Increasing Dissolution Rates and Gastrointestinal Absorption of Drugs via Solid Solutions and Eutectic mixtures III

Goldberg, Arthur H.; Gibaldi, Milo; Kanig, Joseph L.

doi:10.1002/jps.2600550508

Cited by 119 publications

(55 citation statements)

References 9 publications

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“…Solid dispersions on the other hand may provide the advantages of the solid solution while having fewer physical stability problems. The key empirical distinction of a solid dispersion is that drug retains its unique physical state after processing and hence the reversion to more stable crystalline form is not a major concern (Goldberg, Gibaldi, and Kanig 1966b;Leuner and Dressman 1000).…”

mentioning

confidence: 99%

Improving the Dissolution Rate of Poorly Water Soluble Drug by Solid Dispersion and Solid Solution—Pros and Cons

et al. 2007

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confidence: 99%

Improving the Dissolution Rate of Poorly Water Soluble Drug by Solid Dispersion and Solid Solution—Pros and Cons

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“…The melted mixture is then solidified rapidly in an ice bath under vigorous stirring. The final solid mass is crushed, pulverized and sieved 67 .…”

Section: Melting Methods (Fusion)mentioning

confidence: 99%

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2012

IJPSR

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Solubility is an important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. Among all newly discovered chemical entities most of the drugs are lipophillic and fail to reach market due to their poor water solubility. The solubility behavior remains one of the most challenging aspect informational development. Hence various techniques are used for the improvement of solubility of poorly water soluble drugs which include micronization, chemical modification, pH adjustment, solid dispersion, complexation, co-solvency micellar solubilization, hydrotrophy etc. Of all these approaches solid dispersion have attracted tremendous interest as an efficient means of improving the dissolution rate and hence the bioavailability to arrange of hydrophobic drugs. This article reviews the various preparation techniques and types of solid dispersion based on molecular arrangement. Finally some of the practical aspects have also been considered for the preparation of dispersions.

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“… Dispersions obtained through the fusion process are often called melts. 3 : A physical mixture of an active agent and a water soluble carrier is heated until it is melted. The melt is solidified rapidly in an ice bath under continuous stirring.…”

Section: Definitionmentioning

confidence: 99%

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2011

IJPSR

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The poor dissolution rate of water-insoluble drugs is still a major problem conforming the pharmaceutical industry. The most common method for improving the solubility is by increasing the surface area of the drug through micronization. But, in practice the effect of micronization is often disappointing, especially when the drugs are encapsulated or tablet. It is generally recognized that low solubility or dissolution rate often becomes a rate-limiting step in absorption of poorly water soluble drugs. Therefore, the enhancement of the dissolution rate of poorly water-soluble drugs after oral administration is one of the most challenging aspects of modern pharmaceutics. Olanzepine (2-methyl-4-(4-methyl-1-piperazinyl) -10H-thieno [2, b] [1, 5]benzodiazepine possess antipsychotic activity and exhibits very slight solubility in water and as a consequence it exhibit low bioavailability after oral administration Therefore, the improvement of olanzepine dissolution from its oral solid dosage forms is an important issue for enhancing its bioavailability and therapeutic efficacy. The purpose of present work is to improve the solubility of Olanzepine by preparing its dispersion with polymer PEG (Poly Ethylene Glycol) using solvent evaporation technique.

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Increasing Dissolution Rates and Gastrointestinal Absorption of Drugs via Solid Solutions and Eutectic mixtures III

Cited by 119 publications

References 9 publications

Improving the Dissolution Rate of Poorly Water Soluble Drug by Solid Dispersion and Solid Solution—Pros and Cons

Improving the Dissolution Rate of Poorly Water Soluble Drug by Solid Dispersion and Solid Solution—Pros and Cons

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