Single-Tablet Telmisartan–SGLT-2 Formulation for Stable Dissolution
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Solution Overview
Problem
Conventional drug treatments for hypertension with diabetes often require separate administration of Telmisartan and SGLT-2 inhibitors, leading to low medication convenience and compliance due to drug-drug interaction issues, particularly with Telmisartan's low solubility and moisture absorption affecting Dapagliflozin stability.
Innovation Solution
A combined oral pharmaceutical preparation of Telmisartan or its pharmaceutically acceptable salt, a sodium-glucose cotransporter-2 (SGLT-2) inhibitor such as Dapagliflozin or Empagliflozin, and an excipient, formulated to maintain stability and solubility, allowing a single tablet administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If Telmisartan and SGLT-2 inhibitor are administered separately, then drug stability is maintained, but medication convenience and compliance deteriorate
Solution Approach 1:
The patent combines Telmisartan and SGLT-2 inhibitor into a single tablet formulation, allowing both drugs to be administered simultaneously in one dose. This merging of two separate medications into one combined preparation directly improves medication convenience and compliance while maintaining drug stability through controlled formulation science.
2Ease of operation
If Telmisartan and SGLT-2 inhibitor are combined in a single tablet, then medication convenience improves, but drug-drug interaction and stability issues worsen
Solution Approach 1:
The patent introduces specific excipients and formulation components as intermediaries between Telmisartan and SGLT-2 inhibitor. These intermediary substances act as buffers and protectors that prevent direct harmful interactions between the two drugs while allowing them to coexist in a stable combined formulation, thus enabling convenient single-tablet administration.
Solution Approach 2:
The patent employs controlled parameter changes in the formulation, including adjustment of pH levels, moisture content, and physical structure of the tablet. By carefully controlling these parameters, the formulation maintains drug stability and prevents harmful interactions between Telmisartan and SGLT-2 inhibitor while enabling their combined administration in one tablet.
3Power
If Telmisartan is used at high concentration, then antihypertensive effect improves, but solubility and dissolution rate deteriorate
Solution Approach 1:
The patent applies parameter changes by adjusting the physical and chemical properties of Telmisartan in the formulation, including pH adjustment and use of solubility-enhancing excipients. These parameter modifications enable Telmisartan to maintain high concentration for effective antihypertensive action while improving its solubility and dissolution rate in the combined tablet formulation.
Solution Approach 2:
The patent creates a composite material system combining Telmisartan, SGLT-2 inhibitor, and specific excipients in a synergistic formulation. This composite structure allows Telmisartan to achieve high therapeutic concentration while the composite formulation itself provides improved solubility and dissolution characteristics through the combined properties of all ingredients.
Data Source
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Figure 2A~2B
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AI summary
The present invention relates to an oral pharmaceutical preparation comprising a sodium-glucose cotransporter-2 inhibitor and an angiotensin II receptor blocker, which enables the sodium-glucose cotransporter-2 inhibitor and the angiotensin II receptor blocker, which have conventionally been taken separately, to be manufactured into a single combination that can be orally administered, and can be implemented in a relatively small size, thereby improving convenience of administration and patient compliance, and since there are no drug-drug interaction issues, the present invention can be effectively utilized in patients who need to take the medication for a long period of time, such as type 2 diabetes, hypertension, hypertension with diabetes, and heart failure.