A Method for the Preparation of Submicron Particles of Sparingly Water-Soluble Drugs by Precipitation in Oil-in-Water Emulsions. I: Influence of Emulsification and Surfactant Concentration

Recently, submicron particles have been discussed as a means to increase the bioavailability of poorly water-soluble drugs. Separation of these small particles is done with both fibre and membrane filters, as well as electrostatic precipitators. A major disadvantage of an electrostatic precipitator (ESP) is the agglomerate formation on the precipitation electrode. These agglomerates frequently show low bioavailability, due to the decreased specific surface area and poor wettability. In this work, a new melt electrostatic precipitator was developed and tested to convert submicron particles into a solid dispersion in order to increase the bioavailability of active pharmaceutical ingredients. The submicron particles were generated by spray drying and transferred to the ESP, where the collection electrode is covered with a melt, which served as matrix after solidification. The newly developed melt electrostatic precipitator was able to collect isolated naproxen particles in a molten carrier. A solid naproxen xylitol dispersion was prepared, which showed a reduction of the dissolution time by 82%, and a release of 80% of the total drug, compared to the physical mixture.

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Triterpene Saponin Glycosides Impact the Percutaneous Delivery of Water Soluble Drugs

10.1557/proc-1140-hh05-32 ◽

2008 ◽

Cited By ~ 1

Author(s):

V. Prasad Shastri ◽

Christopher Pino ◽

Michael A. Scherer ◽

Chenxia Monica. Guan

Keyword(s):

Water Soluble ◽

Triterpene Saponin ◽

Water Soluble Drugs

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Solid Dispersions: A Review

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v4i2.8857 ◽

2014 ◽

Vol 4 (2) ◽

Author(s):

Sumant Saini ◽

Yashwant .

Keyword(s):

Solid Dispersions ◽

Physicochemical Characterization ◽

Water Soluble ◽

Absolute Minimum ◽

Technology Transfers ◽

Molecular Arrangement ◽

Water Soluble Drugs ◽

Carrier Solvent ◽

Preparation Techniques ◽

Selection Of

Solid dispersions are one of the most promising strategies to improve the oral bioavailability of poorly water soluble drugs. By reducing drug particle size to the absolute minimum, and hence improving drug wettability, bioavailability may be significantly improved. This article reviews the various preparation techniques for solid dispersion and compiles some of the recent technology transfers. The different types of solid dispersions based on the molecular arrangement have been highlighted. Some of the practical aspects to be considered for the preparation of solid dispersions, such as selection of carrier, solvent and methods of physicochemical characterization, along with an insight into the molecular arrangement of drugs in solid dispersions are also discussed. In this review, it is intended to discuss the recent advances related on the area of solid dispersions.

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Biphasic Dissolution Studies of Poorly Water Soluble Drugs

10.26226/morressier.57d6b2bdd462b8028d88da47 ◽

2016 ◽

Author(s):

Karl Box

Keyword(s):

Water Soluble ◽

Poorly Water Soluble Drugs ◽

Dissolution Studies ◽

Water Soluble Drugs ◽

Poorly Water Soluble

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Solubilization of Itraconazole by Surfactants and Phospholipid-Surfactant Mixtures: Interplay of Amphiphile Structure, pH and Electrostatic Interactions

10.26434/chemrxiv.12038682 ◽

2020 ◽

Author(s):

Zahari Vinarov ◽

Gabriela Gancheva ◽

Nikola Burdzhiev ◽

Slavka S. Tcholakova

Keyword(s):

