Croscarmellose sodium
Encyclopedia
Croscarmellose sodium is an internally cross-linked sodium carboxymethylcellulose for use as a disintegrant
in pharmaceutical formulations.
while still allowing the material to swell (like a sponge) and absorb many times its weight in water. As a result, it provides superior drug dissolution
and disintegration characteristics, thus improving formulas' subsequent bioavailability
by bringing the active ingredients into better contact with bodily fluids.
Croscarmellose sodium also resolves formulators' concerns over long-term functional stability, reduced effectiveness at high tablet hardness levels, and similar problems associated with other products developed to enhance drug dissolution. Croscarmellose sodium is a very commonly used pharmaceutical additive approved by the U.S. Food and Drug Administration. Its purpose in most tablets - including dietary supplements - is to assist the tablet in disintegrating in the intestinal tract at the required location. If a tablet disintegrating agent is not included, the tablet could disintegrate too slowly, in the wrong part of the intestine or not at all, thereby reducing the efficacy and bioavailability
of the active ingredients.
Croscarmellose sodium is made by first soaking crude cellulose
in sodium hydroxide, and then reacting the cellulose with sodium monochloroacetate to form sodium carboxymethylcellulose. Excess sodium monochloroacetate slowly hydrolyzes to glycolic acid and the glycolic acid catalyzes the cross-linkage to form croscarmellose sodium.
Chemically, croscarmellose sodium is the sodium salt of a cross-linked, partly O-(carboxymethylated) cellulose.
It was regarded as promoting bad stomach flora by Elaine Gottschall and is "illegal" under the Specific Carbohydrate Diet
.
Croscarmellose sodium was first used as a stabilizer
in horse supplements.
Excipient
An excipient is generally a pharmacologically inactive substance used as a carrier for the active ingredients of a medication. In many cases, an "active" substance may not be easily administered and absorbed by the human body; in such cases the substance in question may be dissolved into or...
in pharmaceutical formulations.
Background
The cross-linking reduces water solubilitySolubility
Solubility is the property of a solid, liquid, or gaseous chemical substance called solute to dissolve in a solid, liquid, or gaseous solvent to form a homogeneous solution of the solute in the solvent. The solubility of a substance fundamentally depends on the used solvent as well as on...
while still allowing the material to swell (like a sponge) and absorb many times its weight in water. As a result, it provides superior drug dissolution
Dissolution (chemistry)
Dissolution is the process by which a solid, liquid or gas forms a solution in a solvent. In solids this can be explained as the breakdown of the crystal lattice into individual ions, atoms or molecules and their transport into the solvent. For liquids and gases, the molecules must be compatible...
and disintegration characteristics, thus improving formulas' subsequent bioavailability
Bioavailability
In pharmacology, bioavailability is a subcategory of absorption and is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. By definition, when a medication is administered...
by bringing the active ingredients into better contact with bodily fluids.
Croscarmellose sodium also resolves formulators' concerns over long-term functional stability, reduced effectiveness at high tablet hardness levels, and similar problems associated with other products developed to enhance drug dissolution. Croscarmellose sodium is a very commonly used pharmaceutical additive approved by the U.S. Food and Drug Administration. Its purpose in most tablets - including dietary supplements - is to assist the tablet in disintegrating in the intestinal tract at the required location. If a tablet disintegrating agent is not included, the tablet could disintegrate too slowly, in the wrong part of the intestine or not at all, thereby reducing the efficacy and bioavailability
Bioavailability
In pharmacology, bioavailability is a subcategory of absorption and is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. By definition, when a medication is administered...
of the active ingredients.
Croscarmellose sodium is made by first soaking crude cellulose
Cellulose
Cellulose is an organic compound with the formula , a polysaccharide consisting of a linear chain of several hundred to over ten thousand β linked D-glucose units....
in sodium hydroxide, and then reacting the cellulose with sodium monochloroacetate to form sodium carboxymethylcellulose. Excess sodium monochloroacetate slowly hydrolyzes to glycolic acid and the glycolic acid catalyzes the cross-linkage to form croscarmellose sodium.
Chemically, croscarmellose sodium is the sodium salt of a cross-linked, partly O-(carboxymethylated) cellulose.
It was regarded as promoting bad stomach flora by Elaine Gottschall and is "illegal" under the Specific Carbohydrate Diet
Specific Carbohydrate Diet
The Specific Carbohydrate Diet is a nutritional regimen, created by Dr. Sidney V. Haas and popularized by biochemist and author Elaine Gottschall, which restricts the use of complex carbohydrates and eliminates refined sugar, all grains and starch from the diet...
.
Croscarmellose sodium was first used as a stabilizer
Stabilizer (chemistry)
In chemistry a stabilizer is a chemical which tends to inhibit the reaction between two or more other chemicals. It can be thought of as the antonym to a catalyst...
in horse supplements.