Bioavailability is a pivotal parameter in pharmacokinetics (PK) that defines the rate and extent to which an active pharmaceutical ingredient (API) is absorbed from a drug product and becomes available at the site of action. In the early stages of drug discovery, poor bioavailability is a leading cause of candidate attrition. Therefore, rigorous bioavailability analysis is essential for optimizing lead compounds and predicting in vivo efficacy. BOC Sciences provides comprehensive bioavailability assessment services designed for research and development (R&D). Utilizing advanced LC-MS/MS platforms and diverse in vitro/in vivo models, we help clients evaluate drug exposure, determine absorption mechanics, and accelerate the transition from hit-to-lead to candidate selection with high-confidence data.
We provide definitive determination of Absolute Bioavailability by comparing the plasma concentration-time curve (AUC) of an extravascular dose (e.g., oral) against an intravenous (IV) reference dose. This service quantifies the exact fraction of the drug that reaches systemic circulation, critical for understanding absorption efficiency and first-pass effects.
Our team conducts Relative Bioavailability studies to compare different formulations (e.g., suspension vs. capsule) or different routes of administration (e.g., oral vs. subcutaneous). This data is essential for selecting the optimal vehicle, ranking lead candidates, and bridging data between different study phases.
To complement bioavailability data, we evaluate key absorption factors including intestinal permeability (Caco-2, PAMPA) and metabolic stability. We identify whether low bioavailability is driven by poor absorption, high efflux, or rapid metabolism, providing a complete picture of the drug's disposition.
BOC Sciences delivers high-throughput bioavailability data to guide your lead optimization and formulation strategies.
Represents the total drug exposure over time (AUC0-t and AUC∞). It is the primary metric for determining the extent of absorption and comparing bioavailability between different formulations or dosing routes.
Indicates the maximum serum concentration achieved after administration. Monitoring Cmax is crucial for establishing safety margins (toxicity risks) and ensuring therapeutic thresholds are met.
Reflects the rate of absorption. A shorter Tmax suggests rapid onset of action, while a delayed Tmax is characteristic of controlled-release formulations or drugs with absorption rate-limiting steps.
The percentage of the administered dose that reaches the systemic circulation unchanged. We calculate F utilizing plasma concentration data from both IV and non-IV arms to guide dose adjustment.
The time required for the concentration of the drug to reduce by half. This parameter helps in determining the dosing frequency required to maintain steady-state therapeutic levels.
We evaluate systemic Clearance (efficiency of drug removal) and Volume of Distribution (theoretical volume drug is distributed in) to understand the drug's behavior in tissues versus plasma.
BOC Sciences supports a comprehensive range of test articles. We categorize samples by physicochemical profile, structural class, and dosage form to tailor extraction and bioanalytical strategies for your specific research needs.
Submit your compound information. Our experts will design a bioavailability study tailored to your molecule's physicochemical properties.
We review the compound's solubility, stability, and known properties to select the appropriate in vitro or in vivo models and dosing routes (IV/PO/SC).
Rapid optimization of LC-MS/MS conditions or bioanalytical methods to ensure specificity and sensitivity for the target molecule in the chosen matrix.
Conducting the study (e.g., Caco-2 assay or Rodent PK) under controlled experimental conditions, followed by sample processing and analytical quantification.
Calculation of key PK parameters (AUC0-t, Cmax, t1/2, F%) using professional PK software. Delivery of a detailed R&D report.
For BCS (Biopharmaceutics Classification System) Class II compounds where solubility limits absorption, we provide comparative PK studies of different vehicle/excipient combinations (e.g., cyclodextrins, surfactants) to identify formulations that enhance systemic exposure.
We assess the bioconversion of prodrugs into active moieties. By monitoring both parent and metabolite concentrations in plasma, we help clients verify whether the prodrug strategy effectively improves oral bioavailability.
When high clearance limits bioavailability, we assist in identifying metabolic soft spots via microsome stability assays and testing alternative routes (e.g., sublingual, transdermal) in animal models to bypass hepatic metabolism.
Using cassette dosing (dosing multiple compounds simultaneously), we provide a rapid ranking of multiple lead candidates based on their oral availability, allowing for efficient resource allocation to the most promising molecules.
Don't let poor bioavailability derail your drug program. Partner with BOC Sciences for robust PK data that illuminates the absorption profile of your candidates. Fast, accurate, and research-focused.
Our advanced mass spectrometry platforms achieve lower limits of quantification (LLOQ), ensuring precise definition of the terminal elimination phase and accurate AUC calculation.
We don't just measure levels; we explain them. By correlating PK data with permeability and metabolism assays, we provide mechanistic insights into why a drug has low or high bioavailability.
We offer fit-for-purpose study designs ranging from rapid "snapshot" PK screens to full-profile bioavailability studies, tailored to the specific stage of your discovery pipeline.
We understand the pace of drug discovery. Our streamlined workflows ensure rapid data delivery, enabling timely iterative cycles of chemical synthesis and testing.
