Search PubMedSearch

Biomedical subjects

B Selmeczi

Publications and source records attributed to B Selmeczi.

At least 19 recordsLinked to original sources

[Formulation and in vitro investigation of antibacterial vaginal suppositories. Part 1. Considerations in selecting the vehicle. Methods and results of the physical examination].

Vaginal suppositories frequently used in gynaecological therapy were studied. Several antibacterial pharmacons are used for the topical treatment of vaginitis of various origins. However, the choice of the vaginal suppository base was often considered to be of minor importance for a long time. In view of the fact that the liberation of the given active substance and the subsequent therapeutic effect may be improved or inhibited by the vehicle, their aim was to find the optimal suppository base for vaginal suppositories containing sulphadimidine, chloramphenicol and gentamicin-sulphate by means of in vitro experiments. On the basis of breaking hardness, disintegration time and spreading properties the French Suppocire NA product, and compositions of macrogols with lower molecular weight proved to be the best lipophilic and hydrophilic bases respectively.

Anti-Infective Agents, Local

[Formulation and in vitro investigation of antibacterial vaginal suppositories. Part 2. In vitro membrane diffusion and microbiologic studies].

After the physical parameters had been determined, the in vitro drug liberation from vaginal suppositories containing 100 mg of antibacterial agent (sulphadimine, chloramphenicol, gentamicin-sulphate) was studied by membrane diffusion and microbiological methods. Among the vehicles available in Hungary the hydrophylic Massa macrogoli was found to be the best for this purpose. Among the lipophilic bases the in vitro drug liberation of the French Suppocire NA product was significantly better (p < 0.05) compared to the other lipophilic bases. This vehicle is recommended by the authors for the topical treatment of vaginitis, as these suppositories have the further advantage that they can easily be produced on a magistral, galenical or industrial scale as well. In the first part of the publication the formulation and some important physical parameters of lipophilic and hydrophilic antibacterial suppositories for vaginal use were described. In the present paper the drug liberation ability of the compositions with proper physical parameters was studied. The published results were obtained from measurements performed 1 week after formulation.

Anti-Infective Agents, Local

[Formulation and analysis of suppositories containing papaverine hydrochloride. Part 1. Choice of the optimal vehicle and determination of the physical parameters of the suppositories].

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.

Chemical Phenomena

[Formulation and analysis of suppositories containing papaverine hydrochloride. Part 2. In vitro membrane diffusion studies].

Rectal suppositories with 0.10 g/2.0 g Papaverine hydrochloride content were made with 12 different vehicles. The membrane diffusion method was used to study the factors influencing the in vitro drug liberation. The Polysorbate 20 and 61 tenside pair, the optimal concentration of which was 5% each, was found to influence diffusion favourably. Neutral oils softening the consistency (Miglyol 812 and Estasan), similarly in 5%, also had a favourable effect on the in vitro diffusion by increasing the spreading properties. As to the lipophil suppository masses with high and low hydroxyl numbers, only the latter could be used favourably. The 6-month-long storage resulted in drug retention in several experimental series. Correlation was found in several cases between the physical parameters of the suppositories and their in vitro drug liberation. Finally, with the help of linear regression calculation and in view of the in vitro relative bioavailability values the optimal vehicle is suggested for the formulation of suppositories containing Papaverine hydrochloride. The triglyceride type Estaram 299 was found to be the most suitable in every respect, either in itself or combined with 5% neutral oil.

Diffusion

[Deformation phenomena occurring during compression. III. Changes of maximal compression strength in quasi-static condition].

Four materials of different properties in respect of compressibility, lactose, sodium chloride, microcrystalline cellulose (Avicel PH 101) and so-called simple granulate were investigated. In function of time and that of actual pressing force decrease of axial force on upper punch were measured in quasi-state. Evaluating relations it was established that both pressing time and pressing force had influence on deformation structural changes occurring inside compressed form. Furthermore, summing up of results showed that useful conclusions could be drawn from diagrams--which represented decrease of force--to compressibility properties of materials too.

