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 An Overview on Recent Patents and Technologies on Solid Dispersion

2020 ◽  
Vol 14 (1) ◽  
pp. 63-74 ◽  
Author(s):  
Ritu Kaushik ◽  
Vikas Budhwar ◽  
Deepak Kaushik
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Formulation Development ◽  
Bioavailability Enhancement ◽  
Molecular Arrangement ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Cryogenic Processing

The oral bioavailability enhancement of poorly water-soluble medicaments is still one of the most complicated aspects of the formulation development. Various approaches are currently available for solubility and rate of dissolution enhancement such as salt formation, solubilization and reduction of particle size, each with its own limitations and advantages. Solid dispersion is one of the most suitable approaches for the formulation development of poorly water-soluble drugs. The popularity of solid dispersion is evident from the increasing number of patent applications and patents granted in this field during recent years. This article reviews the various approaches for the preparation of solid dispersion such as a solvent melting, hot-melt extrusion method, solvent evaporation method, cryogenic processing approaches etc. from the perspective of patents filed or granted for these techniques. Some of the aspects taken into account before the preparation of solid dispersions are carrier selection and physicchemical testing along with an insight into the molecular arrangement of medicaments in solid dispersion. The manuscript further highlights various commercial patented technology platforms such as Solumertm, Hovione and Kinetisol which are based on the concept of solid dispersions.

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 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

Surface Solid Dispersion – A Review

2013 ◽  
Vol 6 (1) ◽  
pp. 1915-1925
Author(s):  
Sadhna Khatry ◽  
Neha Sood ◽  
Sandeep Arora
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
High Surface ◽  
High Surface Area ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Insoluble Drugs ◽  
Poorly Water Soluble

Preparation of an effective formulation of poorly water-soluble drugs is a key challenge in pharmaceutical technology. Dissolution rate and solubility are the rate- limiting steps for increasing the bioavailability of poorly water‐soluble drugs. Solid dispersion is an efficient technique for improving dissolution rate and subsequently, the bioavailability of poorly water‐soluble drugs. Surface sSolid dDispersion is a novel technique of solid dispersion for dispersing one or more active ingredients on a water insoluble carrier of high surface area in order to achieve increased dissolution rates and bioavailability of insoluble drugs. The Vvarious polymers used in this technique are Avicel, Crosspovidone, sSodium starch glycolate, pPregelatinized starch, Cab-o-sil, Ac-di-sol, KyronT-314, Primojel and pPotato sStarch. This article reviews the various methods of preparation and characterization of surface solid dispersion and compiles some of the drugs formulated as surface solid dispersions. Some of the practical aspects to be considered for preparing surface solid dispersion are selection of a suitable carrier and method of preparation of surface solid dispersion.

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 Molecular Interactions in Solid Dispersions of Poorly Water-Soluble Drugs

Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 745
Author(s):  
Thao T. D. Tran ◽  
Phuong H. L. Tran
Keyword(s):  
Molecular Interactions ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Potent Drug

Physicochemical characterization is a crucial step for the successful development of solid dispersions, including the determination of drug crystallinity and molecular interactions. Typically, the detection of molecular interactions will assist in the explanation of different drug performances (e.g., dissolution, solubility, stability) in solid dispersions. Various prominent reviews on solid dispersions have been reported recently. However, there is still no overview of recent techniques for evaluating the molecular interactions that occur within solid dispersions of poorly water-soluble drugs. In this review, we aim to overview common methods that have been used for solid dispersions to identify different bond formations and forces via the determination of interaction energy. In addition, a brief background on the important role of molecular interactions will also be described. The summary and discussion of methods used in the determination of molecular interactions will contribute to further developments in solid dispersions, especially for quick and potent drug delivery applications.

scholarly journals SOLUBILITY ENHANCEMENT OF POORLY WATER SOLUBLE DRUGS BY VARIOUS TECHNIQUES

2019 ◽  
Vol 8 (1) ◽  
Author(s):  
Sakshi Minocha ◽  
Dr. Shilpa Pahwa ◽  
Dr. Vandana Arora
Keyword(s):  
Solid Dispersion ◽  
Water Solubility ◽  
Water Soluble ◽  
Formulation Development ◽  
Particle Size Reduction ◽  
Bioavailability Enhancement ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Poor Water Solubility

Solubility is not the ability to dissolve or thaw a substance; it may happen not only due to dissolution but also because of a chemical reaction. Solubility is the phenomenon of dissolution of solid in liquid phase to provide a homogenous system. Solubility is one of the vital factors for accomplishing desired concentration of drug in systemic circulation for pharmacological response. Low aqueous solubility is the major problem seen with formulation development of new chemical entities as well as for the generic development. With all new discovered chemical entities about 40% drugs are lipophilic and doesn’t shown therapeutic range due to their poor water solubility. Drug with poor water solubility shows slow dissolution rates, incomplete absorption and low bioavailability when taken orally. Drug solubility and bioavailability enhancement are the important in the formulation of pharmaceuticals. The Biopharmaceutics Classification System shows that Class II and IV drugs have low water solubility, poor dissolution, and low bioavailability. This review mentions different approaches used for the enhancement of the solubility of poorly water-soluble drugs that includes particle size reduction, pH adjustment, and solid dispersion. This describes the techniques of solubilizaton for the attainment of effective absorption and improved bioavailability. Keywords: Solubility, BCS classification, Bioavailability, Solid-dispersion.

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