ABSTRACT
BACKGROUND AND OBJECTIVES:
Pain is considered a major clinical problem worldwide. Faster pain relief was reportedly achieved using a fast-dissolving paracetamol (APAP) tablet. Microcrystalline cellulose (MCC) is the most widely used excipient to produce fast-dissolving APAP tablet formulations, but it retards the dissolution of APAP. The present investigation reports incorporation of croscarmellose sodium (CCS) instead of MCC into APAP commercial tablet formulations to enhance the dissolution rate of APAP.
METHODS:
A wet granulation method was used to prepare APAP tablets with various CCS concentrations, using a factorial design with 31 CCS concentrations as independent variables, while the dissolution percentage of the drug release at different time intervals was used as dependent variable. The disintegration time and dissolution rate of these APAP tablets were determined and compared with the dissolution rate of Amidol® and Panadol®, commercial APAP tablets available in Sudan.
RESULTS:
The mean time to complete disintegration of the APAP tablets with CCS was faster than that for the commercial APAP tablets, both Amidol® (0.58 min vs. 2.43 min) and Panadol® (0.58 min vs. 1.32 min), and these differences were statistically significant for Amidol (p≤0.001) and Panadol® (p≤0.01). Moreover, the dissolution rate for the APAP tablets with CCS was significantly faster than those for Amidol® and Panadol®.
CONCLUSION:
The dissolution of APAP from Amidol® and Panadol® can be successfully enhanced by incorporating CCS in their formulation and can be considered as a simple approach for fast-pain relieving using APAP.
Keywords
Croscarmellose sodium; Disintegration time; Factorial design; Fast-dissolving tablets; Microcrystalline cellulose; Pain; Paracetamol; Tablet dissolution rate
HIGHLIGHTS
A simple 31 factorial design was applied to prepare new APAP tablets for quick pain relief.
APAP tablets with CCS disintegrate quicker than Panadol® and Amidol® tablets.
Significantly, APAP tablets with CCS dissolve much faster than Panadol® and Amidol® tablets.
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(A) The hardness values of batches B1, B2 and B3. (B) The hardness values of B3, Amidol® and Panadol® . Data are presented as mean ± SD (n=3). Where: ns: statistically insignificant; * and **: p< 0.050 and 0.01.
Data are presented as mean ± SD (n=3). Where: * and **: p<0.050 and 0.01.
(A) The disintegration time of tablets of batches B1, B2 and B3. (B) The disintegration time for tablets of batch B3, Amidol® and Panadol® tablets. Data are presented as mean ± SD (n = 6). Where: ns; statistically insignificant, *, ***: p< 0.050, 0.001.
(A) The cumulative dissolution curves for batches B1, B2 and B3. (B) The cumulative dissolution curves for batch B3, Amidol® and Panadol® . Data are presented as mean ± SD (n = 3), where: *, **: p < 0.050 and 0.010.