Single-dose pharmacokinetics of sublingual versus oral administration of micronized 17-estradiol

Price, Thomas M.; Blauer, Keith L.; Hansen, M.A.; Stanczyk, Frank Z.; Løbo, Rogerio A.; Bates, G W

doi:10.1016/s0029-7844(96)00513-3

Cited by 67 publications

(38 citation statements)

References 18 publications

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“…Interest in the sublingual route as a readily accessible and non-invasive route of administration has been increasing recently for a wide range of medications [13][14][15][27][28][29][30]. The high vascularity of the sublingual mucosa facilitates rapid drug absorption directly into the venous circulation through the sublingual and frenular veins, bypassing the gastrointestinal tract, the hepatic portal circulation and hepatic first-pass metabolism.…”

Section: Discussionmentioning

confidence: 99%

Epinephrine for the treatment of anaphylaxis: do all 40 mg sublingual epinephrine tablet formulations with similar in vitro characteristics have the same bioavailability?

Rawas‐Qalaji

Simons

2006

Biopharm & Drug Disp

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Epinephrine autoinjectors are underutilized in the first aid emergency treatment of anaphylaxis in the community; so non-invasive sublingual epinephrine administration is being proposed. In order to determine the effect of changing excipients on the bioavailability of sublingual epinephrine, four distinct fast-disintegrating epinephrine 40 mg tablet formulations, A, B, C and D, were manufactured using direct compression. All formulations were evaluated for tablet hardness (H), disintegration time (DT) and wetting time (WT). In a prospective 5-way crossover study, four sublingual formulations and epinephrine 0.3 mg i.m. as a control were tested sequentially in a validated rabbit model. Blood samples were collected before dosing and at intervals afterwards. Epinephrine plasma concentrations were measured using HPLC-EC. All tablet formulations met USP standards for weight variation and content uniformity, and resulted in similar mean H, DT and WT (n=6). The area under the curve (AUC), maximum concentration (C(max)) and time at which C(max) was achieved (T(max)) did not differ significantly after the sublingual administration of formulation A and epinephrine 0.3 mg i.m. The AUC after B, C and D were significantly lower (p<0.05) than after epinephrine 0.3 mg i.m. These results suggest that the selection of excipients used in these tablet formulations can affect the bioavailability of sublingually administered epinephrine.

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Section: Discussionmentioning

confidence: 99%

Epinephrine for the treatment of anaphylaxis: do all 40 mg sublingual epinephrine tablet formulations with similar in vitro characteristics have the same bioavailability?

Rawas‐Qalaji

Simons

2006

Biopharm & Drug Disp

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“…It has been a developing field in the administration of many vitamins and minerals which are found to be readily and thoroughly absorbed by this method [2].…”

Section: Introductionmentioning

confidence: 99%

Sublingual Drug Delivery: An Indication of Potential Alternative Route

Saha

Verma

Das

2017

Int J Curr Pharm Sci

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Sublingual literally meaning is "under the tongue", refers to a method of administrating substance via mouth in such a way that the substance is rapidly absorbed via blood vessels under tongue. Sublingual route is useful when a rapid onset of action is desired with better patient compliance than orally ingested tablets. Drugs that are given sublingually reach directly into the systemic circulation through the ventral surface of the tongue and floor of the mouth. The portion of drug absorbed through the sublingual blood vessels bypasses the hepatic first-pass metabolic processes giving acceptable bioavailability. As nowadays most of the people need effective relief within a short period of time so sublingual is the most suitable form of administration. New sublingual technologies address many pharmaceutical and patient needs, ranging from enhanced life-cycle management to convenient dosing for paediatric, geriatric, and psychiatric patients with dysphagia.

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“…The drug can then be absorbed partially or entirely into the systemic circulation from blood vessels in the sublingual mucosa, or it can be swallowed as a solution to be absorbed from the gastrointestinal tract [3][4][5].…”

Section: Introductionmentioning

confidence: 99%

Formulation and evaluation of taste masked Amlodipine Besylate Fast-dissolving Sublingual Tablets

Thulluru¹,

Venkatesh²,

Chowdhary³

et al. 2017

IJRDPL

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Single-dose pharmacokinetics of sublingual versus oral administration of micronized 17-estradiol

Abstract: Sublingual administration of micronized 17 beta-estradiol results in a rapid, burst-like absorption into the systemic circulation, yielding high E2 levels that fall rapidly over the first 6 hours.

Cited by 67 publications

References 18 publications

Epinephrine for the treatment of anaphylaxis: do all 40 mg sublingual epinephrine tablet formulations with similar in vitro characteristics have the same bioavailability?

Epinephrine for the treatment of anaphylaxis: do all 40 mg sublingual epinephrine tablet formulations with similar in vitro characteristics have the same bioavailability?

Sublingual Drug Delivery: An Indication of Potential Alternative Route

Formulation and evaluation of taste masked Amlodipine Besylate Fast-dissolving Sublingual Tablets

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