Application of supercritical fluid technology for solid dispersion to enhance solubility and bioavailability of poorly water-soluble drugs

2021 ◽  
pp. 121247
Author(s):  
Phuong Tran ◽  
Jeong-Sook Park
Keyword(s):  
Supercritical Fluid ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Supercritical Fluid Technology ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

scholarly journals Recent and Relevant Methodology in the Advancement of Solid Dispersion

2021 ◽  
Vol 11 (4-S) ◽  
pp. 247-257
Author(s):  
Shruti Talla ◽  
Kamlesh Wadher ◽  
Milind Umekar ◽  
R.T. Lohiya
Keyword(s):  
Solid Dispersion ◽  
Water Solubility ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Pharmaceutical Therapy ◽  
Supercritical Fluid Technology ◽  
Water Soluble Drugs ◽  
Recent Trends ◽  
Poorly Water Soluble ◽  
Preparation Techniques

Most of the promising drugs in development channels are poorly water-soluble drugs which limit formulation approaches, clinical application because of their low dissolution and bioavailability. And the major current challenges of the pharmaceutical industry are apropos strategies that improve the water solubility of drugs.  Solid dispersion has been considered one of the major evolutions in overcoming these issues with several successfully marketed products. Though solid dispersion has been outlined as an efficient drug delivery system, the design of specific dosage forms for pharmaceutical therapy is necessary to improve the solubility and bioavailability of poorly water-soluble drugs. Solid dispersion can be prepared by several methods such as solvent evaporation, melting, and supercritical fluid technology.  This review intends to provide an updated overview of the recent trends over the past few years in solid dispersion preparation techniques and polymer used. Along with the various pharmaceutical strategies and future visions for the solubilization of poorly water-soluble drugs Keywords: Solid dispersion, Bioavailability, Solubility, Dissolution parameters, Polymeric carrier

scholarly journals REVIEW ARTICLE: SOLUBILITY ENHANCEMENT BY SOLID DISPERSION

2017 ◽  
Vol 9 (3) ◽  
pp. 15
Author(s):  
A. N. Patil ◽  
D. M. Shinkar ◽  
R. B. Saudagar
Keyword(s):  
Solid Dispersion ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Full Potential ◽  
Drug Selection ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
New Chemical Entities ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Enhancement of solubility, dissolution rate and bioavailability of the drug is a very challenging task in drug development, nearly 40% of the new chemical entities currently being discovered are poorly water soluble drugs. The solubility behaviour of the drugs remains one of the most challenging aspects in formulation development. This results in important products not reaching the market or not achieving their full potential. Solid dispersion is one of the techniques adopted for the formulation of such drugs and various methods are used for the preparation of solid dispersion. Solid dispersion is generally prepared with a drug which is having poor aqueous solubility and hydrophilic carrier. This article review various methods and concept of solid dispersion, criteria for drug selection, advantage and disadvantage, characterization, and application.

scholarly journals Insoluble Polymers in Solid Dispersions for Improving Bioavailability of Poorly Water-Soluble Drugs

Polymers ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 1679
Author(s):  
Thao T.D. Tran ◽  
Phuong H.L. Tran
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Insoluble Polymers

In recent decades, solid dispersions have been demonstrated as an effective approach for improving the bioavailability of poorly water-soluble drugs, as have solid dispersion techniques that include the application of nanotechnology. Many studies have reported on the ability to change drug crystallinity and molecular interactions to enhance the dissolution rate of solid dispersions using hydrophilic carriers. However, numerous studies have indicated that insoluble carriers are also promising excipients in solid dispersions. In this report, an overview of solid dispersion strategies involving insoluble carriers has been provided. In addition to the role of solubility and dissolution enhancement, the perspectives of the use of these polymers in controlled release solid dispersions have been classified and discussed. Moreover, the compatibility between methods and carriers and between drug and carrier is mentioned. In general, this report on solid dispersions using insoluble carriers could provide a specific approach and/or a selection of these polymers for further formulation development and clinical applications.

scholarly journals Supercritical fluid technology for solubilization of poorly water soluble drugs via micro- and naonosized particle generation

ADMET & DMPK ◽  
2020 ◽  
Author(s):  
Shashi Kiran Misra ◽  
Kamla Pathak
Keyword(s):  
Supercritical Fluid ◽  
High Throughput Screening ◽  
Green Technology ◽  
Water Soluble ◽  
Rapid Expansion ◽  
Particle Generation ◽  
Particulate Solids ◽  
Supercritical Fluid Technology ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

