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Dr.Niraj Limbachiya ☆ India, 2010-02-06 10:15 (5574 d 14:10 ago) Posting: # 4721 Views: 13,355 |
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Dear HS, please tell me how alcohol will affect drug bioavailability? regards Dr.Niraj Limbachiya Edit: Subject line changed. [Helmut] |
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Helmut ★★★   Vienna, Austria, 2010-02-06 14:32 (5574 d 09:54 ago) @ Dr.Niraj Limbachiya Posting: # 4723 Views: 12,080 |
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Dear Niraj! ❝ Dear HS, ^^Not interested in the opinions of other forum members? ❝ please tell me how alcohol will affect drug bioavailability? Mainly by increasing GI blood flow. Spirits may even lead to a pyloric spasm which will delay absorption (decrease or increase of absorption based on the properties of the drug). There is also the possibility of an interaction with metabolizing enzymes (if your drug contains an aliphatic OH-radical competitive with alcohol dehydrogenase), etc… A better release of the API from the formulation (enhanced solubility) I would consider a myth, because alcohol is one the few drugs which are very rapidly absorbed from the stomach – so nothing will be left before the absorption from the formulation will have a chance to start. — Dif-tor heh smusma 🖖🏼 Довге життя Україна! ![[image]](https://static.bebac.at/pics/Blue_and_yellow_ribbon_UA.png) Helmut Schütz ![[image]](https://static.bebac.at/img/CC by.png) The quality of responses received is directly proportional to the quality of the question asked. 🚮 Science Quotes |
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Ohlbe ★★★ France, 2010-02-08 00:54 (5572 d 23:31 ago) @ Helmut Posting: # 4728 Views: 11,941 |
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Dear Helmut, ❝ A better release of the API from the formulation (enhanced solubility) I would consider a myth, because alcohol is one the few drugs which are very rapidly absorbed from the stomach – so nothing will be left before the absorption from the formulation will have a chance to start. Well... There are discussions about some modified release formulations, where the coating could be damaged by alcohol, resulting in dose dumping. Avoid taking your ER morphine with a large glass of whisky. Regards Ohlbe |
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Helmut ★★★ Vienna, Austria, 2010-02-08 00:58 (5572 d 23:27 ago) @ Ohlbe Posting: # 4729 Views: 12,094 |
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Dear Ohlbe! ❝ Well… There are discussions about some modified release formulations, where the coating could be damaged by alcohol, resulting in dose dumping. Do you have a reference? ❝ Avoid taking your ER morphine with a large glass of whisky. Well… — Dif-tor heh smusma 🖖🏼 Довге життя Україна! Helmut Schütz The quality of responses received is directly proportional to the quality of the question asked. 🚮 Science Quotes |
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Ohlbe ★★★ France, 2010-02-08 01:36 (5572 d 22:49 ago) @ Helmut Posting: # 4730 Views: 11,962 |
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Dear Helmut, ❝ Do you have a reference? Scientific, no (but I didn't search either). Regulatory, yes. (Hey, I said discussions, not proof  . A nice negative case in a referral, by the way).Regards Ohlbe — Regards Ohlbe |
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Helmut ★★★ Vienna, Austria, 2010-02-08 15:08 (5572 d 09:17 ago) @ Ohlbe Posting: # 4732 Views: 12,006 |
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Dear Ohlbe! Well, I knew that one – I would file it in the myth-section. The company showed no influence on the release in vitro (which in that case is more rigourous than any in vivo study: dissolution in 40% alcohol), but had to place a warning in the SPC… Recently I had to deal with the DCP of a paediatric (!), where similar concerns were expressed. — Dif-tor heh smusma 🖖🏼 Довге життя Україна! Helmut Schütz The quality of responses received is directly proportional to the quality of the question asked. 🚮 Science Quotes |
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Ohlbe ★★★ France, 2010-02-08 18:01 (5572 d 06:24 ago) @ Helmut Posting: # 4734 Views: 11,951 |
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Dear Helmut, I've heard of other products (unpublished data, as far as I know), where in vitro data did show problems. Not tablets: coated pellets in a capsule. Regards Ohlbe -- Edit: in vitro, not in vivo. Sorry. Ohlbe — Regards Ohlbe |
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Helmut ★★★ Vienna, Austria, 2010-02-08 18:07 (5572 d 06:18 ago) @ Ohlbe Posting: # 4735 Views: 11,990 |
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Dear Ohlbe! ❝ I've heard of other products (unpublished data, as far as I know), where OK, possible – I would call this a bad coating.  Of course no company would publish such a result… — Dif-tor heh smusma 🖖🏼 Довге життя Україна! Helmut Schütz The quality of responses received is directly proportional to the quality of the question asked. 🚮 Science Quotes |
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ElMaestro ★★★ Denmark, 2010-02-08 19:19 (5572 d 05:06 ago) @ Helmut Posting: # 4736 Views: 11,935 |
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❝ Of course no company would publish such a result… Unless, of course, said company was an originator company resorting to aggressive brand protection activities. EM. |
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mvgchakravarthi ☆ India, 2010-02-15 18:41 (5565 d 05:44 ago) @ ElMaestro Posting: # 4765 Views: 11,915 |
