An Investigation into the Influence of Experimental Conditions on In Vitro Drug Release from Immediate-Release Tablets of Levothyroxine Sodium and Its Relation to Oral Bioavailability

Kocic, Ivana; Homšek, Irena; Dačević, Mirjana; Parojčić, Jelena; Miljković, Branislava

doi:10.1208/s12249-011-9660-8

Cited by 13 publications

(11 citation statements)

References 30 publications

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“…However, the dissolution time does not fully explain the subsequent absorption rate. In fact, Kocic et al (119) have shown that the dissolution rate and the absorption rate in the first two hours may diverge, indicating that dissolution does not greatly influence the absorption of levothyroxine in the period of time (1.66 hours) in which the maximal absorption take place (37). Noticeably, a better absorption of thyroxine has been observed in patients simultaneously taking vitamin C (120, 121) which may lower gastric pH in patients with impaired acid secretion (109).…”

Section: Drugs Interference At Gastric Levelmentioning

confidence: 99%

Gastrointestinal Malabsorption of Thyroxine

et al. 2018

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at the modification stage), and do not reflect editorial changes. No corrections/changes to the PDF manuscripts are accepted. Accordingly, there likely will be differences between the Advance Article manuscripts and the final, typeset articles. The manuscripts remain listed on the Advance Article page until the final, typeset articles are posted. At that point, the manuscripts are removed from the Advance Article page. DISCLAIMER: These manuscripts are provided "as is" without warranty of any kind, either express or particular purpose, or non-infringement. Changes will be made to these manuscripts before publication. Review and/or use or reliance on these materials is at the discretion and risk of the reader/user. In no event shall the Endocrine Society be liable for damages of any kind arising references to, products or publications do not imply endorsement of that product or publication.

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Section: Drugs Interference At Gastric Levelmentioning

confidence: 99%

Gastrointestinal Malabsorption of Thyroxine

et al. 2018

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“…This bioequivalence study was divided into 2 separate trials in which the timing of drug administration differed: fasting administration and postprandial administration. In both trials, a single‐center, randomized, open‐label, single‐dose, 2‐formulation, 2‐period, 2‐sequence crossover design, and a 14‐day washout period were adopted 9 …”

Section: Methodsmentioning

confidence: 99%

Pharmacokinetics, Bioequivalence, and Safety Studies of Pantoprazole Sodium Enteric‐Coated Tablets in Healthy Subjects

Chen¹,

Gan

Rao

et al. 2020

Clinical Pharm in Drug Dev

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This study aimed to evaluate the bioequivalence of 2 pantoprazole sodium enteric‐coated tablet formulations, a generic formulation and a branded formulation, and to investigate their pharmacokinetic and safety profiles. The study was designed as a single‐center, randomized, open‐label, single‐dose, dual‐period, and 2‐sequence crossover trial, and was divided into fasting and postprandial human bioequivalence trials. In the first trial, 36 subjects were fasted overnight before they were given generic or branded tablets (during 2 separate administration periods). Separately, 42 subjects were provided a high‐fat meal 1 hour before the drugs were administered. Blood specimens of each subject were obtained up to 24 hours after drug administration. No significant differences were observed between the pharmacokinetic profiles of the generic and branded pantoprazole sodium enteric‐coated tablets. Bioequivalence was evaluated using 90% confidence intervals for the ratio of test/reference log area under the concentration‐time curve over 24 hours, log area under the concentration‐time curve to infinity (AUC0‐∞), and log peak concentration (Cmax). The 90% confidence intervals of the least squares geometric mean ratio of Cmax, area under the concentration‐time curve from time zero to the last measurable concentration (AUC0‐t), and AUC0‐∞ of 36 subjects in the fasting trial and of 40 of 41 subjects in the postprandial trial (Cmax [41], AUC0‐t [41], and AUC0‐∞ [40]) were in accordance with the bioequivalence criteria. No severe adverse effects were detected. The generic and branded pantoprazole sodium enteric‐coated tablets were considered bioequivalent with similar safety profiles.

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“…Based on the solubility and the permeability rates high or low, drugs are in fact classified into one of four categories of the BCS. This has been proven difficult for levothyroxine sodium since there are sources classifying it as belonging to each of the abovementioned classes ( 26 , 27 ). Interestingly, also the formation of large aggregates in aqueous media may enable the compound to reach concentration even higher than 15 mg/100 ml ( 26 ).…”

Section: Levothyroxine Structurementioning

confidence: 99%

Levothyroxine Therapy in Gastric Malabsorptive Disorders

et al. 2021

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Oral levothyroxine sodium is absorbed in the small intestine, mainly in the jejunum and the ileum being lower the absorption rate at duodenal level. The time interval between the ingestion of oral thyroxine and its appearance in the plasma renders unlike a gastric absorption of the hormone. However, several evidence confirm the key role of the stomach as a prerequisite for an efficient absorption of oral levothyroxine. In the stomach, in fact, occur key steps leading to the dissolution of thyroxine from the solid form, the process bringing the active ingredient from the pharmaceutical preparation to the aqueous solution. In particular, gastric juice pH, volume, viscosity, as well as gastric emptying time seem to be the most important limiting factors. These hypotheses are confirmed by the detection of an increased need for levothyroxine in patients with Helicobacter pylori infection, chronic atrophic gastritis, gastroparesis, or in simultaneous treatment with drugs interfering with gastric acidic output. The aim of the present article is to focus on the knowledge of pathophysiologic events that determine the absorptive fate of traditional (tablet) and alternative thyroxine preparations (softgel capsule and liquid solution) in patients bearing gastric disorders.

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An Investigation into the Influence of Experimental Conditions on In Vitro Drug Release from Immediate-Release Tablets of Levothyroxine Sodium and Its Relation to Oral Bioavailability

Cited by 13 publications

References 30 publications

Gastrointestinal Malabsorption of Thyroxine

Gastrointestinal Malabsorption of Thyroxine

Pharmacokinetics, Bioequivalence, and Safety Studies of Pantoprazole Sodium Enteric‐Coated Tablets in Healthy Subjects

Levothyroxine Therapy in Gastric Malabsorptive Disorders

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