Stabilized Pharmaceutical Solid Preparation Using Colorants
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Solution Overview
Problem
Developing pharmaceutical solid preparations of [(1R, 5S, 6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid monobenzenesulfonate (compound I) that are stabilized by containing colorants, as existing methods face challenges in maintaining stability and effectiveness.
Innovation Solution
Formulating pharmaceutical solid preparations of compound I in combination with D-mannitol, lactose, corn starch, carmellose calcium, and specific iron oxides as colorants, with controlled particle sizes and concentrations, and incorporating a coating agent to enhance stability, particularly in the form of coated tablets.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If compound (I) is formulated as a pharmaceutical solid preparation without colorants, then the preparation maintains simplicity in formulation, but the compound deteriorates due to light exposure and lacks stability
Solution Approach 1:
Colorants are introduced as intermediary substances that mediate between light and compound (I). The colorants absorb harmful light wavelengths and convert them to harmless energy, protecting compound (I) from photodeterioration. This intermediary approach resolves the contradiction by adding a protective layer without fundamentally changing the core formulation.
Solution Approach 2:
The pharmaceutical preparation is formulated as a composite material containing compound (I), colorants, and excipients. This composite structure combines the therapeutic compound with stabilizing colorants and functional excipients, achieving enhanced stability while maintaining a relatively simple overall formulation architecture.
2Reliability
If colorants are added to stabilize compound (I), then light-induced degradation is reduced and stability is improved, but the formulation becomes more complex
Solution Approach 1:
The colorants in the formulation serve multiple functions: they act as stabilizers to protect compound (I) from light, contribute to the desired aesthetic appearance of the preparation, and can provide additional therapeutic or protective effects. This multi-functionality reduces the need for separate additives, thereby limiting the increase in formulation complexity.
3Ease of manufacture
If compound (I) is exposed to light, then the compound can be used in transparent or clear formulations, but the compound undergoes deterioration and loses effectiveness
Solution Approach 1:
The optical properties of the formulation are modified by selecting colorants with specific absorption characteristics. The colorants are chosen to absorb in the ultraviolet and visible ranges while maintaining the desired transparency or color appearance. This parameter adjustment allows the formulation to maintain both transparency and stability.
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 approach results in a stabilized pharmaceutical solid preparation of compound I, achieving improved stability and effectiveness, as evidenced by reduced light-induced degradation and enhanced production of stable coated tablets.
Implementation Method 1
rutile type titanium oxide, red iron sesquioxide, and yellow iron sesquioxide, as colorants
Data Source
AI summary
An object of the present invention is to provide [(1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid monobenzenesulfonate as a stabilized pharmaceutical solid preparation. The object can be attained by a pharmaceutical solid preparation comprising [(1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid monobenzenesulfonate which is compound represented by the following formula (I) in combination with (i) one or two or more components selected from the group consisting of D-mannitol, lactose, corn starch, and crystalline cellulose, (ii) carmellose calcium, and (iii) colorants.