scholarly journals Co-Spray Drying of Paracetamol and Propyphenazone with Polymeric Binders for Enabling Compaction and Stability Improvement in a Combination Tablet

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1259
Author(s):  
Ioannis Partheniadis ◽  
Ioannis Nikolakakis ◽  
Constantinos K. Zacharis ◽  
Kyriakos Kachrimanis ◽  
Nizar Al-Zoubi

Paracetamol (PCT) and propyphenazone (PRP) are analgesic drugs that are often combined in a single dosage form for enhanced pharmacological action. In this work, PCT and PRP were co-spray dried separately with hydroxypropyl methylcellulose (HPMC) and hydroxypropyl cellulose (HPC) using drug suspensions in polymer solutions as feed liquids. It was thought that because of polymer adherence to the surface of drug particles, the risk of PCT–PRP contact and interaction could be reduced. Such interaction may be caused by localized temperature gradients due to frictional forces during tableting, or during storage under harsh conditions. A worst-case scenario would be eutectic formation due to variations in powder mixture homogeneity since eutectic and therapeutic mass PCT/PRP ratios are close (65:35 and 60:40, respectively) and eutectic temperature is low (~56 °C). Uniform particle size, round shape, compaction improvement and faster release of the analgesics were important additional benefits of co-spray drying. Experimental design was first applied for each drug to optimize the polymer concentration on the yield of spray drying and melting point separation (Δmp) of heated binary mixtures of co-spray dried PCT/neat PRP, and vice versa, with the two drugs always included at their therapeutic 60:40 ratio. Optimal combinations with largest Δmp and production yield were: co-spray dried PCT (15% HPC) with neat PRP and co-spray dried PRP (10% HPMC) with neat PCT. Compression studies of these combinations showed tableting improvement due to the polymers, as reflected in greater work of compaction and solid fraction, greater fracture toughness and tablet strength, easier tablet detachment from the punch surface and ejectability. Faster release of both drugs was obtained from the tablet of co-spray dried PCT (15% HPC) with neat PRP. A one-month stability test (75% RH/40 °C) showed moisture-induced alteration tablet strength.

Author(s):  
Ankit Rampal ◽  
Manmeet Singh ◽  
Shanta Mahajan ◽  
Neena Bedi

Objective: The aim of the present study was to investigate the effect of novel polymeric carriers and to develop solid dispersion formulation that could improve in vitro profile of Fenofibrate (FB). Methods: Spray drying technique was used to fabricate solid dispersions with hydrophilic carriers, mainly hydroxypropyl methylcellulose (HPMC) and hydroxypropyl methylcellulose acetate succinate (HPMCAS). Solid dispersions in the form of spray-dried powder were characterized with respect to the pure drug and the corresponding physical mixtures by optical microscopy, x-ray diffraction (XRD), fourier transform infrared (FT-IR) spectroscopy and differential scanning calorimetry (DSC). Size and morphology of optimized solid dispersion were performed by scanning electron microscopy (SEM). Furthermore, in vitro dissolution comparisons were carried out between the optimized solid dispersion against the pure drug and the physical mixtures. Results: Solubility studies demonstrated that the solubility of FB was not affected by pH change. The transformation of crystalline FB into an amorphous solid dispersion powder has been clearly demonstrated by optical microscopy. The molecular dispersion of drug in the dispersion matrix prepared by spray drying was confirmed in XRD and DSC studies. IR spectroscopy was observed with negligible incompatibility of the drug with polymers. Spherical morphology was observed in SEM with no evidence of FB crystals. The prepared solid dispersions exhibited dissolution improvement as compared to the pure drug and spray dried FB in 0.05 M SLS, with HPMCAS as the superior carrier over HPMC. Conclusion: The present study vouches better in vitro profile of FB from spray-dried HPMCAS based solid dispersions.


