Buffering the stomach content enhances the absorption of diflunisal in man

Nuernberg, Bernd; Brune, Kay

doi:10.1002/bdd.2510100405

Cited by 9 publications

(3 citation statements)

References 7 publications

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“…For quantification of acteylsalicylic acid (ASA) and salicylic acid (SA) an isocratic high performance liquid chromatographic ultraviolet-method was used, according to Amick and Mason [29], Nieder et al [30], see also [31]. The detection limits for ASA and SA were found to be less than 1 gg/ml.…”

Section: Materials and Methods For Determination Of Blood Plasma Levelsmentioning

confidence: 99%

Effects of pentazocine and acetylsalicylic acid on pain-rating, pain-related evoked potentials and vigilance in relationship to pharmakokinetic parameters

et al. 1990

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Achieving objective and quantitative measurement of experimental pain in human volunteers and establishing the impact of drugs remains a difficult task. This problem may be overcome by employing a method which allows the simultaneous measurement of pain ratings elicited by standardized stimulation of the nasal mucosa by carbon dioxide, together with pain-related chemo-somatosensory evoked potentials (CSSEP) and vigilance. We assessed the effect of pentazocine and acetylsalicylic acid on these parameters in 14 human volunteers and related the effects to the pharmacokinetic parameters of the drugs measured at the same time. Pentazocine was found to reduce the pain ratings as well as the amplitudes of the pain-related evoked potentials and to increase their latencies. Vigilance (measured by EEG power spectra and performance of a tracking task) was also significantly reduced. These effects were observed during the distribution phase and the first period of the terminal elimination phase of the drug. Acetylsalicylic acid had no significant effects on pain ratings, but reduced the amplitudes of the event-related potentials when compared to placebo controls. At the same time a slight, but significant, effect on vigilance (reduced performance of the tracking task) was observed. These effects could not be related to the presence of unmetabolized acetylsalicylic acid in the plasma. They appeared at later times when only salicylic acid was left. It is concluded that chemical stimuli of sufficient intensity produce pain which may be suppressed by opioid analgesics such as pentazocine. The effect of acetylsalicylic acid on this experimental pain did not reach significance for all measured parameters under the experimental conditions chosen. The changes in vigilance and in the amplitudes of pain-related chemo-somatosensory evoked potentials indicated as yet unknown CNS-effects of this non-steroidal anti-inflammatory drug.

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Section: Materials and Methods For Determination Of Blood Plasma Levelsmentioning

confidence: 99%

Effects of pentazocine and acetylsalicylic acid on pain-rating, pain-related evoked potentials and vigilance in relationship to pharmakokinetic parameters

et al. 1990

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“…Based on PubChem, the solubility of diflunisal is 14.5 mg/L at neutral or acidic pH, which is impractical to be formulated into a solution for oral desensitization. One study has shown that buffering gastric pH toward neutral using sodium bicarbonate has enhanced the absorption of diflunisal in addition to its bioavailability [10]. Hence, it was extrapolated that the solubility of diflunisal may be improved with the use of sodium bicarbonate as the solvent.…”

Section: Discussionmentioning

confidence: 99%

Successful Diflunisal Desensitization in a Transthyretin Amyloidosis Patient With Ibuprofen Allergy: A Case Report

Aw¹,

Low²,

Lim³

et al. 2022

PBR

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Background: Amyloid diseases are hereditary and include transthyretin (TTR) amyloidosis where subunit protein mutations may occur in genes for TTR, leading to the deposition of fibrils (low molecular weight subunits (5 to 25 KD of proteins) in extracellular tissues. By reducing the formation of TTR amyloid, diflunisal, a nonsteroidal anti-inflammatory drug, can preserve the quality of life and significantly reduce disease progression. We present a case of a 61-year-old male patient with a history of ibuprofen allergy, diagnosed with TTR amyloidosis, complicated with peripheral neuropathy, cardiac, and liver amyloid. He developed bilateral mild eye swelling from the ibuprofen oral provocation test. With a similar structural backbone of carboxylic acid, he could develop pseudoallergy to diflunisal with an unknown likelihood of developing an allergic reaction. Objectives: This study aims to design successful diflunisal desensitization in a patient with TTR amyloidosis. Methods: The patient underwent a 14-step diflunisal desensitization procedure using 2 tablets of diflunisal 500 mg that was dissolved in 40 mL of sodium bicarbonate 8.4% injection to create serial 10-fold dilutions. Oral desensitization was administered in the escalation of the doses at 30-min intervals, with a starting dose of 0.1 mg until a final dose of 250 mg was reached. Results: The patient tolerated diflunisal desensitization and was continued on diflunisal treatment without any evidence of an allergic reaction. Conclusion: Diflunisal desensitization can be considered in patients with a history of ibuprofen allergy if there are no available alternative treatments. To the best of our knowledge, this is the first article describing a patient with angioedema to ibuprofen who could tolerate oral diflunisal after desensitization.

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“…14  Reduced gastrointestinal irritation: By buffering the stomach acid, effervescent formulations might lessen the gastrointestinal irritation brought on by some drugs. 15  Improved portability: When compared to liquid dose forms, effervescent tablets are easier to store and transport because of their compact form. 10  Increased palatability: Flavouring agents are frequently used in the formulation of effervescent tablets to enhance their flavour and increase patient acceptability.…”

Section: Pros Of Effervescent Tabletsmentioning

confidence: 99%

A Comprehensive Review on Effervescent Tablets

Vanhere,

Derle,

Khatale

et al. 2023

J. Drug Delivery Ther.

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Effervescent tablets are becoming increasingly popular due to their ease of administration and rapid onset of action. They typically contain acidic materials and carbonates or bicarbonates that react quickly in the presence of water, releasing carbon dioxide and improving API solubility and flavour masking. However, effervescent tablets can be bulky, and the reaction rate is difficult to control due to water's catalytic effect. This article discusses the advantages and disadvantages of effervescent tablets, common effervescent reactions, active ingredients that can be formulated, and the preparation and manufacturing process. It also evaluates effervescent granules and tablets and explores the latest advancements in effervescent technology. Overall, effervescent tablets offer a promising option for drug delivery, and ongoing research will undoubtedly yield even more advanced formulations in the future. Keywords: Effervescent granules, Effervescent tablets, Hot melt granulation, Carbon dioxide content, Water activity

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Buffering the stomach content enhances the absorption of diflunisal in man

Cited by 9 publications

References 7 publications

Effects of pentazocine and acetylsalicylic acid on pain-rating, pain-related evoked potentials and vigilance in relationship to pharmakokinetic parameters

Effects of pentazocine and acetylsalicylic acid on pain-rating, pain-related evoked potentials and vigilance in relationship to pharmakokinetic parameters

Successful Diflunisal Desensitization in a Transthyretin Amyloidosis Patient With Ibuprofen Allergy: A Case Report

A Comprehensive Review on Effervescent Tablets

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