Characterisation of a novel, multifunctional, co-processed excipient and its effect on release profile of paracetamol from tablets prepared by direct compression

Objective: To characterise a novel multifunctional pharmaceutical excipient and investigate its effect on paracetamol release from tablets prepared by direct compression. Methods: The excipient was prepared by co-processing gelatinized maize starch with sodium carboxymethyl cellulose and microcrystalline cellulose in a ratio of 2:1:1, dried and pulverized into powder. The excipient formulated was characterized using Fourier transform infrared spectroscopy and differential scanning calorimetry. The excipient was used to prepare batches of tablets by direct compression with drug-excipient ratios of 1:1, 1:2, 1:3 and 1:4. Parameters evaluated on tablets include crushing strength, friability and in vitro dissolution studies. Results: Differential scanning calorimetry analysis revealed a crystalline excipient while Fourier transform infrared spectroscopy showed no interaction between the excipient and paracetamol. Tablets from all the batches gave average crushing strength values between 3.47 and 4.88 kp. The 1:1 and 1:2 tablet batches were comparable to each other while 1:3 and 1:4 were also comparable to one another in their dissolution profiles. The dissolution parameters of the 1:4 batch was faster with - m

Formulation and in vitro release studies of pegylated mucin based matrix tablets

The effects of polymer concentration on the flow properties of granules and in-vitro release profiles from matrix tablets of three model drugs formulated from pegylated mucin base was investigated. Mucin was extracted from the African giant snail and in combination with PEG was used to produce a copolymer matrix base, which was mixed with the model drugs using wet granulation method. The granules and tablets were evaluated according to official and unofficial requirements. Results showed best flow with Acetylsalicylic acid [ASA] and Chloroquine Phosphate [CQ] granules with Hausner ratio of 1.04-1.2, Carr's index of 4.2-17.5% and angle of repose between 19°-26°. The tablets met B.P specifications with respect to tablet weights, friability and drug content. The release profiles showed faster release of the drug with high content of PEG and a slower release with high concentration of mucin. Pegylated mucin base will find useful application in the development of a wide range of formulations

Influence of formulation technique on acrylate methacrylate copolymer modified paracetamol matrix tablets

This work was designed to evaluate the influence of various methods such as dry granulation [DG], wet granulation [using the polymer in an ethanolic solution [WGO] or aqueous dispersion [WGA] and solid dispersion [SD] techniques, on properties of paracetamol matrix tablets prepared using varying concentrations of acrylate methacrylate copolymer. Tablet properties were investigated using official and unofficial standards. Drug dissolution profile assessed at pH 1.2 was studied spectrophotometrically at lambda[max] of 245 nm. With the use of various kinetic models, the release mechanism of the drug was analyzed. The parameters, maximum amount of drug release [m[infinity]] at time t[infinity] were obtained, m[infinity] was >/= 91.36 %, while t[infinity] was >/= 4.5 h. The release rate constant [k] for DG tablets was 15.61 h[-1], while, WGO, WGA and SD tablets were 12.90, 11.03 and 10.75 h[-1] respectively. The matrix tablets, which exhibited marked retardation in drug release displayed a Higuchi square root of time model [R[2] > 0.98]. The mechanism through which the drug was released was governed by Fickian diffusion release [n values < 0.5]. The performance of the drug was affected by the formulation technique in the order of SD > WGO > WGA > DG