This development program aimed to develop an aqueous,multi-dose oral suspension formulation of a novel drug candidate at a concentration of 20mg/ml that would be appropriate for the treatment of kidney disease in pediatric patients aged 2 years and older. A liquid formulation was favored over a coated granule formulation. 

Download Quotient Sciences' poster, 'EuPFI 2019 Poster-Development of a Paediatric Oral Suspension of a Novel Drug for the Treatment of Kidney Disease'.

Presented at AAPS 2019: Both micronization and co-micronization can improve the rate and extent of drug dissolution. However, co-micronization of Drug A with a precipitation inhibitor HPC and further blending with a wetting agent SLS could significantly increase the drug dissolution to achieve a supersaturated state for Drug A. In the presence of a precipitation inhibitor, the solubilized drug was maintained in the metastable over some time with a slow precipitation rate. The addition of a precipitation inhibitor has successfully maintained Drug A in the solubilized form for an extended period allowing greater potential for drug absorption. In vivo studies will be conducted to evaluate the bioavailability of the final formulation. The final results demonstrate the co-micronization process managed to improve the bioavailability of the poorly soluble drug investigated.

Download Quotient Sciences' poster, 'AAPS 2019 Poster: Development of a Solubilised Capsule Formulation Using Co-Micronization & Precipitation Inhibition'.

Presented at AAPS 2019: Translational Pharmaceutics was used to evaluate three BOS172767 formulations in an integrated clinical study, and successfully identified the micronized capsule as the new lead formulation. This formulation had superior exposure compared to the IR reference capsules, and an approximate proportional increase in exposure up to 800 mg. The food effect observed at 100 mg was reduced compared to that previously seen at 200 mg (FIH capsule) and elevated gastric pH (subjects taking PPIs) had minimal effect on exposure. A Level C IVIVC was achieved with a biorelevant dissolution test, which provides valuable information for future formulation development and setting of product specifications.

Presented at AAPS 2019: Aqueous solubility is a prerequisite for oral absorption of a drug and the pH-dependence of aqueous solubility is critical information to guide formulation development strategies. The purpose of this study was to evaluate the physical property modules in two commercially available in-silico modeling programs in predicting the pH solubility profiles as described by the ionization constant (pKa) and the intrinsic solubility of the unionized form.

Request a copy of our scientific poster titled, 'Comparison of Two In-Silico Modeling Programs, ADMET Predictor® and Percepta® to Predict Intrinsic Solubility and pKa of Poorly Soluble Drugs'.

Download our poster from AAPS 2019 titled, 'Applications and Benefits of Healthy Volunteer Trials to Accelerate Oncology Drug Development.'

Presented at AAPS 2019: Phase I drug development for oncology compounds is traditionally conducted directly in patient populations. Oncology molecules have historically been cytotoxic, meaning their safety and risk-benefit profile makes them unviable for dosing in healthy subjects. While this ensures reduced nonclinical requirements, rapid access to patient data, and an earlier assessment of efficacious potential, it can also present challenges. For example, patients recruited in Phase I trials typically are in end-of-life care and will be taking multiple co-medications and have multiple co-morbidities (e.g. liver and kidney function may vary greatly among the recruited subjects). Practically, recruiting patients into Phase I studies can also be problematic, requiring multiple clinical sites and protracted recruitment times for what would traditionally be a single site, quickly recruited healthy volunteer studies.

Check out our latest poster from AAPS 2019, 'Clinical Formulation Development for Poorly Soluble 14C Labelled Molecules.' 

Clinical studies involving the administration of 14C radio-labeled drug substances provide critical information during development. The main application is the regulatory ADME study to assess the mass balance, routes, and rates of elimination, and to provide plasma, urine, and faecal samples for metabolite profiling and structural identification.

Request a copy of our scientific poster titled, 'HBI-3000: A Novel Drug for Conversion of Atrial Fibrillation - Phase 1 Study Results.'

HBI-3000 (sulcardine sulfate trihydrate; Bai, et al. 2012) is a multi-ion channel blocker with effects on INa-Peak, INa-Late, ICa,L, and IKr with similar in vitro potencies across these various ion channels in human atrial cardiomyocytes. It is being eveloped by HUYA Bioscience International® (HUYABIO™) for the conversion of recent onset atrial fibrillation (AF).

Presented at AAPS 2019: An integrated CMC and clinical development program successfully identified a commercializable formulation of DRGT-46 meeting required taste and PK attributes as per the Target Product Profile. Real time, adaptive GMP ensured formulation development decisions were taken based on human clinical data. Program efficiencies included minimization of drug substance consumption, lean regulatory CMC data packages, and a reduction in overall upfront CMC investments. The accelerated initiation of a Phase 1 study using an SDD PiB, and rapid transition to commercializable sachet formulation to support Phase III studies was achieved in less than 18 months.

Request a copy of our poster, 'Development of an X-ray Diffraction Method for the Quantification of API Recrystallized API.' Typically, in developing dry powder inhaler (DPI) formulations, a stable crystalline form of the active pharmaceutical ingredient (API) is desired. However, often to produce crystalline particles of suitable size for inhalation, micronization processes will be required, resulting in surface amorphous material which may affect the efficacy of the product. If required, additional conditioning/processing steps may then be applied to the API (or to ensure drug product stability under use) without requiring any additional solid-state characterization of the API in the drug product.

Download a copy of our scientific poster titled, 'A Clinical Assessment of Delayed-Release Coated Capsule Compositions for GI Delivery using Gamma Scintigraphy.' 

Applied Molecular Transport Inc. is evaluating targeted drug delivery capsules for the administration of locally acting drugs directly to the site of action in the gastrointestinal (GI) tract. This study used gamma scintigraphy to evaluate GI transit and release from 3 capsule prototypes with different coating systems (1). In addition, data on pH, temperature, and pressure during GI transit was obtained using SmartPill® and correlated with scintigraphy data (2).