Telmisartan Oral Suspension pH 10 Stability
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Solution Overview
Problem
Current pharmaceutical formulations of angiotensin-II-receptor antagonists, such as telmisartan, are unsuitable for children and pets due to their tablet form and limited dosage flexibility, and acidic solutions are not suitable for long-term use due to astringent effects, while alkaline solutions lack sufficient pH for stability and preservative availability.
Innovation Solution
A drinkable pharmaceutical solution with a pH of 10 or more containing telmisartan, using sugar alcohols to improve flavor and shelf life, and incorporating preservatives like benzalkonium chloride, with sugar alcohol concentrations above 60% meeting USP preservation criteria and reducing sugar content below 1000 ppm to ensure stability and safety.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If tablets are used for administration, then dosage strength is fixed and manufacturing is simple, but dosage flexibility is limited and administration to children and pets is difficult
Solution Approach 1:
The patent divides the fixed-dose tablet into a liquid suspension formulation that can be precisely dosed using calibrated aids (spoons, syringes, cups). This segmentation of the dosage unit allows flexible measurement of different volumes containing appropriate amounts of active substance, enabling adaptation to various weight groups and age categories while maintaining manufacturing feasibility through standard liquid formulation processes.
Solution Approach 2:
The patent changes the physical state parameter from solid tablet to liquid suspension, and adjusts the concentration parameter of active substance in the suspension to enable flexible dosing. By controlling the concentration of telmisartan in the suspension and providing calibrated dosing aids with marked volumes, the formulation achieves adaptable dosing for different patient groups while remaining manufacturable using conventional liquid pharmaceutical processes.
2Reliability
If acidic solution is used for formulation, then solubility is improved and preservatives are available, but astringent effects make it unsuitable for long-term use
Solution Approach 1:
The patent changes the pH parameter from acidic to alkaline (pH 10 or more) to eliminate the astringent effects that make acidic formulations unsuitable for long-term use in children and pets. This parameter change maintains solubility of telmisartan while removing the harmful astringent property, and the patent specifically notes that preservatives are also available for alkaline pH ranges.
3Object-affected harmful factors
If alkaline solution with pH less than 10 is used, then astringent effects are reduced, but pH stability for telmisartan is insufficient
Solution Approach 1:
The patent establishes the pH parameter at 10 or more as the optimal value that simultaneously achieves both goals: eliminating astringent effects and ensuring pH stability for telmisartan. This specific parameter threshold resolves the contradiction by providing a pH level high enough to prevent astringency while maintaining the chemical stability required for the active substance.
4Ease of operation
If sugar alcohols are added to improve flavor and shelf life, then taste is masked and preservation is enhanced, but reducing sugar content must be controlled
Solution Approach 1:
The patent specifies a parameter threshold for reducing sugar content (not exceeding 1000 ppm) in the sugar alcohol ingredients to simultaneously achieve flavor improvement through taste masking and maintain shelf life stability. This parameter control allows the use of sugar alcohols for their beneficial flavor-masking properties while preventing excessive reducing sugar content that could compromise formulation stability during storage.
Data Source
AI summary
A drinkable pharmaceutical solution includes telmisartan or a pharmaceutically acceptable salt, hydrate or polymorph thereof, where the telmisartan has a concentration of 1 to 10 mg/ml within the drinkable pharmaceutical solution, and the drinkable pharmaceutical solution has a pH of 10.