V práci byla hodnocena pevnost tablet v tahu ze suchého pojiva Prosolv SMCC 90 a vliv tří koncentrací mazadla stearanu horečnatého na pevnost tablet z této látky. Výsledky byly srovnávány se stejným hodnocením u Avicelu PH 102. Testované koncenti-ace stearanu byly 0,4; 0,8 a 1,2 %. Tablety byly lisovány třemi lisovacími silami (3; 3,5 a 4 kN). Na základě získaných výsledků lze konstatovat, že samotný Prosolv SMCC 90 poskytuje při stejných lisovacích silách pevnější výlisky než Avicel PH 102. Z hlediska snížení pevnosti výlisků přídavkem stearanu horečnatého je suché pojivo Prosolv SMCC 90 mnohem méně citiivé než Avicel PH 102. U Avicelu PH 102 je výrazné snížení pevnosti zaznamenáno přídavkem 0,4 % stearanu horečnatého, což u Prosolvu SMCC 90 zaznamenáno nebylo. Významnější snížení pevnosti výlisků vykazuje tato látka až u koncentrace stearanu 0,8 %. Nejvyšší použitá koncentrace stearanu 1,2 % snižuje pevnost tablet z Prosolvu SMCC 90 u lisovacích sil 3,5 a 4 kN dvakrát méně než pevnost výlisků z Avicelu PH 102.
The present paper evaluated the tensile strength of tablets made from the dry binder Prosolv SMCC 90 and the influence of three concentrations of the lubricant magnesium stearate on the tensile strength of tablets manufactured firom this material. The results were compared with the same evaluation in Avicel PH102. The tested concentrations of the stearate were 0.4,0.8 and 1.2 %. The tablets were compressed by three press powers (3, 3.5, and 4 kN). On the basis of obtained results it can be stated that under the same press powers Prosolv SMCC 90 alone yields stronger compacts than Avicel PH 102. From the viewpoint of decreased strength of compacts by adding magnesium stearate, the dry binder Prosolv SMCC 90 is much less sensitive than Avicel PH 102. In Avicel PH 102 a marked decrease in tensile strength was recorded with an addition of 0.4 %, which was not observed with Prosolv SMCC 90. Amore significant decrease in the strength of compacts was shown by the substance not until a stearate concentration of 0.8 %. The highest employed stearate concentration of 1.2 % decreases the tensile strength of tablets made from Prosolv SMCC 90 in the press powers of 3.5 and 4 kN two times less than the tensile strength of the compacts from Avicel PH 102.
V práci je studována pevnost a doba rozpadu tablet z nového směsného suchého pojiva Prosolv® Easytab. Výsledky jsou srovnány s Prosolvem® SMCC 90 a s fyzikálními směsmi Prosolvu SMCC 90 s Explotabem (1% nebo 1,5%) a Pruvem (0,5% nebo 1%). Jsou hodnoceny i směsi s léčivými látkami kyselinou askorbovou a kyselinou acetylsalicylovou. Proces lisování nové pomocné látky je studován i z energetického hlediska. Tablety z látky Prosolv Easytab měly nižší pevnost než z Prosolvu SMCC 90 a z fyzikálních směsí Prosolvu SMCC 90 s Explotabem a Pruvem. Doba rozpadu tablet byla výrazně kratší v případě látky Prosolv Easytab než Prosolv SMCC 90, nejkratší byla u tablet z fyzikálních směsí látek. Z energetického hlediska byl Prosolv Easytab nejlépe lisovatelný, neboť hodnota maximální energie byla při dané lisovací síle nejnižší ze všech sledovaných tabletovin, a to především díky nižší energii na tření a energii akumulované tabletou při lisování.
The paper studies the tensile strength and disintegration time of tablets made from the new co-processed dry binder Prosolv® Easytab. The results are compared with Prosolv® SMCC 90 and the physical mixtures of Prosolv SMCC 90 with Explotab (1% or 1.5%) and Pruv (0.5% or 1%). It also evaluates the mixtures with the active ingredients ascorbic acid and acetylsalicylic acid. The process of compaction of the new excipient is studied also from the energetic aspect. The tablets made from the substance Prosolv Easytab possessed a lower strength than those from Prosolv SMCC 90 and the physical mixtures of Prosolv SMCC 90 with Explotab and Pruv. The disintegration time of tablets was markedly shorter in the case of the substance Prosolv Easytab than in Prosolv SMCC 90, the shortest being in the tablets made from the physical mixtures of substances. From the energetic aspect, Prosolv Easytab was the best compressible one, because under the given compression force the value of the maximal energy was the lowest one of the all tableting compositions under study, primarily due to a lower energy for friction and the energy accumulated by the tablet.
- Keywords
- záznam "síla – dráha“, doba rozpadu tablet, pevnost tablet v tahu, Prosolv SMCC 90,
- MeSH
- Aspirin MeSH
- Cellulose MeSH
- Technology, Pharmaceutical MeSH
- Financing, Organized MeSH
- Data Interpretation, Statistical MeSH
- Ascorbic Acid MeSH
- Tensile Strength MeSH
- Compressive Strength MeSH
- Excipients MeSH
- Drug Compounding MeSH
- Statistics as Topic MeSH
The paper deals with a study of tensile strength and disintegration time of compacts made from silicified microcrystalline celluloses, Prosolv SMCC 90, and Prosolv HD 90, in dependence on compression force, addition of two types of lubricants, and two active ingredients. The lubricants were magnesium stearate and sodium stearyl fumarate in a concentration of 0.5%, the active ingredients being ascorbic acid and acetylsalicylic acid in a concentration of 50%. Prosolv SMCC 90 proved to be better compatible than Prosolv HD 90; the compacts were of higher strength, which was markedly increased with increasing compression force. Prosolv HD 90 was more sensitive to additions of lubricants, and a greater decrease in strength was recorded due to the influence of sodium stearyl fumarate. The effect of lubricants on the strength of compacts in the presence of active ingredients was not identical. The disintegration time of compacts from Prosolv HD 90 without as well as with lubricants was shorter than from Prosolv SMCC 90 and was increasing with increasing compression force. Disintegration time was increased with added lubricants, and it was markedly shortened by addition of active ingredients. Compacts containing ascorbic acid possessed a shorter disintegration time than those containing acetylsalicylic acid, and it was not markedly influenced by the presence of lubricants.
