User Tag List

Results 1 to 14 of 14
  1. #1
    Proven Member
    Join Date
    Jan 2012
    Posts
    56
    Mentioned
    0 Post(s)
    Tagged
    0 Thread(s)

    Default Aspirin sublingual

    Is it possible to make either an acetylsalicylic acid sublingual, or gel preparation, to avoid the stomach damaging side-effects?


    http://www.drugbank.ca/drugs/DB00945

  2. #2
    Senior Member Benson's Avatar
    Join Date
    Aug 2004
    Location
    Times Beach, MO
    Posts
    18,195
    Mentioned
    0 Post(s)
    Tagged
    0 Thread(s)

    Default

    It might be possible but you wouldn't want to...it is very bitter.

    You can take it with vitamin c to avoid most of the problems.
    Remember, believe none of what you hear and half of what you see...





  3. #3
    Senior Member
    Join Date
    Apr 2008
    Posts
    4,397
    Blog Entries
    3
    Mentioned
    0 Post(s)
    Tagged
    0 Thread(s)

    Default

    Ya, it would taste awful.

    Why can't you take buffered aspirin? The buffering should help with stomach trouble.

  4. #4
    Senior Member Supnut's Avatar
    Join Date
    Jun 2002
    Posts
    5,086
    Mentioned
    0 Post(s)
    Tagged
    0 Thread(s)

    Default

    Doesn't enteric coated aspirin already solve this issue?
    <span style='font-family:Optima'><span style='color:blue'>Creation is a machine</span></span>

  5. #5
    Senior Member Benson's Avatar
    Join Date
    Aug 2004
    Location
    Times Beach, MO
    Posts
    18,195
    Mentioned
    0 Post(s)
    Tagged
    0 Thread(s)

    Default

    Quote Originally Posted by Supnut View Post
    Doesn't enteric coated aspirin already solve this issue?
    It is not quite as clear as one might imagine.

    http://www.ncbi.nlm.nih.gov/pubmed/8937281
    Remember, believe none of what you hear and half of what you see...





  6. #6
    Proven Member
    Join Date
    Jan 2012
    Posts
    56
    Mentioned
    0 Post(s)
    Tagged
    0 Thread(s)

    Default

    I read the same thing, that buffering doesn't do anything to protect you. I also read that in practice Vitamin C also does nothing to prevent stomach damage.

    A sublingual or gel preparation would avoid the damage i assume. I can't believe there are no subligual Aspirin products on the market already. I've searched for days.

  7. #7
    Senior Member Benson's Avatar
    Join Date
    Aug 2004
    Location
    Times Beach, MO
    Posts
    18,195
    Mentioned
    0 Post(s)
    Tagged
    0 Thread(s)

    Default

    Quote Originally Posted by dontknow View Post
    I also read that in practice Vitamin C also does nothing to prevent stomach damage.
    I am not sure what you have been reading but the protective action of ascorbic acid on ASA-induced gastric erosion is pretty well established in the literature...

    Chewable low-dose aspirin has been available for many years. I would not reccomend you stick that under your tongue, however, because ASA will be just as damaging to your oral mucosa as it is to your gastric mucosa.
    Remember, believe none of what you hear and half of what you see...





  8. #8
    Senior Member
    Join Date
    Apr 2008
    Posts
    4,397
    Blog Entries
    3
    Mentioned
    0 Post(s)
    Tagged
    0 Thread(s)

    Default

    Quote Originally Posted by dontknow View Post
    A sublingual or gel preparation would avoid the damage i assume. I can't believe there are no subligual Aspirin products on the market already. I've searched for days.
    Put an aspirin in your mouth. You'll find out why they haven't made a sublingual version...

  9. Thanks dontknow thanked for this post
  10. #9
    Senior Member
    Join Date
    Apr 2008
    Posts
    4,397
    Blog Entries
    3
    Mentioned
    0 Post(s)
    Tagged
    0 Thread(s)

    Default

    Why not use alka-seltzer?

