Temat: solid dispersion - Prolib Integro

Skocz do pozycji: 1.

Tytuł:: The study of physicochemical properties of solid dispersions of ibuprofen in the presence of chitosan
Autorzy:: Grimling, Bożena
Meler, Jan
Szcześniak, Maria
Pluta, Janusz
Górniak, Agata
Tematy:: chitosan
dissolution
ibuprofen
solid dispersion; Pokaż więcej
Wydawca:: Sieć Badawcza Łukasiewicz - Polskie Towarzystwo Chitynowe
Powiązania:: https://bibliotekanauki.pl/articles/1034797.pdf Link otwiera się w nowym oknie
Opis:: The aim of the present study was to increase the solubility of ibuprofen. Among the methods to increase the solubility selected solid dispersions of the drug with the polymer. Chitosan was used as the polymer. Solid dispersion obtained. Ibuprofen was incorporated into the chitosan type 652 with molar masse chitosan Mη = 429 kDa. Solid dispersions were prepared by using different ratios of ibuprofen and chitosan (1:9. 3:7 and 5:5). Formulations were tested dissolution rate of the ibuprofen. The highest dissolution of ibuprofen, amounting to 12.59%, was observed after 60 minutes from solid dispersion prepared by the evaporation method and 12.18% from physical mixtures with drug-polymer weight ratio 1:9 in the presence chitosan. The solubility of the drug improved more than 60-fold. XRPD analysis indicates the presence of the ibuprofen in amorphous form in the solid dispersion obtained by the modified solvent evaporation.
Dostawca treści:: Biblioteka Nauki

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Skocz do pozycji: 2.

Tytuł:: Physicochemical characterization and dissolution studies of solid dispersions of clotrimazole with chitosan
Autorzy:: Grimling, Bożena
Jasińska, Justyna
Meler, Jan
Szcześniak, Maria
Pluta, Janusz M.
Górniak, Agata
Tematy:: FTIR
XRPD
chitosan
clotrimazole
solid dispersion; Pokaż więcej
Wydawca:: Sieć Badawcza Łukasiewicz - Polskie Towarzystwo Chitynowe
Powiązania:: https://bibliotekanauki.pl/articles/1034642.pdf Link otwiera się w nowym oknie
Opis:: The aim of the present study was to increase the solubility of clotrimazole. Among the methods to increase the solubility selected solid dispersions of the drug with the polymer. Chitosan was used as the polymer. Clotrimazole was incorporated into the chitosan type 652 with molar masse chitosan Mη = 429 kDa. Solid dispersions were prepared by using different ratios of clotrimazole and chitosan (1:9, 3:7, 5:5, 7:3, 9:1). Formulations were tested dissolution rate of the drug. The highest dissolution of clotrimazole, amounting to 47.95%, was observed after 60 minutes from solid dispersion prepared by grinding method and 42.84% from physical mixtures with drug-polymer weight ratio 1:9 in the presence chitosan. The solubility of the drug improved more than 37-fold. XRPD analysis indicates the presence of the clotrimazole in crystalline form in the solid dispersion obtained by kneading method.
Dostawca treści:: Biblioteka Nauki

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Skocz do pozycji: 3.

Tytuł:: Is PVP K-29/32 an efficient stabilizing excipient in amorphous solid dispersions containing the poorly water-soluble drug : bicalutamide?
Autorzy:: Gawlak, Karolina
Antosik-Rogóż, Agata
Mendyk, Aleksander
Szafraniec-Szczęsny, Joanna
Opis:: The stability of amorphous drug substances is a crucial issue in the pharmaceutical field. This study examines the influence of polyvinylpyrrolidone as an excipient on the stabilization of the amorphous drug substance bicalutamide. Solid dispersions of the active substance and the excipient were prepared in different weight ratios using ball milling, then packed into aluminum sachets and stored in a climate chamber for one year. The results indicate successful amorphization of bicalutamide, as confirmed by the absence of crystalline structure in the diffractograms and improved dissolution in the 1:1, 2:1, and 4:1 weight ratio systems. However, the 10:1 drug-to-excipient composition remained crystalline. Our findings demonstrate that PVP effectively stabilizes bicalutamide in its amorphous form. The solid dispersions prepared in weight ratios ranging from 1:1 to 4:1 remained stable under both tested storage conditions throughout the entire study period.
Dostawca treści:: Repozytorium Uniwersytetu Jagiellońskiego

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Skocz do pozycji: 4.

