Co-processed excipients
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Tablety jsou nejpoužívanější lékovou formou. Jejich výhodou je dostupnost, snadné podání, dobrá stabilita a nízká cena. Nejjednodušší technologií pro výrobu tablet je přímé lisování, ačkoliv při použití této metody je nutné překonat určité obtíže, spojené zejména s hmotnostní a obsahovou stejnoměrností, disolucí a radiální pevností tablet. Společně zpracované pomocné látky obsahující běžně zpracované směsi plniv, pojiv, rozvolňovadel, lubrikantů a dalších pomocných látek, se v dnešní době používají stále častěji. Tyto směsi jsou vyráběny různými technologiemi, zejména sprejovým sušením, granulací ve fluidním loži, vlhkou granulací, granulací tavením, suchou granulací a společnou krystalizací. Tento článek popisuje pomocné látky, které se obvykle používají k vytvoření společně zpracovaných směsí, uvádí výrobní technologie a komerčně dostupné společně zpracované pomocné látky pro přímé lisování tablet.
Tablets are the most frequently employed dosage form. Their advantage lies in their availability, easy administration, good stability, and low price. The easiest technology to produce tablets is direct compression, even though the use of the method requires overcoming many obstacles, mainly related to content uniformity and variation of mass, disintegration, dissolution, and radial hardness of tablets. "Co-processed excipients", containing commonly processed blends of fillers, binders, disintegrants, lubricants, and other excipients are more and more widely used nowadays. These mixtures are manufactured by various technologies, chiefly by spray-drying, fluid bed granulation, wet granulation, melt granulation, dry granulation, and co-crystallisation. This review article lists excipients used usually to constitute co-processed excipients, technologies, and commercially available co-processed excipients for direct compression.
- Klíčová slova
- společně zpracované pomocné látky, lisování, fyzikální vlastnosti,
- MeSH
- farmaceutická technologie * metody MeSH
- farmaceutická vehikula MeSH
- farmaceutické pomocné látky * klasifikace MeSH
- tablety * MeSH
- Publikační typ
- přehledy MeSH
Drug loading into mesoporous carriers may help to improve the dissolution of poorly aqueous-soluble drugs. However, both preparation method and carrier properties influence loading efficiency and drug release. Accordingly, this study aimed to compare two preparation methods: formulation into liquisolid systems (LSS) and co-milling for their efficiency in loading the poorly soluble model drug cyclosporine A (CyA) into mesoporous magnesium aluminometasilicate Neusilin® US2 (NEU) or functionalized calcium carbonate (FCC). Scanning electron microscopy was used to visualize the morphology of the samples and evaluate the changes that occurred during the drug loading process. The solid-state characteristics and physical stability of the formulations, prepared at different drug concentrations, were determined using X-ray powder diffraction. In vitro release of the drug was evaluated in biorelevant media simulating intestinal fluid. The obtained results revealed improved drug release profiles of the formulations when compared to the milled (amorphous) CyA alone. The dissolution of CyA from LSS was faster in comparison to the co-milled formulations. Higher drug release was achieved from NEU than FCC formulations presumably due to the higher pore volume and larger surface area of NEU.
- MeSH
- difrakce rentgenového záření MeSH
- pomocné látky * MeSH
- poréznost MeSH
- rozpustnost MeSH
- voda * MeSH
- Publikační typ
- časopisecké články MeSH
This article deals with the study of the energetic relationships during compaction and the properties of tablets produced from a co-processed excipient based on starch and called StarCap 1500®. This article compares it with the substance Starch1500®. The study also includes the mixtures of StarCap 1500® and the granulated directly compressible lactose Pharmatose DCL®15. The tablet properties tested included tensile strength and disintegration time, examined in dependence on compression force, and also a 0.4% addition of magnesium stearate. The results show a better compressibility of StarCap 1500 in comparison with Starch 1500 and a lower elastic component of energy. The tablets were stronger and disintegrated more rapidly, but the substance possessed a higher sensitivity to an addition of a lubricant than Starch 1500. Increasing portions of StarCap 1500 in the mixtures with Pharmatose DCL 15 increased the tensile strength of tablets, disintegration period as well as the sensitivity to an addition of a lubricant. From the energetic viewpoint, energy for friction was decreasing, while the energy accumulated by the tablet during compaction and the elastic component of energy were increased.
Co-processed dry binders for ODTs are important multifunctional excipients for tablet manufacturing by direct compression. Testing their binary mixtures with lubricants is an important aspect of their use in combination with drugs. The aim of this study was to evaluate the rheological and compression properties of lubricated mixtures of co-processed dry binders Parteck® ODT, Prosolv® ODT G2 and Ludiflash®, and subsequently also the compactability and disintegration time of the tablets made thereof. The lubricants employed were magnesium stearate and sodium stearyl fumarate in the concentrations of 0.5% and 1%. The best flowability was shown by Prosolv® ODT G2 combined with magnesium stearate in the concentration of 0.5%. Lubricated mixtures with Prosolv® ODT G2 showed a lower angle of internal friction as well as lower pre-compression energy values. The values of plastic deformation energy were the highest in the case of Prosolv® ODT G2, which was also reflected in the highest tablet strength. On the contrary, the ejection force values were the lowest for this co-processed dry binder. Magnesium stearate reduced the ejection force more effectively than sodium stearyl fumarate. Prosolv® ODT G2 tablets exhibited the highest tensile strength and shortest disintegration time.