2010 ◽  
Vol 93-94 ◽  
pp. 679-682 ◽  
Author(s):  
Varatus Vongsurakrai ◽  
Saiyavit Varavinit

Starch-colloidal silicon dioxide mixtures (Era-Tab SP® ) was prepared by co-spray drying and dry mixing methods and the flow ability and tablet properties of both methods were compared in particular with spray dried rice starch (SNR) alone. In co-spray drying, various percentages of rice starch and colloidal silicon dioxide blends were suspended in distilled water and subjected to spray dryer. The dry mixing method was obtained by blending of the colloidal silicon dioxide and spray dried rice starch at various percentages. It was found that co-spray drying of starch-colloidal silicon dioxide mixtures improved flow ability by reducing of the frictional forces between the granules greater than the dry mixing method. SEM micrographs presented the depositions of colloidal silicon dioxide on the surface of agglomerated starch granules obtained from both methods. The addition of colloidal silicon dioxide increased the tensile strength of the compressed tablet especially via the co-spray drying method by increasing the interaction of hydrogen bonding inside the tablet. Moreover, the co-spray drying method also reduced the friability and the disintegration time of the tablets better than the dry mixing method.


2008 ◽  
Author(s):  
Sonia Savelli ◽  
Susan Joslyn ◽  
Limor Nadav-Greenberg ◽  
Queena Chen

Author(s):  
Kusuma P. ◽  
Syukri Y ◽  
Sholehuddin F. ◽  
Fazzri N. ◽  
Romdhonah . ◽  
...  

The most efficient tablet processing method is direct compression. For this method, the filler-binder can be made by coprocessing via spray drying method. The purpose of this study was to investigate the effect of spray dried co-processing on microcrystalline cellulose (MCC) PH 101, lactose and Kollidon® K 30 as well as to define the optimum proportions. Spray dried MCC PH 101, lactose, and Kollidon® K 30 were varied in 13 different mixture design proportions to obtain compact, free-flowing filler-binder co-processed excipients (CPE). Compactibility and flow properties became the key parameters to determine the optimum proportions of CPE that would be compared to their physical mixtures. The result showed that the optimum proportion of CPE had better compactibility and flow properties than the physical mixtures. The optimum CPE, consisting of only MCC PH 101 and Kollidon® K 30 without lactose, that were characterized using infrared spectrophotometer, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and scanning electron microscope (SEM) indicated no chemical change therein. Therefore, this study showed that spray dried MCC PH 101, lactose and Kollidon® K 30 could be one of the filler-binder alternatives for direct compression process.


Author(s):  
D. V. Vaniukova ◽  
◽  
P. A. Kutsenkov ◽  

The research expedition of the Institute of Oriental studies of the Russian Academy of Sciences has been working in Mali since 2015. Since 2017, it has been attended by employees of the State Museum of the East. The task of the expedition is to study the transformation of traditional Dogon culture in the context of globalization, as well as to collect ethnographic information (life, customs, features of the traditional social and political structure); to collect oral historical legends; to study the history, existence, and transformation of artistic tradition in the villages of the Dogon Country in modern conditions; collecting items of Ethnography and art to add to the collection of the African collection of the. Peter the Great Museum (Kunstkamera, Saint Petersburg) and the State Museum of Oriental Arts (Moscow). The plan of the expedition in January 2020 included additional items, namely, the study of the functioning of the antique market in Mali (the “path” of things from villages to cities, which is important for attributing works of traditional art). The geography of our research was significantly expanded to the regions of Sikasso and Koulikoro in Mali, as well as to the city of Bobo-Dioulasso and its surroundings in Burkina Faso, which is related to the study of migrations to the Bandiagara Highlands. In addition, the plan of the expedition included organization of a photo exhibition in the Museum of the village of Endé and some educational projects. Unfortunately, after the mass murder in March 2019 in the village of Ogossogou-Pel, where more than one hundred and seventy people were killed, events in the Dogon Country began to develop in the worst-case scenario: The incessant provocations after that revived the old feud between the Pel (Fulbe) pastoralists and the Dogon farmers. So far, this hostility and mutual distrust has not yet developed into a full-scale ethnic conflict, but, unfortunately, such a development now seems quite likely.


