Search

The aim of the present study was to formulate polymer microspheres using the emulsion solvent evaporation technique as an approach to mask the bitter taste of enalapril maleate. Five models were prepared with two water-insoluble polymers. Talc was used to stabilize the particle structure. Production yields ranged from 38 % to 53 %; drug loading varied between 17 % and 40 %; the mean particle size ranged from 140 µm to 339 µm. No interaction between enalapril and the polymers was estimated. A drug release study in artificial saliva indicated a negligible amount of enalapril dissolved in the test medium which demonstrated successful taste masking. [ABSTRACT FROM AUTHOR]

The preparation of microspheres by emulsion solvent evaporation technique has become an area of considerable attention in pharmaceutical industry. In the present study, investigation reports the formulation of microspheres of levofloxacin using ethyl cellulose and Eudragit L100 in order to mask the bitter taste of drug. Ten microsphere formulations F1 to F10 were fabricated by varying the ratio of polymers at different stirring speed (700-850 rpm). Particle size, shape, flow properties, encapsulation efficiency and in vitro release profile of the prepared microspheres were studied. Fourier-transform infrared spectroscopy and differential scanning calorimetry showed no significant drug polymer interaction. Kinetic modelling results demonstrated that release data was best fit to Korsmeyer-Peppas model suggesting non-Fickian behaviour. Taste masking was evaluated using a five-point scale of taste evaluation. Taste of the drug was significantly concealed (p<0.05). F3 showed excellent taste concealing and considered as the most palatable formulation. In conclusion, formulated microparticles of levofloxacin could increase patient compliance and palatability. [ABSTRACT FROM AUTHOR]

The oral route of drug administration is mostly preferred by paediatric and geriatric patients. Patient non-compliance due to poor taste and swallowing problems are major issues in paediatric and geriatric drug therapy. Lack of age-appropriate formulations, inadequate labelling instructions, non-compatible and non-palatable medicines are the main reasons for medication errors in paediatric patients. This review mainly highlights major issues of paediatric and geriatric drug therapy and provides the design of oral flexible formulations as an alternative formulation design for age appropriate formulation development. Development of solid oral flexible formulations as an alternative to existing marketed formulations such as conventional tablets, orally disintegrating tablets, chewable and dispersible tablets for paediatric and geriatrics patients is described. Details about drug properties, excipient selection and taste masking approaches were described. The need for bioavailability and bioequivalence studies for flexible formulations also described. Development of flexible formulations as an alternative to marketed different formulations of the same drug would reduce the cost of the formulation for patients particularly developing countries where accessibility to various types of formulations is less. Flexible tablet formulations can be conveniently used by the patients as orally swallowable, orally disintegrating, chewable and as dispersible tablets. Sprinkle formulations such as pellets, granules packed in capsules or sachets can be conveniently used by paediatric and geriatric patients. Properly designed and developed flexible formulations for new chemical entities and off-patent drugs are need of the hour to provide better treatment to varying age groups of paediatrics and geriatrics. [ABSTRACT FROM AUTHOR]

Ion exchange resins are water-insoluble, cross-linked polymers containing salt-forming groups in repeating positions on the polymer chain. Bitter cationic drugs get adsorbed on to weak cationic exchange resins of carboxylic acid functionality like Indion 204, Indion 234 and Tulsion 335 to forms non-bitter complexes. The present investigation aims at taste masking of the bitter clarithromycin using ion exchange resins, which forms complexes, inhibiting its release in saliva. The drug-resin complex loading process was optimized for the content of resin, activation, swelling time, stirring time, influence of pH and temperature for maximum drug loading and was subjected to differential scanning calorimetry to confirm the complex formation. These complexes were used to prepare chewable tablets and to evaluate the taste. Acid-activated resins comprising of Indion 204, Indion 234 and Tulsion 335 with drug:resin ratio of 1:2, stirred in solution of pH 7-8 at 70° for 6 h had a maximum drug loading and masked the bitter taste of clarithromycin. Differential scanning calorimetry of the drug-resin complex revealed that there was interaction leading to complex formation. The drug-resin complex was formulated into chewable tablet formulations (F1-F9) and evaluated. Various pre- and post-compression parameters were found to be within permissible limits. Formulations F3, F6 and F9 containing 1:2 ratios of drug-resin complex of Indion 204, Indion 234 and Tulsion 335 revealed maximum taste masking. This was further confirmed by treatment of taste evaluation scores of the volunteers by ANOVA, Dunnets multiple comparison test and Tukey's multiple comparison test. All the three optimized formulations had a significant difference of P<0.001 when compared to control F10. F6 formulation was widely accepted. Ion exchange complexation could efficiently mask the bitter taste of clarithromycin and achieve palatable taste suitable for paediatric use. [ABSTRACT FROM AUTHOR]

