163 research outputs found
Characteristics of interpolyelectrolyte complexes of Eudragit E 100 with sodium alginate
With a view to the application in oral drug delivery formulations, the possibility to form interpolyelectrolyte complexes (IPEC) of Eudragit E 100 (EE) with sodium alginate (AL) was investigated, employing turbidimetry, apparent viscosity measurements, FT-IR and elementary analysis. The interaction or binding ratio of a unit molecule of AL with EE was largely affected by the pH value of the media, showing a change from 1.5:1 to 1:1.25 (0.66 < Z < 1.25) with increase in pH value from 2.5 to 6.0. Based on the results of elementary analysis and FT-IR, the interaction ratio of each component in the solid complexes was very close to that observed in turbidity and apparent viscosity measurements thus proving that the synthesized products actually can be considered as IPEC. © 2005 Elsevier B.V. All rights reserved
Characteristics of interpolyelectrolyte complexes of Eudragit E100 with Eudragit L100
With a view to the application in oral controlled drug delivery systems, the formation of interpolyelectrolyte complexes (IPEC) between Eudragit E100 (EE) and Eudragit L100 (EL) was investigated, using turbidimetry, solution viscosity measurements and elementary analysis. The structure of the synthesized IPEC was investigated by using FT-IR spectroscopy. The binding ratio of a unit molecule of EL with EE was found to be approximately 1:1 in pH 6.0. Based on the results of elementary analysis, and FT-IR, the binding ratio of each component in the solid complexes was very close to that observed in turbidity and viscosity measurements and indicate that the synthesized products can be considered as IPEC. Due to the structure of the IPEC, two maxima were observed in the swelling behaviour as a function of pH. The release of the model drug ibuprofen was significantly retarded from tablets made up of the IPEC. © 2004 Elsevier B.V. All rights reserved
Comparative evaluation of interpolyelectrolyte complexes of chitosan with Eudragit® L100 and Eudragit® L100-55 as potential carriers for oral controlled drug delivery
With a view to the application in oral controlled drug delivery systems, the formation of interpolyelectrolyte complexes (IPEC) between chitosan (CS) and Eudragit® L100 (L100) or Eudragit® L100-55 (L100-55) was investigated at pH 6.0, using elementary analysis. The interaction or binding ratio of a unit molecule of CS with Eudragit® L copolymers depends on the molecular weight of CS, and changes from 1:0.85 to 1:1.22 (1.17 < φ < 0.82) for L100 and from 1:1.69 to 1:1.26 (0.60 < φ < 0.79) for L100-55, respectively. Based on the results of FT-IR, the structure of the IPECs can change substantially as a function of pH (from 5.8 till 7.4). Swelling behavior of physical mixtures (PM) is definitely different, and potential interactions between the two polyelectrolytes were not observed. The release of the model drug diclofenac sodium (DS) was significantly delayed from tablets made up of the IPEC and can be modified by two ways: choosing Eudragit® L copolymer types and/or changing the molecular weight of CS in the IPECs composition. © 2008 Elsevier B.V. All rights reserved
Drug release modification by interpolymer interaction between countercharged types of Eudragit® RL 30D and FS 30D in double-layer films
Interpolymer interactions between the countercharged methacrylate copolymers Eudragit® RL 30D (polycation) and Eudragit® FS 30D (polyanion), were investigated in conditions mimicking the gastrointestinal environment. The formation of inter-macromolecular ionic bonds between Eudragit® RL 30D and Eudragit® FS 30D was investigated using FT-IR spectroscopy and modulated DSC. The FT-IR spectra of the tested polymeric matrices are characterized by visible changes in the observed IR region indicating the interaction between chains of two oppositely charged copolymers. A new band at 1570 cm-1 appeared which was assigned to the absorption of the carboxylate groups that form the ionic bonds with the quaternary ammonium groups. Moreover, while increasing the pH values from pH 5.8 to 7.4, a decrease of the intensity of the band at 960 cm-1 (quaternary ammonium group vibration) was observed. All binary mixtures were characterized by the presence of only one and narrow Tg, pointing to sample homogeneity, because of the compatibility of components. As a result of electrostatic interaction between the copolymer chains during swelling, the resulting Tg is decreased significantly and was dependent on the quantity of copolymers present in the structure of polycomplexes formed. Overall, the interaction between countercharged copolymers during passage in gastrointestinal tract can strongly modify the release profile of the model drug diclofenac sodium. © 2012 Elsevier B.V. All rights reserved
Combination of (M)DSC and surface analysis to study the phase behaviour and drug distribution of ternary solid dispersions
Purpose: Miscibility of the different compounds that make up a solid dispersion based formulation play a crucial role in the drug release profile and physical stability of the solid dispersion as it defines the phase behaviour of the dispersion. The standard technique to obtain information on phase behaviour of a sample is (modulated) differential scanning calorimetry ((M)DSC). However, for ternary mixtures (M)DSC alone is not sufficient to characterize their phase behaviour and to gain insight into the distribution of the active pharmaceutical ingredient (API) in a two-phased polymeric matrix.
