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Wyświetlanie 1-10 z 16
Tytuł:
Optimization of furosemide liquisolid tablets preparation process leading to their mass and size reduction
Autorzy:
Woyna-Orlewicz, Krzysztof
Kurek, Mateusz
Jachowicz, Renata
Khalid, Mohammad Hassan
Opis:
The great number of drug substances currently used in solid oral dosage forms is characterized by poor water solubility. Therefore, various methods of dissolution rate enhancement are an important topic of research interest in modern drug technology. The purpose of this study was to enhance the furosemide dissolution rate from liquisolid tablets while maintaining an acceptable size and mass. Two types of dibasic calcium phosphate (FujicalinÆ/EmcompressÆ) and microcrystalline cellulose (VivapurÆ 102/VivapurÆ 12) were used as carriers and magnesium aluminometasilicate (NeusilinÆ US2) was used as a coating material. The flowable liquid retention potential for those excipients was tested by measuring the angle of slide. To evaluate the impact of used excipients on tablet properties fourteen tablet formulations were prepared. It was found that LS2 tablets containing spherically granulated dibasic calcium phosphate and magnesium aluminometasilicate exhibit the best dissolution profile and mechanical properties while tablets composed only with NeusilinÆ US2 was characterized by the smallest size and mass with preserved good mechanical properties and furosemide dissolution.
Dostawca treści:
Repozytorium Uniwersytetu Jagiellońskiego
Artykuł
Tytuł:
Mixing of endogenous $CO_{2}$ and meteoric $H_{2}O$ causes extremely efficient carbonate dissolution
Autorzy:
Wróblewski, Wojciech
Bella, Pavel
Duliński, Marek
Drewnik, Marek
Nęcki, Jarosław
Gradziński, Michał
Motyka, Jacek
Sala, Przemysław
Opis:
Karst corrosion of carbonate rocks by water with dissolved gases proceeds in most cases along two major scenarios: (i) meteoric water absorbs $CO_{2}$ from soil and atmosphere, or (ii) ascending water of deep circulation carries with it dissolved endogenous gases, mainly $CO_{2}$ and $H_{2}O$. We have observed a peculiar variant where meteoric water absorbs ascending endogenous gases at a natural gas vent on a travertine mound in Slovakia. Carbonate dissolution's extreme effectiveness is demonstrated by mineralization of rainwater ponded at a gas vent, rising to 3.2 g/L of dissolved solids shortly after the rainfall. One liter of water ponded at the vent and mixing with the venting gas, dissolved up to 800 mg of calcium at a rate exceeding 5.8 mg/L·min. Limestone tablets placed at the vent show signs of significant corrosion, at rates up to 126 mm/ka. The rate is comparable to those in coastal karst, where freshwater is mixing with seawater and to those in sulfuric acid speleogenesis (SAS), both the highest hitherto known rates of karst corrosion in carbonates. The geomorphic effects of the process described are depressions on the surface of travertine near the vents of endogenous $CO_{2}$. This type of corrosion seems to be universal and probably occurs everywhere where endogenous $CO_{2}$ is exhaled to the surface from carbonate rocks.
Dostawca treści:
Repozytorium Uniwersytetu Jagiellońskiego
Artykuł
Tytuł:
A Rational approach to predicting immediate release formulation behavior in multiple gastric motility patterns : a combination of a biorelevant apparatus, design of experiments, and machine learning
Autorzy:
Garbacz, Grzegorz
Myslitska, Daria
Danielak, Dorota
Romanova, Svitlana
Paszkowska, Jadwiga
Staniszewska, Marcela
Dobosz, Justyna
Polak, Sebastian
Romański, Michał
Opis:
Gastric mechanical stress often impacts drug dissolution from solid oral dosage forms, but in vitro experiments cannot recreate the substantial variability of gastric motility in a reasonable time. This study, for the first time, combines a novel dissolution apparatus with the design of experiments (DoE) and machine learning (ML) to overcome this obstacle. The workflow involves the testing of soft gelatin capsules in a set of fasted-state biorelevant dissolution experiments created with DoE. The dissolution results are used by an ML algorithm to build the classification model of the capsule’s opening in response to intragastric stress (IS) within the physiological space of timing and magnitude. Next, a random forest algorithm is used to model the further drug dissolution. The predictive power of the two ML models is verified with independent dissolution tests, and they outperform a polynomial-based DoE model. Moreover, the developed tool reasonably simulates over 50 dissolution profiles under varying IS conditions. Hence, we prove that our method can be utilized for the simulation of dissolution profiles related to the multiplicity of individual gastric motility patterns. In perspective, the developed workflow can improve virtual bioequivalence trials and the patient-centric development of immediate-release oral dosage forms.