Tytuł:: How rotational speed of planetary ball mill and polymer load influence the performance and water vapor sorption in solid dispersions composed of tadalafil and soluplus
Autorzy:: Brniak, Witold
Węgrzyn, Agnieszka
Kubat, Karol
Harańczyk, Hubert
Krupa, Anna
Majda, Dorota
Bogdał, Agata
Opis:: The presence of residual water may deteriorate the performance of amorphous solid dispersions prepared by ball milling, affecting molecular mobility, crystallinity, particle size and finally, the drug dissolution rate. As the stability of these metastable systems depend on both formulation and process variables, the aim of this study was to assess for the first time, the impact that the polymer load and the rotational speed applied upon high energy ball milling could have on the performance of binary co-milled solid dispersions composed of tadalafil (a hydrophobic crystalline drug) and Soluplus (an amphiphilic, hygroscopic amorphous polymer). Each of these variables was tested at three levels. Scanning electron microscopy, laser diffraction and X-ray powder diffraction were used to analyze morphology, particle size distribution and crystallinity of ball milled formulations respectively. Dissolution studies were also carried out. Advanced tools of applied physics, namely solid state 1H NMR and relaxometry were used to assess the structure and water mobility upon gaseous phase hydration on storage. It was shown that both tested variables determined the particle size of the formulation. When the rotational speed of 400 rpm was used, all solid dispersion were XRD-amorphous, but to ensure the immediate release of tadalafil its micellar solubilization in Soluplus was necessary. While the formulation was exposed to water vapor, the hydration level increased with an increasing polymer load as well. Hence, the rotational speed governed the space available for the adsorption of water molecules and their organization in a monolayer or multilayers. Such behavior may have impact on the kinetics of the amorphous drug recrystallization, and finally deteriorate its dissolution.
Dostawca treści:: Repozytorium Uniwersytetu Jagiellońskiego

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Skocz do pozycji: 5.

Tytuł:: The influence of a dental formulation prepared with chitosan on the pharmaceutical availability of clotrimazole
Autorzy:: Grimling, Bożena
Meler, Jan
Szcześniak, Maria
Kocoń, Martyna
Karolewicz, Bożena
Złocińska, Adrianna
Górniak, Agata
Tematy:: FTIR
carrier XRPD
chitosan
clotrimazole
hydrogel
solid dispersion; Pokaż więcej
Wydawca:: Sieć Badawcza Łukasiewicz - Polskie Towarzystwo Chitynowe
Powiązania:: https://bibliotekanauki.pl/articles/1034568.pdf Link otwiera się w nowym oknie
Opis:: The present work involves the development of a dental gel composition obtained on the basis of clotrimazole incorporated into chitosan in order to improve drug solubility. Solid dispersions were prepared by using two methods: grinding and kneading. The solid dispersion varied the ratio of chitosan to drug to increase the volume of the drug; the ratios were 5:5, 3:7, 2:8, 1:9. The mixtures were subjected to the dissolution rate of clotrimazole. The presence of chitosan improved the drug solubility; a better solubility from the solid dispersion prepared by the grinding method was obtained from the ratio of drug to polymer of 1+9. The rate of dissolution of clotrimazole was improved 17 times compared to the pure drug. Fourier transform infrared spectroscopy (both infrared and X-ray diffraction) revealed no new chemical structure of the tested connections and concluded that there was no interaction between the drug and the polymer in the test diffractions. Solid dispersions with the best parameters were used to prepare hydrogels, and the pharmaceutical availability of clotrimazole was analysed. The best properties were characterized by a hydrogel that was composed of the ratio of the amount of drug to polymer 5:5. The study demonstrated the availability of a pharmaceutical drug release at a therapeutic concentration in the first hour of the study. The use of the appropriate balance between clotrimazole and chitosan and the development of the hydrogel composition may affect the improvement of the drug solubility and may create the possibility of obtaining sustained or controlled release of the drug substance.
Dostawca treści:: Biblioteka Nauki

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Skocz do pozycji: 6.

