[Spray products of sparingly soluble drugs. 1. In vitro study of spray products of nitrazepam in a starch hydrolysis product].
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Biomedical subjects
Publications and source records attributed to J Traue.
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Watersoluble polymeric drugs were synthesized on the basis of alternating copolymer of 1-vinyl-2-pyrrolidone and maleic anhydride. Benzocain served as model drug. The drug was bound directly as well as about epsilon-aminocapronic acid as spacer. The pancreatin catalyzed hydrolysis of these polymeric drugs was studied. No hydrolysis was noted, if the drug is directly bound on the copolymer. The polymeric drug with the epsilon-aminocapronic acid as spacer showed a small release. Possible reasons for these facts are discussed.
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.
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.
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 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.
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.
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Owing to the favourable physical conditions of the evaporation process, the technique of spray drying has been used for some time to obtain dried products from solutions, suspensions, emulsions and fluid extracts. In the pharmaceutical industry, it may be utilized as a -drying technique, -micronizing procedure, -procedure for the manufacture of polymorphic or amorphic forms of active substances, -technique for producing microcapsules and spray embeddings, -method for manufacturing direct-tablettable active substances. The technical development which ranges from spray dryers for laboratory experiments to industrial plants, and the continuous operation are favourable prerequisites for research and use on an ever greater scale.