Client Needs: A biotech firm designed an ester prodrug to improve the permeability of their active parent compound. They needed to verify if the prodrug was successfully absorbed and rapidly converted to the parent drug in the systemic circulation.
Challenges: The prodrug was highly unstable in plasma ex vivo, leading to potential artifacts (false high parent levels) during analysis. Additionally, distinguishing the prodrug from the parent molecule required high chromatographic resolution.
Solution: BOC Sciences implemented a custom stabilization protocol using specific esterase inhibitors immediately upon blood collection to prevent ex vivo hydrolysis. Our team then developed a sensitive LC-MS/MS method with optimized chromatographic separation to resolve the prodrug from the parent metabolite, ensuring precise quantification of the conversion rate.
Outcome: The study confirmed a 4-fold increase in the AUC of the active parent drug when administered as the prodrug compared to the parent alone, validating the prodrug strategy for further development.
Client Needs: A researcher developing a peptide drug sought to overcome poor oral bioavailability using lipid nanoparticle (LNP) carriers. They needed to compare three different LNP compositions against a saline control.
Challenges: Peptides are susceptible to enzymatic degradation in the gut, and LNPs create a complex matrix. The assay needed to extract the peptide efficiently from the lipid carrier and detect it at low nanomolar concentrations.
Solution: We developed a specialized liquid-liquid extraction (LLE) protocol to disrupt the LNP structure and release the peptide without degradation. Following this, we performed a comparative PK study in mice using a high-sensitivity MS/MS method. Absolute bioavailability was calculated by comparing oral LNP groups to a standard IV control group.
Outcome: One LNP formulation demonstrated a bioavailability of 12% (vs <1% for saline), providing a clear lead formulation for the client's subsequent efficacy studies.
Client Needs: A pharmaceutical company had a potent lead compound with excellent potency but extremely low water solubility, resulting in variable exposure data. They requested a vehicle screening study to stabilize exposure.
Challenges: Standard suspension formulations resulted in poor and inconsistent absorption (high coefficient of variation). The client required a vehicle that could solubilize the compound sufficiently for reliable dosing without toxicity.
Solution: BOC Sciences screened the compound's solubility in a library of various vehicles (e.g., PEG400, surfactants, cyclodextrins). We selected two optimized co-solvent systems and conducted a parallel rat PK study to evaluate exposure consistency (Cmax variability) and potential precipitation issues in vivo.
Outcome: The study identified a co-solvent system that improved Cmax by 5-fold and significantly reduced inter-subject variability, enabling the client to proceed to dose-escalation toxicity studies with confidence.
Bioavailability analysis aims to quantitatively assess the extent to which a drug or compound is absorbed and reaches systemic circulation. By measuring concentration changes in plasma or tissues, it reveals absorption efficiency and exposure levels, providing guidance for formulation optimization, dosing strategies, and structural modifications. BOC Sciences offers multi-mode detection and data interpretation to ensure accuracy and actionable results.
Common analytical methods for bioavailability analysis include HPLC, LC-MS/MS, and isotope-labeled tracking. Method selection must balance sensitivity, specificity, and sample compatibility. BOC Sciences has extensive experience in method development and validation, providing customized and reproducible data solutions for a variety of compounds.
Plasma, serum, and specific tissues are primary sample types for bioavailability analysis. Proper sample handling is critical for compound stability and recovery, including homogenization, protein precipitation, and low-temperature storage. BOC Sciences provides standardized sample processing workflows to minimize operational errors and enhance data reliability and reproducibility.
Drug absorption is evaluated using time-concentration profiles and key parameters like C_max and AUC. High AUC and rapid C_max typically indicate good absorption, while abnormal profiles may suggest low absorption or metabolic effects. BOC Sciences offers comprehensive data analysis and reporting to help clients quickly understand compound behavior.
Optimization can focus on improving analytical sensitivity, optimizing sampling time points, and refining data processing and interpretation strategies. Well-designed experiments and workflows reduce errors and maximize information. BOC Sciences provides advanced analytical platforms and expert support to deliver precise and reliable bioavailability data tailored to compound characteristics.
The PK data provided by BOC Sciences was instrumental in our decision to drop a lead candidate with poor metabolic stability early on. Their fast turnaround on the microsome and rodent PK studies saved us significant time and budget.
— Dr. Harrison, Director of Medicinal Chemistry
We struggled with a BCS Class IV compound for months. BOC Sciences' formulation screening combined with their precise bioavailability analysis helped us unlock a formulation that finally achieved therapeutic exposure levels.
— Dr. Roberts, Senior Scientist
The sensitivity of their LC-MS/MS methods is impressive. They were able to quantify our highly potent compound in plasma with excellent reproducibility, giving us the confidence we needed in our PK parameters.
— Dr. Li, DMPK Lead
If you have any questions or encounter issues on this page, please don't hesitate to reach out. Our support team is ready to assist you.