Tytuł:: Evaluation of solid dispersions containing magnesium levulinate salts with selected carriers
Ocena stałych rozproszeń zawierających sole lewulinianu magnezowego z wybranymi nośnikami
Autorzy:: Marcoin, W.
Szulc-Musiol, B.
Tematy:: solid dispersion
magnesium levulinate salt
absorption
amino acid
glycine
arginine; Pokaż więcej
Wydawca:: Uniwersytet Warmińsko-Mazurski w Olsztynie / Polskie Towarzystwo Magnezologiczne im. Prof. Juliana Aleksandrowicza
Powiązania:: https://bibliotekanauki.pl/articles/14305.pdf Link otwiera się w nowym oknie
Opis:: Among the methods applied to ensure optimal pharmaceutical availability of a drug is the incorporation of solid dispersions, i.e. combinations containing a therapeutic substance and a carrier deprived of its pharmacological activity. While manufacturing solid dispersions, special attention must be paid to carriers with a polymeric structure and hydrophilic properties, e.g. polyvinylpyrrolidone (PVP) and also phosphatidylcholine (PC). The aim of this study has been to evaluate the influence of the carriers PVP and PC 45 on pharmacokinetic parameters of Mg2+ absorption from Mg(Lev)2, Mg(LevGly), Mg(LevArg) as well as from solid dispersions containing these salts. The o/w partition coefficient was determined and the log P value calculated for pure salts and for solid dispersions containing the salts during this study. The process of Mg2+ absorption was examined in vitro on a model of the rat’s small intestine. Our analysis of the results indicates that addition of PVP or PC 45 to solid dispersions (containing magnesium levulinate salts) significantly improves the degree of Mg2+ ion absorption. It has been found that addition of PVP and PC 45 to solid dispersions with magnesium levulinate salts significantly influences the rate of Mg2+ absorption from the formulations. Moreover, the results indicate that additional ligand (glycine or arginine) in the structure of magnesium levulinate triggers the effect consisting in depressed lipophilicity for these compounds. Using the PVP or PC 45 carriers for making solid dispersions containing magnesium levulinate and derivatives with glycine or arginine ligands is quite a promising solution for attaining improved pharmaceutical availability of drugs.
Jedną z metod osiągnięcia optymalnej dostępności farmaceutycznej leku jest zastosowanie stałych rozproszeń, układów zawierających substancję leczniczą i nośnik, który jest pozbawiony własnego działania farmakologicznego. Przy wytwarzaniu stałych rozproszeń na szczególną uwagę zasługują nośniki o budowie polimerowej i właściwościach hydrofilowych. Należą do nich m.in. poliwinylopirolidon (PVP), a także fosfatydylocholina. Celem badań była ocena wpływu wybranych nośników: poliwinylopirolidonu (PVP) i roztworu fosfatydylocholiny (PC 45) na poprawę parametrów farmakokinetycznych procesu wchłaniania jonów Mg2+ z soli lewulinianu magnezowego Mg(Lev)2, Mg(LevGly), Mg(LevArg) oraz ze stałych rozproszeń zawierających te sole. W badaniach wyznaczono współczynnik podziału o/w i wyliczono wartość log P dla czystych soli oraz dla stałych rozproszeń zawierających te sole. Badania procesu wchłaniania jonów Mg2+ przeprowadzono metodą in vitro na modelu jelita cienkiego szczura. Wykazano, że dodatek PVP lub PC 45 do stałych rozproszeń zawierających sole lewulinianu magnezowego znacząco wpływa na poprawę stopnia wchłaniania. Na podstawie tych badań stwierdzono, że dodatek PVP lub PC 45 do stałych rozproszeń z solami lewulinianu magnezowego istotnie (p=0.01) wpływa na szybkość procesu wchłaniania jonów Mg2+ z otrzymanych formulacji. Ponadto wyniki badań wskazują, że dodatkowy ligand (glicyna, arginina) w strukturze cząsteczki lewulinianu magnezowego wywołuje efekt zmniejszenia lipofilowości dla tych związków. Zastosowanie nośników PVP lub PC 45 do wytwarzania stałych rozproszeń zawierających lewulinian magnezowy i pochodne z ligandami glicyny lub argininy jest obiecujące w poprawie dostępności farmaceutycznej.
Dostawca treści:: Biblioteka Nauki

