Abstract
New carboxymethylcellulose esters were developed with useful properties for oral dosage forms in drug delivery. Normally, commercial cellulose esters are used as the major excipients in oral dosage forms as a coating or a membrane. In applications involving compression tablets, cellulose esters are usually mixed with other more hydrophilic matrix components to facilitate dissolution of the active. In the present study, novel cellulose esters were single component matrix resins. Pharmaceutical actives were cryogenically ground as a physical blend or an amorphous blend with the polymer. Subsequently, tablets were made by direct compression using a single tablet press, or capsules were made by filling them with the ground material. Dissolution tests were completed on the solid dosage forms at pH 1.2, 4.5, 6.8 or 7.4 in a United States Pharmacopeia (USP) II device to determine the release profiles for up to 24 h. Carboxymethylcellulose esters provide an excellent matrix for controlling both the rate of release and the pH at which pharmaceutical actives release into the aqueous environment. When used in suitable quantities, dictated by the active of interest, carboxymethylcellulose acetate butyrate provided zero-order release over sustained time up to 24 h.
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Abbreviations
- Ac:
-
Acetyl
- BCS:
-
Biopharmaceutics Classification System
- Bu:
-
Butyryl
- CA:
-
Cellulose Acetate
- CAB:
-
Cellulose acetate butyrate
- CM:
-
Carboxymethyl
- CMCA:
-
Carboxymethylcellulose acetate
- CMCAB:
-
Carboxymethylcellulose acetate butyrate
- CMCAP:
-
Carboxymethylcellulose acetate propionate
- CMC:
-
Carboxymethylcellulose
- DS:
-
Degree of substitution
- Eastman EB:
-
Ethylene glycol monobutyl ether
- MC:
-
microcrystalline cellulose
- Na-CMC:
-
Sodium carboxymethylcellulose
- NF:
-
National Formulary
- rpm:
-
revolutions per minute
- PEO:
-
polyethylene oxide
- Pr:
-
Propionyl
- TEC:
-
triethyl citrate
- Tg:
-
glass transition temperature
- USP:
-
United States Pharmacopeia
- WHO:
-
World Health Organization
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Posey-Dowty, J.D., Watterson, T.L., Wilson, A.K. et al. Zero-order release formulations using a novel cellulose ester. Cellulose 14, 73–83 (2007). https://doi.org/10.1007/s10570-006-9079-7
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DOI: https://doi.org/10.1007/s10570-006-9079-7
Keywords
- CA
- CAB
- Carboxymethylcellulose ester
- Carboxymethylcellulose acetate
- Carboxymethylcellulose acetate butyrate
- Carboxymethylcellulose acetate propionate
- Cellulose acetate
- Cellulose acetate butyrate
- Cellulose ester
- CMCA
- CMCAB
- CMCAP
- Compression tablet
- Dissolution
- Extended release
- Pharmaceutical drug delivery
- Zero-order release