Artemether Transmucosal Spray for Malaria Treatment
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Solution Overview
Problem
Current malaria treatments face challenges such as drug resistance, difficulty in administering medications to children, especially in resource-limited areas where nutritional status is poor and cultural barriers exist, and existing formulations like rectal suppositories are ineffective due to diarrhea and nutritional requirements.
Innovation Solution
A pharmaceutical composition comprising artemether or arteether with medium chain length triglycerides, short chain triglycerides, or omega-3-marine triglycerides and fish oil, formulated for transmucosal sublingual, buccal, or nasal administration, which can be administered by non-medically qualified personnel, particularly suitable for children in remote settings.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If rectal suppositories are used for malaria treatment, then drug delivery is possible, but absorption is poor due to diarrhea and nutritional deficiencies
Solution Approach 1:
The patent uses sublingual/buccal mucosa as an intermediary absorption route instead of rectal administration. The mucosal tissues in the mouth provide a reliable absorption pathway that bypasses the gastrointestinal tract issues (diarrhea, malnutrition) that compromise rectal suppository effectiveness. This intermediary route ensures consistent drug delivery regardless of gastrointestinal condition.
Solution Approach 2:
The patent changes the administration route parameter from rectal to sublingual/buccal. This parameter change transforms the absorption mechanism from one dependent on gastrointestinal health (rectal) to one dependent on mucosal blood flow (sublingual/buccal), thereby improving reliability in malnourished children with diarrhea.
2Ease of manufacture
If tablets are used for malaria treatment, then dosing is simple, but administration is difficult to children who cannot swallow
Solution Approach 1:
The patent changes the physical form parameter from solid tablets to liquid/oral solution formulation. This allows the medication to be administered in forms suitable for children who cannot swallow tablets, such as drops or liquid that can be given via spoon or syringe, while maintaining precise dosing capabilities.
Solution Approach 2:
The patent uses the sublingual/buccal mucosa as an intermediary that allows drug absorption without requiring swallowing. The medication is placed in the mouth where it dissolves and absorbs directly through the mucosal tissues into the bloodstream, bypassing the need for the child to swallow.
3Speed
If intravenous administration is used for malaria treatment, then rapid delivery is achieved, but trained medical personnel are required
Solution Approach 1:
The patent uses the sublingual/buccal mucosa as an intermediary absorption site that provides rapid drug entry into the systemic circulation without requiring intravenous access. This route achieves speed comparable to intravenous administration but with much simpler administration that can be performed by community health workers or even trained parents.
Solution Approach 2:
The patent replaces the mechanical/invasive intravenous injection system with a non-invasive mucosal absorption system. Instead of requiring needles, veins, and trained personnel for IV administration, the medication is delivered through the mouth and absorbed through the mucosa, substituting a complex medical procedure with a simple self-administerable or community-administerable method.
4Reliability
If artemether is formulated for transmucosal administration, then bioavailability is improved, but formulation stability at high temperatures is challenged
Solution Approach 1:
The patent uses a composite formulation system combining artemether with specific excipients (such as cyclodextrins, lipids, or polymers) that provide both enhanced mucosal absorption and thermal stability. The excipients form a protective matrix that stabilizes the artemether molecule against degradation at high temperatures while facilitating its absorption through the sublingual/buccal mucosa.
Solution Approach 2:
The patent introduces excipients as intermediary substances that mediate between the artemether drug molecule and the environmental conditions (heat, moisture). These excipients protect the artemether from thermal degradation while simultaneously enhancing its solubility and absorption through the mucosal tissues.
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
This formulation provides higher and more reproducible bioavailability of artemether, is stable at high temperatures, and can be effectively absorbed through mucosal routes, reducing the risk of swallowing and improving treatment outcomes in children.
Implementation Method 1
the transmucosal sublingual, transmucosal buccal and transmucosal nasal routes for administration of artemether or arteether are effective for delivery of the pharmaceutical into the systemic circulation
Data Source
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AI summary
The invention provides pharmaceutical compositions for the treatment and prophylaxis of malaria, comprising artemether and a medium chain triglyceride formulated for transmucosal sublingual, buccal or nasal delivery, especially by a spray. Also provided are delivery devices containing the compositions.