[Influence of the pressing force on the physical features of sulfathiazole tablets and the dissolution rate of the active ingredient]. / Einfluss des Pressdruckes auf die physikalischen Eigenschaften von Sulfathiazoltabletten und die Auflösungsgeschwindigkeit des Wirkstoffes.

When the pressing force increased in the examined system, so did the mechanical firmness of the tablets. A logarithmic connection exists between the pressing force and the compression strength and between the pressing force and the porosity, while the connection between the pressing force and the abrasion loss was a connection of power-function. The changing of the pressing force don't alter significantly the disintegration time of the tablets and the dissolution rate of the drug. However there is a considerable difference between the dissolution rate of the sulfathiazolee-powder and that of the tablets. The binders used in the pressing process were surface-active, therefore they accelerated the dissolution by moistening the surface of the sulfathiazol crystals.

Release kinetics of potassium aspartate in polyvinyl chloride matrix formulation.

The authors prepared potassium aspartate matrix tablets in combination with polyvinyl chloride. The physical parameters were measured and the dissolution rates were determined. During the in vitro release rate experiments, it was determined that the dissolution kinetics obey both zero order and Higuchi diffusion model order kinetics.

Formulation and in vitro examination of furosemide containing suppositories and preliminary experiences of their clinical use.

Rectal suppositories containing furosemide (4-chloro-N-furfuryl-5-sulfamoylanthranilic acid) and furosemide sodium were formulated with various suppository bases. The in vitro drug release of Massa Estarinum 299 proved to be the best from the vehicle having various physical-chemical properties. The diuretic effect of the two suppositories was compared in a prospective, crossover clinical trial including 8 patients. Both preparations have induced an increase of urine flow, which was comparable to the diuretic effect of the tablet.

[The liberation of phenylbutazone from tablets]. / Untersuchung der Freisetzung von Phenylbutazon aus Tabletten.

The liberation of phenylbutazone from tablets prepared by wet granulation was examined. It was found that the solution process can be described by the equation c = cs (l-e-K.t alpha). The influence of the binder concentration and the disintegrant on the liberation rate was also studied. The increase of the Klucel MF concentration accelerated the liberation of the agents. Among the disintegrants Polyplasdone XL and cyclodextrin block polymer turned out to be very good.

[Study of the texture of furosemid tablets. Part 2 (author's transl)]. / Untersuchung der Textur von Furosemid-Tabletten. Teil 2.

The authors studied the alterations of the texture and of the physical properties of Furosemid tablets, which are prepared with the aid of hydroxypropylcellulose mucilage, that occur during storage. Klucel MF mucilage proved to be a very good binding agent. Though the film bursted on drying during storage, by which the pore volume of the tablets increased, the mechanical strength remained almost unchanged. The cause of this is the formation of solid bridges.

[Direct compression nitrazepam tablets]. / Untersuchung von direktverpressten Nitrazepamtabletten.

Tablets of nitrazepam were made by direct compression. The influence of different dry binders and other adjuvants on the physical parameters of the tablets and their texture (scanning electron microscope: SEM) were examined. Changes in the physical parameter can be explanded if the texture is known.

[On the compressibility of micronized celluloses of the Avicel and the Heweten type (author's transl)]. / Zur Kompressibilität von mikrokörnigen Cellulosen vom type avicel und Heweten.

Experimental studies on the effect of various micronized celluloses (Avicel PH 101 and Heweten 40) on the compressibility and the dissolution of sulphathiazole showed that the binding power of Heweten 40 is inferior to that of Avicel PH 101, whereas the mechanical strength of the tablets conforms to specifications. Referring to the dissolution rates, it can be said that the use of Heweten 40 is more advantageous.

[On the compression behaviour of spray-dried sulphathiazole (author's transl)]. / Uber das Kompressionsverhalten von sprühgetrocknetem Sulfathiazol.

The authors prepared a spray-dried sulphathiazole product consisting of hollow pellets, the drug being in the form of its metastable modification I (melting point, 200 degrees C). On the basis of force-time diagrams and of current parameters relative to the elasto-plastic deformability of substances intended for tabletting, the compression behaviour of the spraydried product was compared with that of sulphathiazole (modification I) tempered at 180 degrees C for 150 min. Scanning-electron-microscopic studies on tablet surfaces offered further insight into the compressibility of the spraydried product.

