How do pH-modifying excipients like tartaric acid and azelaic acid improve the solubility and dissolution of raloxifene?

Label:chem

Topic
pH-modifying excipients such as tartaric acid and azelaic acid can protonate the basic groups in raloxifene, forming salts that increase the drug's ionization and solubility.
Answer
Tartaric acid and azelaic acid significantly improve the solubility and dissolution of raloxifene by forming salts through protonation of the piperidine nitrogen in raloxifene. The study demonstrated that raloxifene-tartaric acid and raloxifene-azelaic acid complexes achieved solubility increases of up to 800-fold compared to the untreated drug. The coprecipitation method further enhanced the dissolution rates, with raloxifene-tartaric acid Coppt showing the highest dissolution efficiency.
Return to Home Chemical List
Knowledge you may be interested in
What is the role of cyclodextrins in enhancing the solubility and dissolution of raloxifene? How does raloxifene function as an anticancer agent in breast cancer treatment? What are the barriers to the use of mifepristone for EPL management in assisted reproductive technology (ART) pregnancies? How does the combination of mifepristone and misoprostol compare to misoprostol alone in managing EPL? Why is mifepristone not widely used by reproductive endocrinology and infertility specialists for EPL management? What is the role of mifepristone in the management of early pregnancy loss (EPL)? What is the role of mifepristone and misoprostol in the management of early pregnancy loss (EPL)? What is the role of mifepristone in cervical ripening and labor induction? What is the role of halenaquinone (HQ) in the treatment of leukemia, particularly in Molt 4 cells? What role does ropivacaine play in the treatment of nasopharyngeal carcinoma (NPC)? What is the impact of raloxifene-tartaric acid complexes on cytotoxicity in breast cancer cells? How does the cellular uptake of raloxifene complexes with tartaric acid and HP β-CD compare in Caco-2 cells? How do genetic variants in the ESR1 gene influence the treatment response to raloxifene in schizophrenia-spectrum disorders (SSD)? How do genetic variants in the COMT gene influence the treatment response to raloxifene in schizophrenia-spectrum disorders (SSD)? How do genetic variants in the UGT1A8 gene influence the treatment response to raloxifene in schizophrenia-spectrum disorders (SSD)? What is the antibacterial mechanism of riccardin C derivatives against MRSA? What is the role of IDPO-9 in the antibacterial activity against MRSA? What is the role of Riccardin C (RC) in modulating the activity of Liver X Receptors (LXRs)? How does Riccardin C (RC) affect cholesterol efflux in THP-1 cells? What is the role of Riccardin F (RF) in modulating the activity of Liver X Receptors (LXRs)?