Absorption, Distribution and Excretion
Thiamine is primarily absorbed in the jejunum. At low concentrations, it is absorbed via an active transport system involving phosphorylation; at high concentrations, it is absorbed via passive diffusion. Only a small amount of high-dose thiamine is absorbed, and elevated serum concentrations lead to active excretion of the vitamin in the urine. Thiamine is transported in the blood by red blood cells and plasma and excreted in the urine. Thiamine is absorbed in the small intestine and phosphorylated in the intestinal mucosa. Except in cases of malabsorption syndrome, B vitamins are readily absorbed from the gastrointestinal tract. Thiamine is primarily absorbed in the duodenum. For more complete data on the absorption, distribution, and excretion of vitamins B1 (8 in total), please visit the HSDB record page. Metabolism/Metabolites In vivo, it is converted to thiamine diphosphate, a coenzyme for the decarboxylation of α-keto acids.
The compounds 3-(2'-methyl-4'-amino-5'-pyrimidinylmethyl)-4-methylthiazole-5-acetic acid (i.e., thiamine acetic acid), 2-methyl-4-amino-5-carboxymethylpyrimidine, and 5-(2-hydroxyethyl)-4-methylthiazole have been identified as important metabolites of thiamine (vitamin B1).
The biotransformation of thiamine in mammals is generally thought to produce thiochrome, thiamine disulfide, 5-(2-hydroxyethyl)-4-methylthiazole, and several forms corresponding to thiamine pyrimidine residues.
Thiamine is metabolized in the liver of animals. Several urinary metabolites of thiamine have been identified in humans. After administration of physiological doses, little or no unchanged thiamine is excreted in the urine; however, after administration of larger doses, both unchanged thiamine and metabolites are excreted when tissue storage is saturated.
Biological half-life
The biological half-life of this vitamin is 9–18 days.
At higher pharmacological doses, such as repeated oral administration of 250 mg or intramuscular injection of 500 mg, it takes nearly one week to reach steady-state plasma concentrations; the average elimination half-life is estimated to be 1.8 days.
The total amount of thiamine in an adult is estimated to be approximately 30 mg, and the biological half-life of this vitamin is likely between 9 and 18 days.

[1]. Analysis of Chlamydomonas thiamin metabolism in vivo reveals riboswitch plasticity. Proc Natl Acad Sci U S A. 2013 Sep 3;110(36):14622-7.

Thiamine hydrochloride is a hydrochloride salt produced by reacting thiamine chloride with an equimolar amount of hydrochloric acid. It has anthelmintic properties. It is a form of vitamin B1 and is also a hydrochloride salt. It contains thiamine (2+). Thiamine hydrochloride is the hydrochloride form of thiamine, a vitamin essential for aerobic metabolism, cell growth, nerve impulse transmission, and acetylcholine synthesis. Upon hydrolysis, thiamine hydrochloride is phosphorylated by thiamine diphosphate kinase to form active thiamine pyrophosphate (TPP), also known as a cocarboxylase. TPP is a coenzyme involved in many enzymatic reactions related to the metabolism of fatty acids, amino acids, and carbohydrates. See also: Thiamine (with active moiety) Thiamine ion (containing active moiety)... See more...

---

Mechanism of Action
Metabolic control analysis predicts that thiamine (vitamin B1) and other transketone synthesis stimulants can promote high levels of nucleic acid ribose synthesis, which is crucial for tumor cell survival, chemotherapy resistance, and proliferation. Metabolic control analysis also predicts that transketolase inhibitors will have the opposite effect on tumor cells. This could have significant implications for the nutrition and future treatment of cancer patients.

C12H18CL2N4OS

337.2685

336.057

67-03-8

Thiamine monochloride;59-43-8;Thiamine nitrate;532-43-4;Thiamine-d3 hydrochloride;Thiamine-13C3 hydrochloride;Thiamine monochloride-13C4 hydrochloride;1257525-77-1;Thiamine-d4 hydrochloride

6202

White to off-white solid powder

1.401 g/cm3

246-254ºC

100ºC

0

3

6

4

20

269

0

Cl[H].[Cl-].S1C([H])=[N+](C([H])([H])C2=C([H])N=C(C([H])([H])[H])N=C2N([H])[H])C(C([H])([H])[H])=C1C([H])([H])C([H])([H])O[H]

DPJRMOMPQZCRJU-UHFFFAOYSA-M

InChI=1S/C12H17N4OS.2ClH/c1-8-11(3-4-17)18-7-16(8)6-10-5-14-9(2)15-12(10)13;;/h5,7,17H,3-4,6H2,1-2H3,(H2,13,14,15);2*1H/q+1;;/p-1

2-[3-[(4-amino-2-methylpyrimidin-5-yl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethanol;chloride;hydrochloride

Thiamine hydrochloride; Vitamin B1; Thiamine HCl

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~100 mg/mL (~296.50 mM)
DMSO : ~6.67 mg/mL (~19.78 mM)

Solubility in Formulation 1: ≥ 1.25 mg/mL (3.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

---

Solubility in Formulation 2: ≥ 0.67 mg/mL (1.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

---

View More

Solubility in Formulation 3: ≥ 0.67 mg/mL (1.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

---

Solubility in Formulation 4: 33.33 mg/mL (98.82 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

---

 (Please use freshly prepared in vivo formulations for optimal results.)