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Biorelevant Dissolution
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Reveal how an oral drug will be released from a formulation and dissolve in simulated gastrointestinal fluids
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Compare in vitro dissolution profiles of a Test Formulation against the Reference Formulation
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Streamline preclinical development by linking your oral drug's in vitro biorelevant solubility and dissolution to in vivo preclinical bioavailability
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Results help guide formulation development and optimization
Background
For an orally administered drug to be absorbed, it must first undergo dissolution; the drug must be released from its formulation and dissolve within fluids present in the gastrointestinal tract. The way a drug behaves in these fluids strongly influences how much drug is absorbed. To understand this in vivo process, simple in vitro dissolution tests using biorelevant media are performed. These in vitro tests use conventional dissolution apparatus and vessels containing biorelevant media to simulate the specific in vivo fluids found in different sections of the fasted and fed state gut.
Benefits of biorelevant dissolution experiments for new drug development
- Reveal how a formulated drug is likely to behave in vivo after oral administration under fasted and fed conditions
- Identify potential developability challenges such as poor absorption or food effects
- Guide the selection of an appropriate oral formulation strategy
Benefits of biorelevant dissolution experiments for generic drug development
Biorelevant media can be used for discriminatory dissolution studies which enable developers to:
- Compare a Test Formulation against a Reference Formulation
- Detect significant in vitro differences in dissolution behaviour that could affect in vivo performance
- Optimize formulations in vitro before beginning costly in vivo bioequivalence studies thereby reducing the risk of failure and saving costs associated with failed bioequivalence studies
How to conduct the experiments
*Biorelevant dissolution: determine the rate and extent of drug release from the formulation into the biorelevant medium using USP Apparatus II (paddle method)
*Drug analysis: dilute biorelevant dissolution samples and analyse drug release with High-Performance Liquid Chromatography (HPLC)
*Data comparison: dissolution profiles of the Test and Reference Formulations are compared to assess similarity or detect differences that can affect drug absorption
Getting started
We have produced step-by-step guides to help you conduct drug analysis and biorelevant dissolution which you can download below. To run the experiments (n=6) you will need:
BIORELEVANT DISSOLUTION MEDIA TYPES
FaSSIF is made with 3F Powder (FFF02) + FaSSIF Buffer Concentrate (FASBUF)
FeSSIF is made with 3F Powder (FFF02) + FeSSIF Buffer Concentrate (FESBUF)
FaSSGF is made with 3F Powder (FFF01) + FaSSGF Buffer Concentrate (FASGBUF)
FaSSIF-V2 is made with FaSSIF-V2 Powder (V2FAS) + FaSSIF-V2 Buffer Concentrate (V2FASBUF)
FeSSIF-V2 is made with FeSSIF-V2 Powder (V2FES) and FeSSIF-V2 Buffer Concentrate (V2FESBUF)
FEDGAS Early is made with FEDGAS Gel (FDG-GEL) + FEDGAS Buffer Concentrate pH6 (FDG-BUF6)
FEDGAS Mid is made with FEDGAS Gel (FDG-GEL) + FEDGAS Buffer Concentrate pH4.5 (FDG-BUF45)
FEDGAS Late is made with FEDGAS Gel (FDG-GEL) + FEDGAS Buffer Concentrate pH3 (FDG-BUF3)
Canine FaSSIF is made with Canine Powder (K9FAS)
Canine FaSSGF pH6.5 is made with Canine Powder (K9FAS)
Canine FaSSGF pH1.5 is made with Canine Powder (K9FAS)
SELECT BIORELEVANT DISSOLUTION MEDIUM
RECOMMENDED MATERIALS
For biorelevant dissolution in FaSSIF, we recommend 1 x FFF02, 5 x FASBUF and 1 x GMF13.
FaSSIF= Fasted State Simulated Intestinal Fluid
RECOMMENDED MATERIALS
For biorelevant dissolution in FeSSIF, we recommend 1 x FFF02, 2 x FESBUF and 1 x GMF13.
FeSSIF=Fed State Simulated Intestinal Fluid
RECOMMENDED MATERIALS
For biorelevant dissolution in FaSSGF, we recommend 1 x FFF01, 1 x FASGBUF and 1 x GMF13.
FaSSGF=Fasted State Simulated Gastric Fluid
RECOMMENDED MATERIALS
For biorelevant dissolution in FaSSIF-V2, we recommend 1 x V2FAS, 5 x V2FASBUF and 1 x GMF13.
FaSSIF-V2= Fasted State Simualted Intestinal Fluid Version Two
RECOMMENDED MATERIALS
For biorelevant dissolution in FeSSIF-V2, we recommend 1 x V2FES, 1 x V2FESBUF and 1 x GMF13.
FeSSIF-V2= Fed State Simulated Intestinal Fluid Version Two
RECOMMENDED MATERIALS
For biorelevant dissolution in FEDGAS Early (pH6), we recommend 1 x FDG-GEL, 1 x FDG-BUF6 and 1 x GMF13.
900mL of FEDGAS contains the 62.5g of fat present in a high-fat FDA meal along with the bile salts present in the fed stomach
RECOMMENDED MATERIALS
For biorelevant dissolution in FEDGAS Mid (pH4.5), we recommend 1 x FDG-GEL, 1 x FDG-BUF4.5 and 1 x GMF13.
900mL of FEDGAS contains the 62.5g of fat present in a high-fat FDA meal along with the bile salts present in the fed stomach
RECOMMENDED MATERIALS
For biorelevant dissolution in FEDGAS Late (pH3), we recommend 1 x FDG-GEL, 1 x FDG-BUF3 and 1 x GMF13.
900mL of FEDGAS contains the 62.5g of fat present in a high-fat FDA meal along with the bile salts present in the fed stomach
RECOMMENDED MATERIALS
We recommend 1 x K9FAS and 1 x GMF13.
RECOMMENDED MATERIALS
We recommend 1 x K9FAS and 1 x GMF13.
RECOMMENDED MATERIALS
We recommend 1 x K9FAS and 1 x GMF13.
