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<blockquote data-quote="Soundgen" data-source="post: 91306" data-attributes="member: 21269"><p>"Re: Benfotiamine</p><p></p><p>Postby howie on Today, 10:00 am</p><p>hey,</p><p></p><p>found this link too. i'm not against the idea of a thiamine deficiency in diabetics but i'm doubting the capacity of benfotiamine to make up for it. i'm just worried that it's not as effective as they advertise as<strong> i can't find any trials in humans</strong>. apparently in the lab rat trials the benfotiamine wasn't received orally or something it was under some 'special conditions'.</p><p></p><p>http://uk.reuters.com/article/idUKL1148 ... dChannel=0 "</p><p></p><p>Tests in Humans of Benfotiamine uptake from the references cited in the original article that Reuters reported on </p><p></p><p>class="abstitle"1: Ann Nutr Metab. 1991;35(5):292-6.Links </p><p>Bioavailability assessment of the lipophilic benfotiamine as compared to a water-soluble thiamin derivative.</p><p>Bitsch R, Wolf M, Möller J, Heuzeroth L, Grüneklee D. </p><p>FB 6 - Home Economics, Section Nutritional Science, University Paderborn, FRG.</p><p>The bioequivalence of thiamin in 2 therapeutically used preparations was tested in 10 healthy young men. Thiamin was orally administered either as lipophilic benfotiamine or as water-soluble thiamin mononitrate. Biokinetic data, measured as area under the curve and maximal concentration in plasma and hemolysate after ingestion, demonstrated a significantly improved bioavailability from the lipophilic derivative despite an ingested dose of only 40% as compared with the water-soluble salt. A superior cellular efficacy of benfotiamine was also concluded from the short-term stimulation of the thiamin-dependent transketolase activity in erythrocytes.</p><p></p><p></p><p></p><p>class="abstitle"1: Int J Clin Pharmacol Ther. 1998 Apr;36(4):216-21.Links </p><p>Comparative bioavailability of various thiamine derivatives after oral administration.</p><p>Greb A, Bitsch R. </p><p>Department of Human Nutrition, Institute of Nutrition and Environment, Friedrich Schiller University, Jena, Germany.</p><p>In a multiple change-over study the bioequivalence of 3 thiamine preparations, used therapeutically as neurotropic agents for the treatment of polyneuropathies, was tested in a collective of 7 volunteers. After ingestion of a single dose of either 100 mg benfotiamin CS-benzoylthiamine-o-monophosphate), fursultiamin (thiamintetrahydrofurfuryldisulfide) or thiaminedisulfide, thiamine blood levels were analyzed for a 10-hour period. Thiamine was measured by HPLC after precolumn derivatization to thiochrome. The maximal thiamine concentration Cmax and its time (tmax) in plasma and hemolysate, the area under concentration time curve (AUC), and thiamine excretion in 24-hour urine were assessed as criteria of bioavailability. Additionally the erythrocytic transketolase activity (ETK) and alphaETK were determined as indicators of the cellular thiamine availability. After benfotiamin ingestion a more rapid and earlier increase of thiamine in plasma and hemolysate was observed in contrast to fursultiamin and the disulfide. All biokinetic data demonstrated a significantly improved thiamine bioavailability from benfotiamin compared with the other preparations. The lowest bioavailability was detected with thiamindisulfide. From our results it can be concluded that oral administration of benfotiamin is best suitable for therapeutical purposes owing to its excellent absorption characteristics.</p><p></p><p></p><p></p><p></p><p></p><p>class="abstitle"1: Int J Clin Pharmacol Ther. 1996 Feb;34(2):47-50.Links </p><p>Pharmacokinetics of thiamine derivatives especially of benfotiamine.</p><p>Loew D. </p><p>Wuppertal, Germany.</p><p>Pharmacokinetic data of orally administered lipid-soluble thiamine analogues like benfotiamine are reviewed and assessed. It is quite clear that benfotiamine is absorbed much more better than water-soluble thiamine salts: maximum plasma levels of thiamine are about 5 times higher after benfotiamine, the bioavailability is at maximum about 3.6 times as high as that of thiamine hydrochloride and better than other lipophilic thiamine derivates. The physiological activity (alphaETK) increased only after benfotiamine was given. Due to its excellent pharmacokinetic profile benfotiamine should be preferred in treatment of relevant indications.</p></blockquote><p></p>
