Levothyroxine Sodium Pentahydrate Tablets – Formulation Considerations

Kaur, Navpreet; Suryanarayanan, Raj

doi:10.1016/j.xphs.2021.08.006

“…Due to the slow progression of thyroid cancer and the low degree of malignancy, it has been reported that palliative treatment with thyroid hormones after tumor resection could achieve favorable results [ 16 ]. However, prior research has shown that most recurrence and metastasis occur within 5 years after surgery [ 17 , 18 ], which was similar to the results of the present study. In the present study, the results showed that the total effective rate of the control group was significantly higher than that of the observation group; there was no significant difference in cancer recurrence and metastasis rate between the control group and the observation group one year after operation; the cancer recurrence and metastasis rates of the control group at 3 years and 5 years after surgery were significantly lower than those in the observation group; there was no significant difference in the survival rate of 3-year after surgery; the 5-year survival rate in the control group was significantly higher than that in the observation group.…”

Section: Discussionsupporting

confidence: 92%

“…These results indicated that active postoperative treatment measures are essential for patients with thyroid cancer to reduce the risk of cancer recurrence and metastasis and improve their long-term survival. This also shows that levothyroxine tablets combined with iodine-131 therapy significantly improve the clinical treatment efficiency of patients and lower the risk of cancer recurrence and metastasis [ 17 ], thereby improving the long-term survival of patients [ 18 , 19 ]. TgAb is an inhibitory autoimmune antibody produced by Tg.…”

Section: Discussionmentioning

confidence: 99%

Effectiveness and Safety of Levothyroxine Tablets Combined with Iodine-131 in the Treatment of Thyroid Cancer

Bai

¹

,

Jin

²

,

Liu

³

et al. 2022

Journal of Oncology

1

0

View full text Add to dashboard Cite

Objective. To explore the effectiveness of levothyroxine tablets combined with iodine-131 in thyroid cancer patients after radical thyroidectomy and the effect on their serum thyroglobulin (Tg) and thyroglobulin antibody (TgAb) levels. Methods. A total of 70 thyroid cancer patients receiving radical thyroidectomy in our hospital from July 2015 to April 2016 were recruited and were assigned via different treatment methods (1 : 1) to receive either levothyroxine tablets (observation group) or levothyroxine tablets plus iodine-131 (control group). Outcome measures included treatment efficiency, 1, 3, and 5-year recurrence and metastasis, serum Tg and TgAb levels, postoperative survival, and adverse reactions. Results. The total effective rate of treatment in the control group was significantly higher than that in the observation group ( P < 0.05 ). There was no significant difference in cancer recurrence and metastasis rate between the two groups one year postoperatively ( P > 0.05 ). The rate of cancer recurrence and metastasis in the control group was significantly lower than that in the observation group 3 and 5 years after surgery ( P < 0.05 ). Before treatment, there was no significant difference in serum Tg and TgAb levels between the two groups ( P > 0.05 ). After treatment, serum Tg and TgAb levels decreased in both groups, with lower results in the control group ( P < 0.05 ). There was no significant difference in the 1 and 3-year survival rates between the two groups ( P > 0.05 ). The 5-year survival rate in the control group was significantly higher than that in the observation group ( P < 0.05 ). There was no significant difference in adverse reactions between the two groups ( P > 0.05 ). Conclusion. Levothyroxine tablets combined with iodine-131 for thyroid cancer patients undergoing radical thyroidectomy effectively could improve the treatment efficiency, reduce the risk of cancer recurrence and metastasis after surgery, lower the serum Tg and TgAb levels of patients, and prolong the survival of patients, with a high safety profile. Further trials are, however, required prior to clinical promotion.

show abstract

“…The main component of levothyroxine sodium tablets is levothyroxine sodium [ 13 ] which is currently mostly used in the treatment of non-toxic goiter [ 14 ], post-thyroidectomy suppressive therapy, and adjuvant therapy of hyperthyroidism [ 15 ]. The synthetic levothyroxine it contains is identical to the thyroxine naturally secreted by the thyroid gland and is converted to T3 in peripheral organs, which then exerts its specific effects by binding to T3 receptors [ 16 ].…”

Section: Introductionmentioning

confidence: 99%

Clinical Efficacy of Levothyroxine Sodium plus I 131 in the Treatment of Patients with Thyroidectomy and Its Effect on the Levels of Thyroglobulin and Thyrotropin

