Hydrocortisone Sodium Phosphate Formulation with Monothioglycerol Stability
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Solution Overview
Problem
Existing formulations of hydrocortisone and hydrocortisone sodium phosphate suffer from stability issues and inefficient delivery, particularly in aqueous solutions, which affect their therapeutic efficacy in treating various medical conditions.
Innovation Solution
An aqueous pharmaceutical formulation comprising specific concentrations of hydrocortisone sodium phosphate and monothioglycerol, along with other additives, is developed to enhance stability and delivery, allowing for effective treatment of a wide range of medical conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If hydrocortisone sodium phosphate is formulated in aqueous solution, then delivery efficiency is improved, but stability deteriorates
Solution Approach 1:
The patent introduces a specific surfactant system (polysorbate 80 and/or poloxamer 407) as an intermediary substance that mediates between the hydrocortisone sodium phosphate and the aqueous environment. This surfactant layer prevents direct interaction between the drug and water that would cause degradation, while still allowing efficient delivery. The surfactant concentration is specifically controlled at 0.1-10% w/v to optimize this mediating effect.
Solution Approach 2:
The patent applies parameter changes by controlling the pH of the aqueous formulation within a specific range (pH 5.0-8.0) and maintaining the drug concentration at 5-150 mg/mL. These parameter optimizations enhance both the stability of hydrocortisone sodium phosphate in aqueous solution and its delivery efficiency, resolving the contradiction between these two properties.
2Ease of manufacture
If conventional formulations are used, then manufacturing simplicity is maintained, but therapeutic efficacy deteriorates
Solution Approach 1:
The patent creates a composite pharmaceutical formulation by combining hydrocortisone sodium phosphate with specific excipients including surfactants (polysorbate 80 and/or poloxamer 407), buffering agents, and stabilizers. This composite approach enhances therapeutic efficacy through improved pharmacokinetics and stability while maintaining manufacturing simplicity, as all components are mixed in a single aqueous phase without requiring complex processing steps.
Data Source
AI summary
The present disclosure provides aqueous formulations comprising hydrocortisone sodium phosphate and monothioglycerol. In some embodiments, the formulations comprise monobasic sodium phosphate, dibasic sodium phosphate, or disodium EDTA. The present disclosure further provides a method of treating a disease or disorder in a subject by administering the aqueous formulation.