Current Issue : October - December Volume : 2020 Issue Number : 4 Articles : 5 Articles
Background: Excipients with improved functionality have continued to be developed by the particle engineering\nstrategy of co-processing. The aim of this study was to evaluate the compaction and tableting properties of\ncomposite particles of microcrystalline cellulose (MCC) and crospovidone (CPV) engineered by co-processing.\nResults: Heckel analysis of the compaction behavior revealed a decrease in plasticity of co-processed excipient\n(CPE) when compared to MCC due to an increase in Heckel yield pressure from 144 to 172 MPa. The\ncompressibility-tabletability-compactibility (CTC) profile revealed a decrease in individual parameters for CPE when\ncompared to MCC. CPE was found to be more sensitive to the lubricant effect of sodium stearyl fumarate (SSF)\nwhen compared to MCC and less sensitive to magnesium stearate (MST) when compared to MCC. A higher dilution\npotential was obtained for MCC (60%) compared to 44% for CPE when metronidazole was used as model drug.\nTableting properties revealed that metronidazole tablets generated with CPE by direct compression disintegrated\nwithin 15 min and gave a rapid drug release when compared to MCC as a direct compression (DC) excipient.\nConclusion: The compaction and tableting properties of CPE were characterized and yielded tablets with better\ndisintegration and drug release profile when compared to MCC. This study, therefore, confirms the suitability\nof co-processing as a proven strategy in engineering the performance of excipients.\nKeywords: Particle engineering, Microcrystalline cellulose, Crospovidone, Compaction studies, Tablet...
Magnolol, which is a CYP3A substrate, is a well-known agent that can facilitate\nneuroprotection and reduce ischemic brain damage. However, a well-controlled release formulation\nis needed for the effective delivery of magnolol due to its poor water solubility. In this study,\nwe have developed a formulation for a CYP3A-excipient microemulsion, which can be administrated\nintraperitoneally to increase the solubility and bioavailability of magnolol and increase its\nneuroprotective effect against ischemic brain injury. The results showed a significant improvement\nin the area under the plotted curve of drug concentration versus time curve (AUC0â??t) and mean\nresidence time (MRT) of magnolol in microemulsion compared to when it was dissolved in dimethyl\nsulfoxide (DMSO). Both magnolol in DMSO and microemulsion, administrated after the onset of\nischemia, showed a reduced visual brain infarct size. As such, this demonstrates a therapeutic effect on\nischemic brain injury caused by occlusion, however it is important to note that a pharmacological effect\ncannot be concluded by this study. Ultimately, our study suggests that the excipient inhibitor-based\nmicroemulsion formulation could be a promising concept for the substrate drugs of CYP3A....
The present studies were conducted to show the potential of 2D zeolites as eective and\nnon-toxic carriers of drugs. Layered zeolites exhibit adjustable interlayer porosity which can be\nexploited for controlled drug delivery allowing detailed investigation of the drug release because the\nstructure of the carrier is known exactly. This study was conducted with model drugs ciprofloxacin\nand piracetam, and ZSM-55 with ca 1 nm thick layers, in detemplated and pillared forms. The release\nprofiles differed from the commercial, crystalline forms of drugsâ??the release rate increased for\nciprofloxacin and decreased for piracetam. To understand the dissolution mechanisms the release\ndata were fitted to Korsmeyer-Peppas equation, showing Fickian (for pillared) and anomalous (for\ndetemplated sample) transport. FT-IR studies showed that strong interaction carrier-drug may be\nresponsible for the modified, slowed down release of piracetam while better solubility and faster\nrelease of ciprofloxacin was attributed to formation of the protonated form resulting in weaker\ninteraction with the zeolite than in the pure crystalline form. Two independent tests on L929 mice\nfibroblasts (ToxiLight and PrestoBlue) showed that ZSM-55, in moderate concentrations may be safely\nused as a carrier of drug molecules, not having negative effect on the cells viability or proliferation rate....
Excipients represent the complement of the active principle in any pharmaceutical form.\nTheir function is to provide stability, protection, and to ensure absorption of the drug and acceptability\nin patients. Cellulose is a conventional excipient in many pharmaceutical solid dosage products.\nMost of the sources used to extract microcrystalline cellulose come from cotton or wood, which\nare expensive and in high demand from other industries. As plants are considered the main\nsource of excipient production, we have taken advantage of the biodiversity of Ecuador to evaluate\nmicrocrystalline cellulose extracted from borojó (Alibertia patinoi), a native plant, as an excipient for\nsolid dosage formulations. The method of choice for tablet manufacturing was direct compression\nsince it is a conventional fabrication method in the pharmaceutical industry. First, we performed\nscanning electron microscopy (SEM), Fourier-transform infrared (FTIR) spectroscopy, and X-ray\ndiffraction (XRD) in order to compare the structure and characteristics of the extracted cellulose\nwith two reference commercial cellulose materials. Second, we performed quality tests to evaluate\nthe use of the isolate as an excipient including fluidity, hardness, friability, and disintegration.\nCompared with commercial and microcrystalline cellulose, the extracted cellulose from the native\nplant showed comparable characteristics and is consequently a potential excipient that could be used\nin the pharmaceutical industry. Last, we performed a dissolution test in which we concluded that all\ntablets have a short release time of active principle.\nKeywords: pharmaceutical excipient; cellulose; tablets; drug...
The influence of two tuning agents, polyglycerol ester (PE) and triblock copolymer (TC),\non the properties of glycerol monooleate (MO) liquid crystalline phase (LCP) was investigated to\nachieve the therapeutic concentration of vancomycin hydrochloride (VHCl) into the eye, topically\nduring 60 min (1 h) and intravitreally during 2880 min (48 h). Different techniques were used to\nelucidate the impact of surfactants on the structure of the LCP: polarized light microscopy (PLM),\nsmall-angle X-ray scattering (SAXS), and in vitro release tests I and II (simulating local and intravitreal\napplication in the eye). The structure analysis by SAXS depicts that the inclusion of PE into the MO\nLCP provided partial transition of a hexagonal phase into a lamellar phase, and TC induced a partial\ntransition of a hexagonal phase into an LCP which identification was difficult. The LCP modulated\nwith PE and TC demonstrated different VHClâ??s release patterns and were evaluated by comparing\nour release data with the literature data. The comparison indicated that the LCP modulated with 30%\nw/w PE could be a promising VHCl delivery system intravitreally during 2880 min....
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