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Impact of hydrophilic binders on stability of lipid-based sustained release matrices of quetiapine fumarate by the continuous twin screw melt granulation technique.

ABSTRACT: Dose dumping is the major drawback of sustained release (SR) matrices. The current research aimed to develop the stable lipid-based SR matrices of quetiapine fumarate (QTF) using Geleol™ (glyceryl monostearate; GMS) as the lipid matrix carrier and Klucel™ EF (HPC EF), Kollidon^® VA64, and Kollidon^® 12PF as hydrophilic binders. Formulations were developed using advanced twin screw melt granulation (TSMG) approach and the direct compression (DC) technique. Compared with the blends of DC, the granules of TSMG exhibited improved flow properties and tabletability. Solid-state characterization by differential scanning calorimetry of the prepared granules exhibited the crystalline nature of the lipid. Fourier transform infrared spectroscopy demonstrated no interaction between the formulation ingredients. The compressed matrices of TSMG and DC resulted in the sustained release of a drug over 16-24 h. Upon storage under accelerated conditions for 6 months, the matrices of TSMG retained their sustained release characteristics with no dose dumping in alcohol, whereas the matrices of DC resulted in the dose dumping of the drug attributing to the loss of matrix integrity and phase separation of lipid. Thus, it is concluded that the uniform distribution of a softened binder into a molten lipid carrier results in the stable matrices of TSMG.

SUBMITTER: Nyavanandi D

PROVIDER: S-EPMC8274555 | biostudies-literature |

REPOSITORIES: biostudies-literature

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Project description:Serial (femtosecond) crystallography at synchrotron and X-ray free-electron laser (XFEL) sources distributes the absorbed radiation dose over all crystals used for data collection and therefore allows measurement of radiation damage prone systems, including the use of microcrystals for room-temperature measurements. Serial crystallography relies on fast and efficient exchange of crystals upon X-ray exposure, which can be achieved using a variety of methods, including various injection techniques. The latter vary significantly in their flow rates - gas dynamic virtual nozzle based injectors provide very thin fast-flowing jets, whereas high-viscosity extrusion injectors produce much thicker streams with flow rates two to three orders of magnitude lower. High-viscosity extrusion results in much lower sample consumption, as its sample delivery speed is commensurate both with typical XFEL repetition rates and with data acquisition rates at synchrotron sources. An obvious viscous injection medium is lipidic cubic phase (LCP) as it is used for in meso membrane protein crystallization. However, LCP has limited compatibility with many crystallization conditions. While a few other viscous media have been described in the literature, there is an ongoing need to identify additional injection media for crystal embedding. Critical attributes are reliable injection properties and a broad chemical compatibility to accommodate samples as heterogeneous and sensitive as protein crystals. Here, the use of two novel hydro-gels as viscous injection matrices is described, namely sodium carb-oxy-methyl cellulose and the thermo-reversible block polymer Pluronic F-127. Both are compatible with various crystallization conditions and yield acceptable X-ray background. The stability and velocity of the extruded stream were also analysed and the dependence of the stream velocity on the flow rate was measured. In contrast with previously characterized injection media, both new matrices afford very stable adjustable streams suitable for time-resolved measurements.

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Impact of hydrophilic binders on stability of lipid-based sustained release matrices of quetiapine fumarate by the continuous twin screw melt granulation technique.

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