Topical Diol Triol Compositions for Muscle Spasm Relief
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Solution Overview
Problem
Current topical treatments for muscle spasms associated with pain often fail to effectively reduce muscle spasms despite reducing inflammation, as they do not address the spasmodic component effectively, and systemic exposure is a concern with oral NSAIDs.
Innovation Solution
Topical pharmaceutical compositions comprising C4-C8 aliphatic diols or triols, either alone or in combination with NSAIDs or steroidal agents, are developed to provide superior pain relief and muscle spasm reduction, available in various dosage forms including gels, tablets, and nanoemulsions, facilitating localized treatment.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If oral NSAIDs are used to treat muscle spasms, then anti-inflammatory effect is improved, but systemic exposure and side effects increase
Solution Approach 1:
The patent applies local quality by using topical formulations (gels, creams, ointments, lotions) that deliver NSAIDs and diol/triol compounds directly to the affected muscle area. This localized delivery ensures the anti-inflammatory effect is concentrated where needed while minimizing systemic absorption and associated side effects.
Solution Approach 2:
The patent introduces diol and triol compounds as intermediary substances that enhance the penetration and effectiveness of NSAIDs through the skin and into muscle tissue. These compounds act as penetration enhancers and co-actives that improve drug delivery to the target site while reducing the need for high systemic doses.
2Object-affected harmful factors
If topical anti-inflammatory agents are used, then systemic exposure is reduced, but muscle spasm relief is insufficient
Solution Approach 1:
The patent merges two distinct therapeutic approaches by combining anti-inflammatory NSAIDs with antispasmodic diol and triol compounds in a single topical formulation. This combination allows simultaneous treatment of both inflammation and muscle spasm, addressing the full spectrum of muscle pain pathology while maintaining topical delivery benefits.
Solution Approach 2:
The patent creates composite pharmaceutical formulations that integrate multiple active ingredients (NSAIDs, diols, triols) with various excipients and penetration enhancers. These composite materials work synergistically to provide both anti-inflammatory and antispasmodic effects through topical application, enhancing overall therapeutic efficacy.
3Reliability
If diol or triol compounds are applied topically, then muscle spasm relief is improved, but penetration into tissue is limited
Solution Approach 1:
The patent uses specific excipients and penetration enhancers as intermediary substances that facilitate the delivery of diol and triol compounds through the skin barrier and into underlying muscle tissue. These intermediaries improve the penetration rate and bioavailability of the active antispasmodic ingredients.
Solution Approach 2:
The patent optimizes various formulation parameters including pH, solubility, viscosity, and concentration of active ingredients to enhance the penetration and effectiveness of diol and triol compounds. By adjusting these parameters, the formulation achieves better tissue penetration while maintaining therapeutic stability.
Data Source
AI summary
The present invention is directed to pharmaceutical compositions comprising antispasmodic C4-C8aliphatic-l,2-diols and C4-C8aliphatic-l,2,3-triols and their use to relieve the spasms associated with pain. These agents may be administered topically or orally and may be combined with anti-inflammatory agents such as a non-steroidal anti-inflammatory drug or a corticosteroid. Administration of the C4-C8aliphatic-l,2-diols and C4-C8aliphatic-l,2,3-triols with vitamin D3 is indicated for conditions such as bone loss, weight gain and autoimmune diseases such as lupus and rheumatoid arthritis.