A sensitive and high-throughput LC-ESI-MS/MS method to detect budesonide in human plasma: application to an evaluation of pharmacokinetics of budesonide intranasal formulations with and without charcoal-block in healthy volunteers

Li, Xin; Tong, Huan; Xu, Bing; Deng, Yang; Li, Yuan; Huang, Junchen; Mao, Yong; Liu, Mengqin; Zhang, Ping; Guo, Siwei

doi:10.1080/03639045.2021.1879842

Cited by 3 publications

(3 citation statements)

References 24 publications

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“…The PK results showed that the difference between AUC with or without active charcoal block was very small (<10%), suggesting that the major systemic absorption of budesonide comes from the nasal mucosa. 18 The PK parameters of the present study were close to the data from a previous study, whether using charcoal or not. The t max was very similar, while AUC 0-t and C max were both slightly higher, and this may be due to a more skilled operation of drug administration.…”

Section: Discussionsupporting

confidence: 87%

“…In our previous 4‐period and 2‐sequence (TRTR or RTRT) study that was conducted in 12 healthy Chinese subjects, charcoal was used in the last 2 periods to block potential gastrointestinal tract absorption. The PK results showed that the difference between AUC with or without active charcoal block was very small (<10%), suggesting that the major systemic absorption of budesonide comes from the nasal mucosa 18 . The PK parameters of the present study were close to the data from a previous study, whether using charcoal or not.…”

Section: Discussionsupporting

confidence: 84%

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Pharmacokinetics and Bioequivalence of a Generic and a Branded Budesonide Nasal Spray in Healthy Chinese Subjects

et al. 2021

Clinical Pharm in Drug Dev

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The aim of this study was to evaluate the pharmacokinetic bioequivalence of a generic budesonide nasal spray and a branded product in healthy Chinese subjects under fasting condition. A single-center, single-dose, randomized, open-label, crossover study was conducted in 32 healthy Chinese subjects under fasting condition. The subjects were administered 256 μg of generic budesonide nasal spray (test drug) or branded budesonide nasal spray (RHINOCORT AQUA,reference drug), respectively. For each period, the subjects were administered with 64 μg of budesonide per spray and 2 sprays for each nostril followed by a washout period of 7 days. Plasma concentration of budesonide was determined by a validated high-performance liquid chromatography-tandem mass spectrometry method. The pharmacokinetic (PK) parameters were calculated, and the bioequivalence was compared using the noncompartment model with the Phoenix WinNonlin 7.0 program. Results show that the 90% confidence intervals of the test/reference ratios of maximum concentration, area under the plasma concentration-time curve from time 0 to the last measurable concentration, and area under the plasma concentration-time curve from time 0 to infinity for the budesonide concentration were 84.8% to 102.7%, 84.6% to 94.4%, and 85.4% to 95.2%, respectively, all fall within the bioequivalent range of 80% to 125%. The test and reference budesonide nasal sprays were PK bioequivalents in healthy Chinese subjects with comparable PK parameters. No serious adverse events were reported, and the 2 products have a good and similar safety profile.

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Section: Discussionsupporting

confidence: 87%

Section: Discussionsupporting

confidence: 84%

Pharmacokinetics and Bioequivalence of a Generic and a Branded Budesonide Nasal Spray in Healthy Chinese Subjects

et al. 2021

Clinical Pharm in Drug Dev

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“…In the last two decades, several research groups have developed in-house validated LC-MS/MS methods for the quantification of synthetic glucocorticoids in serum for clinical applications. Most of published research works dealing with therapeutic drug monitoring and pharmacokinetic studies describe LC-MS/MS methods aiming at the monitoring of a single exogenous compound (e.g., betamethasone, beclomethasone dipropionate, budesonide, prednisone and prednisolone), eventually also measuring within the same analysis relative target metabolites and/or circulating F [20][21][22][23]. A few examples of extended panels were also described: Taylor et al [24] set up a 15 min LC-MS/MS method for the detection and quantification of 15 exogenous corticoids (including Dex) plus F to be applied to both serum and urine samples, as well as to tablet extracts; and Methlie et al [25] developed a sensitive method that is capable of measuring serum concentrations of Dex, prednisone and prednisolone together with a small panel of clinically relevant steroid hormones.…”

