Creative Biolabs provides various custom-designed studies to investigate ADME (absorption, distribution, metabolism and excretion) of novel pharmaceuticals to support lead optimization phase. We offer physicochemical properties characterization service to understand ADME better.

Physicochemical Characterization Figure 1. Examples of natural product leads and their corresponding drugs (Camp et al. 2015)

Physicochemical properties of drugs include the aspects of ionization, stability, lipophilicity, solubility, hydrogen bonding, molecular size, etc. Understanding and optimizing the physicochemical properties of compounds are the fundamental for drug formulation development and absorption, distribution studies in vivo. Besides, actual physical and chemical properties are the bases of PK models. If a drug lead is properly analyzed before formulation development stage, it will save a lot of costs and time for rational drug design. Creative Biolabs has rich knowledge and experience in characterizing biopharmaceutical properties. Our professionality gives us valuable insight into formulation development and ADMET determination. Our physicochemical characterization services include:

Aqueous Solubility Studies

Aqueous solubility is one of the most critical properties of a therapeutic compound. Many metabolic activities do not put adequate efforts if not ensuring compounds are soluble and achieve reasonable exposure. Creative Biolabs offers various high throughput solubility assessments including kinetic solubility and thermodynamic solubility. We also devote to development strategies that address the multifaceted solubility issues.

Lipophilicity Studies

Lipophilicity refers to the ability of a chemical compound dissolving in fats, oils, lipids, and non-polar solvents. It is a crucial physicochemical property in medicinal chemistry which affects drug transport through lipid membranes as well as a drug interaction with the target protein. Creative Biolabs provides a number of experimental protocols for logP/logD determination and alteration, such as reversed phase high-performance liquid chromatography (RP-HPLC) or thin-layer chromatography (TLC).

Stability Studies

Physical stability is of paramount importance. It must be understood as degradation or inactive products lead to loss of efficacy (changes in appearance and performance) and may cause side effects or even toxicities. Creative Biolabs provides several aspects of stability studies, which include accelerated stress studies, forced degradation studies, photostability testing, stability storage, and degradation products testing. The purpose of stability testing is to provide evidence on how the efficiency and integrity of a drug substance or drug product vary with time under the influence of a variety of physical, chemical or microbiological changes, such as temperature, PH, humidity, light and radiations. Our stability evaluation services adhere to International Conference on Harmonization (ICH) guidelines Q1A and Q1B, and cover requirements for climate zones I to IV.

For more detailed information, please feel free to contact us or directly sent us an inquiry.

Reference

  1. Camp D, Garavelas A, and Campitelli M (2015). “Analysis of Physicochemical Properties for Drugs of Natural Origin.” J Nat Prod 78 (6): 1370–1382. DOI: 10.1021/acs.jnatprod.5b00255

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