Browsing by Author "Vikas Anand Saharan"

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A proposed methodology for in vitro evaluation of bitterness in drug solutions and in vitro drug release samples
(Springer New York LLC, 2014) Kapil Dev; Vandana Kharb; Anupama Singh; Vikas Anand Saharan; Hemant Jadhav; Suresh Purohit
Purpose: Ethical and safety concerns, paediatric taste panels and predictivity in early drug development for strategic decisions are some of the reasons for seeking in vitro methods of bitterness evaluation for drugs and drug products. In this study, taste panel studies and in vitro drug release studies have been performed, correlated to each other and proposed as an analytical tool for evaluation of bitterness. Methods: Bitterness threshold and bitterness scores for different solutions of ondansetron hydrochloride (ONS) were estimated by taste panel studies. In vitro drug release studies on taste-masked drug product in pharmacopoeial apparatus and an in-house-developed apparatus were performed and correlated to drug release studies in oral cavity. Results: Concentration of 22 μg/ml and below was perceived bitterless by all the volunteers of taste panel. A second-order polynomial equation (y = 0.6206x 2 - 0.2011x - 0.7796; correlation coefficient R 2 = 0.991) was derived as a relationship between bitterness score and log ONS concentration. Drug release in in-house-assembled apparatus and oral cavity were not statistically different (α = 0.05) at both 60 and 120 s. Conclusions: Bitterness threshold and bitterness scores are helpful in evaluation of bitterness in drug solutions and samples obtained from drug release studies. © 2014 Springer Science+Business Media.
Bitterness Score and its Correlation to Drug Concentration: An Approach for Estimating Bitterness Suppression in a Marketed Product of Ofloxacin
(Taylor and Francis Ltd., 2014) Vikas Anand Saharan; Kapil Dev; Vandana Kharb; Anupama Singh; Hemant Jadhav; Suresh Purohit
Abstract: In vitro approaches for assessing taste characteristics of taste masked drug and drug products are useful in reducing reliance on human panel tests. In this study, taste panel studies were used to determine bitterness threshold and bitterness score of various solutions of ofloxacin followed by correlation and the application of this approach in estimating bitterness suppression. Bitterness scores for different solutions of ofloxacin were estimated by trained human volunteers of a taste panel. Bitterness scores were correlated to ofloxacin concentration followed by determination of bitterness scores for various dissolution samples obtained from in vitro drug release study of ofloxacin taste masked drug product. Concentration of 80 µg/ml and below was perceived bitterless by all the volunteers of taste panel. A third order polynomial equation (y=13.51x3-91.08x2+206.7x-156.6; R2 = 0.973) was derived as a relationship between bitterness score (y) and log ofloxacin concentration (x). Marketed taste masked product achieved concentrations below bitterness threshold in in vitro drug release studies performed in pharmacopoeial apparatus at initial time points (0-5 min). Bitterness threshold and bitterness scores are helpful in estimating bitterness of ofloxacin solutions provided suitable correlation has been found between them. The suggested approach, which is applicable to any bitter or objectionable tasting drug, has potential to be used as analytical tool in formulation development and quality control. © 2014, Har Krishan Bhalla & Sons.
Formulation and characterization of taste masked ondansetron-magnesium aluminum silicate adsorption systems
(Taylor and Francis Ltd., 2016) Vandana Kharb; Vikas Anand Saharan; Vivek Kharb; Hemant Jadhav; Suresh Purohit
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. © 2016 Informa UK Limited, trading as Taylor & Francis Group.
Formulation and evaluation of lipid based taste masked granules of ondansetron HCl
(Elsevier, 2014) Vandana Kharb; Vikas Anand Saharan; Vivek Kharb; Hemant Jadhav; Suresh Purohit
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. © 2014 Elsevier B.V. All rights reserved.
Formulation, evaluation and 32 full factorial design-based optimization of Ondansetron hydrochloride incorporated taste masked microspheres
(Informa Healthcare, 2014) Vandana Kharb; Vikas Anand Saharan; Kapil Dev; Hemant Jadhav; Suresh Purohit
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 pHsensitive polymer and 32 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 32 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. © 2014 Informa Healthcare USA, Inc.