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❝ ❝ Of course no company would publish such a result… ❝ ❝ Unless, of course, said company was an originator company resorting to aggressive brand protection activities. Dear all Let me know exact
M.V.G.Chakravarthi |
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ElMaestro ★★★ Denmark, 2010-02-15 19:31 (5565 d 04:54 ago) @ mvgchakravarthi Posting: # 4766 Views: 11,894 |
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Dear M.V.G.Chakravarthi ❝ 1. definition of Dose dumping? ❝ 2. Is there any limits permitted for this? ❝ 3. when we compared with innovator is it compulsory to match dissolution in 40% v/v alcohol? I am no expert, but here are my guesses:
EM. |
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mvgchakravarthi ☆ India, 2010-02-16 16:32 (5564 d 07:53 ago) (edited on 2010-02-16 17:05) @ ElMaestro Posting: # 4773 Views: 11,808 |
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Dear EM Very nice and your answers are interesting my question is when i compared dissolution of BCS class I molecule in 40% alcohol with Reference sample i got 8% for test and whereas 3% for Reference at 2hrs.is it indicates test sample is dose dumping? pls suggest me Thanks & regards M.V.g.chakravarthi Edit: Full quote removed. Please delete anything from the text of the original poster which is not necessary in understanding your answer; see also this post! [Ohlbe] |
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Ohlbe ★★★ France, 2010-02-16 18:11 (5564 d 06:14 ago) @ mvgchakravarthi Posting: # 4774 Views: 11,930 |
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Dear M.V.g.chakravarthi ❝ my question is when i compared dissolution of BCS class I molecule in 40% alcohol with Reference sample i got 8% for test and whereas 3% for Reference at 2hrs. is it indicates test sample is dose dumping? No. If you only have 8 % dissolution after 2 h, considering the time during which the drug will be in contact with alcohol in the stomach, no problem. Regards Ohlbe — Regards Ohlbe |
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Ohlbe ★★★ France, 2010-08-05 02:27 (5394 d 22:59 ago) @ Helmut Posting: # 5720 Views: 11,461 |
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Dear Helmut, ❝ OK, possible - I would call this a bad coating. ❝ Of course no company would publish such a result... Companies, no. EMA, yes. Regards Ohlbe — Regards Ohlbe |
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Helmut ★★★ Vienna, Austria, 2010-08-05 02:45 (5394 d 22:40 ago) @ Ohlbe Posting: # 5721 Views: 11,529 |
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Dear Ohlbe, welcome back! ❝ ❝ Of course no company would publish such a result... ❝ ❝ Companies, no. EMA, yes. Ah, I see: [...] for one of the controlled-release systems tested - once-daily capsules using a polymethacrylate-triethylcitrate coating to control the release of morphine - there was a significant interaction with alcohol. When these capsules were put into a 20% alcohol solution, 80% of the active substance was released within 15 minutes. This means that almost a full day’s dose of morphine would be released all at once if a patient were to take the capsule with large drink of neat strong liquor, such as whisky or vodka. That's descriptive: [...] capsules were put (sic!) into a 20% alcohol solution [...]How many, what volume of the nice stuff?  — Dif-tor heh smusma 🖖🏼 Довге життя Україна! Helmut Schütz The quality of responses received is directly proportional to the quality of the question asked. 🚮 Science Quotes |
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Ohlbe ★★★ France, 2010-08-07 00:21 (5393 d 01:04 ago) @ Helmut Posting: # 5736 Views: 11,434 |
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Dear Helmut, ❝ How many, what volume of the nice stuff? According to insider information I have: 40 ml of Irish whiskey (Jameson, I've been told), diluted 1/2 with water. No ice. I have to ask my source in what type of container the test was done (directly in a tumbler ?) Regards Ohlbe — Regards Ohlbe |
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Ohlbe ★★★ France, 2010-02-16 18:17 (5564 d 06:08 ago) @ Helmut Posting: # 4775 Views: 11,792 |
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Dear Helmut (and I'm sure ElMaestro will be interested in this somewhat off-topic discussion), ❝ alcohol is one the few drugs which are very rapidly absorbed from the stomach - so nothing will be left before the absorption from the formulation will have a chance to start. I think there is a need for further studies on the influence of various factors such as the way you drink your whisky: dry, or with ice, or with carbonated water, or both. This could influence gastric emptying. Also what you eat along could introduce some variability (how much, and how fat it is). Once again dissolution testing will never replace human studies. Regards Ohlbe — Regards Ohlbe |
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ElMaestro ★★★ Denmark, 2010-02-16 22:11 (5564 d 02:15 ago) @ Ohlbe Posting: # 4776 Views: 11,893 |
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Dear Ohlbe, ❝ I think there is a need for further studies on the influence of various factors such as the way you drink your whisky: dry, or with ice, or with carbonated water, or both. This could influence gastric emptying. Also what you eat along could introduce some variability (how much, and how fat it is). I completely agree, there is a an unmeet need for insight. While it is of the human nature to be egocentric, I am willing -for the benefit of mankind- to contribute to this noble endeavour for knowledge, so in case you know of a clinic seeking volunteers for the above mentioned studies, can you please give me a call? EM. |
Ing. Helmut Schütz