Prediction of the drug release stability of different polymeric matrix tablets containing metronidazole

Szente, Virág; Baska, Ferenc; Zelkó, Romána; Süvegh, Károly

doi:10.1016/j.jpba.2010.11.005

Cited by 10 publications

(7 citation statements)

References 7 publications

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“…As compared with the earlier studies regarding the technology of matrix tablet manufacture with metronidazole, where Carbopol, Kollidon SR and Povidon were included in the composition as substances modifying release [20], in formulations based on Eudragits, it was possible to obtain a smaller ejection of the substance during the 2h of release in 0.1 N hydrochloric acid. Hence, owing to the different parameters utilized within the dissolution test for metronidazole tablets of matrixes consisting of HPMC [14] lipids [4], it was impossible to compare the previously obtained release profiles, with the results obtained in our study.…”

Section: Dissolution Studiesmentioning

confidence: 99%

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Eudragit FS 30D as a potential polymer for use in the technology of preparing matrix tablets contain metronidazole – an experimental and mathematical modeling study

Letmanski

Kodym

Weber

et al. 2015

Current Issues in Pharmacy and Medical Sciences

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The aim of this study was to examine the usefulness of a pH-dependent copolymer - Eudragit FS - for employment in the technology of preparing modified release metronidazole matrix tablets. In addition, in our work, Eudragit RL and Eudragit RS were included in the composition of some formulations, as well as sodium lauryl sulfate and polysorbate 80. As part of the study of the dissolution test, the similarity coefficient (f2) for the obtained profiles was calculated, and mathematic models were used to estimate the kinetics and mechanism of active substance release. In our work, it was observed that the inclusion of polymer Eudragit FS alone in the tablet composition ensured a modified release of the active substance for 10 h. After this time period, the amount of metronidazole determined in the acceptor fluid was 71% - 81% of the declared dose. Modification of the composition by the addition of surfactants resulted in an increased release of the active substance of up to 98%. This effect was dependent on the type of surfactant and its quantitative ratio to the Eudragit FS. Similar release profiles were obtained for tablets containing Eudragit RS and sodium lauryl sulfate, as well as Eudragit RS and polysorbate 80. Depending on the composition of tablets, metronidazole release proceeded in accordance with either first or second-order kinetics. We calculated as well, that the differing masses of Eudragit FS in the studied formulations correlates with the order of release kinetics (p < 0.002). Such an effect was validated using the Weibull model, wherein, in all the studied formulations, the release rate was seen as a decreasing function of time. An analysis of data according to the Ritger-Peppas model and the Peppas-Sahlin model for some formulations, indicated that the mechanism of active substance release from matrix tablets is diffusion.

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Section: Dissolution Studiesmentioning

confidence: 99%

“…The dissolution test was also conducted during an artificial aging, at 40°C ± 2°C and 75% ± 5% RH for 4 weeks. Based on the obtained results, we eliminated the possibility of employing Carbopol 71G as an excipient in designing such matrixes [20].…”

mentioning

confidence: 99%

Eudragit FS 30D as a potential polymer for use in the technology of preparing matrix tablets contain metronidazole – an experimental and mathematical modeling study

Letmanski

Kodym

Weber

et al. 2015

Current Issues in Pharmacy and Medical Sciences

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“…Polymeric matrix systems were extensively studied due to their simple preparation by direct compression and their easily available excipients. Hydrophilic polymers such as hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC), and sodium carboxymethyl cellulose (CMCS) were used in the formulation of controlled release matrices, individually or as mixtures, and the drug transport kinetics depended on polymer hydration, swelling, and further erosion, as well as on drug dissolution and diffusion through the formed gel 10,11. On the other hand, insoluble matrices formed with hydrophobic polymers such as ethyl cellulose, Eudragit ® RS (Evonik, Essen, Germany), or Kollidon ® SR (BASF, Ludwigshafen, Germany) form porous structures upon hydration, and the dissolved active principle diffuses slowly through the pores into the liquid media 12–14…”

Section: Introductionmentioning

confidence: 99%

Risk assessment and experimental design in the development of a prolonged release drug delivery system with paliperidone

Iurian

Turdean

Tomuță

2017

DDDT

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This study focuses on the development of a drug product based on a risk assessment-based approach, within the quality by design paradigm. A prolonged release system was proposed for paliperidone (Pal) delivery, containing Kollidon® SR as an insoluble matrix agent and hydroxypropyl cellulose, hydroxypropyl methylcellulose (HPMC), or sodium carboxymethyl cellulose as a hydrophilic polymer. The experimental part was preceded by the identification of potential sources of variability through Ishikawa diagrams, and failure mode and effects analysis was used to deliver the critical process parameters that were further optimized by design of experiments. A D-optimal design was used to investigate the effects of Kollidon SR ratio (X1), the type of hydrophilic polymer (X2), and the percentage of hydrophilic polymer (X3) on the percentages of dissolved Pal over 24 h (Y1–Y9). Effects expressed as regression coefficients and response surfaces were generated, along with a design space for the preparation of a target formulation in an experimental area with low error risk. The optimal formulation contained 27.62% Kollidon SR and 8.73% HPMC and achieved the prolonged release of Pal, with low burst effect, at ratios that were very close to the ones predicted by the model. Thus, the parameters with the highest impact on the final product quality were studied, and safe ranges were established for their variations. Finally, a risk mitigation and control strategy was proposed to assure the quality of the system, by constant process monitoring.

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“…Water-soluble low-molecular-weight fractions of N-polyvinylpyrrolidone (PVP) (MM 5000-15,000) are polymers that satisfy these requirements. PVP is among the most widely used polymers in production of various medicinal forms (tablets, pills, injection solutions) and contrast agents [1][2][3][4][5]. One of the first successful applications of PVP was development of Povidone-iodine, Abbreviations: PVP, N-polyvinylpyrrolidone; GP, gossypol; CCl4, carbon tetrachloride; TBA, thiobarbituric acid; DPPH • , 1,1-diphenyl-2-picrylhydrazyl; ABTS • + , 2,2 -azino-bis(3-ethylbenzothiazoline-6-sulfonic acid); HRP, horseradish peroxidase; LPO, lipid peroxidation; TBARSs, thiobarbituric acid reactive substances; DCs, diene conjugates; LPC, lyso-phosphatidylcholine; LPE, lysophosphatidylethanolamine; LCL, lyso-cardiolipin; ROS, reactive oxygen species.…”

Section: Introductionmentioning

confidence: 99%

“…PVP can form complexes with various organic compounds. When a poorly soluble drug forms a complex with a PVP macromolecule, its solubility in water is increased, and so are its stability in the solution and the long blood half-life duration of its action within the organism [1,[6][7][8]. Gossypol (GP) is a natural polyphenolic compound extracted from cotton plants (Gossypium spp.).…”

Section: Introductionmentioning

confidence: 99%

Stability and antioxidant activity of gossypol derivative immobilized on N-polyvinylpyrrolidone

Йонов

Gordiyenko

Zukowska

et al. 2012

International Journal of Biological Macromolecules

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Prediction of the drug release stability of different polymeric matrix tablets containing metronidazole

Cited by 10 publications

References 7 publications

Eudragit FS 30D as a potential polymer for use in the technology of preparing matrix tablets contain metronidazole – an experimental and mathematical modeling study

Eudragit FS 30D as a potential polymer for use in the technology of preparing matrix tablets contain metronidazole – an experimental and mathematical modeling study

Risk assessment and experimental design in the development of a prolonged release drug delivery system with paliperidone

Stability and antioxidant activity of gossypol derivative immobilized on N-polyvinylpyrrolidone

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