Effect of Particle Size on Blood Griseofulvin-Levels in Man

Atkinson, R. M.; Bedford, Carole; Child, Korean J; Tomich, E. G.

doi:10.1038/193588a0

Cited by 113 publications

(29 citation statements)

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“…The presence of very fine and large ibuprofen particles caused an increase in span values, indicating wider particle size dissolution. However, enhancing the dissolution of poorly water soluble drugs by grinding such as griseofulvin 26 and naproxen 27 has been reported.…”

Section: Dissolution Studiesmentioning

confidence: 99%

The dissolution and solid-state behaviours of coground ibuprofen–glucosamine HCl

Al-Hamidi

Asare-Addo

Desai

et al. 2014

Drug Development and Industrial Pharmacy

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The cogrinding technique is one of most effective methods for improving the dissolution of poorly water soluble drugs and it is superior to other approaches from an economical as well as an environmental stand point, as the technique does not require any toxic organic solvents.Present work explores the role of D-glucosamine HCl (GL) as a potential excipient to improve dissolution of a low melting point drug, ibuprofen (Ibu), using physical mixtures and coground formulations. The dissolution of the poorly soluble drug has been improved by changing the ratio of Ibu:GL and also grinding time. The results also showed that although GL can enhance the solubility of Ibu, it also reduces pH around the Ibu particles which led to poor dissolution performance when the concentration of GL is high. The effect of GL on the solubility of Ibu could be misleading if the pH of the final solution was not measured.Grinding reduced the particle size of GL significantly but in case of Ibu it was less effective.Solid state analysis (XRPD, DSC and FT-IR) showed that ibuprofen is stable under grinding conditions, but the presence of high concentration of GL in samples subjected to high grinding times caused changes in FT-IR spectrum of Ibu which could be due to intermolecular hydrogen bond or esterification between the carboxylic acid group in the ibuprofen and hydroxyl group in the GL.

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Section: Dissolution Studiesmentioning

confidence: 99%

The dissolution and solid-state behaviours of coground ibuprofen–glucosamine HCl

Al-Hamidi

Asare-Addo

Desai

et al. 2014

Drug Development and Industrial Pharmacy

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show abstract

“…The pharmaceutical scientific foundation of our understanding of the effect of reducing particle size on bioavailability essentially began with griseofulvin in 1962 (Atkinson et al, 1962) (Fig. 13.9).…”

Section: Dissolution-rate-limited Absorptionmentioning

confidence: 99%

Pharmacokinetic Behaviors of Orally Administered Drugs

Yáñez

Brocks

Forrest

et al. 2011

Oral Bioavailability

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“…The increase in surface area by reduction in particle size has been reported to result in a proportional increase in dissolution rate (1). However, with the micronized drugs that are strongly agglomerated do not always exhibit an improved dissolution rate (2).…”

Section: Introductionmentioning

confidence: 98%

High Energy Ordered Mixture for Improving the Dissolution Rate of Sparingly Soluble Compounds

Shah

Phuapradit

Bachynsky

et al. 1994

Drug Development and Industrial Pharmacy

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Bioavailability of a sparingly soluble drug is often limited by the rate of dissolution of the drug substance. The drug in a micronized form is generally employed to maximize the bioavailability. However, the micronized drugs tend to agglomerates and do not always exhibit an improved dissolution rate. In this study, a simple processing using a high energy mill was demonstrated as an effective means to utilize the entire surface area available for drug release of the micronized drug. An experimental hydrophobic drug in a micronized form was milled with a carrier, hydrous lactose using Micropulverizer to achieve a uniform mixture so-called "high energy ordered mixture". The high energy ordered mixture provided a contact surface area taking part in dissolution 4-fold greater than the micronized drug agglomerates. Therefore, the dissolution was significantly improved, irrespective of test parameters such as agitation and the presence of surfactant. This high energy ordered mixture provided the advantages over a simple ordered mixture for: (i) complete 873 Copyright 0 1994 by Marcel Dekker, Inc. Drug Dev Ind Pharm Downloaded from informahealthcare.com by Nyu Medical Center on 06/05/15 For personal use only. 874 SHAH ET AL.deaggregation of the micronized drug to fine primary particles, (ii) improving the efficiency of the carrier by increasing contact surface area, and (iii) enhancing the bonding effect between the drug and lactose particles due to free water molecules released from the crystal lattices of hydrous lactose during milling. This procedure could be applied to overcome dissolution problems of sparingly soluble drugs with cohesive nature.

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Effect of Particle Size on Blood Griseofulvin-Levels in Man

Cited by 113 publications

References 1 publication

The dissolution and solid-state behaviours of coground ibuprofen–glucosamine HCl

The dissolution and solid-state behaviours of coground ibuprofen–glucosamine HCl

Pharmacokinetic Behaviors of Orally Administered Drugs

High Energy Ordered Mixture for Improving the Dissolution Rate of Sparingly Soluble Compounds

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