Validation of a Novel RP-HPLC Technique for Simultaneous Estimation of Lignocaine Hydrochloride and Tibezonium Iodide: Greenness Estimation Using AGREE Penalties

Article

Author: Algahtani, Mohammad M ; Rashid, Ahmad Junaid ; Alharby, Tareq Nafea ; Sarfraz, Rai Muhammad ; Alanazi, Muteb ; Alanazi, Jowaher ; Syed, Muhammad Ali ; Hanif, Sana

Herein, we reported an HPLC method for the simultaneous determination of tibezonium iodide (TBN) and lignocaine hydrochloride (LGN). The method was developed according to the International Conference for Harmonization guidelines (ICH) Q2R1 using Agilent^® 1260 with a mobile phase consisting of acetonitrile and phosphate buffer (pH 4.5) in a volumetric ratio of 70:30 and flowing through a C₈ Agilent^® column at 1 mL/min. The results revealed that TBN and LGN peaks were isolated at 4.20 and 2.33 min, respectively, with a resolution of 2.59. The accuracy of TBN and LGN was calculated to be 100.01 ± 1.72% and 99.05 ± 0.65% at 100% concentration, respectively. Similarly, the respective precision was 100.03 ± 1.61% and 99.05 ± 0.48%. The repeatability for TBN and LGN was found to be 99.05 ± 0.48% and 99.19 ± 1.72%, respectively, indicating that the method was precise. The respective regression co-efficient (r²) for TBN and LGN was found to be 0.9995 and 0.9992. Moreover, the LOD and LOQ values for TBN were 0.012 and 0.037 µg/mL, respectively, while for LGN, they were 0.115 and 0.384 µg/mL, respectively. The calculated greenness of the method for ecological safety was found to be 0.83, depicting a green contour on the AGREE scale. No interfering peaks were found when the analyte was estimated in dosage form and in volunteers' saliva, depicting the specificity of the method. Conclusively, a robust, fast, accurate, precise and specific method was successfully validated to estimate TBN and LGN.

03 Aug 2021·Drug Development and Industrial PharmacyQ4 · MEDICINE

Development and optimization of tibezonium iodide and lignocaine hydrochloride containing novel mucoadhesive buccal tablets: a pharmacokinetic investigation among healthy humans

Q4 · MEDICINE

Article

Author: Syed, Muhammad Ali ; Mahmood, Asif ; Irfan, Muhammad ; Minhas, Muhammad Usman ; Hanif, Sana ; Sarfraz, Rai Muhammad

OBJECTIVEIt is clinically important to deliver a sustained-release mucoadhesive dosage of local anesthetic and antimicrobial agents for pain control. The current study aimed to develop and evaluate chitosan (CHI) based buccal mucoadhesive delivery for the local release of tibezonium iodide (TBN) and lignocaine hydrochloride (LGN).METHODSDirect compression technique was employed, aided by other mucoadhesive polymers like hydroxypropylmethylcellulose (HPMC) and sodium alginate (SA) and evaluated for physicochemical and in vivo character.RESULTSFourier transform infrared spectral analysis (FTIR), powdered X-ray diffraction (XRPD), and differential scanning calorimetry (DSC) absence of physical interaction between ingredients. The physical parameters complied with USP specifications for all formulations. Optimum swellability (551.9%) was offered from formulation TL15, containing 30% SA. The highest ex vivo mucoadhesive strength (24.79 g) and time (18.39 h) was found with TL8. Formulation TL8 also exhibited maximum in vivo residence time (11.37 h). Almost complete drug release at 6 h was possessed by formulation TL5 (HPMC and CHI, 20% each) for TBN (99.98%) and LGN (99.06%). The optimized formulation TL5 exhibited dosage stability up to 6 months at 75% relative humidity and retained drug contents. TL5 was well tolerated by the volunteers with no inflammation, pain or irritation found. Almost 73% of volunteers reported an increase in salivary secretion. The first-order salivary C_max of TBN and LGN were found as 16.02 and 7.80 µg/mL within 4 h, respectively.CONCLUSIONTherefore, the sustained release mucoadhesive dosage form of TBN and LGN can be an effective and alternative option to conventional delivery.

01 Jan 1983·Arzneimittel-Forschung

Mutagenicity studies on tibezonium, a new oropharyngeal disinfectant.

Article

Author: Bertoncini, A ; Veronese, M ; Barzaghi, D

N,N-Diethyl-N-methyl-[2-[[4-(4-phenylthio) phenyl]-3H-1,5-benzodiazepin-2-yl]thio]-ethanaminium iodide) (tibezonium iodide; CAS-54663-47-7), a new oropharyngeal disinfectant, was tested, using the Ames procedure with and without metabolic activation, on five strains of Salmonella typhimurium and using the host mediated assay with Schizosaccharomyces pombe as microorganism test. In both tests the drug did not show any mutagenic activity when compared with mutagenic standards.

100 Deals associated with Tibezonium Iodide

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KEGG	Wiki	ATC	Drug Bank
D02712	Tibezonium Iodide	A01AB15	DB13702

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