Enhanced Stabilization of Phenobarbital Sodium for Injection
Legal Citation
Summary of the Inventive Concept
This invention provides a novel system, method, and composition for stabilizing phenobarbital sodium for injection, ensuring improved efficacy, safety, and efficiency in neonatal seizure treatment.
Background and Problem Solved
The original patent disclosed a lyophilized pharmaceutical composition of phenobarbital or salts thereof with an ethanol content in a specific range. However, this composition may still degrade over time, leading to impurities and reduced efficacy. The present inventive concept addresses these limitations by introducing a system and method for minimizing total impurities during reconstitution, improving storage conditions, and formulating the composition to reduce impurity formation.
Detailed Description of the Inventive Concept
The novel system comprises a lyophilized pharmaceutical composition having an ethanol content in the range from about 5000 ppm to about 70000 ppm, and a reconstitution device for mixing the lyophilized composition with a vehicle/diluent. The method involves lyophilizing a pharmaceutical composition having an ethanol content in the range from about 12000 ppm to about 25000 ppm, and storing the lyophilized composition at a temperature range of 2-8° C. to reduce degradation. The composition is formulated to reduce the formation of 2-phenyl-2-ethyl acetyl urea impurities, ensuring a total impurity content of less than 0.1% following 36 months of storage at 20-25° C.
Novelty and Inventive Step
The inventive concept's novelty lies in the integration of a reconstitution device, controlled storage conditions, and a formulation designed to minimize impurities. This combination provides a significant improvement over the original patent, as it ensures the stability and efficacy of phenobarbital sodium for injection over an extended period.
Alternative Embodiments and Variations
Alternative embodiments may include varying the ethanol content range, using different vehicle/diluents, or incorporating additional stabilizers. Variations of the method may involve adjusting the storage temperature or using different lyophilization techniques.
Potential Commercial Applications and Market
This inventive concept has significant commercial potential in the pharmaceutical industry, particularly in the treatment of neonatal seizures. The improved stability and efficacy of phenobarbital sodium for injection can lead to better patient outcomes, reduced healthcare costs, and increased market share for pharmaceutical companies.
CPC Classifications
| Section | Class | Group |
|---|---|---|
| A | A61 | A61K9/19 |
| A | A61 | A61K9/08 |
| A | A61 | A61K31/515 |
| A | A61 | A61K47/10 |
| A | A61 | A61P25/08 |
Section 103 Obviousness Analysis (PHOSITA)
Field of Art
Pharmaceutical formulation and drug delivery, specifically focused on lyophilized injectable compositions for neurological treatments, with expertise in pharmaceutical chemistry, stabilization techniques, and parenteral drug preparation
Person of Ordinary Skill (PHOSITA) Profile
A pharmaceutical scientist or formulation engineer with advanced degree in pharmaceutical sciences, experience in drug stability testing, lyophilization techniques, and injectable medication development, familiar with impurity management and pharmaceutical preservation strategies
Obviousness Rationale
A PHOSITA would recognize that the PTD represents a predictable variation of the source patent's core teachings, extending the original phenobarbital sodium stabilization method through incremental modifications in ethanol content range, storage conditions, and impurity management that would be considered routine optimization within pharmaceutical formulation development.
Obvious Combinations & Variations
Original Patent Information
| Patent Number | US 11,857,683 |
|---|---|
| Title | Stabilization of phenobarbital sodium for injection |
| Assignee(s) | SUN PHARMA ADVANCED RESEARCH COMPANY LIMITED |