The Bioavailability of Allergens in Allergy Tablets Depends on Several Factors

Mascarell, Laurent; Batard, Thierry; Cuiné, Jean; Nony, Emmanuel

doi:10.1159/000486960

Cited by 6 publications

(7 citation statements)

References 10 publications

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“…Characteristic 1-grass pollen SLIT tablet 5-grass pollen SLIT tablet Administration [4,5] Perennial Pre-/coseasonal Dosing Optimal [8,9] Licensed [4,5] Not determined 75,000 SQ-T 300 IR 300 IR Tablet potency [7] 2,800 BAU 9,000 BAU Dissolution time in vitro [27,28] Physical disintegration of tablet To release ≥85% of allergenic activity 2 s 15 s…”

Section: Article Highlightsmentioning

confidence: 99%

“…The European Medicines Agency defines bioavailability as 'the rate and extent to which the active substance or active moiety is absorbed from a pharmaceutical form and becomes available at the site of action' [26]. Therefore, any rigorous assessment of allergen bioavailability from SLIT tablets should consider several parameters, including allergen content and release kinetics after tablet dissolution, the effect of salivary components on allergen degradation, and the extent of allergen uptake by epithelial cells and APCs in the sublingual mucosa [27].…”

Section: Tablet Dissolution and Allergen Releasementioning

confidence: 99%

“…Eur. 2.9.3 dissolution test for solid dosage forms, apparatus 4 flow-through cell [31]), ≥85% of total allergenic activity is shown to be released from 300 IR and 100 IR HDM and 5 grass SLIT tablets within 2 minutes (Figure 1) [27].…”

Section: Tablet Dissolution and Allergen Releasementioning

confidence: 99%

“…2.9.3 dissolution test for solid dosage forms, apparatus 4 flow-through cell [31]) was used to investigate the dissolution time of 6 replicate samples of the 300 IR or 100 IR HDM and 5 grass pollen SLIT tablets, and the amount of allergenic activity released at each time point was measured using an ELISA-based assayELISA, enzyme-linked immunosorbent assay; HDM, house dust mite; IR, index of reactivity; SLIT, sublingual immunotherapy. [27]. The kinetics of allergen uptake by APCs in the sublingual mucosa are dose-dependent up to the point of saturation, and therefore are an important contributor to allergen bioavailability [32].…”

Section: Tablet Dissolution and Allergen Releasementioning

confidence: 99%

“…Such effects are difficult, if not impossible, to model and assess using in vitro dissolution assays. For these reasons, although differences in dissolution times can be demonstrated using in vitro dissolution assays, these cannot serve as a surrogate of bioavailability, because they lack any direct correlation with an in vivo sustained effect [27].…”

Section: Tablet Dissolution and Allergen Releasementioning

confidence: 99%

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Clinical efficacy of sublingual immunotherapy tablets for allergic rhinitis is unlikely to be derived from in vitro allergen-release data

Canonica

Devillier

Casale

et al. 2019

Expert Review of Clinical Immunology

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Introduction: Allergen bioavailability underpins the efficacy and safety of SLIT tablets. Three productrelated factors are likely to influence this: tablet potency, formulation and sublingual holding time. Areas covered: Tablet formulation determines the rate and extent of solubilized allergen release. Using validated in vitro dissolution assays, the two licensed grass pollen SLIT tablets are shown to release ≥85% of their total allergenic activity within several minutes. Sublingual holding time affects the contact duration between solubilized allergens and sublingual tissue. Maximal uptake of allergens by sublingual tissue requires~5 minutes, with little uptake occurring within the first minute. A higher potency tablet with longer sublingual holding time would provide higher bioavailability, while faster rates of allergen release in vitro are unlikely to translate to a greater increase in bioavailability. Differences in dissolution times cannot serve as a surrogate of in vivo bioavailability, and are not related to differences in efficacy at the marketed tablet dosages. Rapid in vitro dissolution is likely not a key requirement for inducing a potent immune response. Expert opinion: In vitro dissolution cannot predict the clinical efficacy of SLIT tablets but could be important in immune tolerance and safety. In addition, a discontinuous administration regimen may have benefits for adherence and cost without compromising efficacy.

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Section: Article Highlightsmentioning

confidence: 99%

Section: Tablet Dissolution and Allergen Releasementioning

confidence: 99%

Section: Tablet Dissolution and Allergen Releasementioning

confidence: 99%

Section: Tablet Dissolution and Allergen Releasementioning

confidence: 99%

Section: Tablet Dissolution and Allergen Releasementioning

confidence: 99%

See 3 more Smart Citations

Clinical efficacy of sublingual immunotherapy tablets for allergic rhinitis is unlikely to be derived from in vitro allergen-release data

Canonica

Devillier

Casale

et al. 2019

Expert Review of Clinical Immunology

Self Cite

View full text Add to dashboard Cite

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Allergen-Immuntherapie bei Hausstaubmilben-assoziierter allergischer Rhinitis: Wirksamkeit der 300 IR-Milbentablette

Klimek¹,

Casper²,

Klimek³

et al. 2023

Allergo J

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Allergen immunotherapy in house dust mite-associated allergic rhinitis: efficacy of the 300 IR mite tablet

et al. 2023

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Background A perennial house dust mite-associated allergic rhinitis has a major impact on the quality of life of patients and is associated with a high socioeconomic burden. The most common symptoms of allergic rhinitis include a runny nose and nasal congestion, sneezing, itching of nose, mouth and/or throat, and/or ocular symptoms. Affected patients often develop allergic bronchial asthma. Therapy options for allergic rhinitis include allergen avoidance, symptomatic treatment, and allergen immunotherapy. Allergen immunotherapy is the only disease-modifying treatment that can permanently alleviate the symptoms of allergic rhinitis. In July 2021, a new sublingual mite tablet was approved in Germany. Methods This review summarizes clinical studies on the 300 IR (index of reactivity) mite tablet in adolescents and adults with house dust mite-associated allergic rhinitis and presents the results. Results In the phase II and phase III studies considered here, different dosages of the mite tablet were investigated. The 300 IR mite tablet showed the best benefit–risk profile and has been approved in Europe, Japan, South Korea, Australia, and New Zealand for the treatment of house dust mite-associated allergic rhinitis. Conclusion Allergen immunotherapy with the 300 IR mite tablet is an effective treatment that relieves allergic symptoms, reduces the need for symptomatic medication, and improves the quality of life in both adults and adolescents with house dust mite-associated allergic rhinitis. At the same time, treatment with the 300 IR mite tablet is well tolerated. Mild to moderate reactions at the application site subside after a few days.

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The Bioavailability of Allergens in Allergy Tablets Depends on Several Factors

Cited by 6 publications

References 10 publications

Clinical efficacy of sublingual immunotherapy tablets for allergic rhinitis is unlikely to be derived from in vitro allergen-release data

Clinical efficacy of sublingual immunotherapy tablets for allergic rhinitis is unlikely to be derived from in vitro allergen-release data

Allergen-Immuntherapie bei Hausstaubmilben-assoziierter allergischer Rhinitis: Wirksamkeit der 300 IR-Milbentablette

Allergen immunotherapy in house dust mite-associated allergic rhinitis: efficacy of the 300 IR mite tablet

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