active ingredient to the dissolution medium, increasing solubility.
Some common surfactants: sodium lauryl sulfate, tween 80, span.

SEDDS self-emulsifying drug delivery system:

Small emulsion particles will help increase the solubility of the active ingredient.
Improves the solubility of active ingredients such as: Nabumetone, Simvastatin.

Sugars:

Sucrose, in addition to its ability to mask taste, also has the ability to act as a natural surfactant.
Mannitol also used to increase the solubility of the active ingredient.