Formulation and evaluation of a sublingual tablet containing terbutaline sulphate: optimisation and in vivo studies
Keywords:
Crospovidone, Factorial design, Microcrystalline cellulose, Optimisation, Sublingual tablets, Terbutaline sulphateAbstract
The objective of this research was to formulate a sublingual tablet formulation of terbutaline for rapidaction, and to improve both bioavailability and patient compliance to therapy. A wet granulation techniquewas adapted to prepare the granules. Granule formulations were prepared using an adapted wet granulationtechnique based on a 32 full factorial design. The formulation variables were expressed as follows;quantity of microcrystalline cellulose (MCC), (X1), and bioadhesive component crospovidone, (X2),while crushing strength, friability and disintegration time (DT) were determined as response variables.The main effects and interaction terms were quantitatively evaluated using a quadratic model. The resultsobtained showed that the quantity of MCC and crospovidone significantly affect response variables. Anoptimised tablet formulation, containing 31.5 mg of MCC and 4.5 mg of crospovidone, provides a shortDT of 30.2 + 5.5 sec with sufficient crushing strength and acceptable friability, while DT for serumconcentrations of terbutaline were obtained within 5 min. The results indicate that the inclusion ofcrospovidone, a bioadhesive component, in sublingual tablet formulations, makes the swallowing of tablets unnecessary, because the release and absorption of the terbutaline in such formulations isacceptably effective. In conclusion, the developed sublingual tablet formulations is of interest, becauseit can be extrapolated to other drugs, where rapid absorption is desirable.Downloads
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