Thermoreversible API Formulation for Ambient-Solid Dispensing
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Solution Overview
Problem
The development of dispenseable formulations for active pharmaceutical ingredients (APIs) is challenging due to the need for physiochemical properties that allow dispensability at moderate temperatures while being solid at ambient temperatures, and suitability for a broad range of APIs.
Innovation Solution
A formulation comprising 5-30 wt.-% gelling agents like gelatin or agar, 0.5-5 wt.-% silica, 10-35 wt.-% hydrated vegetable fats with a melting point of 35° C. to 55° C., 10-30 wt.-% carbohydrates or sugar alcohols, and 40-70 wt.-% solvents, which are thermoreversible and suitable for a wide range of APIs.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If the formulation uses gelling agents and lipid-based excipients to enable dispensability at moderate temperatures, then the dispensability is improved, but the formulation complexity increases
Solution Approach 1:
The formulation uses a composite system combining gelling agents (gelatin, agar) with lipid-based excipients (hydrated vegetable fats) to create a material that exhibits both solid-like stability at ambient temperature and liquid-like dispensability at moderate temperature. This composite approach allows the formulation to achieve contradictory properties of being both structurally stable and easily dispensable under different conditions.
Solution Approach 2:
The formulation exploits temperature as a critical parameter to change its physical state. By selecting lipid-based excipients with melting points between 35-55°C, the formulation transitions from a solid state at ambient temperature to a liquid state at moderate temperature, enabling dispensability only when needed without compromising storage stability.
2Stability of the object's composition
If the formulation is designed to be solid at ambient temperature for stability, then the storage stability is improved, but the dispensability at moderate temperature deteriorates
Solution Approach 1:
The formulation is designed to undergo a phase transition from solid to liquid at a specific temperature range (35-55°C). The lipid-based excipients are selected based on their melting points within this range, allowing the formulation to remain solid and stable during storage at ambient temperature, then transition to a liquid state for easy dispensing when heated to moderate temperatures during the dispensing process.
3Adaptability or versatility
If the formulation uses a broad range of excipients to suit various APIs, then the versatility is improved, but the manufacturing complexity increases
Solution Approach 1:
The formulation employs excipients that serve multiple functions simultaneously. The gelling agents provide both structural stability and temperature-responsive gelation, while the lipid-based excipients provide both solubility enhancement and temperature-dependent flow properties. This multi-functionality reduces the need for additional specialized excipients for different API types, simplifying the overall formulation approach despite the broad applicability.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The formulation enables precise, cost-effective, and environmentally friendly production of personalized solid dosage forms with tailored dosages and release characteristics, suitable for a broad range of APIs, reducing waste and environmental burden.
Implementation Method 1
The formulation should be dispenseable at moderate temperature while solid at ambient temperature
Implementation Method 2
the melting point of the one or more hydrated vegetable fats is from 35° C. to 55° C.
Implementation Method 3
5-30 wt.-% of one or more gelling agents selected from a group consisting of gelatin, agar, and combinations thereof
Implementation Method 4
the formulation should be suitable for a broad range of active pharmaceutical ingredients
Data Source
AI summary
The present disclosure relates to formulations which can be admixed with active pharmaceutical ingredients (API) to produce dispenseable dispersions. The disclosure also relates to methods for preparing solid dosage formulations of APIs using the formulations. The formulations include 5-30 wt.-% one or more gelling agents, 0.5-15 wt.-% silica, 10-35 wt.-% of one or more lipid-based excipients, such as cocoa butter and/or hydrated coconut oil, 10-30 wt.-% carbohydrates and/or sugar alcohols, and 40-70 wt.-% one or more solvents.