Effect of plasticiser type on the hot melt extrusion of venlafaxine hydrochloride

Bounartzi, Melina; Panagopoulou, Athanasia; Kantiranis, Nikolaos; Malamataris, S.; Nikolakakis, Ioannis

doi:10.1111/jphp.12117

Cited by 18 publications

(13 citation statements)

References 23 publications

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“…[111] in 26.1% of the CAMS prepared by the thermodynamic pathway and 20.4% were obtained by solvent removal, which is a method commonly used to obtain (co-)crystals but also exploited for the formulation of CAMS [92]. Other preparation methods include for example inkjet-printing (thermodynamic pathway) [93], hot melt extrusion (mainly thermodynamic pathway) [94][95][96], in situ co-amorphization [97][98][99][100], co-precipitation (thermodynamic pathway) [101], and co-grinding (kinetic pathway; defined as manually grinded) [102], of which some are difficult to assign to a certain pathway (thermodynamic or kinetic). Interestingly, in some cases, depending on the used preparation method, a drug and a co-former could form a CAMS or not.…”

Section: Preparation Methods Of Camsmentioning

confidence: 99%

“…Despite these promising examples using ternary CAMS, potential risks should also be taken into consideration. A similar concept (i.e., adding a small molecule into ASDs to improve the performance of ASDs) has been applied in the polymer ASD research [96,152]. However, it was recently discovered that the addition of saccharin or tryptophan resulted in a decreased physical stability of carbamazepine-PVP ASD in both predictions and experiment validations [56].…”

Section: Acyclovirmentioning

confidence: 99%

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Co-Amorphous Drug Formulations in Numbers: Recent Advances in Co-Amorphous Drug Formulations with Focus on Co-Formability, Molar Ratio, Preparation Methods, Physical Stability, In Vitro and In Vivo Performance, and New Formulation Strategies

Grohganz

Hempel

2021

Pharmaceutics

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Co-amorphous drug delivery systems (CAMS) are characterized by the combination of two or more (initially crystalline) low molecular weight components that form a homogeneous single-phase amorphous system. Over the past decades, CAMS have been widely investigated as a promising approach to address the challenge of low water solubility of many active pharmaceutical ingredients. Most of the studies on CAMS were performed on a case-by-case basis, and only a few systematic studies are available. A quantitative analysis of the literature on CAMS under certain aspects highlights not only which aspects have been of great interest, but also which future developments are necessary to expand this research field. This review provides a comprehensive updated overview on the current published work on CAMS using a quantitative approach, focusing on three critical quality attributes of CAMS, i.e., co-formability, physical stability, and dissolution performance. Specifically, co-formability, molar ratio of drug and co-former, preparation methods, physical stability, and in vitro and in vivo performance were covered. For each aspect, a quantitative assessment on the current status was performed, allowing both recent advances and remaining research gaps to be identified. Furthermore, novel research aspects such as the design of ternary CAMS are discussed.

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Section: Preparation Methods Of Camsmentioning

confidence: 99%

Section: Acyclovirmentioning

confidence: 99%

Co-Amorphous Drug Formulations in Numbers: Recent Advances in Co-Amorphous Drug Formulations with Focus on Co-Formability, Molar Ratio, Preparation Methods, Physical Stability, In Vitro and In Vivo Performance, and New Formulation Strategies

Grohganz

Hempel

2021

Pharmaceutics

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“…Materials with similar δ t values are considered miscible or that one can dissolve in the other. Therefore, comparison of δ t values can be used to predict miscibility of PG with the examined polymers [30]. From the values given in Table 2, it can be seen that the contribution of dispersive forces (δ d ) is similar for all materials, but the polar (δ p ) and H-bonding (δ hb ) components are different, with cellulose-based excipients showing higher δ p , δ hb and hence, higher δ t values (from 30.6 to 39.3 MPa 1/2 compared with 18.9 to 21.9 MPa 1/2 ).…”

