Abstract
A new, simple, and rapid stereoselective normal phase-liquid chromatographic (NP-LC) method was developed to separate and quantify the solifenacin succinate and its three stereoisomers. The stereoisomeric separation was achieved on Chiralpak IC ( mm ID) column. The mobile phase was consisting of n-hexane, ethanol, isopropyl alcohol, and diethylamine in the ratio (60 : 15 : 25 : 0.1, v/v/v/v), and the flow rate was maintained at 1.0 mL min−1. UV detection was carried out at 220 nm. In addition, chiroptical detection was carried out using laser polarimeter to understand the elution orders. Resolution between all the stereoisomers was not less than 3. Effect of column temperature on resolution between the stereoisomers was studied. The method was validated as per ICH guideline and found to be robust. The proposed NP-LC method was successfully applied to the analysis of commercial formulation. The method could be of use not only for routine evaluation of the quality of solifenacin succinate in bulk drug manufacturing unit but also for detection of impurities in pharmaceutical formulations.
Highlights
Solifenacin, a well-known muscaranic receptor antagonist belongs to the anticholinergics used for the treatment of patients with overactive bladder such as urinary urgency, urinary incontinence, and high urinary frequency
Stereoiso- mers of racemic drugs often differ in pharmacokinetic behavior or pharmacological action, and among the four stereoisomers, the pharmacological action of (SR)-stereoisomer, that is, solifenacin shows high affinity and selectivity for the M3 receptor and has been approved as the drug [8]
The precision of the method was carried out by injecting six individual preparations of solifenacin succinate spiked with 0.15% of all the stereoisomers (Isomer1 to Isomer-3) with respect to target analyte concentration (i.e., 1.0 mg mL−1)
Summary
Solifenacin, a well-known muscaranic receptor antagonist belongs to the anticholinergics used for the treatment of patients with overactive bladder such as urinary urgency, urinary incontinence, and high urinary frequency. It acts as a selective antagonist to the M(3) receptor and works by relaxing the bladder muscles to prevent urgent, frequent, or uncontrolled urination. It is available in the market under the brand name Vesicare in the form of tablets for oral administration containing 5 or 10 mg of solifenacin succinate taken once daily [1,2,3,4,5,6,7]. The efforts paid to develop the method to achieve better resolution between all the stereoisomers and solifenacin using different chiral stationary phases and chiroptical detection using laser polarimeter in our laboratory are presented in this paper. The developed method was validated to ensure the compliance in accordance with USP and ICH guideline [17, 18]
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