Cellulose

[Biopharmaceutical study of aminophenazone-containing suppositories. 1. Experimental materials and methods, determination of physical qualities of the suppositories].

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.

Aminopyrine

[Biopharmaceutical study of aminophenazone-containing suppositories. 2. Results of in vitro drug release and in vivo drug absorption].

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.

Aminopyrine

[Deformation phenomena occurring during compression. II].

Compressed forms were prepared from sodium chloride of given granule size with mildly concave punches applying 4, 12 and 20 kN pressing force. Pressing was regulated in order to get maximum pressing force effect for 0.1 s, 30 s and 60 s. Textures of side of compressed forms as well as edge and middle of surface of compressed forms were investigated by scanning electron microscope. Photos made with different enlargement have proved that secondary structural changes have begun (colour changes, new crystals have come to being etc.) on side stronger but also well observable on surface of compressed forms which in function of pressing force and that of time of pressing force effect have increased and grown considerably.

Microscopy, Electron, Scanning

[Deformation phenomena occurring during compression. I].

Tablets were prepared from sodium chloride of given granule size with 4, 12 and 20 kN pressing force. Pressing was regulated in order to get maximum pressing force effect for 0.1 s, 30 s and 60 s. With the intention of studying deformation changes texture investigation of breaking surface of tablets was carried out by scanning electron microscope. Investigation results documented with photos of different enlargement showed that both pressing force and pressing force effect influenced deformation changes and also structure of tablets. Increase of time of pressing force effect resulted in perfection of deformation changes.

Microscopy, Electron, Scanning

[Effect of gelatin solution on parameters of tablets containing well-compressible active principles].

Theobromine tablets have been prepared by wet granulation using gelatin solutions of various concentrations. It has been established that film formed from 2 per cent gelatin solution does not assure sufficient binding force. Lamella forming tendency could be observed on tablets. Furthermore, it has been ascertained that tablets proper in respects of both physical parameters and active principle release can be prepared with 5 per cent gelatin solution. It seems to be unnecessary to use 10 per cent gelatin solution. Behaviour of gelatin solutions at compression of starch and their role in active principle release have been discussed. Attention has been drawn to loss of biological value because of the "aging" of the gelatin film.

Gelatin

[Application of beta-cyclodextrin during direct pressing of tablets].

In case of tablets prepared by direct procedure the compressibility of beta-cyclodextrin has been studied. It has been established that beta-cyclodextrin--because of its very good flowing behaviour--can successfully be applied as ingredient in direct pressing. When hardness of tablets has to be increased 20% Avicel pH 101 (VN) has been recommended. By comparative test of 1:1 mol physical mixture of chloramphenicol-beta-cyclodextrin and the granulated product it has been ascertained that method of preparation of products, behaviour of applied solid binding materials and degree of applied pressing force decisively influence the compressibility of products. Furthermore, it has been found that application of beta-cyclodextrin influences advantageously the dissolution rate of active principle from tablets.

Cyclodextrins

Formulation of Polyethylene Glycol ointment bases suitable for tropical and subtropical climates. II.

Attention has been focused on the suitability of PEG ointment bases in tropical and subtropical regions. Penetrometer studies were carried out at 33, 37 and 50 degrees C respectively. Penetrometer experiments indicate that the type and amount of PEG will greatly affect the penentration time, and a large number of selected PEGs showed softening in the second month. Rotovisco experiments were conducted at 35 and 45 degrees C. Experiments conducted by Rotovisco at 35 degrees C indicate that PEG bases exhibit plastic flow and rheopexy, and there is an increase in yield values during the twelve months. Experiments worked out by Rotovisco at 45 degrees C reflected that an increase in temperature resulted in a decrease in rheopexy, viscosity, area of histeresis loop and yield values. Results obtained by the two methods demonstrate that PEG 4000 in the presence of equal amounts of PEG 400 has a good texture and might be a suitable ointment base for tropical and subtropical areas.

Climate

[The liberation of phenylbutazone from tablets].

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.

Drug Compounding

[Direct compression nitrazepam tablets].

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.

Drug Compounding