[QUOTE="Soundgen, post: 91306, member: 21269"] "Re: Benfotiamine Postby howie on Today, 10:00 am hey, found this link too. i'm not against the idea of a thiamine deficiency in diabetics but i'm doubting the capacity of benfotiamine to make up for it. i'm just worried that it's not as effective as they advertise as[b] i can't find any trials in humans[/b]. apparently in the lab rat trials the benfotiamine wasn't received orally or something it was under some 'special conditions'. http://uk.reuters.com/article/idUKL1148 ... dChannel=0 " Tests in Humans of Benfotiamine uptake from the references cited in the original article that Reuters reported on class="abstitle"1: Ann Nutr Metab. 1991;35(5):292-6.Links Bioavailability assessment of the lipophilic benfotiamine as compared to a water-soluble thiamin derivative. Bitsch R, Wolf M, Möller J, Heuzeroth L, Grüneklee D. FB 6 - Home Economics, Section Nutritional Science, University Paderborn, FRG. The bioequivalence of thiamin in 2 therapeutically used preparations was tested in 10 healthy young men. Thiamin was orally administered either as lipophilic benfotiamine or as water-soluble thiamin mononitrate. Biokinetic data, measured as area under the curve and maximal concentration in plasma and hemolysate after ingestion, demonstrated a significantly improved bioavailability from the lipophilic derivative despite an ingested dose of only 40% as compared with the water-soluble salt. A superior cellular efficacy of benfotiamine was also concluded from the short-term stimulation of the thiamin-dependent transketolase activity in erythrocytes. class="abstitle"1: Int J Clin Pharmacol Ther. 1998 Apr;36(4):216-21.Links Comparative bioavailability of various thiamine derivatives after oral administration. Greb A, Bitsch R. Department of Human Nutrition, Institute of Nutrition and Environment, Friedrich Schiller University, Jena, Germany. In a multiple change-over study the bioequivalence of 3 thiamine preparations, used therapeutically as neurotropic agents for the treatment of polyneuropathies, was tested in a collective of 7 volunteers. After ingestion of a single dose of either 100 mg benfotiamin CS-benzoylthiamine-o-monophosphate), fursultiamin (thiamintetrahydrofurfuryldisulfide) or thiaminedisulfide, thiamine blood levels were analyzed for a 10-hour period. Thiamine was measured by HPLC after precolumn derivatization to thiochrome. The maximal thiamine concentration Cmax and its time (tmax) in plasma and hemolysate, the area under concentration time curve (AUC), and thiamine excretion in 24-hour urine were assessed as criteria of bioavailability. Additionally the erythrocytic transketolase activity (ETK) and alphaETK were determined as indicators of the cellular thiamine availability. After benfotiamin ingestion a more rapid and earlier increase of thiamine in plasma and hemolysate was observed in contrast to fursultiamin and the disulfide. All biokinetic data demonstrated a significantly improved thiamine bioavailability from benfotiamin compared with the other preparations. The lowest bioavailability was detected with thiamindisulfide. From our results it can be concluded that oral administration of benfotiamin is best suitable for therapeutical purposes owing to its excellent absorption characteristics. class="abstitle"1: Int J Clin Pharmacol Ther. 1996 Feb;34(2):47-50.Links Pharmacokinetics of thiamine derivatives especially of benfotiamine. Loew D. Wuppertal, Germany. Pharmacokinetic data of orally administered lipid-soluble thiamine analogues like benfotiamine are reviewed and assessed. It is quite clear that benfotiamine is absorbed much more better than water-soluble thiamine salts: maximum plasma levels of thiamine are about 5 times higher after benfotiamine, the bioavailability is at maximum about 3.6 times as high as that of thiamine hydrochloride and better than other lipophilic thiamine derivates. The physiological activity (alphaETK) increased only after benfotiamine was given. Due to its excellent pharmacokinetic profile benfotiamine should be preferred in treatment of relevant indications. [/QUOTE]
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