Rapid and correct production of generic solid dosage forms requires a large amount of analytical data and conclusions. Modern analytical techniques have a good resolution and accuracy and allow obtaining a lot of information about the original product. Scanning electron microscopy (SEM) is used for observation and assessing individual layers, core and surface of solid dosage forms. Fourier transform infrared (FTIR) spectroscopy mapping allows determining the distribution and characterization of individual components in a solid dosage form. However, the samples prepared by common way, using scalpel or tablet splitter, are not good enough. It was the reason for development of a new and better method of sample preparation, which uses microtome. Well-prepared samples analyzed by SEM and FTIR mapping allow to determine a solid dosage form formulation, excipient content and distribution of excipient and active pharmaceutical ingredient.

• MeSH
• chemie farmaceutická metody   MeSH
• lékové formy MeSH
• mikroskopie elektronová rastrovací metody   MeSH
• pomocné látky chemie   MeSH
• spektroskopie infračervená s Fourierovou transformací metody   MeSH
• tablety chemie   MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• lékové formy MeSH
• pomocné látky MeSH
• tablety MeSH

The presented review article is a compilation of several foreign reviews and experimental papers, as well as several authority guidelines, which deal with the phenomenon of dose dumping of solid dosage forms with modified drug release. The aim of the publication is to present this often-neglected issue to a wider domestic audience. The work deals with two basic types of dose dumping, i.e., alcohol-induced dose dumping and food-induced dose dumping. It contains basic factors affecting this phenomenon as well as possible formulation solutions that can be used to eliminate it. Last but not least, the current requirements of the authorities are also mentioned, especially for testing newly introduced products with the presumed potential risk of dose dumping.

• Klíčová slova
• alcohol, dose dumping, modified release, modified release dosage forms,
• MeSH
• chemie farmaceutická * MeSH
• ethanol * MeSH
• lékové formy MeSH
• léky s prodlouženým účinkem MeSH
• uvolňování léčiv MeSH
• Publikační typ
• časopisecké články MeSH
• přehledy MeSH
• Názvy látek
• ethanol * MeSH
• lékové formy MeSH
• léky s prodlouženým účinkem MeSH

A method of preparing tablets called liquisolid technique is currently emerging. In these formulations, an important role is played by porous carriers, which are the basic building blocks of liquisolid systems (LSSs). The most common are microcrystalline cellulose (MCC), magnesium aluminometasilicates, silica aerogels, mesoporous silicates, clays, etc. In this study, magnesium aluminometasilicate is used to prepare modified LSS formulations with plant extracts as model drugs dissolved in water (W) or ethanol (E). The modification involves drying tablets in a microwave (MW) and hot air dryer (HA) for a specified period. Powder blends and tablets were evaluated for physical properties, and their antioxidant activity (AA) was measured in a modified dissolution by ferric reducing antioxidant power assay (FRAP). PLS and ANOVA were used to compare tablets properties depending on the composition and technology. The experiment is based on a previous one, in which the plant extracts were processed into tablets using a similar method. Therefore, extending the study to include more plants and the robust statistical evaluation and comparison of the products was a procedure to justify the suitability of the presented method for a wide range of liquid plant extracts. As a result, we obtained tablets with excellent physical properties, including a short disintegration and dissolution, which is problematic in tableted extracts.

• Klíčová slova
• adsorption, antioxidant activity, liquisolid systems, magnesium aluminometasilicates, plant extracts, porous carriers,
• Publikační typ
• časopisecké články MeSH

This paper links up with Part I and deals with the other medicinal preparations, which were originally included in the Austrian book of prescriptions Dispensatorium pharmaceuticum Viennense and then taken over to the Austrian provincial pharmacopoeia Pharmacopoea austriaco-provincialis, repeatedly published between 1774 and 1794. This part discusses semisolid dosage forms, e.g. Electuaria, Mella, Pulpae, Unguenta, and solid dosage forms, e.g. Emplastra, Extracta, Morsulae, Pilulae, Pulveres, Rotulae, Tabulae, Trochisci. The final part of the paper also lists chemical substances (Chymica et consimilia) prepared in pharmacies and presents general evaluation of the provincial Pharmacopoeia.

