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Cx1 F1
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Cx1 F4
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Cx1 F1Cx1 F2Cx1 F3Cx1 F4Linear (Cx1 F1)Linear (Cx1 F2)Linear (Cx1 F3)Linear (Cx1 F4)
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Cx2 F1Cx2 F2Cx2 F3Cx2 F4Linear (Cx2 F1)Linear (Cx2 F2)Linear (Cx2 F3)Linear (Cx2 F4)
OBJECTIVES
The aim was to develop and adequately characterize, through structural analaysis and in-vitro drug release evaluations, new topical semisolid hydrophilic gels, used for administration of organometalic complexes on skin and mucosa.
The hydrophilic semisolid formulations developed based on polyoxyethylene-polyoxypropylene block copolymers showed adequate properties as vehicles for the hydrophobic organometalic complexes. They displayed pseudoplastic behavior, and in-vitro release profiles highly dependent on the solubility within the semisolid matrix.
The hysteresis loop test indicated a pseudoplastic character, demonstrated by the applicability of the Ostwald de Waele model and by the values of the flow behavior index lower than 1. The in-vitro release rates were unexpectedly high (in some instances, higher than 1 µg/cm2/min1/2), with an apparent dependence on the physico-chemical properties of the complex.
Structural and in-vitro release evaluations of poloxamer gel containing metal-oxicam coordination compounds
Ana Andreea Stănescu1, Adina Cimpoieșu2, Adrian A. Andrieș3, Sultana Niță4, Dalia Simona Miron5, Flavian Stefan Radulescu3
University of Medicine and Pharmacy „Carol Davila” Bucharest,1Faculty of Pharmacy, Department of Pharmaceutical Technology and Biopharmaceutics, 6, Traian Vuia Street, 020956, Bucharest, Romania. 2Faculty of Pharmacy, Department of Drug Control, 6, Traian Vuia Street, 020956, Bucharest, Romania.3Faculty of Pharmacy, Department of Drug Industry and Pharmaceutical Biotechnologies, 6, Traian Vuia Street, 020956, Bucharest, Romania.4National Institute for Chemical Pharmaceutical Research and Development, 112 Calea Vitan, 031299, Bucharest, Romania.5Faculty of Medicine, Department of Pharmaceutical Physics and Informatics, 6, Traian Vuia Street, 020956, Bucharest, Romania.Corresponding author: [email protected]
RESULTS AND DISCUSSION
CONCLUSIONS
REFERENCES
[1] Lee CH, Moturi V, Lee Y. Thixotropic property in pharmaceutical formulations. J Control Release. 2009;136(2):88-98. [2] United States Pharmacopoeia 36 - National Formulary 31, First supplement. Chapter <1724>.
ACKNOWLEDGEMENT
This work was supported by the Romanian Partnership Programme PN II - supported by the National Agency for Scientific Research - ANCS, CNDI - UEFISCDI, contract number 126/2012.
MATERIALS AND METHODS
The first stage was focused on the design of the vehicle and selection of a manufacturing procedure, able to generate a molecular dispersion of the hydrophobic active ingredient (noted Cx1 and Cx2, differening in the type of organic ligand). A hydrophilic polyoxyethylene-polyoxypropylene block copolymers matrix (micronized poloxamer 407, BASF GmbH) was selected, based on the its remarkable biocompatibility. A minimum quantity of cosolvent mixture was added, 10% ethanol absolute and 5% nonionic tensioactive or standardized mixture of surfactants, isopropyl-myristate (F1); Cremophor EL (F2); Saboderm G20 (F3) and Saboderm SHO (F4).The thermosensitive hydrogels were analyzed by a set of correlated tests, including the analysis of the rheological behavior (hysteresis loop test, [1]) and the evaluation of in-vitro release profiles using a vertical diffusion cell system [2].
Figure 1. Figure 2.
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Cx2 F1
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Cx2 F3
Cx2 F4
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Release rate(µg/cm2/min1/2)
0,79 0,41 0,49 0,62
Lag time (min1/2) 0,80 0,52 0,22 3,56
R2 0,9966 0,9927 0,9978 0,9926
Release rate(µg/cm2/min1/2)
1,11 0,66 1,31 0,24
Lag time (min1/2) 6,44 9,17 6,35 5,25
R2 0,9957 0,9479 0,9985 0,9914
Table 1. Parameters of the Higuchi model applied to in-vitro release profile of Cx1
Table 2. Parameters of the Higuchi model applied to in-vitro release profile of Cx2
Figure 3. Figure 4.
Figure 5. Figure 6.
