Surrogate functionality of celluloses as tablet excipients.
BACKGROUND
The variety of excipients from different sources and prices to which we have access gives rise to the necessity to evaluate their functional characteristics. The aim of this work is to determine some physical and technological characteristics of celluloses from different sources, India and United States, to ascertain their functionality as tablet excipients.


METHODS
The used surrogate functionality properties are particle morphology and particle size distribution, compactibility, ejection pressure, and the disintegration properties of pure excipients and their compressed tablets.


RESULTS
The innovators Avicel and Croscarmellose show advantages over the generic celluloses Alfacel and Carmacel. Avicel PH 101 and 102 show an average of 26% greater compactibility than both types of Alfacel, whereas the compactibility of Croscarmellose is greater than that of Carmacel in about 50%. Avicel tablets compacted at a compaction pressure of 47 MPa exhibit shorter disintegration times (3.7 minutes) than Alfacel tablets (28 minutes), whereas Carmacel show better disintegrant properties than Croscarmellose. This occurs regardless of the similar particle morphology, size, and size distribution. As expected, all celluloses show low ejection pressures.


CONCLUSIONS
The surrogate functionality properties of the generic celluloses are still considered as satisfactory to be used as tablet excipients, although they are inferior in some aspects to innovator celluloses. Alfacel and Carmacel have the potential to be used as filler, binder, and disintegrant, in the design of tablets. Moreover, one should bear in mind that the differences reported here may be altered because of a possible inter-batch variability and variations in the moisture content.
Díaz Ramírez
Carmen Cristina
CC
Department of Pharmacy, National School of Biological Sciences, National Polytechnic Institute of Mexico, Santo Tomás, DF, México, Mexico.
Robles
Leopoldo Villafuerte
LV
D002266:Carboxymethylcellulose Sodium / Q000737:chemistry; D002482:Cellulose / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D003460:Crystallization; D005079:Excipients / Q000737:chemistry / Q000592:standards*; D006813:Humidity; D007194:India; D010316:Particle Size; D011312:Pressure; D011786:Quality Control; D013607:Tablets / Q000737:chemistry*; D014481:United States
D005079:Excipients; D013607:Tablets; D002482:Cellulose; D002266:Carboxymethylcellulose Sodium