Chemical Properties
Crospovidone is a white to creamy-white, finely divided, freeflowing, practically tasteless, odorless or nearly odorless, hygroscopic powder.
Uses
Pharmaceutic aid (tablet excipient).
Production Methods
Acetylene and formaldehyde are reacted in the presence of a highly active catalyst to form butynediol, which is hydrogenated to butanediol and then cyclodehydrogenated to form butyrolactone. Pyrrolidone is produced by reacting butyrolactone with ammonia. This is followed by a vinylation reaction in which pyrrolidone and acetylene are reacted under pressure. The monomer vinylpyrrolidone is then polymerized in solution,using a catalyst.Crospovidone is prepared by a ‘popcorn polymerization’ process.
brand name
Kollidon CL (BASF); Kollidon CLM (BASF); Polyplasdone (International Specialty Products).
Pharmaceutical Applications
Crospovidone is a water-insoluble tablet disintegrant and dissolution agent used at 2–5% concentration in tablets prepared by direct compression or wet- and dry-granulation methods. It rapidly exhibits high capillary activity and pronounced hydration capacity, with little tendency to form gels.Studies suggest that the particle size of crospovidone strongly influences disintegration of analgesic tablets. Larger particles provide a faster disintegration than smaller particles. Crospovidone can also be used as a solubility enhancer. With the technique of co-evaporation, crospovidone can be used to enhance the solubility of poorly soluble drugs. The drug is adsorbed on to crospovidone in the presence of a suitable solvent and the solvent is then evaporated. This technique results in faster dissolution rate.
Safety
Crospovidone is used in oral pharmaceutical formulations and is generally regarded as a nontoxic and nonirritant material. Shortterm animal toxicity studies have shown no adverse effects associated with crospovidone. However, owing to the lack of available data, an acceptable daily intake in humans has not been specified by the WHO.
LD50 (mouse, IP): 12g/kg
storage
Since crospovidone is hygroscopic, it should be stored in an airtight container in a cool, dry place.
Incompatibilities
Crospovidone is compatible with most organic and inorganic pharmaceutical ingredients. When exposed to a high water level, crospovidone may form molecular adducts with some materials.
Regulatory Status
Accepted for use as a food additive in Europe. Included in the FDA Inactive Ingredients Database (IM injections, oral capsules and tablets; topical, transdermal, and vaginal preparations). Included in nonparenteral medicines licensed in the UK. Included in the Canadian List of Acceptable Non-medicinal Ingredients.
