Promethazine HCl is a first generation H1 receptor antagonist used medically as an antihistamine and antiemetic. It is an effective and well tolerated antiemetic, especially used in motion sickness condition. It has been associated with a wide variety of chemotherapy and radiotherapy regimens, but in conventional dosage forms it undergoes first pass metabolism where the oral bioavailability (88%) was reduced to 27%.
The present study is an attempt to develop and formulate rapid dissolving tablets of Promethazine HCl, with superdisintegrants which disintegrates in matter of seconds in the oral cavity, thereby reducing the time of onset of pharmacological action and to prevent the first pass metabolism of Promethazine HCl.
The identification characterstics of drug like solubility, melting point, λmax were performed to findout the purity of drug. All the parameters observed were satisfactory and were within the prescribed official limits.
In this system direct compression method was used, microcrystalline cellulose (MCC) is used as a diluent, sodium starch glycolate (SSG), crosscarmellose and crospovidone were used as superdisintegrants, talc is used as flow promoter, magnesium sterate was used as lubricant, aspartame as sweetener and raspberry flavour is used to improve mouth feel.
The drug- polymer compatibility was confirmed by FTIR studies. The results obtained by FTIR studies revealed that there was no chemical interaction between the pure drug and excipients. Direct compression method was employed to formulate the tablets, because of its cost effectiveness and due to reduced number of manufacturing steps.
The pre-compression parameters like bulk density, tapped density, Carr’s ‘index and angle of repose were determined. The final formulation showed acceptable flow properties. The post-compression parameters like the thickness, hardness, friability and in vitro dispersion time, wetting time, water absorption ratio and in vitro drug release were carried out and the values were found to be within IP, BP limits.
The final optimized formulation of Promethazine HCl tablets containing 5% crospovidone (PF9) was compared with marked conventional tablets of Promethazine HCl (Phenargan) and the results reveled that formulated rapid dissolving tablets of Promethazine HCl were effective and better to meet patient compliance.
Hence based on the formulation development and their results, direct compression method is more suitable for Promethazine HCl rapid dissolving tablets in terms of palatability, physical and chemical properties better with reference product