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Skocz do pozycji: 7.

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

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Skocz do pozycji: 8.

Tytuł:: Estimation of absorption of magnesium nicotinate and its derivatives with selected amino acids
Ocena wchlaniania nikotynianu magnezowego i jego pochodnych z wybranymi aminokwasami
Autorzy:: Marcoin, W
Szulc-Musiol, B.
Tematy:: magnesium nicotinate
absorption
amino acid
ligand
glycine
arginine
solid dispersion
partition coefficient; Pokaż więcej
Wydawca:: Uniwersytet Warmińsko-Mazurski w Olsztynie / Polskie Towarzystwo Magnezologiczne im. Prof. Juliana Aleksandrowicza
Powiązania:: https://bibliotekanauki.pl/articles/13564.pdf Link otwiera się w nowym oknie
Opis:: Preparation of solid dispersions is a popular pharmaceutical technology designed to improve the solubility and absorption characteristics of drugs. Solubilizing and moisturizing of carriers show influence on therapeutic substances; although dissolution of molecular dispersion of particles of the therapeutic substance in a neutral carrier is of utmost importance. This paper present the results of the research on influence of modification the structure of magnesium nicotinate Mg(Nic) with ligands, glycine and arginine, on the absorption process of Mg2+ions in vitro. The absorption area was the small intestine of a rat. It was found that structural changes with an additional arginine or glycine ligand affect the absorption process of Mg2+ions. Moreover, the effect of hydrophilic carriers on the partition coefficient (log P) for the system of n-octanol and phosphate buffer was investigated for the solid dispersions containing the examined magnesium salts. Phosphatidylcholine (PC-45) and polyvinylpirrolidone (PVP K-30) were used as carriers for solid dispersions with of magnesium salts. It was confirmed that using auxiliary substances PC-45 and PVP changes significantly (p<0.05) P values, corresponding to increasing hydrophobic properties of solid dispersions of the examined salts. It was found that modification of the structure of magnesium nicotinate by amino acids such as arginine or glycine positively influences the absorption process Mg2+ ions. The research carried out on properties of the solid dispersions containing magnesium salts and phospatidylcholine (PC-45) or magnesium salts and polyvinylpirrolidone (PVP K30) showed positive influence of these auxiliary substances.
Wytwarzanie stałych dyspersji jest popularną metodą technologiczną stosowaną w celu poprawy rozpuszczalności i wchłaniania leków. Właściwości solubilizujące oraz zwilżające nośników mają wpływ na proces rozpuszczania substancji leczniczych. W pracy przedstawiono badania wpływu modyfikacji struktury nikotynianu magnezowego Mg(Nik) aminokwasami (argininą lub glicyną) na proces wchłaniania jonów Mg2+in vitro. Powierzchnię absorpcji stanowiło jelito cienkie szczura. Stwierdzono, że dodatkowy ligand argininy lub glicyny w strukturze nikotynanu magnezu wpływa na zmianę parametrów procesu wchłaniania jonów Mg2+. Ponadto badano wpływ nośników hydrofilowych na współczynnik podziału o/w układu n-oktanol/bufor fosforanowy wybranych soli magnezowych stałych rozproszeń. Do sporządzenia stałych rozproszeń z badanymi solami magnezowymi zastosowano fosfatydylocholinę 45% (PC-45) i polivinylopirolidon (PVP K-30). Stwierdzono, że zastosowanie substancji pomocniczych PC-45, PVP znacząco (p<0.05) wpływa na zmianę wartości log P, a zatem wzrasta hydrofobowość stałych rozproszeń badanych soli. Wykazano, że modyfikacja struktury nikotynianu magnezu argininą lub glicyną wpływa na poprawę absorpcji jonów magnezowych. Badania właściwości stałych rozproszeń zawierających sole magnezowe – fosfatydylocholinę (PC-45) lub sole magnezowe – poliwinylopirolidon (PVP K-30) wykazały pozytywny wpływ zastosowanych substancji pomocniczych.
Dostawca treści:: Biblioteka Nauki

