Endocrine Abstracts (2012) 29 P1626

A liquid formulation of L-thyroxine (L-T4) solves problems of incomplete normalization/suppression of serum TSH caused by proton pump inhibitors (PPI) on conventional tablet formulations of L-T4

G. Saraceno1, R. Vita1, F. Trimarchi1 & S. Benvenga1,2,3

1Policlinico Universitario, Messina, Italy; 2Università di Messina, Messina, Italy; 3A.O.U. Policlinico G. Martino, Messina, Italy.

Background: PPI are known to diminish the intestinal absorption of L-T4, which is commonly ingested as tablets of L-T4 sodium salt. However, a liquid formulation is available (Tirosint, oral solution, IBSA Farmaceutici Italia s.r.l., Italy), in which the hormone is solubilized in 28.8% ethyl alcohol. One ml of this formulation (=28 drops) contains 100 mcg L-T4 sodium salt in 243 mg ethanol. Because this formulation contains L-T4 (which is a lipophilic hormone) already solubilized in an organic solvent, as opposed to L-T4 contained in a powder within a tablet, there could be the advantage of virtually skipping the dissolution in the stomach, and subsequent quick, direct arrival of L-T4 in the upper intestine segments (duodenum, jejunum) where most of it is absorbed.

Patients & methods: Upon consent, 1 woman under replacement therapy [100–125 mcg/day] and 9 patients (7 women and 2 men) under TSH suppressive therapy [82–135 mcg/day], all 10 with PPI-induced malabsorption of LT4, were switched to Tirosint oral solution while maintaining the daily dose of L-T4 and continuing ingesting the PPI as before. The PPI were: lansoprazole, omeprazole or pantoprazole. Post-switch serum TSH was re-assayed after a minimum of 2 months.

Results: In the hypothyroid woman, TSH fell to 2.0–2.7 mU/L down from 5.0–7.3. In the other 9 patients, TSH fell to <0.01 to 1.97 mU/L (median: 0.10; mean ±SD: 0.68±0.91), down from 0.28–2.95 (median: 0.81; mean ±SD 1.02±0.74; P=0.0004 by ANOVA after log10-transformation), and with 65% of the post-switch TSH levels at 0.10 mU/L or below compared to 0% (zero%) of the pre-switch levels (P< 0.0001 by Fisher’s exact test).

Conclusion: The liquid formulation of L-T4 is an extremely effective means to circumvent the problem of incomplete absorption of the L-T4 caused by the PPI-induced increase of the gastric pH.

Declaration of interest: The authors declare that there is no conflict of interest that could be perceived as prejudicing the impartiality of the research project.

Funding: This research did not receive any specific grant from any funding agency in the public, commercial or not-for-profit sector

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