Use of a temperature ramp approach (TRA) to design an optimum and robust freeze-drying process for pharmaceutical formulations

Abstract Ibuprofen, a weakly acidic non-steroidal anti-inflammatory drug having poor aqueous solubility, is a challenging drug for the development of pharmaceutical formulations, resulting in numerous research attempts focusing on improvement of its solubility and consequently bioavailability. Most studies have been done for solid dosage forms, with very little attention paid to parenterals. Hence, the main purpose of the present study was to enhance ibuprofen solubility as a result of formulation composition and the freeze drying process. Moreover, the purpose was to prepare a freeze dried dosage form with improved ibuprofen solubility that could, after simple reconstitution with water for injection, result in an isotonic parenteral solution. Solubility of ibuprofen was modified by various excipients suitable for parenteral application. Drug interactions with selected excipients in the final product/lyophilisate were studied by a combined use of XRPD, DSC, Raman and ss-NMR. Analyses of lyophilized samples showed solubility enhancement of ibuprofen and in situ formation of an ibuprofen salt with the alkaline excipients used.

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Video real-time imaging of artificial membranes during freeze-drying by cryo-electron microscopy

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s042482010010216x ◽

1988 ◽

Vol 46 ◽

pp. 16-17

Author(s):

Alan S. Rudolph ◽

Ronald R. Price

Keyword(s):

Real Time ◽

Self Assembly ◽

Freeze Drying ◽

Video Capture ◽

Drying Process ◽

Artificial Membranes ◽

The Past ◽

Cryo Electron Microscopy ◽

Spherical Structures ◽

Capture Techniques

We have employed cryoelectron microscopy to visualize events that occur during the freeze-drying of artificial membranes by employing real time video capture techniques. Artificial membranes or liposomes which are spherical structures within internal aqueous space are stabilized by water which provides the driving force for spontaneous self-assembly of these structures. Previous assays of damage to these structures which are induced by freeze drying reveal that the two principal deleterious events that occur are 1) fusion of liposomes and 2) leakage of contents trapped within the liposome [1]. In the past the only way to access these events was to examine the liposomes following the dehydration event. This technique allows the event to be monitored in real time as the liposomes destabilize and as water is sublimed at cryo temperatures in the vacuum of the microscope. The method by which liposomes are compromised by freeze-drying are largely unknown. This technique has shown that cryo-protectants such as glycerol and carbohydrates are able to maintain liposomal structure throughout the drying process.

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Effects of freeze drying process on the production of cashew apple powder: Determination of bioactive compounds and fruit powder properties

Journal of Food Processing and Preservation ◽

10.1111/jfpp.15466 ◽

2021 ◽

Author(s):

R Harin ◽

G Nandhini Devi

Keyword(s):

Bioactive Compounds ◽

Freeze Drying ◽

Drying Process ◽

Cashew Apple ◽

Powder Properties ◽

Fruit Powder

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Strengthening of Porcine Plasma Protein Superabsorbent Materials through a Solubilization-Freeze-Drying Process

Polymers ◽

10.3390/polym13050772 ◽

2021 ◽

Vol 13 (5) ◽

pp. 772

Author(s):

Estefanía Álvarez-Castillo ◽

Carlos Bengoechea ◽

Antonio Guerrero

Keyword(s):

Water Uptake ◽

Plasma Protein ◽

Freeze Drying ◽

Meat Industry ◽

Drying Process ◽

Uptake Capacity ◽

Water Uptake Capacity ◽

Protein Flour ◽

Hydrophilic Materials ◽

By Products

The replacement of common acrylic derivatives by biodegradable materials in the formulation of superabsorbent materials would lessen the associated environmental impact. Moreover, the use of by-products or biowastes from the food industry that are usually discarded would promote a desired circular economy. The present study deals with the development of superabsorbent materials based on a by-product from the meat industry, namely plasma protein, focusing on the effects of a freeze-drying stage before blending with glycerol and eventual injection molding. More specifically, this freeze-drying stage is carried out either directly on the protein flour or after its solubilization in deionized water (10% w/w). Superabsorbent materials obtained after this solubilization-freeze-drying process display higher Young’s modulus and tensile strength values, without affecting their water uptake capacity. As greater water uptake is commonly related to poorer mechanical properties, the proposed solubilization-freeze-drying process is a useful strategy for producing strengthened hydrophilic materials.

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An experimental study of drying behaviour in ice patterns formed during spin freezing and its influence on the freeze-drying process

Heat and Mass Transfer ◽

10.1007/s00231-019-02596-z ◽

2019 ◽

Vol 55 (9) ◽

pp. 2469-2481

Author(s):

G. Srinivasan ◽

B. Raja

Keyword(s):

Experimental Study ◽

Freeze Drying ◽

Drying Process ◽

Spin Freezing ◽

Drying Behaviour

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Effect of multi-mode dual-frequency ultrasound pretreatment on the vacuum freeze-drying process and quality attributes of the strawberry slices

Ultrasonics Sonochemistry ◽

10.1016/j.ultsonch.2021.105714 ◽

2021 ◽

pp. 105714

Author(s):

Baoguo Xu ◽

Jianan Chen ◽

Essodézam Sylvain Tiliwa ◽

Weiqiang Yan ◽

SM Roknul Azam ◽

...

Keyword(s):

Freeze Drying ◽

Quality Attributes ◽

Dual Frequency ◽

Drying Process ◽

Multi Mode ◽

Ultrasound Pretreatment ◽

Frequency Ultrasound

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Studies on the Catalytic Properties of Crude Freeze-Dried Preparations of Yarrowia lipolytica Extracellular Lipases for Geranyl Ester Derivative Synthesis

Biomolecules ◽

10.3390/biom11060839 ◽

2021 ◽

Vol 11 (6) ◽

pp. 839

Author(s):

Karina Jasińska ◽

Bartłomiej Zieniuk ◽

Dorota Nowak ◽

Agata Fabiszewska

Keyword(s):

Freeze Drying ◽

Antioxidant Properties ◽

Antibacterial Properties ◽

Synthetic Activity ◽

Drying Process ◽

Enzyme Preparations ◽

Ester Derivative ◽

Freeze Dried ◽

The Impact ◽

Geranyl Ester

The study aimed to evaluate the impact of selected factors of the freeze-drying process on the hydrolytic and synthetic activity of the extracellular lipases of Y. lipolytica KKP 379 and to attempt the use of the crude enzyme preparation as a biocatalyst in the synthesis of geranyl 4-hydroxyphenylpropanoate. Antioxidant and antibacterial properties of the geranyl ester derivative were also investigated in order to evaluate their usefulness as a novel food additive. The studies confirmed that freeze-drying was an effective method of dehydrating yeast supernatant and allowed for obtaining lyophilizates with low water activity from 0.055 to 0.160. The type and concentration of the additive (2–6% whey protein hydrolyzate, 0.5% and 1% ammonium sulphate) had a significant effect on the hydrolytic activity of enzyme preparations, while the selected variants of drying temperature during the freeze-drying process were not significant (10 °C and 50 °C). Low yield of geranyl 4-hydroxyphenylopropionate was shown when the lyophilized supernatant was used (5.3%), but the yield of ester synthesis increased when the freeze-dried Y. lipolytica yeast biomass was applied (47.9%). The study confirmed the antioxidant properties of the synthesized ester by the DPPH• and CUPRAC methods, as well as higher antibacterial activity against tested bacteria than its precursor with 0.125 mM MIC (minimal inhibitory concentration) against L. monocytogenes.

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