Rolitetracycline API is a semisynthetic tetracycline-class antibacterial agent developed as a pyrrolidinomethyl derivative of tetracycline. It belongs to the tetracycline family of antibiotics and has historically been used when parenteral administration was required or oral administration was impractical. Rolitetracycline is also known by names such as Rolitetracycline, Pyrrolidinomethyltetracycline, Reverin, Syntetrin and TMS-related historical designations.
Rolitetracycline has the CAS number 751-97-3, molecular formula C₂₇H₃₃N₃O₈, and molecular weight 527.57 g/mol. FDA GSRS identifies Rolitetracycline with UNII GH9IW85221.
The molecule is a tetracycline derivative in which the amide functionality is modified with a pyrrolidinomethyl group. This structural modification is associated with substantially increased water solubility compared with tetracycline itself, making the compound historically useful for injectable pharmaceutical preparations.
Rolitetracycline is a complex, stereochemically defined tetracycline derivative containing multiple hydroxyl groups, a dimethylamino group and a pyrrolidinomethyl substituent.
Rolitetracycline should not be confused with tetracycline hydrochloride. Historical regulatory literature specifically distinguishes Rolitetracycline as a pyrrolidinomethyl derivative of tetracycline rather than simply tetracycline hydrochloride.
The commonly encountered parenteral pharmaceutical form is Rolitetracycline Nitrate, which provides the salt form used historically for injectable administration.
Rolitetracycline is a broad-spectrum tetracycline antibiotic that inhibits bacterial protein synthesis. It has historically been used for infections caused by susceptible organisms, particularly where an initial high antibiotic concentration was required or oral administration was impractical.
Its ATC classification is J01AA09, placing it within systemic tetracycline antibacterials.
Quality evaluation of Rolitetracycline should consider its complex tetracycline structure and susceptibility to degradation.
Analytical characterization can include UV-visible spectroscopy, FTIR, HPLC/UPLC, microbiological potency testing, water determination, residue on ignition and chromatographic related-substance testing.
Historical U.S. regulatory material describes microbiological assay procedures for Rolitetracycline and specifically identifies chemical/color reactions used for identity testing.
Manufacturing Rolitetracycline API requires controlled reaction, purification and isolation processes to maintain consistent potency and impurity profiles. For Rolitetracycline nitrate, control of the salt form and pharmaceutical-grade purity is particularly important because the nitrate form has historically been used for parenteral formulations.
Analytical documentation should support identity, potency, related substances, water content and other applicable quality attributes.
Rolitetracycline should be packaged in suitable well-closed pharmaceutical containers that protect the material from moisture and environmental contamination.
Because tetracycline derivatives can undergo degradation under unsuitable conditions, storage should follow validated stability data for the particular API and packaging configuration.
Typical documentation can include:
Rolitetracycline is a well-characterized semisynthetic tetracycline derivative with a long pharmaceutical-development history and established microbiological and analytical testing approaches. Its modified molecular structure provides enhanced aqueous solubility compared with conventional tetracycline, supporting its historical role in parenteral antibacterial formulations.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 0.5% |
| Residue on Ignition | NMT 0.2% |
| Water Content | NMT 0.5% |