pH-independent dissolution enhancement for multiple poorly water-soluble drugs by nano-sized solid dispersions based on hydrophobic–hydrophilic conjugates

2019 ◽  
Vol 45 (3) ◽  
pp. 514-519 ◽  
Author(s):  
Chau T. M. Tran ◽  
Phuong H. L. Tran ◽  
Thao T. D. Tran
Keyword(s):  
Solid Dispersions ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

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.

It is Possible to Achieve Tablets with Good Tabletability from Solid Dispersions – the Case of the High Dose Drug Gemfibrozil

2020 ◽  
Vol 17 ◽  
Author(s):  
Eduarda Rocha Bigogno ◽  
Luciano Soares ◽  
Matheus Henrique Ruela Mews ◽  
Melissa Zétola ◽  
Giovana Carolina Bazzo ◽  
...  
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Croscarmellose Sodium ◽  
Poorly Water Soluble

Background: Solid dispersions (SDs) have been extensively used to increase dissolution of poorly water-soluble drugs. However, there are few studies exploring SDs properties that must be considered during tablet development, like tabletability. Poorly water-soluble drugs with poor compression properties and high therapeutic doses, like gemfibrozil, are an additional challenge in the production of SDs-based tablets. Objective: This study evaluates the applicability of SDs to improve both tabletability and dissolution rate of gemfibrozil. A SD-based tablet formulation was also proposed. Method: SDs were prepared by ball milling, using hydroxypropyl methylcellulose (HPMC) as carrier, according to a 23 factorial design. The formulation variables were: gemfibrozil:HPMC ratio, milling speed, and milling time. The response in the factorial analysis was the tensile strength of the compacted SDs. Dissolution rate and solid-state characterization of SDs were also performed. Results: SDs showed simultaneous drug dissolution enhancement and improved tabletability when compared to corresponding physical mixtures and gemfibrozil. The main variable influencing drug dissolution and tabletability was the gemfibrozil:HPMC ratio. Tablets containing gemfibrozil-HPMC-SD (1:0.250 w/w) and croscarmellose sodium showed fast and complete drug release while those containing the same SD and sodium starch glycolate exhibited poor drug release due to their prolonged disintegration time. Conclusion: SDs proved to be effective for simultaneously improving tabletability and dissolution profile of gemfibrozil. Tablets containing gemfibrozil-HPMC-SD and croscarmellose sodium as disintegrating agent showed improved drug release and good mechanical strength, demonstrating the potential of HPMC-based SDs to simultaneously overcome the poor dissolution and tabletability properties of this drug.

scholarly journals Spray Congealing: An Emerging Technology to Prepare Solid Dispersions with Enhanced Oral Bioavailability of Poorly Water Soluble Drugs

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3471 ◽  
Author(s):  
Serena Bertoni ◽  
Beatrice Albertini ◽  
Nadia Passerini
Keyword(s):  
Oral Bioavailability ◽  
Solid Dispersions ◽  
Emerging Technology ◽  
Water Soluble ◽  
Oral Drug ◽  
Dissolution Enhancement ◽  
Drug Bioavailability ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

The low and variable oral bioavailability of poorly water soluble drugs remains a major concern for the pharmaceutical industry. Spray congealing is an emerging technology for the production of solid dispersion to enhance the bioavailability of poorly soluble drugs by using low-melting hydrophilic excipients. The main advantages are the absence of solvents and the possibility to obtain spherical free-flowing microparticles (MPs) by a relatively inexpensive, simple, and one-step process. This review aims to fully describe the composition, structure, physico-chemical properties, and characterization techniques of spray congealed-formulations. Moreover, the influence of these properties on the MPs performance in terms of solubility and dissolution enhancement are examined. Following, an overview of the different spray congealed systems developed to increase the oral drug bioavailability is provided, with a focus on the mechanisms underpinning the bioavailability enhancement. Finally, this work gives specific insights on the main factors to be considered for the rational formulation, manufacturing, and characterization of spray congealed solid dispersions.

