Preformulation Studies | Selection of Dosage Forms for Preclinical Studies | Supplies Phase 1 Clinical Studies
Preformulation Study Service
Preformulation studies characterize physical and chemical properties of a drug molecule alone or combined with excipients at early stage of drug product development to ensure formulation and process development can be carried out leading to a safe, effective, stable, and manufacturable dosage form. Sometimes, the property characterization of functional excipients (e.g. rate-controlling component) is also important to successfully develop a novel dosage form with a desirable release profile. Preformulation studies can be conducted in vitro throughout the drug product development from pre-clinical studies, clinical studies, to final scaling up for commercial launch. Established data from preformulation studies are required by the regulatory agencies to compose the CMC sections.
Services Provided in Preformulation Studies
- Characterization of the Physicochemical Properties of NCE/API
- Identification of the Bulk Properties of NCE/API and/or Drug Preparations
- Investigation of the Stability of NCE/API and/or Drug Preparations
- Reverse Engineering
Preformulation Capabilities
Property Characterizations for NCE/API and Drug Product
Physicochemical Properties
- Melting Point
- pKa
- Water Content
- Hygroscopicity
- Solubility
- pH-Solubility profile
- Polymorphism
- Salt and Crystallinity
Bulk Properties
- Particle Size Distribution
- Bulk and Tapped Density
- Flowability
- Compressibility
- Compactibility
Thermodynamic Properties
- Stability (API & Drug Product)
- Drug-Excipient Compatibility
Typical Preformulation Studies
Solubility
- Aqueous solvents at different pH (2-10) and in organic solvents
- Biorelevant media (FaSSIF, FeSSIF, SGF and PBS)
Stability
- Solid-state stability: physical (PLM, XRPD, DSC, TGA) and chemical (HPLC) at standard conditions
(e.g. 40°C/75%RH, open or close - Photostability (white light and UV, from ICH guideline)
- Solution stability at different temperatures, pH and solution concentrations
Forced Degradation
- Degradation in acidic and basic solutions
- Oxidation (hydrogen peroxide)
- Thermal degradation
Performance for formulation evaluation
- In-vitro dissolution profile in biorelevant media at 37°C
- Solution/suspension stability in formulation vehicles at dose concentrations
- Excipient compatibility study
- Disproportionation for salts, particle properties, logP, etc.
PreFormulation Instruments
Selection of Dosage Forms for Preclinical Studies
Pre-clinical study in drug development is a stage of research before clinical trials which tests a new chemical entity (NCE) in animals to collect information about drug safety and potential administration route, etc. The aim of a pre-clinical study is to determine the safe dose for first-in-human and assess a product's safety profile. We can help to select the best dosage forms for the NCE based on our strengths in preformulation studies and formulation and process development, and produce the supplies of drug product from pre-clinical to Phase I clinical studies.
Capabilities for Early Formulation Services
Supporting Preclinical and FIH Clinical Studies
Preclinical Trial
Single/Multi-Dose Tox/PK
- Solid form study
- Solubility
- Stability
- Disproportionation
- Dose range
- Formulation enabling
Tox (GLP) Formulation for IND
- Form selection
- API process, analytical, etc.
- Use-time stability
- Formulations for different doses and safety (ICH)
- Preliminary solid dosage formulation (e.g. DIC)
- Alignment with FIH DP
Clinical Trial
FIH Formulation Readiness
- Excipient compatibility
- Stability
- API manufacture
- Prototype formulation development
- Bioavailability enhancement (BCS II and IV)
Basic Dosage Forms for Preclinical Studies
Liquids
- Solutions
- Dispersions
- Suspensions
Semisolids
- Ointments
- Creams
- Gels
Solids
- Powders
- Granules
- Tablets
Phase 1 Clinical Supply
With the help of our strength in formulation design and characterization of new drug candidates, our expertise covers the aspects of early drug product development including the preformulation studies and formulation, and process development of novel dosage forms. Our goal is in line with our client's goal to make rapid deliverable drug product supplies in support of preclinical to Phase I clinical studies.
Service to Support Phase 1 Clinical Studies
- Formulation development
- Phase 1 clinical supplies
- Collaborate with Phase 1 Clinical CRO by supplying GMP API and formulation design for on-site compounding
Phase 1 Supply Equipment