- MeSH
- lubrikanty * MeSH
- pevnost v tahu MeSH
- pomocné látky * MeSH
- tablety MeSH
- Publikační typ
- časopisecké články MeSH
An important feature of orodispersible tablets (ODTs) is the convenient administration of the drugs, in some cases, faster onset of action, stability maintenance, and dose precision. This work focused on the preparation of ODTs containing mannitol-based co-processed excipients Prosolv® ODT G2, Ludiflash® and Parteck® ODT in combination with tramadol, captopril, and domperidone by direct compression. Prosolv® ODT G2 showed high energy of plastic deformation due to the content of microcrystalline cellulose. Parteck® ODT provided compact tablets due to the content of granulated mannitol. All drugs decreased tensile strength, increased friability, prolonged disintegration time, and decreased the porosity of tablets. Tablets containing Prosolv® ODT G2 with captopril, domperidone, and tramadol; and Parteck® ODT with domperidone met the requirements for ODTs production, i.e., friability ≤ 1% and disintegration time ≤ 180 s, fast wetting time, high water absorption ratio, and adequate tensile strength. The disintegration time was tested using both the pharmacopeial method and the BJKSN-13 apparatus. The results indicate the significant difference between these methods, with the disintegration time being longer when tested with the BJKSN-13 instrument.
The utilization of co-processed excipients (CPEs) represents a novel approach to the preparation of orally disintegrating tablets by direct compression. Flow, consolidation, and compression properties of four lactose-based CPEs-Cellactose® 80, CombiLac®, MicroceLac® 100, and StarLac®-were investigated using different methods, including granulometry, powder rheometry, and tablet compaction under three pressures. Due to the similar composition and the same preparation technique (spray drying), the properties of CPEs and their compacts were generally comparable. The most pronounced differences were observed in flowability, undissolved fraction after 3 min and 24 h, energy of plastic deformation (E2), ejection force, consolidation behavior, and compact friability. Cellactose® 80 exhibited the most pronounced consolidation behavior, the lowest values of ejection force, and high friability of compacts. CombiLac® showed excellent flow properties but insufficient friability, except for compacts prepared at the highest compression pressure (182 MPa). MicroceLac® 100 displayed the poorest flow properties, lower ejection forces, and the best mechanical resistance of compacts. StarLac® showed excellent flow properties, the lowest amounts of undissolved fraction, the highest ejection force values, and the worst compact mechanical resistance. The obtained results revealed that higher compression pressures need to be used or further excipients have to be added to all tested materials in order to improve the friability and tensile strength of formed tablets, except for MicroceLac® 100.
- Publikační typ
- časopisecké články MeSH
Práce studuje lisovatelnost a dobu rozpadu tablet ze směsného suchého pojiva DisintequikTM MCC v kombinaci se dvěma mazadly ve dvou koncentracích v závislosti na lisovací síle. Dále porovnává stejné parametry u fyzikálních směsí sprejově sušené laktosy Flowlacu? 100 a mikrokrystalické celulosy Microcelu? MC-102 v poměrech 1 : 9, 2 : 8 a 3 : 7 opět v kombinaci se dvěma mazadly ve dvou koncentracích při jedné lisovací síle. Použitá mazadla jsou stearan hořečnatý a poloxamer 407 v koncentraci 1% a 2%. Lisovatelnost je hodnocena pomocí energetické bilance lisování a pevnosti tablet v tahu. DisintequikTM MCC vykazuje vyšší hodnoty celkové energie lisování díky vyšším hodnotám energie akumulované tabletou, vyšší plasticitu, vyšší pevnost a delší dobu rozpadu tablet než obsahově odpovídající fyzikální směs sprejově sušené laktosy a mikrokrystalické celulosy.
The paper studies the compressibility and disintegration time of tablets from the co-processed dry binder DisintequikTM MCC in combination with two lubricants at two concentrations in dependence on compression force. It also compares identical parameters in the physical mixtures of the spray-dried lactose Flowlac? 100 and the microcrystalline cellulose Microcel? MC-102 in the ratios of 9 : 1, 8 : 2 and 7 : 3, again in combination with two lubricants of two concentrations at one compression force. The lubricants employed are magnesium stearate and poloxamer 407 in concentrations of 1% and 2%. Compressibility is evaluated by means of energy balance of compression and tensile strength of tablets. DisintequikTM MCC shows higher values of total energy of compression due to higher values of the energy accumulated by the tablet, higher plasticity, higher strength and a longer disintegration time of tablets than the physical mixture of spray-dried lactose and microcrystalline cellulose of a corresponding content.
- MeSH
- celulosa MeSH
- farmaceutická technologie MeSH
- farmaceutické pomocné látky MeSH
- fyzikální chemie metody MeSH
- lidé MeSH
- pevnost v tahu MeSH
- pevnost v tlaku MeSH
- poloxamer MeSH
- pomocné látky MeSH
- příprava léků MeSH
- rozpustnost MeSH
- stearany MeSH
- tablety MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- práce podpořená grantem MeSH
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.
- Klíčová slova
- záznam "síla – dráha“, doba rozpadu tablet, pevnost tablet v tahu, Prosolv SMCC 90,
- MeSH
- Aspirin MeSH
- celulosa MeSH
- farmaceutická technologie MeSH
- financování organizované MeSH
- interpretace statistických dat MeSH
- kyselina askorbová MeSH
- pevnost v tahu MeSH
- pevnost v tlaku MeSH
- pomocné látky MeSH
- příprava léků MeSH
- statistika jako téma MeSH
