Multilayer Beads for Prostaglandin Drug Stability
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Solution Overview
Problem
Current formulations of prostaglandin drugs, such as 15-keto-16-difluoro prostaglandin compounds, are unstable in water and solids, and patients like pediatrics or geriatrics with dysphagia face challenges in swallowing capsules, necessitating a stable and easily administrable form for gastrointestinal disorders.
Innovation Solution
Multilayer beads with a core particle, optional barrier layer, drug-in-polymer layer using 15-keto prostaglandin drugs and polyvinylpyrrolidone or vinylpyrrolidone-vinylacetate copolymer, and an optional sealant layer, designed for stable drug delivery and ease of administration, particularly for pediatric and geriatric patients.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If prostaglandin drugs are formulated in water or solid forms, then they can be administered to patients, but they become unstable and lose therapeutic efficacy
Solution Approach 1:
The prostaglandin drug is nested within a polymer matrix (polyvinylpyrrolidone or vinylpyrrolidone-vinylacetate copolymer) to form a protective encapsulation. This nested structure allows the drug to be administered in a stable solid form while maintaining its therapeutic efficacy by preventing direct exposure to destabilizing environments.
Solution Approach 2:
The invention creates a composite material system combining the prostaglandin drug with specific polymers (polyvinylpyrrolidone or vinylpyrrolidone-vinylacetate copolymer). This composite formulation provides both the stability needed for storage and the ease of administration required for patient compliance, resolving the contradiction between stability and ease of use.
2Stability of the object's composition
If capsules are used to administer prostaglandin drugs, then they provide stable delivery, but pediatric and geriatric patients with dysphagia cannot swallow them
Solution Approach 1:
The invention segments the drug delivery system into small bead-like particles instead of using a single large capsule. These segmented beads maintain the stability of encapsulated delivery while being small enough to be easily administered to patients with swallowing difficulties, such as pediatric and geriatric populations.
Solution Approach 2:
The invention changes the physical parameters of the dosage form from capsule size to small bead dimensions. This parameter change maintains the protective encapsulation benefits for drug stability while making the formulation suitable for patients who cannot swallow capsules, thus resolving the contradiction between stable delivery and ease of swallowing.
3Ease of manufacture
If prostaglandins are exposed to water or solids, then they can be formulated for administration, but they become significantly unstable and degrade
Solution Approach 1:
The polymer matrix acts as an intermediary between the prostaglandin drug and the external environment (water or solids). This intermediary layer allows the drug to be formulated in various administration forms while protecting it from degradation, maintaining both formulation feasibility and drug stability.
Data Source
AI summary
Multilayer beads for pharmaceutical use having a drug-in-polymer layer are disclosed. The disclosed multilayer beads for pharmaceutical use have (a) a core particle; (b) an optional barrier layer coated on the surface of the core particle; (c) a drug-in-polymer layer coated on the surface of the core or the barrier layer, (d) an optional sealant layer coated on the surface of the drug-in-polymer layer; and (e) optionally one or more outer layers external to the drug-in-polymer layer or the sealant layer. The drug-in-polymer layer consists essentially of (i) a drug selected from the group consisting of a 15-keto prostaglandin drug, a 13,14-dihydro prostaglandin drug, and a 13,14-dihydro-15-keto prostaglandin drug; and (ii) a polymer selected from the group consisting of polyvinylpyrrolidone, vinylpyrrolidone-vinylacetate copolymer or a mixture thereof. The drug-in-polymer layer may be solid dispersion of the drug in the polymer. Pharmaceutical compositions comprising a plurality of multilayer beads and a pharmaceutically acceptable excipient and methods of treating a gastrointestinal disorder are also disclosed.