2020 ◽  
Author(s):  
Ahmed Abdelmoaty ◽  
Wessam Mesbah ◽  
Mohammad A. M. Abdel-Aal ◽  
Ali T. Alawami

In the recent electricity market framework, the profit of the generation companies depends on the decision of the operator on the schedule of its units, the energy price, and the optimal bidding strategies. Due to the expanded integration of uncertain renewable generators which is highly intermittent such as wind plants, the coordination with other facilities to mitigate the risks of imbalances is mandatory. Accordingly, coordination of wind generators with the evolutionary Electric Vehicles (EVs) is expected to boost the performance of the grid. In this paper, we propose a robust optimization approach for the coordination between the wind-thermal generators and the EVs in a virtual<br>power plant (VPP) environment. The objective of maximizing the profit of the VPP Operator (VPPO) is studied. The optimal bidding strategy of the VPPO in the day-ahead market under uncertainties of wind power, energy<br>prices, imbalance prices, and demand is obtained for the worst case scenario. A case study is conducted to assess the e?effectiveness of the proposed model in terms of the VPPO's profit. A comparison between the proposed model and the scenario-based optimization was introduced. Our results confirmed that, although the conservative behavior of the worst-case robust optimization model, it helps the decision maker from the fluctuations of the uncertain parameters involved in the production and bidding processes. In addition, robust optimization is a more tractable problem and does not suffer from<br>the high computation burden associated with scenario-based stochastic programming. This makes it more practical for real-life scenarios.<br>


Author(s):  
Bhikshapathi D. V. R. N. ◽  
Haarika B ◽  
Jyothi Sri S ◽  
K Abbulu

The purpose of present investigation was to develop floating matrix tablets of gemifloxacin mesylate, which after oral administration could prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of irritating drugs. Tablets containing drug, various viscosity grades of hydroxypropyl methylcellulose such as HPMC K4M and HPMC K15M as matrix forming agent, Sodium bicarbonate as gas-forming agent and different additives were tested for their usefulness in formulating gastric floating tablets by direct compression method. The physical parameters, in vitro buoyancy, release characteristics and in vivo radiographic study were investigated in this study. The gemifloxacin mesylate floating tablets were prepared using HPMC K4M polymer giving more sustained drug release than the tablet containing HPMC K15M. All these formulations showed floating lag time of 30 to 47 sec and total floating time more than 12 h. The drug release was decreased when polymer concentration increases and gas generating agent decreases. Formulation that contains maximum concen-tration of both HPMC K15M and sodium bicarbonate (F9) showing sufficiently sustained with 99.2% of drug release at 12 h. The drug release from optimized formulation follows Higuchi model that indicates the diffusion controlled release. The best formulation (F9) was selected based on in vitro characteristics and used in vivo radiographic studies by incorporating barium sulphate as a radio-opaque agent and the tablet remained in the stomach for about 6 h.   


Catalysts ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 491
Author(s):  
Alina E. Kozhukhova ◽  
Stephanus P. du Preez ◽  
Aleksander A. Malakhov ◽  
Dmitri G. Bessarabov