• MeSH
• dějiny 18. století MeSH
• farmakopea jako téma dějiny   MeSH
• lékové formy MeSH
• Check Tag
• dějiny 18. století MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• historické články MeSH
• Geografické názvy
• Rakousko MeSH
• Názvy látek
• lékové formy MeSH

The polymeric cytisine-enriched fibers based on poly(3-hydroxybutyrate) were obtained using electrospinning method. The biocompatibility study, advanced thermal analysis and release of cytisine from the poly(3-hydroxybutyrate) fibers were carried out. The nanofibers' morphology was evaluated by scanning electron microscopy. The formation and description of phases during the thermal processes of fibers by the advanced thermal analysis were examined. The new quantitative thermal analysis of polymeric fibers with cytisine phases based on vibrational, solid and liquid heat capacities was presented. The apparent heat capacity of fibers was measured using the standard differential scanning calorimetry. The quantitative analysis allowed for the study of the glass transition and melting/crystallization process. The mobile amorphous fraction, degree of crystallinity and rigid amorphous fraction were determined depending on the thermal history of semicrystalline polymeric fibers. Furthermore, the cytisine dissolution behaviour was studied. It was observed that the kinetic of the release from polymeric nanofiber is delayed than for the marketed product. The immunosafety of the tested polymeric nanofibers with cytisine was confirmed by the Food and Drug Agency Guidance as well as the European Medicines Agency. The polymeric matrix with cytisine seems to be a promising candidate for the prolonged release formulation.

• Klíčová slova
• Cytisine, Differential scanning calorimetry, Electrospinning, Poly(3-hydroxybutyrate),
• MeSH
• diferenciální skenovací kalorimetrie MeSH
• kyselina 3-hydroxymáselná MeSH
• léky s prodlouženým účinkem chemie   MeSH
• nanovlákna * chemie   MeSH
• polymery * chemie   MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• cytisine MeSH Prohlížeč
• kyselina 3-hydroxymáselná MeSH
• léky s prodlouženým účinkem MeSH
• poly-beta-hydroxybutyrate MeSH Prohlížeč
• polymery * MeSH

A simple and rapid HPLC method was developed to determine terguride in terguride hydrogenmaleate, coated tablets and plasma. The assay was carried out on a glass column of SGX CN (150 x 3.3 mm I.D.) using methanol and phosphate buffer solution (pH 7.0) as the mobile phase, with detection at 227 nm. Terguride was quantified using promethazine as an internal standard. The tablet matrix was extracted into methanol. Plasma samples were deproteinated with acetonitrile and the supernatant was injected into the HPLC system. The method is linear, quantitative and reproducible.

• MeSH
• agonisté dopaminu analýza   krev   MeSH
• krysa rodu Rattus MeSH
• lisurid analogy a deriváty   analýza   krev   MeSH
• námelové alkaloidy izolace a purifikace   MeSH
• tablety MeSH
• vysokoúčinná kapalinová chromatografie MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• agonisté dopaminu MeSH
• dironyl MeSH Prohlížeč
• lisurid MeSH
• námelové alkaloidy MeSH
• tablety MeSH

The work was aimed at evaluating the efficiency of multifunctional magnesium aluminosilicate materials (MAS) as a novel glidant in solid dosage forms. MAS are known for their very low cohesive interactions and their utilization could avoid the disadvantages associated with conventional glidant usage. Flow properties of several mixtures comprising a model excipient (microcrystalline cellulose) and a glidant were characterized using a powder rheometer FT4. The mixtures were formulated to represent effects of glidant types, various levels of glidant loading, particle size and mixing time on flow properties of the model excipient. Pre-conditioning, shear testing, compressibility, flow energy measurements and an additional tapping test were carried out to monitor flow properties. Mixtures were analyzed employing scanning electron microscopy, using a detector of back-scattered electrons to identify a mechanism of MAS towards improving the mixture flow properties. All studied parameters were found to have substantial effects on mixture flow properties, but the effect of mixing time was much less important compared to mixtures based on traditional glidant. The mechanism of MAS glidant action was found to be different compared to that of traditional one, having less process sensitivity, so that MAS utilization as glidant could be advantageous for the formulation performance.

• Klíčová slova
• Flow properties, Flow-enhancer, Glidant, Magnesium aluminosilicate, Powder mixing, Powder rheology,
• MeSH
• pomocné látky * MeSH
• prášky, zásypy, pudry MeSH
• reologie MeSH
• silikáty * MeSH
• sloučeniny hliníku MeSH
• sloučeniny hořčíku MeSH
• velikost částic MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• aluminum magnesium silicate MeSH Prohlížeč
• pomocné látky * MeSH
• prášky, zásypy, pudry MeSH
• silikáty * MeSH
• sloučeniny hliníku MeSH
• sloučeniny hořčíku MeSH

High specific surface area (SSA), porous structure, and suitable technological characteristics (flow, compressibility) predetermine powder carriers to be used in pharmaceutical technology, especially in the formulation of liquisolid systems (LSS) and solid self-emulsifying delivery systems (s-SEDDS). Besides widely used microcrystalline cellulose, other promising materials include magnesium aluminometasilicates, mesoporous silicates, and silica aerogels. Clay minerals with laminar or fibrous internal structures also provide suitable properties for liquid drug incorporation. This work aimed at a comparison of 14 carriers' main properties. Cellulose derivatives, silica, silicates, and clay minerals were evaluated for flow properties, shear cell experiments, SSA, hygroscopicity, pH, particle size, and SEM. The most promising materials were magnesium aluminometasilicates, specifically Neusilin® US2, due to its proper flow, large SSA, etc. Innovative materials such as FujiSil® or Syloid® XDP 3050 were for their properties evaluated as suitable. The obtained data can help choose a suitable carrier for formulations where the liquid phase is incorporated into the solid dosage form. All measurements were conducted by the same methodology and under the same conditions, allowing a seamless comparison of property evaluation between carriers, for which available company or scientific sources do not qualify due to different measurements, conditions, instrumentation, etc.

