Solid dispersions: A technology for improving bioavailability (original) (raw)
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Solid Dispersion: Methods and Polymers to increase the solubility of poorly soluble drugs
2012
Article history: Received on: 27/09/2012 Revised on: 14/10/2012 Accepted on: 24/10/2012 Available online: 30/10/2012 The solubility behaviour of drugs remains one of the most exigent aspects in formulation development. These days, the number of new chemical entities has dramatically increased having hiccups of poor solubility and poor permeability. Solid dispersion as a dosage form has been established a superior option for the drugs having poor aqueous solubility. Solid dispersions in water-soluble carriers have engrossed considerable interest as a means of improving the dissolution rate and bioavailability of hydrophobic drugs. Although solid dispersions have tremendous potential for improving drug solubility and only a few marketed products using this approach. There are various methods available to improve the solubility of the new drug in which solid dispersion emerged promising. A Solid dispersion generally composed of two componentsthe drug and the polymer matrix. Numerous me...
Solid Dispersions: an Approach to Enhance Solubility of poorly Water Soluble Drug
2013
Solid dispersions have attracted considerable interest as an efficient means of improving the dissolution rate and hence the bioavailability of a range of poorly water-soluble drugs. Solid dispersions of poorly water-soluble drugs with water-soluble carriers has reduced the incidence of these problems and enhanced dissolution. The focus of this review article is on the advantages, limitations, various methods of preparation and characterization of the solid dispersion. The different types of solid dispersions based on their molecular arrangement have been highlighted. Some of the practical aspects to be considered for the preparation of solid dispersions, such as selection of carrier and methods of physicochemical characterization have also been discussed. In this review, it is intended to discuss the future prospects related to the area of solid dispersion manufacturing.
A review on solid dispersion : a substitute approach for poorly water soluble drug
2015
The solid dispersion has become a momentous solubilization technology for poorly water soluble drugs.It is usually two component system of drug polymer, which interacts between the drug design and its performance. Solid dispersion in water-soluble carriers have interacted a means of developing the dissolution rate and bioavailability of the hydrophobic drugs. The aim of this present study is to compare the solubility of different drugs with the increased polymer concentration. The solid dispersion is stable under accelerated storage conditions.PVP K30 brings out a way to enhance the solubility and dissolution rate of the certain drug. Solid dispersions have attracted considerable interest as an important means of mounting dissolution rate with various methodologies. The main focus of this article is on advantages, disadvantages, developing various methods and categorization of the solid dispersion. There are various carriers which have been used in the solid dispersion technology an...
Indian Journal of Pharmaceutical Education and Research, 2021
Solid dispersion (SD) is one of the oldest and widely utilized techniques to improve the solubility of slowly dissolving drugs. A variety of pharmaceutically compatible additives using different emerging technology is used for preparing SDs. Multiple approaches were designed to prepare SDs by such as kneading, co-milling, fusion, solvent evaporation and various solvent-associated methods. The selection of appropriate preparation method and carrier is vital for producing a homogenous product affecting its stability and biological activity. Many attempts were recently carried out to improve the scalability of the applied approaches and the results were novel preparation methods such as KinetiSol, Electrospinning and Hot-melt extrusion. In the present review, drug carriers used to formulate SD were classified as small molecular weight carriers, large molecular weight named polymeric carriers and functionalized polymeric ones. Moreover, new attractive SD formulated using the newly emerged natural carriers recently joined the field of the pharmaceutical industry.
2014
Solid dispersions are considered as the one of the most emerging technologies for improving the practically water insoluble drugs dissolution profile thereby increasing the bioavailability of hydrophobic drugs. This article review provides the information about different types of solid dispersions based on their molecular arrangement and type of matrix material employed. Different methods of preparations of solid dispersions and recent advances in preparation methods have been highlighted. Various analytical tools employed in the characterization of solid dispersions are discussed.
Review article: Solid dispersion currently practiced in pharmaceutical field
Improvement of bioavailability of hydrophobic drugs is a great challenge. Over the years a variety of solubilization techniques have been studied and widely used, as more than 40% newly drugs are poorly water soluble in pharmaceutical field. To improve such solubility issues, solid dispersion technique is widely used. This article reviews different technologies of solid dispersion, current trends, advantages and criticisms. The remaining portion of this article is focused on various formulations which are marketed by solid dispersion technology.
