Chemical Properties
Croscarmellose sodium occurs as an odorless, white or grayishwhite powder.
Chemical Properties
pH 5.0-7.0 tablet disintegrant.
Uses
Packaged under nitrogen
Uses
Pharmaceutic aid (tablet disintegrant).
Uses
Used as Disintegrant in Capsules, Tablet and Granule Formulations.
Production Methods
Alkali cellulose is prepared by steeping cellulose, obtained from wood pulp or cotton fibers, in sodium hydroxide solution. The alkali cellulose is then reacted with sodium monochloroacetate to obtain carboxymethylcellulose sodium. After the substitution reaction is completed and all of the sodium hydroxide has been used, the excess sodium monochloroacetate slowly hydrolyzes to glycolic acid. The glycolic acid changes a few of the sodium carboxymethyl groups to the free acid and catalyzes the formation ofcrosslinkstoproducecroscarmellosesodium.Thecroscarmellose sodium is then extracted with aqueous alcohol and any remaining sodium chloride or sodium glycolate is removed. After purification, croscarmellose sodium of purity greater than 99.5% is obtained. The croscarmellose sodium may be milled to break the polymer fibers into shorter lengths and hence improve its flow properties.
Brand name
Ac-Di-Sol (FMC); CLD 2 (Buckeye).
Pharmaceutical Applications
Croscarmellose sodium is used in oral pharmaceutical formulations as a disintegrant for capsules,tablets, and granules.
In tablet formulations, croscarmellose sodium may be used in bothdirect-compressionandwet-granulationprocesses.Whenused in wet granulations, the croscarmellose sodium should be added in both the wet and dry stages of the process (intra- and extragranularly) so that the wicking and swelling ability of the disintegrant is best utilized. Croscarmellose sodium at concentrations up to 5% w/w may be used as a tablet disintegrant, although normally 2% w/w is used in tablets prepared by direct compression and 3% w/w in tablets prepared by a wet-granulation process.
Safety
Croscarmellose sodium is mainly used as a disintegrant in oral pharmaceutical formulations and is generally regarded as an essentially nontoxic and nonirritant material. However, oral consumption of large amounts of croscarmellose sodium may have a laxative effect, although the quantities used in solid dosage formulations are unlikely to cause such problems.
In the UK, croscarmellose sodium is accepted for use in dietary supplements.
The WHO has not specified an acceptable daily intake for the related substance carboxymethylcellulose sodium, used as a food additive, since the levels necessary to achieve a desired effect were not considered sufficient to be a hazard to health.
storage
Croscarmellose sodium is a stable though hygroscopic material.
A model tablet formulation prepared by direct compression, withcroscarmellosesodiumasadisintegrant,showednosignificant differenceindrugdissolutionafterstorageat30°Cfor14months.
Croscarmellose sodium should be stored in a well-closed container in a cool, dry place.
Incompatibilities
The efficacy of disintegrants, such as croscarmellose sodium, may be slightly reduced in tablet formulations prepared by either the wet-granulation or direct-compression process that contain hygroscopic excipients such as sorbitol.
Croscarmellose sodium is not compatible with strong acids or with soluble salts of iron and some other metals such as aluminum, mercury, and zinc.
Regulatory Status
Included in the FDA Inactive Ingredients Database (oral capsules, granules, sublingual tablets, and tablets). Included in nonparenteral medicines licensed in the UK. Included in the Canadian List of Acceptable Non-medicinal Ingredients.