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Skocz do pozycji: 9.

Tytuł:: Development of tablets containing solid dispersion of ibuprofen manufactured by Hot Melt Impregnation process.
Autorzy:: Garbera, Kamil
Woś-Latosi, Katarzyna
Sawicki, Wiesław
Tematy:: Ibuprofen
solid dispersion
hot melt extrusion
hot melt impregnation
amorphisation
solubility enhancement; Pokaż więcej
Wydawca:: Polskie Towarzystwo Farmaceutyczne
Powiązania:: https://bibliotekanauki.pl/articles/895495.pdf Link otwiera się w nowym oknie
Opis:: The main assumption of given study was to develop tablets containing amorphous ibuprofen by hot melt extrusion process. However proposed manufacturing procedure demonstrates quite a few differences in comparison to a conventional hot melt extrusion. Accurately the given manufacturing procedure has been called a hot melt impregnation due to the process characteristics. As a product of described process a fine free flowing extrudate is obtained. Four different compositions have been proposed. Materials prepared by hot melt impregnation technique have been extensively examined in terms of physicochemical properties and then were subjected to tablet compression process. Obtained tablets were examined in terms of thermodynamic stability and compared to marketed product containing ibuprofen.
Dostawca treści:: Biblioteka Nauki

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Skocz do pozycji: 10.

Tytuł:: Characterisation and dissolution properties of ketoprofen in binary solid dispersion with chitosan
Autorzy:: Grimling, Bożena
Górniak, Agata
Meler, Jan
Szcześniak, Maria
Tematy:: different molecular weights of chitosan
dissolution
ketoprofen
solid dispersion prepared solvent evaporation; Pokaż więcej
Wydawca:: Sieć Badawcza Łukasiewicz - Polskie Towarzystwo Chitynowe
Powiązania:: https://bibliotekanauki.pl/articles/1035185.pdf Link otwiera się w nowym oknie
Opis:: BCS class II includes drugs with low solubility and high permeability. Ketoprofen is an example of this class of drugs. The aim of the study was to investigate the effect of chitosan with average molecular weights in various formulations on the dissolution of ketoprofen incorporated into this polymer carrier. The study investigated ketoprofen in solid dispersions using a method of the solvent evaporations at the drug to polymer ratios of 1:9. 3:7, and 5:5. The highest dissolution of fenofibrate, amounting to 98.8%, was observed after 60 minutes from solid dispersions with a drug-polymer weight ratio 1:9 in the presence of chitosan B and was 32-times higher in relation to the amount of added polymer in comparison to the solubility of pure drug. DSC and IR investigations showed that ketoprofen remained in its crystalline state in solid dispersion. There was no change in the chemical structure of the drug after the incorporation of the drug onto the polymer. Chitosan has been proposed as a useful excipient for enhancing the bioavailability of poorly water-soluble compounds.
Dostawca treści:: Biblioteka Nauki

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