[Electron-microscopic studies on the texture of sulphathiazole and sulphathiazole tablets (author's transl)]. / Elektronenmikroskopische Texturuntersuchungen an Sulfathiazol und Sulfathiazol-Tabletten.

The authors performed scanning-electron-microscopic studies to investigate the texture of sulphathiazole tablets. This method permitted to demonstrate the texture-forming effect of micronized celluloses used as dry binding agents. The differences in dissolution rate are interpreted.

[The use of dry binding materials for the direct compression of phenylbutazone]. / Anwendung von Trockenbindemitteln für die Direktpressung von Phenylbutazon.

Direct compression of phenylbutazone is possible only with addition of excipients of several kinds, because its material properties are unfavourable. It is necessary to use besides disintegrant glidant, lubricant and antistatic agents too. The authors investigated the influence of two microcrystalline cellulose binders (Avicel and Heweten) for the pressability of phenylbutazone and on properties of the tablets, respectively. It was determined the physical parameters of the tablets and the dissolution characteristics of the active ingredient. It has been found, that Heweten optimized the exactness of dosage of the tablets as well as resulted in a faster dissolution than Avicel. Therefore, Heweten proved to be the more suitable binder.

Formulation of diazepam containing rectal suppositories and experiences of their biopharmaceutical study.

Methodology and the results of the in vitro membrane diffusion and in vivo bioavailability studies are presented. The results confirm a correlation between in vitro and in vivo findings. Hydrophilic macrogol-mixture with great molecular mass can be recommended as the optimal vehicle for formulation of diazepam suppositories.

[The polymorphism of drugs in powders and tablets. 1. The preparation and characterization of polymorphic modifications of phenobarbital]. / Untersuchungen zur Polymorphie von Arzneistoffen in Pulvern und Tabletten. 1. Mitteilung: Zur Herstellung und Charakterisierung polymorpher Modifikationen des Phenobarbitals.

The characterisation of three phenobarbital modifications by thermic examination procedures (DSC, DTA) is being described. Modification I was obtained by thermic treatment of the brands (modification II) from Hungary and the GDR. The spray product prepared, consisting of very fine hollow spheres, was identified as modification III. Besides the particle size distribution the form of the particle was determined by scanning electron microscopy (REM). The best results regarding saturation solubility and speed of dissolution were found for the spray product.

[The polymorphism of drugs in powders and tablets. 4. The effect of the polymorphism of drugs on the physical properties and drug release of phenobarbital tablets]. / Untersuchungen zur Polymorphie von Arzneistoffen in Pulvern und Tabletten. 4. Mitteilung, Einfluss der Polymorphie des Wirkstoffes auf die physikalischen Eigenschaften und die Wirkstofffreigabe aus Phenobarbitaltabletten.

Four products of phenobarbital (I, II1, II2, III) are manufactured into tablets with the dry binders Avicel PH 101 or Heweten 40 using different pressures by direct tabletting. The physical properties of the resulting tablets are different according to the modification of phenobarbital, the binders used and the pressure during tabletting. The dissolution behaviour of the drug may be changed by the different technological and physical parameters.

[The polymorphism of drugs in powders and tablets. 5. Preparation and characterization of polymorphic forms of tolbutamide]. / Untersuchungen zur Polymorphie von Arzneistoffen in Pulvern und Tabletten. 5. Mitteilung: Zur Herstellung und Charakterisierung polymorpher Formen des Tolbutamids.

The preparation of 4 modifications and 2 spray dried products of tolbutamid is described. The characterization is performed by thermoanalytical methods (thermomicroscopy, DSC). Scanning electron microscopy and investigations of solubility complete the results.

[Polymorphism of drugs in powders and tablets. 6. X-ray diffractometric studies of polymorphic modifications of tolbutamide]. / Untersuchungen zur Polymorphie von Arzneistoffen in Pulvern und Tabletten. 6. Mitteilung: Röntgendiffraktometrische Untersuchungen polymorpher Formen des Tolbutamids.

The modifications and spray dried products of tolbutamide published in a former article, are investigated furthermore by X-Ray diffraction. The indication of the reflexes in X-Ray diffraction patterns of 2 modifications is performed. Transformations of modification are provable in consequence of thermal stress.

[Research work in the Department of Pharmaceutical Technology of the Albert Szent-Györgyi Medical University]. / Kutatómunka a SZOTE Gyógyszertechnológiai Intézetében.