Dostawca treści:
Repozytorium Uniwersytetu Jagiellońskiego
Artykuł
Tytuł:
Preformulation studies on solid self-emulsifying systems in powder form containing magnesium aluminometasilicate as porous carrier
Autorzy:
Jachowicz, Renata
Krupa, Anna
Szlęk, Jakub
Jany, Benedykt
Opis:
The influence of alkaline and the neutral grade of magnesium aluminometasilicate as a porous solid carrier for the liquid self-emulsifying formulation with ibuprofen is investigated. Ibuprofen is dissolved in Labrasol, then this solution is adsorbed on the silicates. The drug to the silicate ratio is 1:2, 1:4, and 1:6, respectively. The properties of formulations obtained are analyzed, using morphological, porosity, crystallinity, and dissolution studies. Three solid self-emulsifying (S-SE) formulations containing Neusilin SG2 and six consisting of Neusilin US2 are in the form of powder without agglomerates. The nitrogen adsorption method shows that the solid carriers are mesoporous but they differ in a specific surface area, pore area, and the volume of pores. The adsorption of liquid SE formulation on solid silicate particles results in a decrease in their porosity. If the neutral grade of magnesium aluminometasilicate is used, the smallest pores, below 10 nm, are completely filled with liquid formulation, but there is still a certain number of pores of 40–100 nm. Dissolution studies of liquid SEDDS carried out in pH = 1.2 show that Labrasol improves the dissolution of ibuprofen as compared to the pure drug. Ibuprofen dissolution from liquid SE formulations examined in pH of 7.2 is immediate. The adsorption of the liquid onto the particles of the silicate causes a decrease in the amount of the drug released. Finally, more ibuprofen is dissolved from S-SE that consist of the neutral grade of magnesium aluminometasilicate than from the formulations containing the alkaline silicate.
Dostawca treści:
Repozytorium Uniwersytetu Jagiellońskiego
Artykuł
Tytuł:
Quality control dissolution data is biopredictive for a modified release ropinirole formulation : virtual experiment with the use of re-developed and verified PBPK model
Autorzy:
Shuklinova, Olha
Polak, Sebastian
Dorożyński, Przemysław
Kulinowski, Piotr
Opis:
Physiologically based pharmacokinetic and absorption modeling are being used by industry and regulatory bodies to address various scientifically challenging questions. While there is high confidence in the prediction of exposure for the BCS class I drugs administered as immediate-release formulations, in the case of prolonged-release formulations, special attention should be given to the input dissolution data. Our goal was to develop and verify a PBPK model for a BCS class I compound, ropinirole, and check the biopredictiveness of the dissolution data for the prolonged-release formulation administered by Parkinson’s patients. The model was built based on quality control dissolution data reported in the certificates of analysis and verified with the use of data derived from five clinical trial reports. The simulated pharmacokinetic parameters being within a two-fold range of the observed values confirmed acceptable model performance, in vivo relevance of the in vitro dissolution profiles, and indirectly indicated ropinirole stable release from the formulation in the patients’ gastro-intestinal tract. Ropinirole PBPK model will be used for exploring potential clinical scenarios while developing a new formulation.
Dostawca treści:
Repozytorium Uniwersytetu Jagiellońskiego
Artykuł
Tytuł:
Impact of gas storage on reservoir rocks : long-term study to investigate the effects on mineral content and fluid chemistry
Autorzy:
Morozova, Daria
Kasina, Monika
Wuerdemann, Hilke
Pudlo, Dieter
Michalik, Marek
Opis:
To study the effects of gas storage, long-term autoclave experiments with rock cores originating from a natural gas reservoir and brines taken from a gas well were conducted at 40 bar and 80o C in a CO_{2} atmosphere. While the main mineral composition of the sandstones was not affected due to CO_{2} exposure over a period of 31 months, the dissolution of rock-forming minerals such as feldspar, quartz or pore-filling anhydrite and calcite was noted. Changes in the brine composition were also detected. A release of iron and total organic carbon (TOC) from the rock samples to the saline fluid was observed. Temporary changes in the acetic acid concentration might have contributed to the dissolution processes. Precipitation and dissolution of minerals in sandstones were mostly related to diagenetic fluid-rock reactions and CO_{2} exposure, but in general the impact of CO_{2} on rock composition was only minor.
Dostawca treści:
Repozytorium Uniwersytetu Jagiellońskiego
Artykuł
Tytuł:
Electrospun amorphous solid dispersions with lopinavir and ritonavir for improved solubility and dissolution rate
Autorzy:
Rezka, Aleksandra
Łyszczarz, Ewelina
Majda, Dorota
Sosna, Oskar
Mendyk, Aleksander
Srebro, Justyna
Opis:
Lopinavir (LPV) and ritonavir (RTV) are two of the essential antiretroviral active pharmaceutical ingredients (APIs) characterized by poor solubility. Hence, attempts have been made to improve both their solubility and dissolution rate. One of the most effective approaches used for this purpose is to prepare amorphous solid dispersions (ASDs). To our best knowledge, this is the first attempt aimed at developing ASDs via the electrospinning technique in the form of fibers containing LPV and RTV. In particular, the impact of the various polymeric carriers, i.e., Kollidon K30 (PVP), Kollidon VA64 (KVA), and Eudragit® E100 (E100), as well as the drug content as a result of the LPV and RTV amorphization were investigated. The characterization of the electrospun fibers included microscopic, DSC, and XRD analyses, the assessment of their wettability, and equilibrium solubility and dissolution studies. The application of the electrospinning process led to the full amorphization of both the APIs, regardless of the drug content and the type of polymer matrix used. The utilization of E100 as a polymeric carrier for LPV and KVA for RTV, despite the beads-on-string morphology, had a favorable impact on the equilibrium solubility and dissolution rate. The results showed that the electrospinning method can be successfully used to manufacture ASDs with poorly soluble APIs.
Dostawca treści:
Repozytorium Uniwersytetu Jagiellońskiego
Artykuł
Wyświetlanie 1-10 z 16

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