<p class="ADMETabstracttext">Approximately two-third of the compounds in the pharmaceutical industry were developed through combinatorial chemistry and high throughput screening of particulate solids. Poor solubility and bioavailability of these pharmaceuticals are challenging attributes confronted by a formulator during product development. Hence, substantial efforts have been directed into the research on particle generation techniques. Although the conventional methods, such as crushing or milling and crystallization or precipitation, are still used; supercritical fluid technology introduced in the mid-1980s presents a new method of particle generation. Supercritical fluid processes not only produce micro- and nanoparticles with a narrow size distribution, they are also employed for the microencapsulation, cocrystallization, and surface coating with polymer. Recognized as a green technology, it has emerged as successful variants chiefly as Rapid Expansion of supercritical solutions (RESS), Supercritical anti-solvent (SAS) and Particles from Gas Saturated Solution (PGSS) depending upon type of solvent, solute, antisolvent and nebulization techniques. Being economical and eco-friendly, supercritical fluid technolgy has garnered considerable interest both in academia and industry for modification of physicochemical properties such as particle size, shape, density and ultimately solubility. The current manuscript is a comprehensive update on different supercritical fluid processes used for particle generation with the purpose of solubility enhancement of drugs and hence bioavailability.</p>

scholarly journals Overview of the Manufacturing Methods of Solid Dispersion Technology for Improving the Solubility of Poorly Water-Soluble Drugs and Application to Anticancer Drugs

Pharmaceutics ◽  
2019 ◽  
Vol 11 (3) ◽  
pp. 132 ◽  
Author(s):  
Phuong Tran ◽  
Yong-Chul Pyo ◽  
Dong-Hyun Kim ◽  
Sang-Eun Lee ◽  
Jin-Ki Kim ◽  
...  
Keyword(s):  
Anticancer Drugs ◽  
Small Molecule ◽  
Solid Dispersion ◽  
Route Of Administration ◽  
Water Soluble ◽  
Biologic Drugs ◽  
Poorly Water Soluble Drugs ◽  
Small Molecule Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Approximately 40% of new chemical entities (NCEs), including anticancer drugs, have been reported as poorly water-soluble compounds. Anticancer drugs are classified into biologic drugs (monoclonal antibodies) and small molecule drugs (nonbiologic anticancer drugs) based on effectiveness and safety profile. Biologic drugs are administered by intravenous (IV) injection due to their large molecular weight, while small molecule drugs are preferentially administered by gastrointestinal route. Even though IV injection is the fastest route of administration and ensures complete bioavailability, this route of administration causes patient inconvenience to visit a hospital for anticancer treatments. In addition, IV administration can cause several side effects such as severe hypersensitivity, myelosuppression, neutropenia, and neurotoxicity. Oral administration is the preferred route for drug delivery due to several advantages such as low cost, pain avoidance, and safety. The main problem of NCEs is a limited aqueous solubility, resulting in poor absorption and low bioavailability. Therefore, improving oral bioavailability of poorly water-soluble drugs is a great challenge in the development of pharmaceutical dosage forms. Several methods such as solid dispersion, complexation, lipid-based systems, micronization, nanonization, and co-crystals were developed to improve the solubility of hydrophobic drugs. Recently, solid dispersion is one of the most widely used and successful techniques in formulation development. This review mainly discusses classification, methods for preparation of solid dispersions, and use of solid dispersion for improving solubility of poorly soluble anticancer drugs.

scholarly journals NOVEL APPLICATION OF MIXED HYDROTROPIC SOLUBILIZATION TECHNIQUE IN THE FORMULATION AND EVALUATION OF SOLID DISPERSION OF FLUPIRTINE MALEATE

2018 ◽  
Vol 8 (5) ◽  
pp. 481-488
Author(s):  
Nisha Kumari Yadav ◽  
Tripti Shukla ◽  
Neeraj Upmanyu ◽  
Sharad Prakash Pandey ◽  
Mohammad Azaz Khan
Keyword(s):  
Particle Size ◽  
Solid Dispersion ◽  
Sodium Benzoate ◽  
Oral Bioavailability ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Evaporation Technique ◽  
Poorly Water Soluble

Flupirtine is an amino pyridine derivative that functions as a centrally acting non-opioid, non-steroidal analgesic. It is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties. Its muscle relaxant properties make it popular for back pain and other orthopedics uses. In the present investigation, recently developed mixed hydrotropic solid dispersion technology precludes the use of organic solvent and also decreases the individual concentration of hydrotropic agents, simultaneously decreasing their toxic potential. Mixed-hydrotropic solubilisation technique is the experience to increase the solubility of poorly water soluble drugs in the aqueous solution containing blends of hydrotropic agents, which may give synergistic enhancement effect on solubility of poorly water-soluble drugs and to reduce concentrations of each individual hydrotropic agent to minimize their toxic effects due to high concentration of hydrotropic agents. The Flupirtine loaded solid dispersion was prepared by a solvent evaporation technique using sodium benzoate and a niacinamide hydrotropic mixture. The prepared solid dispersions were valuated regarding their solubility, mean particle size, in-vitro drug release. The prepared solid dispersions were found very stable (chemically). The superior dissolution rate due to its reduced particle size may have contributed to the increased oral bioavailability. This study demonstrated that mixed-solvency may be an alternative approach for poorly soluble drugs to improve their solubility and oral bioavailability. Keywords: Flupirtine, Solid dispersion, Mixed-hydrotropic solubilisation, Solvent evaporation technique, Sodium benzoate, Niacinamide

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