Fast Dissolving/Disintegrating Dosage Forms of Natural Active Compounds and Alternative Medicines.

Fast Dissolving/Disintegrating Dosage Forms (FDDFs) are a group of dosage forms which dissolve or disintegrate quickly, leading to fast distribution of active ingredients at the site of administration; thereby providing ease of oral ingestion of solid unit dosage forms and have the potential to enhance transmucosal absorption. With time, the use of FDDFs in alternative systems has significantly increased. Homeopathic systems and traditional Chinese medicine have embraced FDDFs for the delivery of active compounds. Most of the patents in this area are from China or by the Chinese innovators. In Europe and US, FDDFs have been extensively studied for the delivery of natural active compounds. It was fascinating to know that some new dosage forms and new routes of delivering active compounds are also making their way to the family of FDDFs. The dose of active compound, size of dosage forms, standardization of extracts, polyherbal mixtures, stability of active compounds, safety, efficacy and pharmacokinetics are challenging issues for developing FDDF herbal formulations or phytopharmaceuticals.

Formulation and characterization of taste masked ondansetron-magnesium aluminum silicate adsorption systems.

CONTEXT: Taste masking greatly influences the acceptability of bitter tasting formulation; moreover, it governs the commercial and therapeutic success of drug products. OBJECTIVE: This work is directed toward masking the bitter taste of ondansetron HCl (ONS) utilizing the excipient, which can delay the reach of drug to the taste buds. MATERIAL AND METHODS: Magnesium aluminum silicate (Veegum F), a clay material having capability to adsorb the drugs onto it, was used. The adsorption systems of ONS with Veegum were obtained by dynamic adsorption technique and examined by scanning electron microscopy, differential scanning calorimetry, Fourier transform infrared (FTIR) spectroscopy, and X-ray diffraction (XRD) for morphology, thermal behavior, and interactions. The taste assessment of prepared systems was done by in vitro method based on drug release. RESULTS: The molecular interaction between ONS and Veegum in the system was revealed by FTIR spectroscopy. A change in thermal behavior of the system was observed owing to interaction or replacement of the cationic groups of Veegum with that of ONS. XRD studies revealed that the prepared system was having lower crystallinity as compared to ONS. The in vitro drug release study showed that ONS release from the system was relatively slow in basic environment than the acidic one. DISCUSSION: Adsorption of ONS on the surface of Veegum was mainly due to electrostatic interactions and hydrogen bonding. CONCLUSION: The experimental results reveal the successful intercalation of ONS into the space available between the layers of Veegum. Furthermore, this resulted in a control on drug release in salivary pH resulting in a concentration lower than bitterness threshold.

Formulation and evaluation of lipid based taste masked granules of ondansetron HCl.

INTRODUCTION AND AIM: Various taste masking approaches comprising the excipients which delay the reach of the drug to taste buds are reported. Lipidic substances can act as release retarding agent and provides a matrix base responsible for suppressing the bitter taste of drug. This work was aimed to study the influence of different proportions of a lipid carrier on the inhibition of bitterness of the drug vis-a-vis in vitro release of drug from the granules. METHODS: The lipid-matrix granules of ondansetron HCl with Geleol pellets (glycerol monostearate) were obtained by manual hot melt fusion technique. The prepared granules were characterized by SEM, DSC and XRD. The taste assessment of prepared granules was done by in vitro method based on drug release. RESULTS: Distribution of drug inside the lipid-matrix granules was not properly analyzed by DSC and XRD, moreover these studies revealed no interaction between the drug and lipid. The dissolution tests displayed the significant retardation of drug release from the granules compared to pure drug and additionally indicated the attainment of matrix system via appearance of unbroken granules during in vitro testing. Higuchi relationship for drug release was obtained by drug release kinetics, which also revealed the functioning drug release mechanism, as diffusion controlled but the addition of hydrophilic substance (Cab-o-sil) has changed the mechanism of drug release. CONCLUSION: The proportions of Geleol and Cab-o-sil taken in granules had affected the dissolution profile. Higher amount of GE resulted in high taste masking ability.

Formulation, evaluation and 3(2) full factorial design-based optimization of ondansetron hydrochloride incorporated taste masked microspheres.

CONTEXT: Masking the bitter taste of Ondansetron hydrochloride (ONS) may improve palatability, acceptance and compliance of ONS products. OBJECTIVE: ONS-loaded, taste-masked microspheres were prepared with a polycationic pH-sensitive polymer and 3(2) full factorial design (FFD) was applied to optimize microsphere batches. MATERIALS AND METHODS: Solvent evaporation, in acetone--methanol/liquid paraffin system, was used to prepare taste-masked ONS microspheres. The effect of varying drug/polymer (D/P) ratios on microspheres characteristics were studied by 3(2) FFD. Desirability function was used to search the optimum formulation. Microspheres were evaluated by FTIR, XRD and DSC to examine interaction and effect of microencapsulation process. In vitro taste assessment approach based on bitterness threshold and drug release was used to assess bitterness scores. RESULTS: Prepared ONS microspheres were spherical and surface was wrinkled. ONS was molecularly dispersed in microspheres without any incompatibility with EE100. In hydrochloric acid buffer pH 1.2, ONS released completely from microsphere in just 10 min. Contrary to this, ONS release at initial 5 min from taste-masked microspheres was less than the bitterness threshold. CONCLUSION: Full factorial design and in vitro taste assessment approach, coupled together, was successfully applied to develop and optimize batches of ONS incorporated taste-masked microspheres.

Taste assessment trials for sensory analysis of oral pharmaceutical products.

Taste assessment trials are conducted with an aim to evaluate taste of tastants (food, chemical, drug etc.) and involve estimation of gustatory sensation responses in healthy human volunteers within well controlled procedures. Taste assessment trials are the standard and so far preferred method of taste assessment. Several in vitro taste assessment approaches have emerged as subsidiary methods but none could replace Taste assessment trials. The article provides an overview on conduct of taste assessment trials in healthy adult human volunteers and children.