scholarly journals SOLID DISPERSIONS: RESUSCITATING ORAL DELIVERY OF HYDROPHOBIC DRUGS

2019 ◽  
pp. 213-217
Author(s):  
RUCHI AGRAWAL ◽  
ABID RAZA ◽  
OM PRAKASH PATEL
Keyword(s):  
Oral Delivery ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Future Trends ◽  
Hydrophobic Drugs ◽  
Poorly Water Soluble Drugs ◽  
Advantages And Disadvantages ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Viable Method

Objective: This review article explores solid dispersions (SDs) as one of the suitable approaches to formulate poorly water-soluble drugs. The objective of this review on SD techniques is to explore their utility as a feasible, simple, and economically viable method for augmentation of dissolution of hydrophobic drugs. Methods: Various types of SDs are classified and compared. Use of surfactants to stabilize the SDs and their potential advantages and disadvantages has been discussed. Different techniques for preparing and evaluating SDs are appraised along with discussions on scalability and industrial production. Review of the current research on SD along with future trends is also offered. Results: Based on the various researches, SDs offer an efficient means of improving bioavailability while concurrently contributing to lower toxicity and dose-reduction. Conclusion: Solid-dispersions have been and continue to be one of the key technologies for solving the issue of poor solubility for newer hydrophobic molecules which are being discovered. This would give a new lease of life for such drugs enabling them to be delivered in an effective way.

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

scholarly journals A Review on Solid Dispersion and Carriers Used Therein for Solubility Enhancement of Poorly Water Soluble Drugs

2020 ◽  
Vol 10 (3) ◽  
pp. 359-369
Author(s):  
Avinash Ramrao Tekade ◽  
Jyoti Narayan Yadav
Keyword(s):  
Recent Trend ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Immediate Release ◽  
Water Soluble ◽  
Amorphous Solid Dispersions ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Enhanced Properties

A large number of hydrophilic and hydrophobic carriers in pharmaceutical excipients are available today which are used for formulation of solid dispersions. Depending on nature of carriers the immediate release solid dispersions and/or controlled release solid dispersions can be formulated. Initially crystalline carriers were used which are transformed into amorphous solid dispersions with enhanced properties. The carriers used previously were mostly synthetic one. Recent trend towards the use of natural carriers have replaced the use of synthetic carriers. This review is the overview of various synthetic, natural, semisynthetic, modified natural hydrophilic carriers used for formulation of solid dispersions.

scholarly journals Continuous Formulation Approaches of Amorphous Solid Dispersions: Significance of Powder Flow Properties and Feeding Performance

Pharmaceutics ◽  
2019 ◽  
Vol 11 (12) ◽  
pp. 654 ◽  
Author(s):  
Edina Szabó ◽  
Balázs Démuth ◽  
Dorián László Galata ◽  
Panna Vass ◽  
Edit Hirsch ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Scale Up ◽  
Amorphous Solid ◽  
Downstream Processing ◽  
Water Soluble ◽  
Content Uniformity ◽  
Amorphous Solid Dispersions ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Preparation and formulation of amorphous solid dispersions (ASDs) are becoming more and more popular in the pharmaceutical field because the dissolution of poorly water-soluble drugs can be effectively improved this way, which can lead to increased bioavailability in many cases. During downstream processing of ASDs, technologists need to keep in mind both traditional challenges and the newest trends. In the last decade, the pharmaceutical industry began to display considerable interest in continuous processing, which can be explained with their potential advantages such as smaller footprint, easier scale-up, and more consistent product, better quality and quality assurance. Continuous downstream processing of drug-loaded ASDs opens new ways for automatic operation. Therefore, the formulation of poorly water-soluble drugs may be more effective and safe. However, developments can be challenging due to the poor flowability and feeding properties of ASDs. Consequently, this review pays special attention to these characteristics since the feeding of the components greatly influences the content uniformity in the final dosage form. The main purpose of this paper is to summarize the most important steps of the possible ASD-based continuous downstream processes in order to give a clear overview of current course lines and future perspectives.

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