Nmr Spectroscopy ◽

Electrostatic Interactions ◽

Triazole Ring ◽

Water Soluble ◽

Single Chain ◽

Surfactant Mixtures ◽

Solubilization Capacity ◽

Water Soluble Drugs ◽

Hydrophobic Chain ◽

Brick Dust

Although surfactants are frequently used in enabling formulations of poorly water-soluble drugs, the link between their structure and drug solubilization capacity is still unclear. We studied the solubilization of the “brick-dust” molecule itraconazole by 16 surfactants and 3 phospholipid:surfactant mixtures. NMR spectroscopy was used to study in more details the drug-surfactant interactions. Very high solubility of itraconazole (up to 3.6 g/L) was measured in anionic surfactant micelles at pH = 3, due to electrostatic attraction between the oppositely charged (at this pH) drug and surfactant molecules. <sup>1</sup>H NMR spectroscopy showed that itraconazole is ionized at two sites (2+ charge) at these conditions: in the phenoxy-linked piperazine nitrogen and in the dioxolane-linked triazole ring. The increase of amphiphile hydrophobic chain length had a markedly different effect, depending on the amphiphile type: the solubilization capacity of single-chain surfactants increased, whereas a decrease was observed for double-chained surfactants (phosphatidylglycerols). The excellent correlation between the chain melting temperatures of phosphatidylglycerols and itraconazole solubilization illustrated the importance of hydrophobic chain mobility. This study provides rules for selection of itraconazole solubilizers among classical single-chain surfactants and phospholipids. The basic physics underpinning the described effects suggests that these rules should be transferrable to other “brick-dust” molecules.

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Improved Dissolution Properties of Ketoconazole through Application of Liquisolid Techniques

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2015.8.4.9 ◽

2015 ◽

Vol 8 (4) ◽

pp. 3053-3059

Author(s):

Sudarshan Singh ◽

S S Shyale ◽

H G Sandip

Keyword(s):

Drug Release ◽

Immediate Release ◽

Water Soluble ◽

Wet Granulation ◽

Wetting Properties ◽

Enhanced Dissolution ◽

Water Soluble Drug ◽

Drug Concentrations ◽

Water Soluble Drugs ◽

Liquisolid Compacts

In present investigation liquisolid compact technique is investigated as a tool for enhanced dissolution of poorly water-soluble drug Ketoconazole. The liquisolid tablets were formulated with liquid medications, namely Propylene Glycol (PG) drug concentrations, 60% w/w, 70% w/w and 80% w/w. Avicel pH102 was used as a carrier material, Aerosil 200 as a coating material and Sodium starch glycollate as a super-disintegrant. Quality control tests, such as uniformity of tablet weight, uniformity of drug content, tablet hardness, friability test, disintegration and dissolution tests were performed to evaluate prepared tablets. For further confirmation of results the liquisolid compacts were evaluated by XRD and FTIR studies to prove that, solubility of Ketoconazole has been increased by liquisolid compact technique. From the results obtained, it was be speculated that such systems exhibit enhanced drug release profiles due to increased wetting properties and surface of drug available for dissolution. As liquisolid compacts demonstrated significantly higher drug release rates, in PG as compared to directly compressible tablets and conventional wet granulation, we lead to conclusion that it could be a promising strategy in improving the dissolution of poor water soluble drugs and formulating immediate release solid dosage forms.

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Mesoporous Silica Molecular Sieve based Nanocarriers: Transpiring Drug Dissolution Research

Current Pharmaceutical Design ◽

10.2174/1381612822666161026162005 ◽

2017 ◽

Vol 23 (3) ◽

pp. 467-480 ◽

Cited By ~ 8

Author(s):

Satyanarayan Pattnaik ◽

Kamla Pathak

Keyword(s):

Drug Release ◽

Mesoporous Silica ◽

Molecular Sieves ◽

Release Kinetics ◽

Drug Loading ◽

Scale Up ◽

Water Soluble ◽

Drug Dissolution ◽

Water Soluble Drugs ◽

Loading Methods

Background: Improvement of oral bioavailability through enhancement of dissolution for poorly soluble drugs has been a very promising approach. Recently, mesoporous silica based molecular sieves have demonstrated excellent properties to enhance the dissolution velocity of poorly water-soluble drugs. Description: Current research in this area is focused on investigating the factors influencing the drug release from these carriers, the kinetics of drug release and manufacturing approaches to scale-up production for commercial manufacture. Conclusion: This comprehensive review provides an overview of different methods adopted for synthesis of mesoporous materials, influence of processing factors on properties of these materials and drug loading methods. The drug release kinetics from mesoporous silica systems, the manufacturability and stability of these formulations are reviewed. Finally, the safety and biocompatibility issues related to these silica based materials are discussed.

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