ChemInform Abstract: Improved Dissolution Behavior of Lipophilic Drugs by Solid Dispersions: The Production Process as Starting Point for Formulation Considerations (original) (raw)
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Solid dispersions: A feasible technique to improve the aqueous solubility of poorly soluble drugs
Solid dispersion technology deals with dispersing one or more active ingredients in an inert matrix in the solid state in order to achieve enhanced dissolution rate and stability. Upon increasing the dissolution rate in the gastro intestinal tract, the rate of absorption is increased as long as the dissolution rate is still the rate-limiting step. Various carriers have been used in the formation of solid dispersion, which can facilitate in improving the dissolution rate of poorly soluble drugs to improve better bioavailability.
Solid Dispersion: A Technology for the Improvement of Oral Bioavailability of Poorly Soluble Drugs
Solid dispersions are one of the most promising strategies to improve the oral bioavailability of poorly water soluble drugs. By reducing drug particle size to the absolute minimum, and hence improving drug wettability, bioavailability may be significantly improved. This article reviews the various preparation techniques for solid dispersion and compiles some of the recent technology transfers. The different types of solid dispersions based on the molecular arrangement have been highlighted. Some of the practical aspects to be considered for the preparation of solid dispersions, such as selection of carrier, solvent and methods of physicochemical characterization, along with an insight into the molecular arrangement of drugs in solid dispersions are also discussed. In this review, it is intended to discuss the recent advances related on the area of solid dispersions.
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.
Solid Dispersion: Solubility Enhancement for Poorly Water Soluble Drug
Research Journal of Pharmacy and Technology, 2012
Solid dispersion is used for enhancing dissolution rate of a therapeutically active substance and in turns its absorption and in vivo efficacy. Solid dispersion is generally prepared with drug which is having poor aqueous solubility and hydrophilic carrier. Generally Polyethylene Glycol, Polyvinyl Pyrrolidone, Mannitol, Urea, Gums, Eudragit are used as hydrophilic carriers. Certain Hydrophilic Swellable Polymers Sodium Carboxy Methyl Cellulose, Pregelatinized Starch, Sodium Starch Glycolate are also used. Sometimes surfactant is also added to further improve wetting property of solid dispersion. In solid dispersion particle size of drug is reduced or a crystalline pure drug is converted into amorphous form and hence the solubility of drug is increased. Solid dispersion is not only used in improving dissolution rate of poorly water soluble drug but also in masking the taste of the drug substance, preparing rapid disintegration oral tablets and in producing sustained release microspheres. Various methods are available to prepare solid dispersion generally solvent evaporation method, melting method, melt solvent method, kneading method, cogrinding method, co-precipitation method, modified solvent evaporation method, spray drying, gel entrapment technique, co-precipitation with supercritical fluid. Evaluations of solid dispersion are done by Fourier Transform infra-red spectroscopy, X-Ray diffractometry, scanning electron microscopy, differential scanning calorimetry, solubility and dissolution experiments.
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.
Solid Dispersions: A Method to Improve Bioavailability of Oral Drug Dosage Form
Journal of Biomedical and Pharmaceutical Research
Presently only few percent of drugs having high aqueous solubility, Number of drugs are belonging to biopharmaceutical classification system class II that means possessing poor aqueous solubility eventually results in low level of drug in systemic circulation. To overcome this problem, various strategies have been come out into notion such as self emulsifying drug delivery system solid dispersions, use of surface active agents, complex formation. Solid dispersions is found to be promising approach to increase bioavailability by use of various polymers. This review focuses on the mechanism of drug release from solid dispersion with its method of preparation and applications. Key words: dissolution, particle size, solid dispersion
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...