Section: Introductionmentioning

confidence: 99%

Simultaneous Measurement of Cortisol, Cortisone, Dexamethasone and Additional Exogenous Corticosteroids by Rapid and Sensitive LC–MS/MS Analysis

Ponzetto

Parasiliti-Caprino

Settanni³

et al. 2022

Molecules

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The simultaneous measurement of dexamethasone and cortisol has proven the ability to increase the diagnostic performance of the overnight dexamethasone-suppression test. Furthermore, the therapeutic drug monitoring of administered corticosteroid drugs could represent a crucial tool for investigating unexpected variations of steroid hormones’ circulating levels. In this work, an LC–MS/MS method for the quantification of cortisol, cortisone, dexamethasone and six additional exogenous corticosteroids in the serum/plasma matrix was developed and validated in compliance with the ISO/IEC requirements. To assess the efficiency of the validated method, serum samples of 75 patients undergoing the dexamethasone-suppression test and 21 plasma samples of patients under immunosuppressive treatment after kidney transplant were analyzed. In all dexamethasone-suppression test samples, it was possible to measure the circulating levels of cortisol, cortisone and dexamethasone. Concentrations of the latter were for all tested patients above the proposed cutoff for the dexamethasone-suppression test’s results, and the cortisol concentrations showed good correlation with the ones measured by routine immunometric analysis, therefore confirming the screening outcome for all enrolled patients. Prednisone was detected and quantified in all enrolled patients, confirming the use of such a corticosteroid for immunosuppressive therapy. Thanks to these two applications, we proved the overall performance of the developed LC–MS/MS method for four target analytes. The future implementation of such an analytical tool in the clinical biochemistry laboratory’s routine will guarantee a single and versatile tool for simultaneously monitoring dexamethasone-suppression-test results and corticosteroid drugs’ administration.

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Design, Development and In vivo Evaluation of Core in Cup Tablets of Budesonide

Parija¹,

Mohanta

Nanda³

et al. 2022

RJPT

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Budesonide is widely used drug for treatment of active inflammatory bowel disease (IBD). Core in-cup tablets were prepared to achieve a prolonged release of Budesonide and for alleviating the symptoms of inflammatory bowel disease. The objective of this study was to investigate differences in the pharmacokinetic patterns between an optimized core in cup tablet formulation and pure Budesonide suspension. In-vivo evaluation studies were performed based on the uniform and reliable results of in-vitro drug release studies. Various pharmacokinetic parameters were compared to obtain mean plasma drug concentration curve versus time. The pure drug suspension and Core-in-cup tablets formulation of Budesonide were administered to two groups of white New Zealand rabbits (n=6) through the oral route following cross over design pattern. The drug concentration in plasma samples were measured using LC-MS/MS method. Pharmacokinetic parameters were determined for each formulation. The comparison of the plasma time curves of the dosage forms showed that each dosage form caused significant differences in the drug plasma levels. The optimized core in cup tablet formulation shown some lag phase initially before releasing the drug. The mean residence time of core in cup tablet formulation was found to be more than the pure drug suspension formulation. The oral administration of Budesonide resulted in a low and quite variable AUC of 154.1±1.44 ng/ml/hr., whereas the optimized core-in-cup tablets resulted in AUC of 918.2±3.11 ng/ml/hr. The bioavailability of optimized formulation was enhanced six times compared with pure drug suspension. From the above results, it can be concluded that the prepared core in cup tablet can be considered as one of the promising formulation techniques for chronotherapeutic management of inflammatory bowel disease.

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A sensitive and high-throughput LC-ESI-MS/MS method to detect budesonide in human plasma: application to an evaluation of pharmacokinetics of budesonide intranasal formulations with and without charcoal-block in healthy volunteers

Cited by 3 publications

References 24 publications

Pharmacokinetics and Bioequivalence of a Generic and a Branded Budesonide Nasal Spray in Healthy Chinese Subjects

Pharmacokinetics and Bioequivalence of a Generic and a Branded Budesonide Nasal Spray in Healthy Chinese Subjects

Simultaneous Measurement of Cortisol, Cortisone, Dexamethasone and Additional Exogenous Corticosteroids by Rapid and Sensitive LC–MS/MS Analysis

Design, Development and In vivo Evaluation of Core in Cup Tablets of Budesonide

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