A simple sample preparation with HPLC–UV method for estimation of tiropramide from plasma: Application to bioequivalence study

Khan, Imran Mahmood; Loya, Punnamchand; Natvarlal, Saraf Madhusudan

doi:10.1016/j.jpba.2006.10.001

Cited by 3 publications

(3 citation statements)

References 4 publications

(5 reference statements)

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“…In other words, the previously reported PK parameter values of tiropramide were similar to our PK results obtained by NCA analysis. After oral administration of 100 mg of tiropramide in humans, the obtained NCA PK parameters (as previously reported values) were 2.34-6.99 h for t 1/2 , 0.66-1.6 h for T max , 77.4-111 ng/mL for C max , and 267.7-812.7 h•ng/mL for AUC [6,12,[18][19][20][21]. On the other hand, the NCA PK parameters in this study were 3.41 ± 1.99 h for t 1/2 , 1.74 ± 0.63 h for T max , 69.07 ± 59.74 ng/mL for C max , and 280.34 ± 199.96 h•ng/mL for AUC, which were similar to the previously reported values.…”

Section: Discussionsupporting

confidence: 79%

Population Pharmacokinetic Analysis of Tiropramide in Healthy Korean Subjects

et al. 2020

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The purpose of this study was to perform population pharmacokinetic (PPK) analysis of tiropramide in healthy Korean subjects, as well as to investigate the possible effects of various covariates on pharmacokinetic (PK) parameters of tiropramide. Although tiropramide is commonly used in digestive system-related diseases as an antispasmodic, PPK reporting and factors affecting PKs are not clearly reported. Thus, this study for healthy subjects is very significant because it could find new covariates in patients that had not been reported before or predict PPK for patients in the clinic by establishing PPK in healthy adults. By using Phoenix NLME, PK, demographic, and genetic data (collected to explain PK diversity of tiropramide in population) analyses were performed. As a basic model, a one-compartment with first-order absorption and lag-time was established and extended to include covariates that influenced the inter-subject variability. The total protein significantly influenced the distribution volume and systemic clearance of tiropramide, but genetic factors such as ABCB1 (1236C>T, 2677G>T/A, and 3435C>T), CYP2D6 (*1 and *10), OCT2 (808G>T), and PEPT1 (1287G>C) genes did not show any significant association with PK parameters of tiropramide. The final PPK model of tiropramide was validated, and suggested that some of the PK diversity in the population could be explained. Herein, we first describe the establishment of the PPK model of tiropramide for healthy Korean subjects, which may be useful as a dosing algorithm for the diseased population.

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Section: Discussionsupporting

confidence: 79%

Population Pharmacokinetic Analysis of Tiropramide in Healthy Korean Subjects

et al. 2020

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“…It is used as a synthetic antispasmodic drug derived from tyrosine amino acid, which is devoid of atropine like actions and acts on smooth muscular bro cells, however avoiding, atony since it does not bind itself to calmodulin. This drug shows its therapeutic activity by predominantly increasing Ca 2+ in ux and cAMP concentration in smooth muscle possibly because of inhibition of cAMP catabolism to a lesser extent [1].Some analytical methods were reported in the literature for the determination of tiropramide in plasma [2,3] and its metabolite pro ling [4]. No information is available on stress studies of this drug substance.…”

Section: Introductionmentioning

confidence: 99%

“…This drug exhibits its therapeutic activity by predominantly increasing Ca 2+ influx and cyclic adenosine monophosphate (cAMP) concentration in smooth muscles possibly because of the inhibition of cAMP catabolism to a lesser extent (Tsutomu et al, 1992). Some analytical methods were reported in the literature for the determination of tiropramide in plasma (Imran et al, 2007; Lee et al, 2003) and its metabolite profiling (Arigoni et al, 1988). No information is available on the stress studies of this drug substance.…”

Section: Introductionmentioning

confidence: 99%

Chromatographic separation of tiropramide hydrochloride and its degradation products along with their structural characterization using liquid chromatography quadrupole time‐of‐flight tandem mass spectrometry and nuclear magnetic resonance

Tidke

Golla

Kushwah

et al. 2023

Biomedical Chromatography

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Tiropramide HCl, an antispasmodic drug is subjected to various stress conditions (hydrolytic, oxidative, photolytic and thermal) as per ICH guidelines. The drug is widely used as an antispasmodic agent but there were no comprehensive degradation studies reported on it. Hence, forced degradation studies of tiropramide HCl were carried out to establish the degradation pro le and the storage conditions to maintain its quality attributes during the shelf life and usage. A selective HPLC method was developed to separate the drug as well as all of its degradation products using Agilent C18 (250×4.6 mm; 5 µm) column. The mobile phase of 10mM ammonium formate at pH 3.6 (solvent A) and methanol (solvent B) with gradient elution at a ow rate of 1.00 mL/min was used. Tiropramide was susceptible to acidic, basic hydrolytic exposure and oxidative stress conditions in the solution. This drug was found to be stable in neutral, thermal and photolytic conditions in both solution and solid-state. Five degradation products were detected under different stress conditions. The mass spectrometric fragmentation pattern of tiropramide and its degradation products was extensively studied using LC-Q-TOF-MS/MS for their structural characterization. The position of the oxygen atom in the N-oxide degradation product was con rmed by NMR studies. The knowledge gained by these studies was used to predict drug degradation pro les which is helpful in the development of the dosage form.

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Chromatographic separation of tiropramide hydrochloride and its degradation products along with their structural characterization using LC-QTOF-MS/MS and NMR

Tidke¹,

Golla²,

Kushwah³

et al. 2022

Preprint

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Tiropramide HCl, an antispasmodic drug is subjected to various stress conditions (hydrolytic, oxidative, photolytic and thermal) as per ICH guidelines. The drug is widely used as an antispasmodic agent but there were no comprehensive degradation studies reported on it. Hence, forced degradation studies of tiropramide HCl were carried out to establish the degradation profile and the storage conditions to maintain its quality attributes during the shelf life and usage. A selective HPLC method was developed to separate the drug as well as all of its degradation products using Agilent C18 (250×4.6 mm; 5 µm) column. The mobile phase of 10mM ammonium formate at pH 3.6 (solvent A) and methanol (solvent B) with gradient elution at a flow rate of 1.00 mL/min was used. Tiropramide was susceptible to acidic, basic hydrolytic exposure and oxidative stress conditions in the solution. This drug was found to be stable in neutral, thermal and photolytic conditions in both solution and solid-state. Five degradation products were detected under different stress conditions. The mass spectrometric fragmentation pattern of tiropramide and its degradation products was extensively studied using LC-Q-TOF-MS/MS for their structural characterization. The position of the oxygen atom in the N-oxide degradation product was confirmed by NMR studies. The knowledge gained by these studies was used to predict drug degradation profiles which is helpful in the development of the dosage form.

show abstract

A simple sample preparation with HPLC–UV method for estimation of tiropramide from plasma: Application to bioequivalence study

Cited by 3 publications

References 4 publications

Population Pharmacokinetic Analysis of Tiropramide in Healthy Korean Subjects

Population Pharmacokinetic Analysis of Tiropramide in Healthy Korean Subjects

Chromatographic separation of tiropramide hydrochloride and its degradation products along with their structural characterization using liquid chromatography quadrupole time‐of‐flight tandem mass spectrometry and nuclear magnetic resonance

Chromatographic separation of tiropramide hydrochloride and its degradation products along with their structural characterization using LC-QTOF-MS/MS and NMR

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