- MeSH
- Aspirin chemistry MeSH
- Cellulose chemistry MeSH
- Chemistry, Pharmaceutical MeSH
- Technology, Pharmaceutical MeSH
- Financing, Organized MeSH
- Fumarates chemistry MeSH
- Ascorbic Acid chemistry MeSH
- Stearic Acids chemistry MeSH
- Lubrication MeSH
- Silicon Dioxide chemistry MeSH
- Tensile Strength MeSH
- Excipients chemistry MeSH
- Tablets chemistry MeSH
- Publication type
- Comparative Study MeSH
The paper evaluates and compares the compressibility and compactibility of directly compressible tableting materials for the preparation of hydrophilic gel matrix tablets containing tramadol hydrochloride and the coprocessed dry binders Prosolv® SMCC 90 and Disintequik™ MCC 25. The selected types of hypromellose are Methocel™ Premium K4M and Methocel™ Premium K100M in 30 and 50 % concentrations, the lubricant being magnesium stearate in a 1 % concentration. Compressibility is evaluated by means of the energy profile of compression process and compactibility by the tensile strength of tablets. The values of total energy of compression and plasticity were higher in the tableting materials containing Prosolv® SMCC 90 than in those containing Disintequik™ MCC 25. Tramadol slightly decreased the values of total energy of compression and plasticity. Tableting materials containing Prosolv® SMCC 90 yielded stronger tablets. Tramadol decreased the strength of tablets from both coprocessed dry binders.
- MeSH
- Cellulose chemistry MeSH
- Hypromellose Derivatives chemistry MeSH
- Gels MeSH
- Hydrophobic and Hydrophilic Interactions MeSH
- Stearic Acids chemistry MeSH
- Mechanical Phenomena MeSH
- Analgesics, Opioid chemistry MeSH
- Tensile Strength MeSH
- Compressive Strength MeSH
- Excipients chemistry MeSH
- Energy Transfer MeSH
- Drug Compounding * MeSH
- Elasticity MeSH
- Tablets MeSH
- Tramadol chemistry MeSH
- Viscosity MeSH
- Publication type
- Journal Article MeSH
- Comparative Study MeSH
- Geographicals
- Czech Republic MeSH
The paper compared two spray-dried lactoses Flowlac 100 and SuperTab 14SD from the standpoint of tensile strength and disintegration time of tablets, the effect of an addition of the lubricant magnesium stearate and silicified microcrystalline cellulose on these properties, and also from the standpoint of the energy profile of compression. The comparison of the values was performed at the compression force of 15 kN. The strength of tablets was higher in the case of SuperTab 14SD, an increase in the concentration of magnesium stearate did not decrease tablet strength. Prosolv SMCC 90 increased the strength of tablets and made it equal for both lactoses, but it also increased the sensitivity to the added lubricant. The disintegration time of tablets was shorter in the case of SuperTab 14SD, an increased concentration of magnesium stearate prolonged it, and an addition of Prosolv SMCC 90 shortened it and made it equal for both lactoses. From the energy standpoint, the maximal energy was higher in the case of SuperTab 14SD, an addition of Prosolv SMCC 90 increased it and again made it equal for both lactoses. The differences in the values of the maximal energy were primarily due to the values of the energy for friction and the energy accumulated by the tablet after compression, and there was no marked difference in the values of the energy of decompression. SuperTab 14SD showed a higher plasticity than Flowlac 100.
- MeSH
- Aerosols MeSH
- Cellulose chemistry MeSH
- Chemistry, Pharmaceutical MeSH
- Technology, Pharmaceutical methods MeSH
- Kinetics MeSH
- Stearic Acids chemistry MeSH
- Lactose chemistry MeSH
- Lubricants chemistry MeSH
- Tensile Strength MeSH
- Compressive Strength MeSH
- Excipients chemistry MeSH
- Solubility MeSH
- Tablets MeSH
- Desiccation MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Comparative Study MeSH
The aim of this study is to present the possibility of using of co-processed dry binders for formulation of matrix tablets with drug controlled release. Hydrophilic matrix tablets with tramadol hydrochloride, hypromellose and different co-processed dry binders were prepared by direct compression method. Hypromelloses Methocel™ K4M Premium CR or Methocel™ K100M Premium CR were used as controlled release agents and Prosolv® SMCC 90 or Disintequik™ MCC 25 were used as co-processed dry binders. Homogeneity of the tablets was evaluated using scanning electron microscopy and energy dispersive X-ray microanalysis. The release of tramadol hydrochloride from prepared formulations was studied by dissolution test method. The dissolution profiles obtained were evaluated by non-linear regression analysis, release rate constants and other kinetic parameters were determined. It was found that matrix tablets based on Prosolv® SMCC 90 and Methocel™ Premium CR cannot control the tramadol release effectively for >12h and tablets containing Disintequik™ MCC 25 and Methocel™ Premium CR >8h.
