2 edition of Approaches for enhancing the dissolution of poorly soluble drugs. found in the catalog.
Approaches for enhancing the dissolution of poorly soluble drugs.
Written in English
Thesis (Ph.D.) - University of Brighton.
|Contributions||University of Brighton. School of Pharmacy and Biomolecular Sciences.|
One of the modern approaches that provides both dramatic increase in drug dissolution rate and suitable supersaturation conditions is to modify the solid-state properties of the drug. Several approaches have been investigated to improve the dissolution rates and bioavailability of poorly water-soluble drugs, including crystal modifications (Blagden et al., , Serajuddin, , Li et al., ), particle size reductions (Scholz et al., , Shegokar and Muller, ), amorphizations (Onoue et al., ), cyclodextrin complexation (Brewster and Loftsson, ), .
presents an overall approach to the factors affecting the dissolution and oral bioavailability of BCS-classes II and IV drugs and a brief review of the state-of-the-art of solid dispersion technology. Administration Of Poorly Water-Soluble Drugs. Thus, solubility and rate of dissolution of the drug are of major importance and many approaches to absorption enhancement concern the optimization of these properties. Poorly soluble drugs present a major challenge in dosage form development. In simple terms, a material must be in solution if it is to pass from the intestine to the systemic.
Dhillon BD, Goyal NK, Malviya R, Sharma PK () Poorly water-soluble drugs: change in solubility for improved dissolution characteristics. Glob J Pharm (1)–35 Google Scholar 3. Intrinsic dissolution evaluation of poorly soluble drugs / Michele Georges Issa and Humberto Gomes Ferraz -- 5. Oral delivery of poorly soluble drugs / Dev Prasad, Akash Jain, and Sudhakar Garad -- 6. A staged approach to pharmaceutical dissolution testing .
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This book is the first text to provide a comprehensive assessment of the application of fundamental principles of dissolution and drug release testing to poorly soluble compounds and formulations. Such drug products are, vis-à-vis their physical and chemical properties, inherently incompatible with aqueous by: 3.
The enhancement of oral bioavailability of poorly water-soluble drugs remains one of the challenging aspects of drug development.1 Techniques that have commonly been used to improve the dissolution and bioavailability of poorly water-soluble drugs include micronization, salt formation, solubilization, and formation of solid dispersions.2,3.
In recent years, newer physical modifications (e.g., microemulsions and nanocrystals) are giving promising results in enhancement of drug dissolution and bioavailability of poorly soluble drugs.
dissolution of poorly soluble drugs, including nanotechnology methods for enhancing solubility to reduce the percentage of poorly soluble drug candidates eliminated from the development. Selection of this solubility enhancing method mainly depends on drug property, site.
The solubility behavior of drug is one of most challenging aspect in formulation development. Thus a greater understanding of dissolution & absorption behavior of drug with low aqueous solubility is required to successfully formulate them into more soluble and hence bioavailable drug product.
Therefore different approaches are being explored to enhance the solubility of poorly water soluble. Dissolution of drug is the rate determining step for oral absorption of the poorly water soluble drugs and solubility is the basic requirement for the absorption of the drug from GIT.
The various techniques described above alone or in combination can be used to enhance the solubility of the drugs. Currently, Lipid-based drug delivery has gained more attention for enhancing the solubility and ultimately bioavailability of poorly water-soluble drugs.
Objectives: This review represents a new approach for enhancing the solubility as well as bioavailability for oral administration of poor solubility of drugs. d-α-Tocopheryl polyethylene glycol succinate (TPGS) has been widely used in a variety of oral applications to enhance dissolution, solubility, and/or bioavailability of poorly-water soluble drugs.
This review discusses BCS classification, carriers for solubility enhancement and different techniques for solubility s techniques are used for the enhancement of the solubility of poorly soluble drugs which include micronization, nanonization, sonocrystallization, supercritical fluid method, spray freezing into liquid and lyophilization, evaporative precipitation into aqueous solution, use of surfactant, use of co-solvent, hydrotropy method, use of salt forms, solvent.
Ritonavir is an antiretroviral drug characterized by low solubility and high permeability which corresponds to BCS class II drug. The purpose of the study was to develop solid dispersion by different methods and investigate them for in vitro and in vivo performance for enhancing dissolution and bioavailability, respectively.
Since the drug possesses food-related absorption, the effect of. Self Emulsifying Drug Delivery System: A Novel Approach for Enhancing Solubility Profile of Poorly Soluble Drugs [Pujara, Naisarg] on *FREE* shipping on qualifying offers.
Self Emulsifying Drug Delivery System: A Novel Approach for Enhancing Solubility Profile of Poorly Soluble Drugs. the majority of new drugs to improve dissolution rates and controlled release because these newly discovered drugs are poorly water-soluble [1–5].
The limited solubility of these drugs could lead to low oral availability, potential toxicity, low half-lives, and di cult formulations [6–9].
To achieve high. Many different approaches have been developed to overcome the solubility problem of poorly soluble drugs including solubilisation, inclusion compounds, and complexation. An alternative to these methods developed was drug nanoparticle formulation. Techniques for solubility enhancement of poorly soluble drugs: An overview.
approach, the buffer capacity and tolerability dissolution of drug (11). Several approaches have been applied to enhance oral bioavailability of poorly water soluble drugs such as hydrotrophy, solid dispersions, and micronisation.
In recent years, nanocarriers are gaining tremendous interest and have shown remarkable advantages over conventional dosage forms in oral drug delivery of hydrophobic drugs [ 6, 7 ]. According to this review article, it is consultable that the proper selection of solvent during crystallization may be used beneficially for enhancing the dissolution of poorly soluble drugs through modifying crystal habit or by formation of agglomerated crystals.
To enhance the solubility and dissolution rate, several approaches have been developed, such as nano/micro-particle based formulations, amorphous solid dispersions, lipid-based drug delivery systems, pro-drugs, and co-crystals.
INTRODUCTION: Insufficient aqueous solubility results in poor bioavailability, high intra and inter-subject variability, lack of dose, gastric, and enzymatic drug degradation. About % of all newly discovered drugs experience the same limitation while entering in drug development.
Micronization of solids, preparation of solid dispersion, salt formation, nanoparticles, or conversion of API. Currently only 8% of new drug candidates have both high solubility and permeability and 40% of the drugs are poorly soluble which leads to poor dissolution in the gastro intestinal tract (GIT) 4.
This paper evaluates the process of co-grinding with a surfactant as a new approach to enhance physicochemical and biopharmaceutical properties of praziquantel (PZQ), a poorly soluble drug that is essential for the treatment of schistosomiasis, a neglected tropical disease.
Background: The present work describes the role of melt granulation and microenviron-mental pH modulation technique in solubility enhancement of a poorly water soluble NSAID, Aceclofenac (ACL). ACL is a BCS Class II drug showing dissolution rate limited absorption and pH dependent solubility, with higher solubility at alkaline pH.such as their aqueous solubility and rate of dissolution.
Among the various approaches, preparation of inclusion complexes with cyclodextrin have proven to be successful in enhancing the solubility of poorly water soluble drugs[3,4,5]. Among the three types of CDs β -.
Dissolution Enhancement Using Different Formulation Approaches: Dissolution Enhancement of a Poorly Soluble Model Drugs Using Different Formulation Approaches for Immediate Release [Srivastava, Vikas Kumar, Mishra, Garima] on *FREE* shipping on .