Technical Note: Miniaturized Intrinsic Dissolution Rate (Mini-IDR™) Measurement of Griseofulvin and Carbamazepine

Berger, Cynthia M.; Tsinman, Oksana; Voloboy, Dmytro; Lipp, Dana; Stones, Steven; Avdeef, Alex

doi:10.14227/dt140407p39

Cited by 26 publications

(18 citation statements)

References 8 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…The type of water was not specified in 19 of 51 studies (37%) (38)(39)(40)(41)(42)(43)(44)(45)(46)(47)(48)(49)(50)(51)(52)(53)(54)(55)(56).…”

Section: Watermentioning

confidence: 99%

“…This literature review found that phosphate buffer solutions, in the range of pH 5.8-8.0, were employed in 32.6% of cases as medium for the shake-flask method (15 of 46 studies) (8,11,19,31,32,37,(41)(42)(43)45,46,48,51,57,58) and in 40.0% as dissolution medium (8 of 20 studies) (10,11,22,24,(51)(52)(53)56). Acetate buffer was used less frequently, in 4 of 46 studies (8.7%) (41,42,45,49) as medium for the shake-flask method and in 2 of 20 studies (10.0%) as dissolution medium (52,56).…”

Section: Buffer Solutionsmentioning

confidence: 99%

See 1 more Smart Citation

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Bou‐Chacra

Melo

Morales

et al. 2017

AAPS J

View full text Add to dashboard Cite

Abstract.The introduction of the biopharmaceutics drug classification system (Biopharmaceutics Classification System (BCS)), in 1995, provided a simple way to describe the biopharmaceutics behavior of a drug. Solubility and permeability are among the major parameters, which determine the fraction dose absorbed of a drug substance and consequently its chances to be bioavailable. The purpose of this review is to summarize the evolution of the media used for determining solubility and dissolution and how this can be used in modern drug development. Over the years, physiologically adapted media and buffers were introduced with the intention to better predict the in vivo solubility and dissolution of drug substances. Water, buffer solutions, compendial media, micellar solubilization media, and biorelevant media are reviewed. At this time point, there is no universal medium available which can be used to predict every drug substance's solubility or a drug product's in vivo dissolution behavior. However, there have been many improvements and additions made to media to optimize their in vivo predictability; for example, the current phosphate concentrations in buffers seem to be too high to correlate with the carbonate buffer concentrations in vivo. Biorelevant media were updated to correlate them better with the composition of human intestinal fluids. The BCS was introduced into regulatory sciences as a scientific risk management tool to waive bioequivalence studies under certain conditions. Today's different guidance documents define the dose-solubility ratio differently. As shown for amoxicillin, this can cause more confusion than certainty for globally operating companies. Harmonization of BCS guidelines is highly desirable.

show abstract

“…The type of water was not specified in 19 of 51 studies (37%) (38)(39)(40)(41)(42)(43)(44)(45)(46)(47)(48)(49)(50)(51)(52)(53)(54)(55)(56).…”

Section: Watermentioning

confidence: 99%

Section: Buffer Solutionsmentioning

confidence: 99%

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Bou‐Chacra

Melo

Morales

et al. 2017

AAPS J

View full text Add to dashboard Cite

show abstract

“…A good correlation of results is observed compared with the fixed-disk system and even other systems not detailed in pharmacopeias but tested in several studies to determine the intrinsic dissolution rate. The latter include the flowcell system and a miniature apparatus (Mini-IDR) similar to the rotating disk (32,33,36,42,43).…”

Section: Apparatus Used To Determine the Idrmentioning

confidence: 99%

Intrinsic Dissolution as a Tool for Evaluating Drug Solubility in Accordance with the Biopharmaceutics Classification System

Issa¹,

Ferraz²

2011

Dissolution Technol.

View full text Add to dashboard Cite

The Biopharmaceutics Classification System (BCS) is a tool that was created to categorize drugs into different groups according to their solubility and permeability characteristics. Through a combination of these factors and physiological parameters, it is possible to understand the absorption behavior of a drug in the gastrointestinal tract, thus contributing to cost and time reductions in drug development, as well as reducing exposure of human subjects during in vivo trials. Solubility is attained by determining the equilibrium under conditions of physiological pH, while different methods may be employed for evaluating permeability. On the other hand, the intrinsic dissolution rate (IDR), which is defined as the rate of dissolution of a pure substance under constant temperature, pH, and surface area conditions, among others, may present greater correlation to the in vivo dissolution dynamic than the solubility test. The purpose of this work is to discuss the intrinsic dissolution test as a tool for determining the solubility of drugs within the scope of the Biopharmaceutics Classification System (BCS).

show abstract

“…This is because the particle size, and consequently the surface area, of a drug substance are not well controlled at the drug discovery stage. Determination of the IDR of a compound very early in the process enables successful screening of drug candidates and their solid forms, and it also helps with understanding of dissolution behavior of a compound under different biophysiological pH conditions (4,5).…”

Section: Introductionmentioning

confidence: 99%

Determination of Intrinsic Dissolution Rate Using Miniaturized Rotating and Stationary Disk Systems

Tseng¹,

Patel²,

Zhao³

2014

Dissolution Technol.

View full text Add to dashboard Cite

The objective of this study was to assess the feasibility and reliability of using miniaturized disk dissolution apparatus for intrinsic dissolution rate (IDR) measurement in the early drug discovery process when bulk drug supply is very limited. The two apparatus, a miniaturized rotating disk system (mRDS) and a miniaturized stationary disk system (mSDS), were evaluated using chloramphenicol as a model drug with sample sizes of 3-10 mg. Wood's rotating disk system (wRDS) was used as control with a sample size of 150 mg.The effect of various experimental parameters on IDR was studied on the two miniaturized apparatus. While compression force, disk distance, dissolution volume, and drug loading did not have significant effects on IDR measured by mRDS, dissolution volume and disk distance showed significant effects by mSDS. When all experimental parameters were held constant, the stationary system generated significantly higher IDRs compared with the two rotating systems (mRDS and wRDS). The mRDS yielded IDR values comparable to those by wRDS at 25 rpm (a slower rotation speed).These study results indicate that both miniaturized systems produce reliable IDR measurements with a small quantity of material, which provides a desirable advantage over other methods (e.g., wRDS, solubility measurement) in the early drug discovery phase.

show abstract

Technical Note: Miniaturized Intrinsic Dissolution Rate (Mini-IDR™) Measurement of Griseofulvin and Carbamazepine

Cited by 26 publications

References 8 publications

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Intrinsic Dissolution as a Tool for Evaluating Drug Solubility in Accordance with the Biopharmaceutics Classification System

Determination of Intrinsic Dissolution Rate Using Miniaturized Rotating and Stationary Disk Systems

Contact Info

Product

Resources

About