Improving the Chemical Stability of Amorphous Solid Dispersion with Cocrystal Technique by Hot Melt Extrusion

Liu, Xu; Lü, Ming; Guo, Zhefei; Huang, Lin; Feng, Xinliang; Wu, Chuanbin

doi:10.1007/s11095-011-0605-4

Cited by 150 publications

(106 citation statements)

References 44 publications

(45 reference statements)

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“…5c), more than 85% of dipyridamole and theophylline were released within the first 30 min. This confirms the suitability of PVP as a hydrophilic carrier for engineering immediate release 3D printed dosage forms (43).…”

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confidence: 73%

A Lower Temperature FDM 3D Printing for the Manufacture of Patient-Specific Immediate Release Tablets

et al. 2016

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2 ABSTRACTPurpose. The fabrication of a ready-to-use immediate release tablets via 3D printing provides a powerful tool to on-demand individualization of dosage form. This work aims to adapt a widely used pharmaceutical grade polymer, polyvinylpyrrolidone (PVP), for instant on-demand production of immediate release tablets via FDM 3D printing.Methods. Dipyridamole or theophylline loaded filaments were produced via processing a physical mixture of API (10%) and PVP in the presence of plasticizer through hot-melt extrusion (HME). Computer software was utilized to design a capletshaped tablet. The surface morphology of the printed tablet was assessed using scanning electron microscopy (SEM). The physical form of drug and its integrity following an FDM 3D printing were assessed using x-ray powder diffractometry (XRPD), thermal analysis and HPLC. In vitro drug release studies for all 3D printed tablets were conducted in a USP II dissolution apparatus.Results. Bridging 3D printing process with HME in the presence of a thermostable filler, talc, enabled the fabrication immediate release tablets at temperatures as low as 110 o C. The integrity of two models drugs was maintained following HME and FDM 3D printing. XRPD indicated that a portion of the loaded theophylline remained crystalline in the tablet. The fabricated tablets demonstrated excellent mechanical properties, acceptable in-batch variability and an immediate in vitro release pattern. Conclusions.Combining the advantages of PVP as an impeding polymer with FDM 3D printing at low temperatures, this approach holds a potential in expanding the spectrum of drugs that could be used in FDM 3D printing for on demand manufacturing of individualised dosage forms.

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confidence: 73%

A Lower Temperature FDM 3D Printing for the Manufacture of Patient-Specific Immediate Release Tablets

et al. 2016

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“…In fusion, the competition mechanism between CBZ and NIC with HPMC to form hydrogen bonds has been proposed (11). When the physical mixture of CBZ III, NIC and HPMC was heated up, NIC was molten first and then both CBZ III and HPMC can dissolve in molten NIC and form intermolecular hydrogen bonds between three components (15).…”

Section: Discussionmentioning

confidence: 99%

Investigation of the Effect of Hydroxypropyl Methylcellulose on the Phase Transformation and Release Profiles of Carbamazepine-Nicotinamide Cocrystal

Qiu

et al. 2014

Pharm Res

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Purpose: the aim of this work was to investigate the influence of hydroxypropyl methylcellulose (HPMC) on the phase transformation and release profile of carbamazepinenicotinamide (CBZ-NIC) cocrystal in solution and in sustained release matrix tablets.Methods: The polymorphic transitions of the CBZ-NIC cocrystal and its crystalline properties were examined by differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), Raman spectroscopy, and scanning electron microscopy (SEM).Results: The apparent CBZ solubility and dissolution rate of CBZ-NIC cocrystal were constant in different concentrations of HPMC solutions. In a lower percentage of HPMC in the matrix tablets, the CBZ release profile of the CBZ-NIC cocrystal was nonlinear and declined over time. With an increased HPMC content in the tablets, the CBZ-NIC cocrystal formulation showed a significantly higher CBZ release rate in comparison with the other two formulations of CBZ III and the physical mixture.Conclusions: Because of a significantly improved dissolution rate of the CBZ-NIC cocrystal, the rate of CBZ enteringinto solution is significantly faster than the rate of formation of the CBZ-HPMC soluble complex in solution, leading to a higher supersaturation level of CBZ and subsequently precipitation of CBZ dihydrate.

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“…indication of crystalline carbamazepine. 33 The differential scanning calorimetric thermogram for crystalline carbamazepine shows a single sharp endothermic peak at 190°C 34 ( Figure 6A), corresponding to its intrinsic melting point. In turn, in the thermograms for 10% and 20% SBA-15-CBZ ( Figure 6C and D), no peak relative to drug melting was observed, confirming the absence of carbamazepine crystals in the drug-loaded silica.…”

Section: Drug-loading Capacitymentioning

confidence: 99%

Increasing the oral bioavailability of poorly water-soluble carbamazepine using immediate-release pellets supported on SBA-15 mesoporous silica

Wang¹,

Bao²,

Quan³

et al. 2012

IJN

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Background and methods:The aim of this study was to develop an immediate-release pellet formulation with improved drug dissolution and adsorption. Carbamazepine, a poorly watersoluble drug, was adsorbed into mesoporous silica (SBA-15-CBZ) via a wetness impregnation method and then processed by extrusion/spheronization into pellets. Physicochemical characterization of the preparation was carried out by scanning electron microscopy, transmission electron microscopy, nitrogen adsorption, small-angle and wide-angle x-ray diffraction, and differential scanning calorimetry. Flowability and wettability of the drug-loaded silica powder were evaluated by bulk and tapped density and by the angle of repose and contact angle, respectively. The drug-loaded silica powder was formulated into pellets to improve flowability. Results: With maximum drug loading in SBA-15 matrices determined to be 20% wt, in vitro release studies demonstrated that the carbamazepine dissolution rate was notably improved from both the SBA-15 powder and the corresponding pellets as compared with the bulk drug. Correspondingly, the oral bioavailability of SBA-15-CBZ pellets was increased considerably by 1.57-fold in dogs (P , 0.05) compared with fast-release commercial carbamazepine tablets. Conclusion: Immediate-release carbamazepine pellets prepared from drug-loaded silica provide a feasible approach for development of a rapidly acting oral formulation for this poorly water-soluble drug and with better absorption.

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Improving the Chemical Stability of Amorphous Solid Dispersion with Cocrystal Technique by Hot Melt Extrusion

Abstract: By in-situ forming cocrystal, chemically stable amorphous solid dispersions were prepared by MM and HME at a depressed processing temperature. This method provides an attractive opportunity for HME of heat-sensitive drugs.

Cited by 150 publications

References 44 publications

A Lower Temperature FDM 3D Printing for the Manufacture of Patient-Specific Immediate Release Tablets

A Lower Temperature FDM 3D Printing for the Manufacture of Patient-Specific Immediate Release Tablets

Investigation of the Effect of Hydroxypropyl Methylcellulose on the Phase Transformation and Release Profiles of Carbamazepine-Nicotinamide Cocrystal

Increasing the oral bioavailability of poorly water-soluble carbamazepine using immediate-release pellets supported on SBA-15 mesoporous silica

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