Section: Hansen Solubility Parametersmentioning

confidence: 99%

Solubility Improvement of Progesterone from Solid Dispersions Prepared by Solvent Evaporation and Co-milling

et al. 2020

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The aim of this contribution was to evaluate the impact of processing methods and polymeric carriers on the physicochemical properties of solid dispersions of the poorly soluble drug progesterone (PG). Five polymers: hydroxypropyl methylcellulose (HPMC), hydroxypropyl methylcellulose acetate succinate (HPMCAS), microcrystalline cellulose (MCC), polyvinylpyrrolidone (PVP) and silica (SiO2), and two processing methods: solvent evaporation (SE) and mechano-chemical activation by co-milling (BM) were applied. H-bonding was demonstrated by FTIR spectra as clear shifting of drug peaks at 1707 cm−1 (C20 carbonyl) and 1668 cm−1 (C3 carbonyl). Additionally, spectroscopic and thermal analysis revealed the presence of unstable PG II polymorphic form and a second heating DSC cycle, the presence of another polymorph possibly assigned to form III, but their influence on drug solubility was not apparent. Except for PG–MCC, solid dispersions improved drug solubility compared to physical mixtures. For SE dispersions, an inverse relationship was found between drug water solubility and drug–polymer Hansen solubility parameter difference (Δδt), whereas for BM dispersions, the solubility was influenced by both the intermolecular interactions and the polymer Tg. Solubility improvement with SE was demonstrated for all except PG–MCC dispersions, whereas improvement with BM was demonstrated by the PG–HPMC, PG–PVP and PG–HPMCAS dispersions, the last showing impressive increase from 34.21 to 82.13 μg/mL. The extensive H-bonding between PG and HPMCAS was proved by FTIR analysis of the dispersion in the liquid state. In conclusion, although SE improved drug solubility, BM gave more than twice greater improvement. This indicates that directly operating intermolecular forces are more efficient than the solvent mediated.

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“…Small differences in the molecular arrangement and/or environment due to non-specific intermolecular interactions, H-bonds or π−π interactions underline interactions and formation of heterodimers [ 12 , 66 ]. Changes in the FTIR spectra may also indicate salt formation e.g., between IND and ARG in co-amorphous SDs or even esterification e.g., between venlafaxine and citric acid [ 55 , 67 ].…”

Section: Solid State Characterizationmentioning

confidence: 99%

“…PEO reduced the melt viscosity, prevented phase separation (despite Tg reduction) and resulted in a ternary amorphous SD where PEO acted as co-solvent for both drugs. Bounartzi et al [ 67 ] applied HME using the ternary mixture citric acid-Eudragit RSPO-venlafaxine hydrochloride (CA-RSPO-VEN) and produced co-amorphous transparent SD. Since in the binary CA-VEN extrudate some crystalline reflections of plasticizer existed, it was concluded that the matrix polymer was essential for the formation and stabilization of the CA-VEN co-amorphous dispersion.…”

Section: Preparation Of Co-amorphous Solid Dispersionsmentioning

confidence: 99%

Co-Amorphous Solid Dispersions for Solubility and Absorption Improvement of Drugs: Composition, Preparation, Characterization and Formulations for Oral Delivery

2018

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The amorphous solid state offers an improved apparent solubility and dissolution rate. However, due to thermodynamic instability and recrystallization tendencies during processing, storage and dissolution, their potential application is limited. For this reason, the production of amorphous drugs with adequate stability remains a major challenge and formulation strategies based on solid molecular dispersions are being exploited. Co-amorphous systems are a new formulation approach where the amorphous drug is stabilized through strong intermolecular interactions by a low molecular co-former. This review covers several topics applicable to co-amorphous drug delivery systems. In particular, it describes recent advances in the co-amorphous composition, preparation and solid-state characterization, as well as improvements of dissolution performance and absorption are detailed. Examples of drug-drug, drug-carboxylic acid and drug-amino acid co-amorphous dispersions interacting via hydrogen bonding, π−π interactions and ionic forces, are presented together with corresponding final dosage forms.

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Effect of plasticiser type on the hot melt extrusion of venlafaxine hydrochloride

Abstract: CAMH and Lutrol have different reactivities towards venlafaxine HCl and also different plasticising mechanisms for Eudragit RSPO because of hydrogen bonding and because of similar overall molecular attractive forces, respectively.

Cited by 18 publications

References 23 publications

Co-Amorphous Drug Formulations in Numbers: Recent Advances in Co-Amorphous Drug Formulations with Focus on Co-Formability, Molar Ratio, Preparation Methods, Physical Stability, In Vitro and In Vivo Performance, and New Formulation Strategies

Co-Amorphous Drug Formulations in Numbers: Recent Advances in Co-Amorphous Drug Formulations with Focus on Co-Formability, Molar Ratio, Preparation Methods, Physical Stability, In Vitro and In Vivo Performance, and New Formulation Strategies

Solubility Improvement of Progesterone from Solid Dispersions Prepared by Solvent Evaporation and Co-milling

Co-Amorphous Solid Dispersions for Solubility and Absorption Improvement of Drugs: Composition, Preparation, Characterization and Formulations for Oral Delivery

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