The report provides a detailed analysis essential for establishing a rimexolone production plant. It encompasses all critical aspects necessary for rimexolone production, including the cost of rimexolone production, rimexolone plant cost, rimexolone production costs, and the overall rimexolone production plant cost. Additionally, the study covers specific expenditures associated with setting up and operating a rimexolone production plant. These encompass production processes, raw material requirements, utility requirements, infrastructure needs, machinery and technology requirements, manpower requirements, packaging requirements, transportation requirements, and more.
Rimexolone is a glucocorticoid corticosteroid that is used as a 1% ophthalmic suspension. It is used to treat postoperative ocular inflammation following surgeries like cataract procedures and anterior uveitis, reducing edema, cellular infiltration, and scar formation. It works by stopping prostaglandin and leukotriene biosynthesis via glucocorticoid receptor agonism. It offers equivalent efficacy to prednisolone acetate with potentially lower intraocular pressure elevation risk. It is also used in other inflammatory eye conditions like conjunctivitis, keratitis, and rheumatoid arthritis, for intra-articular therapy due to its sustained release from crystal suspensions. Its common side effects include blurred vision, eye redness, irritation, and pain, discharge, dryness, itching, increased intraocular pressure, headache, and photophobia.
The market for rimexolone is driven by rising eye disease cases (cataracts, uveitis, conjunctivitis). The expanding geriatric population, increasing cataract surgeries worldwide, and growing ophthalmic drug demand contribute to its market growth. The API supply chain dependency on specialised steroid manufacturers and strict GMP and ICH regulatory compliance for ophthalmic purity influences industrial rimexolone procurement. Other factors, like high raw material costs from complex steroid synthesis and generic competition post-patent expiry impacts its sourcing strategies. Also, reimbursement limitations in outpatient eye care and formulation challenges requiring sterile suspension stability testing further affect its market dynamics.
Raw Material for Rimexolone Production
According to the rimexolone production plant project report, the key raw materials used in the production of rimexolone include prednisolone, iodine monochloride or N-iodosuccinimide, pyridine, and sodium iodide.
Production Process of Rimexolone
The extensive rimexolone production cost report consists of the following major industrial production process:
- From prednisolone: The production process of rimexolone involves several steps. It starts with prednisolone iodination in pyridine using iodine monochloride or N-iodosuccinimide. This is followed by extraction and crystallisation to yield 21-iodo-prednisolone. The 21-iodo intermediate goes through reduction with sodium iodide in refluxing acetone, again monitored by TLC, extracted, and purified to give 21-deoxy-21-iodoprednisolone. The ketone groups are then protected as bis-semicarbazones by reaction with semicarbazide hydrochloride in buffered aqueous acetic acid, with the product precipitating for filtration and collection. The selective acidic hydrolysis in aqueous organic solvent regenerates the 3-ketone and hydrolyses the C20-semicarbazone to form the 17α-hydroxyprogesterone derivative. This undergoes enolate formation with a strong base, followed by stereoselective 16α-methylation using methyl iodide. The 17α-hydroxyl is acylated with propionic anhydride or propionyl chloride and pyridine to install the 17α-propionyl ester. Final deprotection via acidic or basic hydrolysis yields rimexolone as the final product.
Rimexolone is a white to off-white, crystalline powder that is insoluble in water but soluble in organic solvents like chloroform and methanol. It has the molecular formula of C24H34O3 and a molecular weight of 370.53 g/mol. It features a pregnadiene steroid backbone with 3-keto, 11β-hydroxy, 16α-methyl, and 17α-propionyloxy substitutions. It shows specific rotation between +47 degree to +54 degree (in chloroform) with a melting point around 220-230 degree Celsius. It has a pKa value of 12.1 due to enolisable ketone and a low logP value of 3.8, which makes it moderately lipophilic. It is suitable for ocular penetration and shows stability in neutral pH suspensions (6.0-8.0).