Evaluation Of Local Gum Of Acacia Polyacantha As A Binder In Tablet Formulations

Acacia gums are dried gummy exudates obtained from the stems and branches of acaica spp.rn(fam. Leguminosae). A. senegal is the source of most gum arabic of international trade and itrnfinds wide applications in pharmaceutical, food and cosmetic industries. Other African acaciarnspecies of economic importance include A. seyal, A. drepanolobium and A. polyacantha. Inrnthis study, a local gum of A. polyacantha was evaluated as a tablet binder. Paracetamol andrnchloroquine phosphate were used as model drugs. The physico-chemical properties of thernpurified gum, and its rheological properties were investigated. The gum was found to havernsimilar properties to Acacia BP (odourless, white to yellowish brown, glassy, no tannins, nornstarch or dextrin present and moisture content of 11.6%). It exhibited Newtonian flow up torn40% w/v solution but less viscosity than Acacia BP. Granules prepared with differentrnconcentrations (5 - 30% w/v for paracetamol and 5-20% w/v for chloroquine phosphate) ofrnthe gum mucilage were characterised for particle size distribution, bulk, tapped and truerndensities, friability and flow properties. The granules were mixed with Ac-Di-SolÒ (4%) andrnmagnesium stearate (0.5%) and compressed into tablets at different compression forces. Thernoptimum binder concentration (X1) and compression force (X2) (independent variables) ofrnboth substances (paracetamol and chloroquine phosphate) were investigated using 22 factorialrndesign taking crushing strength (H), disintegration (DT) and friability (Fr) as responsernvariables. Polynomial equations were generated for the responses (H = 84.175 + 26.825X1 +rn33.375X2 + 5.625X1X2; DT = 9.24 + 8.38X1 + 4.59X2 + 4.45X1X2; Fr = 1.9725 – 0.7775X1 –rn1.1225X2 + 0.6275X1X2 for paracetamol and, H = 118.8 + 12.35X1 + 48.05X2 – 1.7X1X2; DTrn= 8.375 + 1.125X1 + 3.875X2 – 0.375X1X2; Fr = 1.08 – 0.22X1 – 0.42X2 + 0.08X1X2 forrnchloroquine phosphate). Surface response curves and contour plots were constructed and thernxi vrnoptimum regions determined by superimposing the contour plots. The optimum values werernre-transformed using the equation: Trans = [2A – (Max + Min)]/ Max – Min, where Trans isrnthe transformed value, A is the actual value of the factor being transformed, and Max and Minrnare the maximum and the minimum values in the range of the factor being transformed,rnrespectively. Granules of the optimum formulations (6.21% w/w of binder for paracetamol,rnand 1.386% w/w of binder for chloroquine phosphate) prepared had mean bulk densities ofrn0.41 and 0.508 g/ml, tapped densities 0.474 and 0.584 g/ml, Carr’s indexes of 13.58 andrn13.01% and Hausner ratios of 1.16 and 1.15 for paracetamol and chloroquine phosphate,rnrespectively. Tablets compressed at compression force of 14 KN (paracetamol) and 16 KNrn(chloroquine phosphate) were compared with predicted values (H: 122 and 119N, DT: 15 andrn8.5 minutes and Fr: 0.6 and 0.9% for paracetamol and chloroquine phosphate, respectively).rnTablets prepared with the gum showed H of 132 and 116N for paracetamol and chloroquinernphosphate, respectively, and Fr of 0.9% for both substances. For comparison purposes,rnchloroquine phosphate tablets were prepared with 5% w/v PVP solution and H values ofrn122N and Fr of 0.9% were obtained. The DTs of the tablets made with the gum were 13 andrn9.3 minutes for paracetamol and chloroquine phosphate, respectively. Dissolution profiles ofrnthe tablets were within the acceptable ranges (³ 80 and ³ 75% of drug release in 30 and 45rnminutes for paracetamol and chloroquine phosphate, respectively). The respectiveT50s were 5rnand 8 minutes. From the foregoing, it can be concluded that gum of A. polyacantha can bernused as an alternative binder in tablet formulations.

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