Solid dispersion is the prerequisite technique for increasing the dissolution and bioavailability of the hydrophobic drugs. The technique generally provides more significant enhancement in solubility or dissolution rate as compared to other techniques which mainly relies only on the reduction of particle size. The factor of re-crystallization associated with reduction of particle size has great negative impact of further reduction of solubility but in more generalized view along with reduction of particle size the factor which increases the wettability by reducing the contact angle between particle and water is mainly important and solid dispersed particles are formulated with this approach only as they composed of matrix dispersion of hydrophobic drug and hydrophilic polymer which increases the wettability of drug molecules and also reduces the size to form molecular dispersion. The recent research in the field of polymerization has also made it possible to make available those polymers which allows intermolecular hydrogen bonding with drug molecules in the solid dispersed particles, these bondings have significant effect over the prevention of precipitation during solubilization of particles. Thorough knowledge regarding the physicochemical properties of the solid dispersed particles are very essential for understanding the relation or mechanism of wetting of particle and the release mechanism of drug. However, in this review the current researches are highlighted with their modifications over the conventional methods.
Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs
European Journal of Pharmaceutics and Biopharmaceutics, 2013
Over 40% of active pharmaceutical ingredients (API) under development pipelines are poorly water-29 soluble drugs which limit formulation approaches, clinical application and marketability because of their 30 low dissolution and bioavailability. Solid dispersion has been considered one of the major advancements 31 in overcoming these issues with several successfully marketed products. A number of key references that 32 describe state-of-the-art technologies have been collected in this review, which addresses various 33 pharmaceutical strategies and future visions for the solubilization of poorly water-soluble drugs 34 according to the four generations of solid dispersions. This article reviews critical aspects and recent 35 advances in formulation, preparation and characterization of solid dispersions as well as in-depth 36 pharmaceutical solutions to overcome some problems and issues that limit the development and market-37 ability of solid dispersion products. 38 Ó 2013 Published by Elsevier B.V. 39 65 emulsions [12], nanoemulsions [13], nanosuspensions [14], solid-66 lipid nanoparticle [15] and solid dispersion which is considered 67 one of the most successful strategies to improve the dissolution 68 profile of poorly soluble drugs. The term solid dispersions has been 69 defined as a dispersion of one or more API in an inert carrier or 70 matrix at the solid state prepared by solvent, melting or solvent-71 melting method [16]. The API in solid dispersions can be dispersed 72 in separate molecules, amorphous particles, or crystalline particles 73 while the carrier can be in crystalline or amorphous state. Numer-74 ous studies on solid dispersions have been published and have 75 showed many advantageous properties of solid dispersions in 76 improving the solubility and dissolution rate of poorly water-77 soluble drugs. These advantages include reducing particle size, 78 possibly to molecular level, enhancing wettability and porosity, 79 as well as changing drug crystalline state, preferably into 80 amorphous state [6]. 81 Despite such high active research interests, the number of mar-82 keted products arising from solid dispersion approaches is disap-83 pointingly low. This low number is mainly due to scale-up 84 problems and physicochemical instability in the manufacturing 85 process or during storage leading to phase separation and 86 crystallization [17-20]. Only a few commercial products have been 87 marketed during the past half-century (Table 1). Therefore, 88 in-depth knowledge that has been acquired on various aspects of 89 solid dispersions such as carrier properties, preparation methods, 90 physicochemical characterization techniques as well as the
Indian Journal of Pharmaceutical Sciences, 2017
Singh, et al.: Solubility Enhancement by Solid Dispersion Solubility is an important determinant in drug liberation and hence drug absorption, which plays a key role in oral bioavailability of formulations. The dissolution rate of a drug directly depends upon its solubility. Most of the new drugs have poor water solubility; thereby pose a difficulty in formulating into drug delivery systems. Therefore, solubility enhancement of poorly water soluble drugs is one of the necessary preformulation steps in the pharmaceutical product development research. Solid dispersion is a unique and promising approach for enhancing the dissolution characteristics and oral bioavailability of poorly water-soluble drugs. The present review highlights portrayal of solid dispersions, its types including eutectic mixtures and solid solutions, method of preparation and also the useful carriers for the preparation of solid dispersions. Furthermore, the wide research conducted hitherto on solid dispersions for enhancing solubility of different efficacious drugs, challenges encountered in the development of solid dispersions and recent advancements to overcome its pitfalls have also been elaborated.
AN OVERVIEW: FORMULATION ASPECT OF SOLID DISPERSION AND ITS PHARMACEUTICAL APPLICATION
Most common problem with conventional dosage form is solubility, so the new approach in the formulation is solid dispersion. Solubility affects the dissolution and hence the bioavailability of a drug. This review emphasizes methods for improving solubility, carrier selection, classification, advantages, disadvantages, application, characterization, and scope of solid dispersion in formulations other than a tablet. Also involves recent research in solid dispersion formulation with drugs, methods of preparation as well as polymer. Methods of preparation for solid dispersion are highlighted in this article, methods like kneading, solvent evaporation, and fusion can be performed on a lab scale. Solid dispersion enhances the solvation property of the drug by decreasing its particle size and improving wettability. This article introduces the basic concept of solid dispersion along with different types of carriers which can be useful for the formulation of a more stable solid dispersion product. Hence this study involves detailed insight into aspects of solid dispersion and its pertinence in different formulations.