In this study, a Pt/anodized aluminum oxide (AAO) catalyst was prepared by the anodization of an Al alloy (Al6082, 97.5% Al), followed by the incorporation of Pt via an incipient wet impregnation method. Then, the Pt/AAO catalyst was evaluated for autocatalytic hydrogen recombination. The Pt/AAO catalyst’s morphological characteristics were determined by scanning electron microscopy (SEM) and transmission electron microscopy (TEM). The average Pt particle size was determined to be 3.0 ± 0.6 nm. This Pt/AAO catalyst was tested for the combustion of lean hydrogen (0.5–4 vol% H2 in the air) in a recombiner section testing station. The thermal distribution throughout the catalytic surface was investigated at 3 vol% hydrogen (H2) using an infrared camera. The Al/AAO system had a high thermal conductivity, which prevents the formation of hotspots (areas where localized surface temperature is higher than an average temperature across the entire catalyst surface). In turn, the Pt stability was enhanced during catalytic hydrogen combustion (CHC). A temperature gradient over 70 mm of the Pt/AAO catalyst was 23 °C and 42 °C for catalysts with uniform and nonuniform (worst-case scenario) Pt distributions. The commercial computational fluid dynamics (CFD) code STAR-CCM+ was used to compare the experimentally observed and numerically simulated thermal distribution of the Pt/AAO catalyst. The effect of the initial H2 volume fraction on the combustion temperature and conversion of H2 was investigated. The activation energy for CHC on the Pt/AAO catalyst was 19.2 kJ/mol. Prolonged CHC was performed to assess the durability (reactive metal stability and catalytic activity) of the Pt/AAO catalyst. A stable combustion temperature of 162.8 ± 8.0 °C was maintained over 530 h of CHC. To confirm that Pt aggregation was avoided, the Pt particle size and distribution were determined by TEM before and after prolonged CHC.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 608
Author(s):  
Csilla Bartos ◽  
Patrícia Varga ◽  
Piroska Szabó-Révész ◽  
Rita Ambrus

The absorption of non-steroidal anti-inflammatory drugs (NSAIDs) through the nasal epithelium offers an innovative opportunity in the field of pain therapy. Thanks to the bonding of chitosan to the nasal mucosa and its permeability-enhancing effect, it is an excellent choice to formulate microspheres for the increase of drug bioavailability. The aim of our work includes the preparation of spray-dried cross-linked and non-cross-linked chitosan-based drug delivery systems for intranasal application, the optimization of spray-drying process parameters (inlet air temperature, pump rate), and the composition of samples. Cross-linked products were prepared by using different amounts of sodium tripolyphosphate. On top of these, the micrometric properties, the structural characteristics, the in vitro drug release, and the in vitro permeability of the products were studied. Spray-drying resulted in micronized chitosan particles (2–4 μm) regardless of the process parameters. The meloxicam (MEL)-containing microspheres showed nearly spherical habit, while MEL was present in a molecularly dispersed state. The highest dissolved (>90%) and permeated (~45 µg/cm2) MEL amount was detected from the non-cross-linked sample. Our results indicate that spray-dried MEL-containing chitosan microparticles may be recommended for the development of a novel drug delivery system to decrease acute pain or enhance analgesia by intranasal application.


Sports ◽  
2021 ◽  
Vol 9 (6) ◽  
pp. 76
Author(s):  
Dylan Mernagh ◽  
Anthony Weldon ◽  
Josh Wass ◽  
John Phillips ◽  
Nimai Parmar ◽  
...  

This is the first study to report the whole match, ball-in-play (BiP), ball-out-of-play (BoP), and Max BiP (worst case scenario phases of play) demands of professional soccer players competing in the English Championship. Effective playing time per soccer game is typically <60 min. When the ball is out of play, players spend time repositioning themselves, which is likely less physically demanding. Consequently, reporting whole match demands may under-report the physical requirements of soccer players. Twenty professional soccer players, categorized by position (defenders, midfielders, and forwards), participated in this study. A repeated measures design was used to collect Global Positioning System (GPS) data over eight professional soccer matches in the English Championship. Data were divided into whole match and BiP data, and BiP data were further sub-divided into different time points (30–60 s, 60–90 s, and >90 s), providing peak match demands. Whole match demands recorded were compared to BiP and Max BiP, with BiP data excluding all match stoppages, providing a more precise analysis of match demands. Whole match metrics were significantly lower than BiP metrics (p < 0.05), and Max BiP for 30–60 s was significantly higher than periods between 60–90 s and >90 s. No significant differences were found between positions. BiP analysis allows for a more accurate representation of the game and physical demands imposed on professional soccer players. Through having a clearer understanding of maximum game demands in professional soccer, practitioners can design more specific training methods to better prepare players for worst case scenario passages of play.


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