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Orally disintegrating granules (ODGs) are a pharmaceutical form commonly used for the administration of NSAIDs because of their easy assumption and fast dispersion. The development of ODGs is not easy for drugs like dexketoprofen trometamol (DXKT), which have a bitter and burning taste. In this work, high-shear coating (HSC) was used as an innovative technique for DKXT taste masking. This study focused on coating DXKT granules using the HSC technique with a low-melting lipid excipient, glyceryl distearate (GDS). The HSC technique allowed for the coating to be developed through the thermal rise resulting from the friction generated by the granules movement inside the equipment, causing the coating excipient to soften. The design of the experiment was used to find the best experimental coating conditions in order to gain effective taste masking by suitably reducing the amount of drug released in the oral cavity. The influence of the granule dimensions was also investigated. Coating effectiveness was evaluated using a simulated saliva dissolution test. It was found that low impeller speed (300 rpm) and a 20% coating excipient were effective in suitably reducing the drug dissolution rate and then in taste masking. The coated granules were characterized for their morphology and solid-state properties by SEM, BET, XRPD, DSC, and NIR analyses. A human taste panel test confirmed the masking of DXKT taste in the selected batch granules. [ABSTRACT FROM AUTHOR]

• Mesoporous silica: carriers for glibenclamide tablets with improved dissolution rate • The examined silicas parameters were ranked by importance order: pairwise comparison • Data statistical treatment enabled a systematic classification of the silicas and selection of the best. • Data statistical treatment enabled classification and selection of the best silicas. • Syloid®XDP3150 was the most effective silica in enhancing drug dissolution properties. This work evaluated the suitability of various mesoporous silicas as carriers for developing an oral formulation endowed with improved dissolution properties of glibenclamide, hypoglycemic agent poorly water-soluble. The different silicas were examined for solid-state, morphology, and technological and physical-chemical properties (granulometry, specific surface area, wettability, water content, water activity, apparent density, flowability, compactability). A pairwise comparison allowed a ranking, by importance order, of the parameters examined and, for each parameter, a score was assigned to each silica type. Data statistical treatment (JMP software) indicated Neusilin®US2 and Syloid®XDP3150 as the best materials. Different loading methods were tested: physical mixing; addition of drug dissolved in a volatile solvent, subsequently evaporated; addition of drug dissolved in a solvent. Methods involving drug dissolution enabled drug amorphization and intimate dispersion within the silica porous structure. Dissolution tests indicated Syloid®XDP3150 as the most effective silica in enhancing drug dissolution properties, providing a release rate clearly faster than from commercial tablets. Drug amorphization, improved wettability, increased surface area of the drug, finely dispersed into the highly porous silica, were the main factors responsible for this finding. Moreover, the obtained results suggested that drug dissolution rate can be properly tuned, based on the suited choice of the silica type. [ABSTRACT FROM AUTHOR]

The aim of this work was to evaluate the effectiveness of mesoporous clays or silicas to develop fast-dissolving glyburide tablets based on a liquisolid approach. Selected clay (Neusilin®US2) and silica (Aeroperl®300) allowed preparation of innovative drug liquisolid systems containing dimethylacetamide or 2-pyrrolidone as drug solvents, without using coating materials which are necessary in conventional systems. The obtained liquisolid powders were characterized for solid-state properties, flowability, compressibility, morphology, granulometry, and then used for directly compressed tablet preparation. The developed liquisolid tablets provided a marked drug dissolution increase, reaching 98% dissolved drug after 60 min, compared to 40% and 50% obtained from a reference tablet containing the plain drug, and a commercial tablet. The improved glyburide dissolution was attributed to its increased wetting properties and surface area, due to its amorphization/solubilization within the liquisolid matrix, as confirmed by DSC and PXRD studies. Mesoporous clay and silica, owing to their excellent adsorbent, flow, and compressibility properties, avoided use of coating materials and considerably improved liquid-loading capacity, reducing the carrier amount necessary to obtain freely flowing powders. Neusilin®US2 showed a superior performance than Aeroperl®300 in terms of the tablet's technological properties. Finally, simplicity and cost-effectiveness of the proposed approach make it particularly advantageous for industrial scale-up. [ABSTRACT FROM AUTHOR]

The performance of a series of inorganic salts as direct compression excipients was systematically evaluated. The physical-chemical and technological properties of the different salts were investigated in terms of crystalline/amorphous state, morphology, granulometry, apparent/tapped density, specific surface area, flowability, compressibility, dilution and distribution coefficients. To achieve a comprehensive evaluation of the performance of the different salts, the data obtained by the various analyses were normalized, giving a score to each excipient for each evaluated property/parameter. Statistical elaboration (JMP software) of the full dataset provided a final ranking of the powders based on their effectiveness as direct compression excipients. The salt emerged as the best was used to prepare direct-compression tablets, using cefixime as model drug, by modifying the composition of marketed tablets. A significant improvement of the mechanical properties of the new tablets was observed, compared to the marketed ones, with a crushing strength increase of over 30%, without variations of the drug dissolution profile. Even though the resulted ranking cannot have an absolute value, being the behavior of the different excipients susceptible to the kind of drug and other formulation excipients, the proposed approach can provide a useful model for a systematic evaluation and comparison of potentially similar excipients. [ABSTRACT FROM AUTHOR]

The aim of this work was to develop effective fast-dissolving tablet formulations of glyburide, endowed with improved dissolution and technological properties, investigating the actual effectiveness of the Solid-Self MicroEmulsifying Drug Delivery System (S-SMEDDS) approach. An initial screening aimed to determine the solubility of the drug in different oils, Surfactants and CoSurfactants allowed the selection of the most suitable components for liquid SMEDDS, whose relative amounts were defined by the construction of pseudo-ternary phase diagrams. The selected liquid SMEDDS formulations (Capyol 90 as oil, Tween 20 as Surfactant and Glycofurol or Transcutol as CoSurfactant) were converted into Solid-SMEDDS, by adsorbing them onto Neusilin (1:1 and 1:0.8 w/w S-SMEDDS:carrier), and fully characterized in terms of solid state (DSC and X-ray powder diffraction), morphological (ESEM) and dissolution properties, particle size and reconstitution ability. Finally, the 1:1 S-SMEDDS containing Glycofurol as CoSurfactant, showing the best performance, was selected to prepare two final tablet formulations. The ratio test ( t 10 min ratio and DE60 ratio) and pair-wise procedures (difference ( f 1 ) and similarity ( f 2 ) factors) highlighted the similarity of the new developed tablets and the marked difference between their drug dissolution profiles and those of formulations based on the micronized drug. The S-SMEDDS approach allowed to develop fast-dissolving tablets of glyburide, endowed with good technological properties and able to achieve the complete drug dissolution in a time ranging from 10 to 15 min, depending on the formulation composition. [ABSTRACT FROM AUTHOR]

Abstract: The aim of this work was to develop and validate a method to assess the dissolution behaviour of rociverine sugar-coated tablets. In our laboratories, an HPLC–MS in reverse phase method of analysis was developed for the dosage of unknown rociverine solution. This analytical method was applied to determine the dissolution rate of rociverine tablets produced by the industrial procedure, because there is no official method description. Dissolution tests were carried out in sink conditions as follows: dissolution medium HCl 0.01N, paddle rotation speed 50rpm and vessel volume 1000ml. The dissolution test gave satisfactory results: 95% of the drug was dissolved within 30min and drug dissolution was concluded after 60min. The method was demonstrated to be adequate for Quality Control of rociverine tablets. Validation was inferred from specificity, linearity, precision, accuracy and robustness. [Copyright &y& Elsevier]