Pang

¹

,

Wang²,

Cheng

³

2022

Evidence-Based Complementary and Alternative Medicine

View full text Add to dashboard Cite

Objective. This study was to evaluate the clinical efficacy of levothyroxine sodium tablets combined with I 131 in the treatment of patients after thyroidectomy and the effect on thyroglobulin (Tg) and thyroid stimulating hormone (TSH) levels. Methods. 80 patients with differentiated thyroid cancer who required thyroidectomy after surgery between July 2019 and January 2021 were recruited for prospective study, 40 patients in the control group received levothyroxine sodium tablets, and 40 patients in the experimental group received levothyroxine sodium treatment plus I 131 treatment. Treatment effect, serum Tg and TSH levels, and relapse were measured. Results. The removal rate of residual thyroid tissue in the experimental group (87.50%) was significantly higher than that in the control group (57.50%) ( P < 0.05 ). Levothyroxine sodium tablets plus I 131 was associated with a significantly higher efficacy versus levothyroxine sodium tablets ( P < 0.05 ). There were no significant differences in the serum Tg levels between the two groups before treatment ( P > 0.05 ). After treatment, the serum Tg levels in both groups were significantly decreased, and levothyroxine sodium tablets plus I 131 resulted in a significantly lower Tg level versus levothyroxine sodium tablets ( P < 0.05 ). Before treatment, the two groups showed similar TSH levels ( P > 0.05 ). After treatment, patients receiving levothyroxine sodium tablets plus I 131 had a significantly greater increase in the TSH levels versus levothyroxine sodium tablets ( P < 0.05 ). The recurrence rate of the experimental group was lower than that of the control group ( P < 0.05 ). Conclusion. Levothyroxine sodium tablets plus I 131 for post-operative patients with differentiated thyroid cancer enhance the removal rate of residual thyroid tissue, effectively reduce serum Tg level, and increase TSH level, with significant therapeutic effects, low recurrence rates, and a high safety profile.

show abstract

“…In the softgel LT4 preparation the active ingredient is dissolved in glycerol surrounded by a gelatin envelope ( 3 ). However, in vitro studies also demonstrated that the pH of the medium in which thyroxine is solubilized, is able to influence both the LT4 ionization and conformational status, determined by the relative orientation between the phenolic and the tyrosyl rings ( 30 , 31 ). The ionization status of the molecule leads also to the possible creation of aggregates affecting its solution behavior ( 31 ).…”

Section: Discussionmentioning

confidence: 99%

“…However, in vitro studies also demonstrated that the pH of the medium in which thyroxine is solubilized, is able to influence both the LT4 ionization and conformational status, determined by the relative orientation between the phenolic and the tyrosyl rings ( 30 , 31 ). The ionization status of the molecule leads also to the possible creation of aggregates affecting its solution behavior ( 31 ). To note, thyroxine molecule is an amphipathic compound, with a hydrophilic and a lipophilic part ( 7 , 32 ).…”

Section: Discussionmentioning

confidence: 99%

Daily requirement of softgel thyroxine is independent from gastric juice pH

Virili

¹

,

Capriello²,

Stramazzo³

et al. 2022

View full text Add to dashboard Cite

BackgroundSoftgel levothyroxine (LT4) preparation showed a better in vitro dissolution profile at increasing pH as compared to tablet LT4 preparation. Clinical studies suggested a better performance of softgel LT4 preparation in patients with gastric disorders but whether this finding is related to gastric juice pH variation in vivo is not known.MethodsTwenty-eight hypothyroid patients (24F/4M; median age=50 treated with tablet LT4 (median dose= 1.65 µg/kg/day) and with stable thyroid stimulating hormone (TSH) values on target (<0.8-2.5> mU/l) have been shifted to softgel LT4 preparation. The dose of softgel LT4 has been titrated to obtain a similar individual serum TSH value. All subjects followed a specific treatment schedule, taking LT4 in fasting condition and then abstaining from eating or drinking for at least 1 hour. Owing to the presence of long-lasting dyspepsia or of already known gastric disorders, all patients underwent endoscopy, upon informed consent. Gastric juice has been collected during endoscopy to measure gastric pH. Then we plotted the dose of LT4 with the gastric pH obtained in vivo, before and after the switch tablet/softgel preparation in all patients.ResultsUpon the switch tablet/softgel preparation, the therapeutic LT4 dose was very slightly reduced (-6%) in the whole sample. However, the individual variations revealed the existence of two populations, one without any dose reduction (A) and the other showing a dose reduction >20% (B). Upon matching with the actual gastric pH, patients with normal pH (A: n=17; 14F/3M, median 1.52) no showed a lower softgel LT4 requirement. Instead, among patients with reduced gastric acid production (B: n=11; 10F/1M, median pH 5.02) the vast majority (10/11; 91%, p<0.0001) benefited from a lower dose of softgel LT4 (median = -23%, p<0.0001). Interestingly, the dose of LT4 in tablet correlated with pH value (Spearman’s ρ =0.6409; p = 0.0002) while softgel dose was independent from gastric juice pH (Spearman’s ρ =1.952; p = 0.3194).ConclusionsThese findings provide evidence that softgel LT4 preparation is independent from the actual gastric pH in humans and may represent a significant therapeutic option in patients with increased LT4 requirement, owed to disorders impairing the gastric acidic output.

show abstract

Levothyroxine Sodium Pentahydrate Tablets – Formulation Considerations

Cited by 13 publications

References 209 publications

Effectiveness and Safety of Levothyroxine Tablets Combined with Iodine-131 in the Treatment of Thyroid Cancer

Effectiveness and Safety of Levothyroxine Tablets Combined with Iodine-131 in the Treatment of Thyroid Cancer

Clinical Efficacy of Levothyroxine Sodium plus I 131 in the Treatment of Patients with Thyroidectomy and Its Effect on the Levels of Thyroglobulin and Thyrotropin

Daily requirement of softgel thyroxine is independent from gastric juice pH

Contact Info

Product

Resources

About