Absorption Characteristics of Solid Dispersed and Micronized Griseofulvin in Man

Chiou, Win L.; Riegelman, Sidney

doi:10.1002/jps.2600600919

Cited by 101 publications

(17 citation statements)

References 11 publications

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“…Rats dosed with griseofulvin ASD material showed significantly higher (p< 0.05) exposures (C max and AUC) when compared to rats dosed with physical mixture (Table IV). This finding is in good agreement with literature reports that the absorption of griseofulvin crystalline drug is a dissolution rate/solubilitycontrolled process (38)(39)(40)(41)(42)(43). More importantly, overall exposure as assessed by AUC was not significantly different (p< 0.05) for ASD material generated by SDD, Evap ASD, and Lyo ASD manufacturing processes.…”

Section: Rat Pharmacokinetic Studysupporting

confidence: 91%

In Vitro and In Vivo Evaluation of Amorphous Solid Dispersions Generated by Different Bench-Scale Processes, Using Griseofulvin as a Model Compound

Chiang¹,

Cui²,

Ran³

et al. 2013

AAPS J

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Abstract. Drug polymer-based amorphous solid dispersions (ASD) are widely used in the pharmaceutical industry to improve bioavailability for poorly water-soluble compounds. Spray-drying is the most common process involved in the manufacturing of ASD material. However, spray-drying involves a high investment of material quantity and time. Lower investment manufacturing processes such as fast evaporation and freeze-drying (lyophilization) have been developed to manufacture ASD at the bench level. The general belief is that the overall performance of ASD material is thermodynamically driven and should be independent of the manufacturing process. However, no formal comparison has been made to assess the in vivo performance of material generated by different processes. This study compares the in vitro and in vivo properties of ASD material generated by fast evaporation, lyophilization, and spray-drying methods using griseofulvin as a model compound and hydroxypropyl methylcellulose acetate succinate as the polymer matrix. Our data suggest that despite minor differences in the formulation release properties and stability of the ASD materials, the overall exposure is comparable between the three manufacturing processes under the conditions examined. These results suggest that fast evaporation and lyophilization may be suitable to generate ASD material for oral evaluation. However, caution should be exercised since the general applicability of the present findings will need to be further evaluated.

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Section: Rat Pharmacokinetic Studysupporting

confidence: 91%

In Vitro and In Vivo Evaluation of Amorphous Solid Dispersions Generated by Different Bench-Scale Processes, Using Griseofulvin as a Model Compound

Chiang¹,

Cui²,

Ran³

et al. 2013

AAPS J

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“…Chiou and Riegelman (31) recommended polyethylene glycol, a water-soluble polymer, as an excellent universal carrier for improving the dissolution rate and oral absorption of water-insoluble drugs. They reported that the dissolution of griseofulvin, as well as its absorption and total availability in both dog (32) and man (33), was significantly higher when the solid was dispersed in polyethylene glycol 4000, 6000, or 20,000, as compared with the traditionally micronized form of the drug. Deshpande and Agrawal (34) reported that the dissolution rates of chlorothiazide, hydrochlorothiazide, flumethiazide, and cyclopentathiazide also were increased when dispersed in polyethylene glycol 6000.…”

Section: D) Solid Dispersionsmentioning

confidence: 99%

Dissolution Testing for Poorly Soluble Drugs: A Continuing Perspective

Kuppusamy¹

2010

Dissolution Technol.

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The development of a meaningful dissolution procedure for drug products with limited water solubility has been a challenge to both the pharmaceutical industry and the agencies that regulate them. These challenges include developing and validating the test methods, ensuring that methods are appropriately discriminatory, and addressing the potential for an in vivo-in vitro correlation (IVIVC). Dissolution test media selection should be justified for pH (recommended pH range is 1.2-7.5) as well as surfactant type (ionic versus non-ionic) and amount. If the drug is not soluble in the in vivo pH range, with or without surfactants, then the use of nonaqueous media can be preferred with proper justifications. Physical modifications of the drug, such as particle size reduction, use of metastable polymorphs, eutectic mixtures, solid dispersions, or complexation, are being widely used in the industry to enhance the drug dissolution characteristics. 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. Whatever method is used by the dissolution scientists, it must aim towards the cheaper but most effective approach to enhance the dissolution behavior of poorly soluble drugs.

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“…During processing, excipients may be added to API for a variety of reasons, e.g. to stabilize proteins by reducing denaturation during manufacturing [132], to improve aerosolization performance of powder inhalers [68,133,134], to improve compactability of APIs [135,136] and to improve the solid state stability of amorphous solid dispersions [67]. Hence, the overall outcome after processing depends on the manufacturing route as well as the crystallization and vitrification propensity of the API and/or excipient(s)/co-former(s) in multicomponent systems [137].…”

Section: Role Of Excipients and Co-formersmentioning

confidence: 99%

“…These include chemically modifying the API (e.g., using a prodrug approach), physically modifying the API (through particle size reduction) or employing crystal engineering/solid state modifications (e.g., amorphous, cocrystal or polymorphic forms) [134][135][136]. Generally, physicochemical properties of the API determine the most suitable method from those mentioned above.…”

Section: Role Of Excipients and Co-formersmentioning

confidence: 99%

Pharmaceutical solvates, hydrates and amorphous forms: A special emphasis on cocrystals

Healy

Worku

Kumar

et al. 2017

Advanced Drug Delivery Reviews

283

189

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a b s t r a c t a r t i c l e i n f oActive pharmaceutical ingredients (APIs) may exist in various solid forms, which can lead to differences in the intermolecular interactions, affecting the internal energy and enthalpy, and the degree of disorder, affecting the entropy. Differences in solid forms often lead to differences in thermodynamic parameters and physicochemical properties for example solubility, dissolution rate, stability and mechanical properties of APIs and excipients. Hence, solid forms of APIs play a vital role in drug discovery and development in the context of optimization of bioavailability, filing intellectual property rights and developing suitable manufacturing methods. In this review, the fundamental characteristics and trends observed for pharmaceutical hydrates, solvates and amorphous forms are presented, with special emphasis, due to their relative abundance, on pharmaceutical hydrates with single and two-component (i.e. cocrystal) host molecules.

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Absorption Characteristics of Solid Dispersed and Micronized Griseofulvin in Man

Cited by 101 publications

References 11 publications

In Vitro and In Vivo Evaluation of Amorphous Solid Dispersions Generated by Different Bench-Scale Processes, Using Griseofulvin as a Model Compound

In Vitro and In Vivo Evaluation of Amorphous Solid Dispersions Generated by Different Bench-Scale Processes, Using Griseofulvin as a Model Compound

Dissolution Testing for Poorly Soluble Drugs: A Continuing Perspective

Pharmaceutical solvates, hydrates and amorphous forms: A special emphasis on cocrystals

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