含1-(5-(2,4-二氟苯基)-1-((3-氟苯基)磺酰基)-4-甲氧基-1H-吡咯-3-基)-N-甲基甲胺的口服给药新制剂
By using a specific ratio of lactose hydrate and microcrystalline cellulose as excipients in the oral formulation of 1-(5-(2,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methoxy-1H-pyrrole-3-yl)-N-methylmethylamine, the problems of low water solubility and reduced solubility were solved, resulting in stable solubility and storage stability, and improved efficacy.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- DAEWOONG PHARM CO LTD
- Filing Date
- 2021-12-17
- Publication Date
- 2026-07-17
AI Technical Summary
1-(5-(2,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methoxy-1H-pyrrole-3-yl)-N-methylmethylamine has low water solubility and its solubility decreases over time, resulting in unstable bioavailability and efficacy. Adding soluble additives to existing formulations may trigger allergic reactions.
By using lactose hydrate and microcrystalline cellulose in a specific weight ratio as excipients, combined with appropriate disintegrants and lubricants, the particle size distribution of the active ingredient is adjusted to prepare oral formulations to improve solubility and storage stability.
It exhibits stable solubility in the gastrointestinal environment, ensuring sustained efficacy, avoiding allergic reactions, and improving bioavailability and storage stability.
Smart Images
Figure CN116761589B_ABST