Solubility Enhancement of Poor Water Soluble Drugs by Solid Dispersion: A Review (original) (raw)
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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.
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.
In the present day solubility of drugs in GIT fluids becomes necessary for the preparation of solid unit dosage forms of drugs. Otherwise if the drug has poor solubility then the drug does not show its effect properly in the body. So, solubility is a main aspect in the formulation of unit doses. Various methods like Lyophilization (Freeze drying process), Super critical fluid technology, Nanotechnology, Liquisolid compact technology, Self-emulsifying agents (SMEDDS) etc. are used to improve the solubility and dissolution rate of poorly water soluble drugs.
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.
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.
Review: Solid Dispersion Technique for Enhancement of Solubility of Poorly Soluble Drug
Indian Journal of Pharmaceutical and Biological Research, 2018
Nearly 40% of novel drugs comes in pharmaceutical industries are showing poor capability of solubilization in water. Therefore enhancing the solubilization of such drugs in water to enhance their bioavailability be the major challenge to formulation scientists. So the preparation of solid dispersion from the drug which shows poor solubility in water with carriers having good water solubility has decrease the occurrence of such problems and increase dissolution. Hence solid dispersion found to be attention-grabbing method for solubility enhancing of drugs which showing poor solubility in water. This review, shows an overview on the different solid dispersion types, rationale, their advantages, limitations, manufacturing processes as well as its characterization methods.
The oral solid dosage forms are extremely relevant to drug therapy and responsible for much of the pharmaceutical industry turnover worldwide. However, the development of medicines in solid form involves significant challenges, including obtaining formulations with appropriate bioavailability for low aqueous solubility drugs (classes II and IV of the Biopharmaceutics Classification System). One of the most effective strategies to overcome poor dissolution rate and low absorption of drugs is the solid dispersion technique, however, although it has been the focus of much research in recent decades, there are relatively few commercially available products based on such technology. This is mainly due to problems related to production scale-up and physicochemical instability and creates opportunities for new studies to explore the full potential of the technology. This review presents an overall approach to the factors affecting the dissolution rate and oral bioavailability of BCS-classes II and IV drugs and a brief review of the state-of-the-art of solid dispersion technology.
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...
Solid dispersions : An evergreen solubility enhancement technique for hydrophobic drugs
2016
Oral route is the most preferable route of drug del ivery for most of the drug but it is not suitable f or the drugs which are poorly water soluble. It mainly affects the ora l bioavailability of the drugs. It remains as a mos t challenging aspect in formulation development due to its minima l solubility. To overcome this problem formulation scientists have employed the different techniques. One of the techniques is solid dispersions. These are gaining attracted considerable interest as an efficient means of impr oving the solubility and dissolution which results in increasing the bioavailability of poorly water soluble drugs. The present article mainly focus on the areas of ba sic concept of solid dispersions, advantages, disadvantages, types and various methods of preparation for solid dispe r ions.
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