A short review is given of the research carried out in recent years in the Department of Pharmaceutical Technology headed by the author on the occasion of the 75th birthday of Professor Károly Nikolics. The main results of the scientific activities performed in the four research groups are reported and a few important references to literature are made.

[Formulation and in vitro examination of furosemide-containing suppositories and preliminary experiences of their clinical use]. / Furosemid-tartalmú kúpok elóállítása, in vitro vizsgálata és a preklinikai alkalmazás tapasztalatai.

Rectal suppositories containing Furosemide (4-Chloro-N-furfuryl-5-sulfamoylanthranilic acid) and Furosemide Sodium were formulated with various suppository bases. The in vitro drug release of Massa Estarinum 299 proved to be the best from among the vehicles having various physical-chemical properties. The diuretic effect of the two suppositories was compared in a prospective, cross-over clinical trial including 8 patients. Both preparations have induced and increase of urine flow, which was comparable to the diuretic effect of the tablet. Thus the possibility of rectal use has been added to the modalities of therapeutic Furosemide administration.

[Biopharmaceutical study of aminophenazone-containing suppositories. 1. Experimental materials and methods, determination of physical qualities of the suppositories]. / Aminofenazon-tartalmú kúpok biofarmáciai vizsgálata. I. Kísérleti anyagok és módszerek ismertetése, a kúpok fizikai jellemzöinek meghatározása.

Suppositories containing aminophenazone in quantities of 0.30 g/2 g were prepared by pouring technology. Two kinds of lipophilic suppository masses Witepsol W 35 and Estarinum 299 have been used as vehicles. Both of suppository bases are official in Ph. Hg. VII. As ingredients ten sorts of liquid tensides in concentrations of 5% have been applied. Experimental methods have been described: compression stability, disintegration time, special penetration time and drug release of suppositories by membrane diffusion method. Results of determinations have been discussed in the second part of the publication. On the basis of experimental results it has been established that the physical parameters of Massa Estarinum 299 had proved to be more advantageous. In 5% concentrations tensides softened consistency of suppositories favorably and shortened disintegration time beneficially in the case of both vehicles. The authors think that special penetration time is more suitable for measuring "disintegration" of suppositories of high powder content at 37 degrees C than the classical disintegration time.

[Biopharmaceutical study of aminophenazone-containing suppositories. 2. Results of in vitro drug release and in vivo drug absorption]. / Aminofenazon-tartalmú kúpok biofarmáciai vizsgálata. II. Az in vitro gyógyszerleadás és az in vivo gyógyszerfelszívódás eredményei.

Ten kinds of surface active ingredients of Th. Goldschmidt AG. (Essen-FRG) in concentrations of 5% were mixed with Witepsol W 35 and Massa Estarinum 299 suppository masses of Hüls-Troisdorf AG. Werk (Witten-FRG) which are official in Hungary. According to the authors the above tensides, which have been used advantageously first of all in ointments, creams and cosmetic preparations, can also be applied in rectal preparations. In the publication of two parts it has been established that these ingredients influence physical parameters of suppositories beneficially. They always increase significantly in vitro diffusion values and in some cases with order of magnitude. Massa Estarinum 299 containing 5% of Emulgator BTO proved to be the best in case of chosen suppositories containing aminophenazone. Correlation between in vitro and in vivo investigations has shown the importance of correct selection of base and ingredient materials in biopharmaceutical work.

[Formulation and analysis of suppositories containing papaverine hydrochloride. Part 1. Choice of the optimal vehicle and determination of the physical parameters of the suppositories]. / Papaverinium-klorid-tartalmú végbélkúpok formulálása és vizsgálata. I. Az optimális vehikulum kiválasztása és a kúpok fizikai paramétereinek meghatározása.

Suppositories containing 0.10 g papaverine hydrochloride were made with moulding technology to produce spasmolytic effect. The optimal vehicle was tried to be found for these suppositories. During the experiments 12 different suppository masses were used, including lipophil and lipohydrophil vehicles as well as vehicles with low and high hydroxyl numbers. Five different kinds of physical parameters were determined: melting and drop points, disintegration and special penetration times and breaking hardness. The physical parameters of suppositories without active substance and containing papaverine were examined separately. After 6 months of storage the greater part of the masses showed unfavourable changes (after-hardening, increase of the disintegration time, etc.). In the end the Estaram 299 mass, a triglyceride type of mass with a low hydroxyl number was found satisfactory in every respect, either in itself or combined with 5% Estasan neutral oil.