Release Kinetics of Papaverine Hydrochloride from Tablets with Different Excipients

Abstract

The influence of excipients on the disintegration times of tablets and the release of papaverine hydrochloride (PAP) from tablets were studied. Ten different formulations of tablets with PAP were prepared by direct powder compression. Different binders, disintegrants, fillers, and lubricants were used as excipients. The release of PAP was carried out in the paddle apparatus using 0.1 N HCl as a dissolution medium. The results of the disintegration times of tablets showed that six formulations can be classified as fast dissolving tablets (FDT). FDT formulations contained Avicel PH 101, Avicel PH 102, mannitol, (3-lactose, PVP K 10, gelatinized starch (CPharmGel), Prosolv Easy Tab, Prosolv SMCC 90, magnesium stearate, and the addition of disintegrants such as AcDiSol and Kollidon CL. Drug release kinetics were estimated by the zero- and first-order, Higuchi release rate, and Korsmeyer-Peppas models. Two formulations of the tablets containing PVP (K10) (10%), CPharmGel (10% and 25%), and Prosolv Easy Tab (44% and 60%) without the addition of a disintegrant were well-fitted to the kinetics models such as the Higuchi and zero-order, which are suitable for controlled- or sustained-release.

Influence of Polymer Type on the Physical Properties and Release Profile of Papaverine Hydrochloride From Hard Gelatin Capsules

“…A delaying of the release of PAP (especially within the first five minutes) came from a conversion of polyvinylpyrrolidone to CPharmGel, potato starch or hypromellose 10k. Similar results were observed for tablets containing CPharmGel [15]. Also, granulates with PAP containing polyvinylpyrrolidone had the best flow rates and slightly longer disintegration time, while tablets produced from them slightly delayed release [16].…”

“…There have been a few reports about the influence of polymer PAP release from tablets [15,16], but there are none which concern powders or capsules containing PAP. The purpose of the present study was to examine the effects of different polymers with all other components unchanged, on the physical properties of powders and capsules together with the release profile of the model substance.…”

Evaluation of the Physicochemical and Micromeritic Properties of Exudate Gum of Cussonia arborea Stem Bark in Conventional Tablet Formulation

“…Te pH of a potential excipient such as gum is among the important formulation critical parameters that decide its suitability in pharmaceutical formulations since it directly afects stability, application, and physiological characteristics of preparations [35]. CAPG will be an ideal excipient for formulating acidic, neutral, and weak basic drugs, such as Paracetamol [46] (Maswadeh, 2017), Diclofenac [47,48], Aspirin [49], Allopurinol [50], and Ibuprofen [51].…”