• Klíčová slova
• adsorption, aluminometasilicates, liquisolid systems, pharmaceutical technology, powder carriers, solid dosage form,
• Publikační typ
• časopisecké články MeSH

Despite recent advances in solid-state NMR spectroscopy, the structural characterization of amorphous active pharmaceutical ingredients (APIs) in solid dosage forms continues to be a monumental challenge. To circumvent complications following from low concentrations of APIs in tablet formulations, we propose a new time-saving procedure based on chemometric approach: factor analysis of (19)F MAS NMR spectra. Capability of the proposed method is demonstrated on atorvastatin--a typical representative of fluorinated pharmaceutical substances exhibiting extensive polymorphism. Applying the factor analysis on the recorded (19)F MAS NMR spectra, unique parameters for every sample were derived. In this way every solid form of atorvastatin was characterized and clearly distinguishable even among various amorphous and disordered forms. The proposed method was also found to be suitable for both qualitative and quantitative analysis of mixtures of various forms of atorvastatin. Reliability of the proposed method was extensively examined by comparing the obtained results with other experimental techniques such as (13)C CP/MAS NMR, FTIR and XRPD. As highly linear correlations between the sets of parameters obtained from different experimental data were found, the perspectives of the applied comparative factor analysis to obtain detail structural view on variability of amorphous forms of atorvastatin are also discussed. Although the reported method was tested on atorvastatin, authors expect wider application for any fluorinated compound to give the routine, fast and reliable characterization of amorphous forms of APIs in drug products even at low concentrations (1-5%). Bear in mind that 20-25% of currently developed pharmaceuticals contain at least one fluorine atom in the molecule.

• MeSH
• atorvastatin MeSH
• časové faktory MeSH
• faktorová analýza statistická MeSH
• fluor chemie   MeSH
• krystalizace MeSH
• kyseliny heptylové chemie   MeSH
• magnetická rezonanční spektroskopie metody   MeSH
• prášková difrakce MeSH
• pyrroly chemie   MeSH
• reprodukovatelnost výsledků MeSH
• spektroskopie infračervená s Fourierovou transformací metody   MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• srovnávací studie MeSH
• Názvy látek
• atorvastatin MeSH
• fluor MeSH
• kyseliny heptylové MeSH
• pyrroly MeSH

The preparation of liquisolid systems presents a promising and innovative possibility for enhancing dissolution profiles and improving the bioavailability of poorly soluble drugs. This study aims to evaluate the differences in the properties of liquisolid systems containing combinations of 3 commercially used superdisintegrants (sodium starch glycolate, crospovidone, and croscarmellose sodium). Multiple regression models and contour plots were used to study how the amount and the type of superdisintegrant used affected the quality parameters of liquisolid tablets. The results revealed that an increased amount of crospovidone in the mixture improves disintegration and wetting time and enhances drug release from the prepared liquisolid tablets. Moreover, it was observed that a binary blend of crospovidone and sodium starch glycolate improved tablet disintegration. Considering the obtained results, it could be stated that crospovidone showed the best properties to be used as superdisintegrant for the preparation of liquisolid systems containing rosuvastatin.

• Klíčová slova
• Biopharmaceutics Classification System, dissolution rate, excipients, multivariate analysis, solid dosage form, solid state, solubility, sorption, tableting, wetting,
• MeSH
• chemie farmaceutická metody   MeSH
• farmaceutické pomocné látky chemická syntéza   farmakokinetika   MeSH
• lékové formy MeSH
• pomocné látky chemická syntéza   farmakokinetika   MeSH
• povidon chemická syntéza   metabolismus   MeSH
• rozpustnost MeSH
• škrob analogy a deriváty   chemická syntéza   farmakokinetika   MeSH
• sodná sůl karboxymethylcelulosy chemická syntéza   farmakokinetika   MeSH
• uvolňování léčiv MeSH
• výzkumný projekt MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• farmaceutické pomocné látky MeSH
• lékové formy MeSH
• pomocné látky MeSH
• povidon MeSH
• škrob MeSH
• sodium starch glycolate MeSH Prohlížeč
• sodná sůl karboxymethylcelulosy MeSH