Methods: MDSC was combined with complementary surface analysis techniques, specifically time-of-flight secondary ion mass spectrometry (ToF-SIMS) and atomic force microscopy (AFM). Three spray-dried model formulations with varying API/PLGA/PVP ratios were analyzed.
Results: The distribution of the API in the ternary solid dispersions depended on formulation parameters. The extent of API surface coverage and therefore the distribution of the API over both polymeric phases differed significantly for the three formulations.
Conclusions: Combining (M)DSC and surface analysis rendered additional insights in the composition of mixed phases in complex systems, like ternary solid dispersions
Interpolyelectrolyte complexes of Eudragit® e PO with sodium alginate as potential carriers for colonic drug delivery: Monitoring of structural transformation and composition changes during swellability and release evaluating
Background: With a view to the application in oral colon drug delivery systems, swelling and release behavior of synthesized interpolyelectrolyte complexes (IPEC) between sodium alginate and Eudragit® EPO were investigated. Method: The microenvironmental changes in IPECs structure as a function of pH during swellability testing were investigated using FT-IR spectroscopy and elementary analysis. Results: All samples of IPECs (Z 0.661.25) during swelling were transformed to a similar structure with approximately the same composition. The release of the model drug diclofenac sodium was significantly delayed from matrices made up of the IPECs and independent from the composition of polycomplexes. Conclusion: According to the obtained results, these IPECs can be considered to have potential in colonic drug delivery as combined pH- and time-dependent systems. © 2009 Informa UK, Ltd
Structural transformations during swelling of polycomplex matrices based on countercharged (meth)acrylate copolymers (Eudragit® EPO/Eudragit® L 100-55)
With a view to the application in oral controlled drug delivery systems (DDS), the design of new interpolyelectrolyte complexes (IPECs) between countercharged types of Eudragit® EPO (EPO) and Eudragit® L 100-55 (L100-55) was investigated. The formation and composition of four new IPECs between EPO and L100-55 were established by elementary analysis. The structure of the synthesized IPEC was investigated using FTIR spectroscopy and modulated-temperature differential scanning calorimetry. The binding ratio of a unit molecule of EPO with L100-55 was found to range between 1:2.75 (Z = 0.36) and 1:0.55 (Z = 1.81) while increasing the pH value from 5.5 to 7.0. As a result of electrostatic interaction between the copolymer chains, the glass transition temperature of the IPEC increased significantly. A large pH-sensitive swelling behavior was observed for different structures of the IPECs. The outcome of swelling and diclofenac sodium release from the polycomplex matrices confirm that they have great potential to be used as a controlled DDS in specified regions of gastrointestinal tract. © 2010 Wiley-Liss, Inc. and the American Pharmacists Association
The phage therapy paradigm: prêt-à-porter or sur-mesure?
The present opinion is the result of discussions on the future of
phage therapy (personalized or large-scale uniform therapy?)
during the first International Congress on Viruses of Microbes,
held at the Institut Pasteur in Paris on June 21–25, 2010
Fizikokemijska karakterizacija čvrstih disperzijskih sustava tadalafila s poloksamerom 407
Dissolution behaviour of a poorly water-soluble drug, tadalafil, from its solid dispersion systems with poloxamer 407 has been investigated. Solid dispersion systems of tadalafil were prepared with poloxamer 407 in 1:0.5, 1:1.5 and 1:2.5 ratios using the melting method. Characterization of binary systems with FTIR and powder XRPD studies demonstrated the presence of strong hydrogen bonding interactions, a significant decrease in crystallinity and the possibility of existence of amorphous entities of the drug. In the binary systems tested, 1:0.5 proportion of tadalafil/poloxamer 407 showed rapid dissolution of tadalafil (DE30 70.9 ± 3.6 %). In contrast, higher proportions of poloxamer 407 (1:1.5 and 1:2.5) offered no advantage towards dissolution enhancement of the drug from corresponding binary systems indicating altered rheological characteristics of the polymer, at its higher concentration, which might have retarded the release rate of tadalafil.U radu je ispitivano oslobađanje u vodi teško topljivog lijeka tadalafila iz čvrstih disperzijskih sustava. Ti sustavi pripravljeni su s poloksamerom 407 u omjeru lijeka i polimera 1:0,5, 1:1,5 i 1:2,5, koristeći metodu taljenja. Karakterizacija binarnih sustava s FTIR i rendgenskom difrakcijom praha XRD ukazuje na prisutnost snažnih vodikovih veza, značajno smanjenje kristaliničnosti i moguću prisutnost amorfnog lijeka. Iz binarnog sustava tadalafil/poloksamer 1:0,5 oslobađanje ljekovite tvari je brzo (DE30 70,9 ± 3,6 %). Nasuprot tome, iz pripravaka s višim omjerima lijeka i polimera (1:1,5 i 1:2,5) oslobađanje ljekovite tvari nije povećano. Usporavanje oslobađanja tadalafila moglo bi biti posljedicom promjene reoloških svojstava polimera pri višim koncentracijama
Investigation of the diurnal variation in bone resorption for optimal drug delivery and efficacy in osteoporosis with oral calcitonin
- …