DEVELOPMENT AND EVALUATION OF DROTOVERINE TASTE MASKED TABLETS WITH IMPROVED DISSOLUTION EFFICIENCY USING SOLID DISPERSION TECHNIQUE
The purpose of this research is to mask the bitter taste of the drug, Drotoverine using solid dispersion technique. The taste-masked drug is formulated in to a conventional tablet by direct compression method for ease of administration. Taste masking was done by solid dispersion using polymer such as urea and mannitol by melting/fusion method Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM) were performed to identify the physicochemical interaction between drug and carrier, hence its effect on dissolution. Conventional taste masked tablets were evaluated for weight variation, disintegration time, hardness and friability. In vitro drug release studies were performed for conventional tablets of drotoverine. Bitterness score was evaluated on volunteers. FTIR spectroscopy and SEM showed no interaction between drug and carriers. Conventional tablets prepared using solid dispersion, showed faster disintegration and complete bitter taste masking of drotoverine. In addition the prepared tablets exhibited better dissolution profile. Taste evaluation of taste masked tablets in human volunteers rated tasteless with a score of 0. Thus, results conclusively demonstrated successful masking of taste and oral disintegration of the formulated tablets in the oral cavity with improved dissolution.
Design and evaluation of taste masked Drotaverine HCl orodispersible tablets using polymethacrylate polymers
The objective of this present study was to mask the in ensely bitter taste of drotaverine hydrochlorid e and to formulate orodispersible tablet. Taste masking w as done by complexing drotaverine HCl with polymethacrylate polymers (Eudragit E100 and Eudrag it RD100) by solvent evaporation technique. The drug: polymer ratio was (1:10) with drug content 40 mg. The granules of two optimized drug-polymer complexes (DPCs) were tested for packing and flow p roperties. These granules were compressed into tablets and evaluated for hardness, friability, dru g content, wetting, in vitro disintegration time an d in vitro taste in simulated salivary fluid (SSF) of pH 6.2. Their dissolution profiles (i.e. F 1 and F2) were compared with commercial formulation (MKT). The opt imized formulations were further characterized with Fourier-Transform Infrared Spectroscopy (FTIR) to investigate any interactions between the drug and the added excipients. The granules of the optim ized DPCs were free flowing with angle of repose <28. The DPCs tablets (i.e. F1 and F2) had hardness an d friability values of ≥ 4kg/cm and <0.9% respectively. These tablets disintegrated rapidly (<75sec) with a wetting time of ≤22sec. It also showed rapid drug release in stimulated gastric fluid (SGF ) compared with marketed formulation. For instance, the maximum release of drotaverine hydrochloride in F1, F2 and MKT were achieved in 30, 15 and 90mins respectively. Taste evaluation of the DPCs t able s (F1 and F2) in human volunteers revealed considerable taste masking with the degree of bitte rness below threshold value. There were also no drug/excipient interactions. This study shows the s uitability of polymethacrylate polymers (Eudragit E 100 and Eudragit RD100) in masking the bitter taste of or dispersible tablets of drotaverine HCl.
THE DISSOLUTION PROCEDURE : DEVELOPMENT AND VALIDATION
1092 The Dissolution Procedure: Development and Validation, USP 36 page 735. This general information chapter is proposed for revision by the General Chapters—Dosage Forms Expert Committee. The proposed chapter content replaces the entire current chapter. The proposed changes are discussed in a Stimuli to the Revision Process article published in this issue of PF. Additionally, minor editorial changes have been made to update the chapter to current USP style. The USP dissolution procedure is a performance test applicable to many dosage forms. It is one test in a series of tests that constitute the dosage form's public specification (tests, procedures for the tests, acceptance criteria). To satisfy the performance test, USP provides the general test chapters Disintegration 701 , Dissolution 711 , and Drug Release 724. These chapters provide information about conditions of the procedure. For dissolution, these include information about (1) medium, (2) apparatus/agitation rate, (3) study design, (4) assay, and (5) acceptance criteria. Overall the dissolution procedure yields data to allow an accept/reject decision relative to the acceptance criteria, which are frequently based on a regulatory decision. This chapter provides recommendations on how to develop and validate a dissolution procedure. GENERAL COMMENTS The dissolution procedure requires an apparatus, a dissolution medium, and test conditions that provide a method that is discriminating yet sufficiently rugged and reproducible for day-today operation and capable of being transferred between laboratories. The acceptance criteria should be representative of multiple batches with the same nominal composition and manufacturing process, typically including key batches used in pivotal studies, and representative of performance in stability studies. The procedure should be appropriately discriminating, capable of distinguishing significant changes in a composition or manufacturing process that might be expected to affect in vivo performance. It is also possible for the procedure to show differences between batches when no significant difference is observed in vivo. This situation requires careful evaluation of whether the procedure is too sensitive or appropriately discriminating. Assessing the results from multiple batches that represent typical variability in composition and manufacturing parameters may assist in this evaluation. It is sometimes valuable to intentionally vary manufacturing parameters, such as lubrication, blend time, compression force, or drying parameters, to further characterize the discriminatory power of the procedure. With regard to stability, the dissolution test should appropriately reflect relevant changes in the drug product over time that are caused by temperature, humidity, photosensitivity, and other stresses. A properly designed …