Taste masked microspheres of ornidazole were prepared using amino alkyl methacrylate copolymers (Eudragit E-100) by solvent evaporation technique. Taste assessment of these microspheres was done by both spectrophotometric taste evaluation technique and panel testing. Compressed tablets of taste masked ornidazole microspheres which rapidly disintegrated in the oral cavity were prepared using microcrystalline cellulose as directly compressible filler and sodium starch glycolate as a super-disintegrant. These were subsequently evaluated for various pharmacopoeial tests, drug release, and disintegration time in the oral cavity. Sensory taste evaluation was carried by panel testing in 20 healthy human volunteers. Results indicate successful formulation of oral fast disintegrating tablets which disintegrated in the oral cavity in about 30 s and possessed good taste. [ABSTRACT FROM AUTHOR]

An attempt was made to sustain the release of metformin HCl as well as to mask the bitter taste by complexation technique using strong cation-exchange resins, indion 244 and indion 264. The drug loading onto ion-exchange resin was optimized for mixing time, activation, effect of pH, mode of mixing, ratio of drug:resin and temperature. The resinate was evaluated for micromeritic properties, taste masking and characterized using XRPD and IR. Using resinate sustained release tablets were formulated using hydoxypropylmethylcellulose K100M. The tablets were evaluated for hardness, thickness, friability, drug content, weight variation and in vitro drug release. Tablets thus formulated (Batch B-6) provided sustained release of drug over a period of 10 h with first order kinetics. The release of metformin HCl from resinate controls the diffusion of drug molecules through the polymeric material into aqueous medium. Results showed that metformin HCl was successfully taste masked and formulated into a sustained dosage form as an alternative to the conventional tablet. [ABSTRACT FROM AUTHOR]

Natural resources in general and plant materials in particular are receiving more attention due to their safety as pharmaceutical excipients. Present work assessed the potential of a natural polysaccharide, pectin to mask the bitter taste of ambroxol hydrochloride, by microencapsulation technique, and its possibility to formulate as a fast disintegrating dosage form. Taste masking is an important developmental challenge in fast dissolving drug delivery system since it dissolves or disintegrates in the patient's mouth in close proximity to the taste buds. The prepared microspheres by emulsion solvent evaporation technique possessed good sphericity, smooth surface morphology, uniform and narrow size distribution (10-90 µm), when analyzed by scanning electron microscopy, laser diffraction and optical microscopy. Method of preparation has influenced the particle size and drug loading efficiency. Drug-polymer compatibility was confirmed by Fourier transform infrared spectroscopy and thin layer chromatography. DSC and X-ray diffraction studies revealed that the drug was dispersed inside the microspheres in the form of an insoluble matrix. The formation of microspheres was affected by glass transition temperature of the polymer, surfactant, type of plasticizers, volume of internal phase, stirrer speed etc. Fast dissolving tablets were prepared by the modification of melt granulation technique. The resulting granules were found to melt fast at body temperature, have smooth mouth feel and good physical stability. This study demonstrated that pectin could be a right choice in developing patient favored formulations for bitter drugs and can be utilized in fast disintegrating dosage forms as well. [ABSTRACT FROM AUTHOR]

In the present study strong cation exchange resin (Amberlite IRP69) was used to improve the physicochemical properties of ranitidine hydrochloride such as taste and bulk properties and to sustain dissolution rate. Drug-resin complexes were prepared using batch method. Drug loading was done under different processing conditions such as temperature, pH, drug-resin ratio, and drug concentration to get the optimum condition for resinate preparation. Resinate prepared under optimized condition was tested for taste, bulk properties and release rate. Degree of bitterness of ranitidine was found to reduce to zero after complexation with resin. Improvement in flow properties was also observed. Angle of repose for resinate was found to be 33.21o as compared to 42.27o for ranitidine HCl. Effect of dissolution medium and particle size on in vitro release of drug from resinate was also investigated. Resinate with drug to resin ratio of 2:3 and particle size >90 µm showed about 90% of drug release within 12 h. The orodispersible tablet formulated from the resinate containing 10% croscarmellose sodium disintegrated within 35 sec in oral cavity and showed similar dissolution profile as the resinate. Tablets were found stable after stability studies with no change in dissolution profile. [ABSTRACT FROM AUTHOR]