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Related Concept Videos

Drug Dissolution: Requirements and Profile Comparison01:14

Drug Dissolution: Requirements and Profile Comparison

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The acceptance criteria for dissolution profile data are anchored in Q values, representing the percentage of drug dissolved within a specified period. This assessment unfolds in three stages:First Stage: The test passes if all six drug dosage units are equal to or greater than Q plus 5%; otherwise, the sample proceeds to the second stage.Second Stage: The average of twelve units must be equal to or greater than Q, with no unit falling below Q - 15% to pass; if not, it progresses to the final...
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Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

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Body:Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
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Drug Delivery: Overview01:16

Drug Delivery: Overview

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The selection of a drug's delivery route depends upon its physicochemical properties, including lipid or water solubility and ionization, as well as the therapeutic requirement, such as immediate or sustained effect. These routes can be divided into three primary categories: enteral, parenteral, and topical.
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
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Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence01:27

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Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
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In Vitro Drug Release Testing: Overview, Development and Validation01:10

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In vitro dissolution and drug release tests assess how quickly and how much of a drug is released from its dosage form into an aqueous medium under standardized laboratory conditions. These tests are essential tools in pharmaceutical development and quality assurance, offering insight into the drug's performance before clinical use.During formulation development, dissolution testing identifies incomplete or inconsistent drug release issues. It also supports decisions on selecting the optimal...
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In Vitro Drug Dissolution: Alternative Methods01:17

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Alternative drug dissolution methods include the rotating bottle, intrinsic dissolution test, peristalsis, and the Franz diffusion cell method. The rotating bottle method involves meticulously rotating tightly capped controlled-release beads in a temperature-controlled bath. Periodic decanting of samples allows for residue assay, followed by refilling with fresh medium and testing at various pH levels to emulate the gastrointestinal tract conditions.In contrast, the intrinsic dissolution test...
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Development of a Once-Daily Modified-Release Formulation for the Short Half-Life RIPK1 Inhibitor GSK2982772 using

Debra Tompson1, Mark Whitaker2, Rennan Pan3

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New DiffCORE™ modified-release formulations of GSK2982772, a RIPK1 inhibitor, achieved consistent once-daily dosing profiles, overcoming previous food effect issues. The MR-16h formulation was chosen for further clinical trials.

Keywords:
DiffCOREGSK2982772RIPK1modified releasetranslational pharmaceutics

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Area of Science:

  • Pharmacology
  • Drug Delivery Systems
  • Clinical Pharmacology

Background:

  • GSK2982772 is a selective RIPK1 inhibitor with a short half-life.
  • Previous modified-release (MR) formulations showed susceptibility to food effects, impacting once-daily (QD) dosing.
  • Novel DiffCORE™ technology was developed to improve drug release profiles.

Purpose of the Study:

  • To evaluate the safety and pharmacokinetics (PK) of novel GSK proprietary DiffCORE™ MR formulations.
  • To assess the impact of food on the PK profiles of these new formulations.
  • To determine the suitability of DiffCORE™ formulations for QD dosing of GSK2982772.

Main Methods:

  • Part A: Single-dose PK of three DiffCORE MR formulations (12h to 18h release) in fasted and fed states.
  • Part B: PK of MR-16h formulation (120-960mg) across different prandial states.
  • Comparison with an immediate-release formulation was performed.

Main Results:

  • All tested DiffCORE MR formulations demonstrated consistent PK profiles in both fasted and fed states.
  • These profiles supported a QD dosing regimen for GSK2982772.
  • The food effect vulnerability seen with prior formulations was overcome.

Conclusions:

  • GSK proprietary DiffCORE™ technology successfully mitigated food effects for GSK2982772.
  • The MR-16h DiffCORE™ formulation is suitable for QD dosing.
  • This formulation was selected for further clinical development (NCT03649412).