  11. #10
    Proven Member
    Join Date
    Jan 2012
    Posts
    56
    Mentioned
    0 Post(s)
    Tagged
    0 Thread(s)

    Default

    Benson:
    I use minimum 350mg of aspirin for migraine prophylaxis. Sometimes twice a day. I was using a few grams of asorbic acid with chewable ASA and still often times had pains in my stomach. I never got my stomach examined, but the thought of ulcers worried me. Also, i think it was either FunkOdyssey or the all-knowing Ex Dubio that told me Vitamin C won't do much in practice to protect from ASA stomach damage. I was using ASA because it was the best treatment I've tried, and the myraid of other health benefits were a bonus.

    @GaWd: I just looked it up and alka-seltzer has efficacy in migraines that's comparable to Asprin in a couple studies, thank you for that! I'm going to get some tomorrow! Are there any known adverse effects of taking alka-seltzer long-term?

  12. #11
    Senior Member Benson's Avatar
    Join Date
    Aug 2004
    Location
    Times Beach, MO
    Posts
    18,195
    Mentioned
    0 Post(s)
    Tagged
    0 Thread(s)

    Default

    Aliment Pharmacol Ther. 2004 Feb 1;19(3):367-74.
    Effects of buffered and plain acetylsalicylic acid formulations with and without ascorbic acid on gastric mucosa in healthy subjects.
    Dammann HG, Saleki M, Torz M, Schulz HU, Krupp S, Schürer M, Timm J, Gessner U.
    Source

    Klinische Forschung Hamburg, Hamburg, Germany. ammann@kfhh.de
    Abstract
    BACKGROUND:

    The most frequently reported adverse events associated with acetylsalicylic acid intake are minor gastrointestinal complaints. Galenic modifications, such as buffered formulations with or without ascorbic acid, may improve the benefit-risk ratio by decreasing the local mucosal side-effects of acetylsalicylic acid.
    AIM:

    To assess endoscopically-proven gastrointestinal lesions and the amount of gastric microbleeding of four different buffered and plain acetylsalicylic acid formulations, one containing paracetamol.
    METHODS:

    A randomized, four-fold cross-over study was performed in 17 healthy subjects who underwent serial oesophago-gastro-duodenoscopy before and after each course of 4-day dosing. Gastric aspirates were collected for the determination of haemoglobin concentrations to detect microbleeding.
    RESULTS:

    Buffered acetylsalicylic acid plus ascorbic acid yielded the lowest Lanza score, the lowest increase in the number of mucosal petechiae and the lowest increase in the amount of gastric microbleeding. Subjects receiving acetylsalicylic acid plus paracetamol plus caffeine showed the highest Lanza score of all treatments, and a considerably greater sum of petechiae in the oesophagus, stomach and duodenum compared with those receiving buffered acetylsalicylic acid plus ascorbic acid.
    CONCLUSIONS:

    The trial confirms that buffering of acetylsalicylic acid improves local gastric tolerability. Acetylsalicylic acid in combination with ascorbic acid shows significantly fewer gastric lesions and the lowest increase in gastric microbleeding compared with the other tested formulations.

    PMID: 14984384


    J Physiol Pharmacol. 2006 Nov;57 Suppl 5:125-36.
    Ascorbic acid attenuates aspirin-induced gastric damage: role of inducible nitric oxide synthase.
    Konturek PC, Kania J, Hahn EG, Konturek JW.
    Source

    First Department of Medicine, University Erlangen-Nuremberg, Germany. pkonturek@aol.com
    Abstract

    Aspirin (ASA) represents an important risk factor for gastric mucosal injury. Recently, vitamin C releasing aspirin (ASA-VitC) has been shown to reduce gastric toxicity of ASA in animal model of gastric injury. The aim of the present study was to compare the effect of ASA and ASA-VitC on the gastric mucosal damage before and after Helicobacter pylori (Hp) eradication in 10 young healthy Hp-positive volunteers. All subjects underwent endoscopy at day 0 (before ASA or ASA-VitC treatment) and at day 3 following treatment (1.6 g ASA/day or 1.6 g ASA + 0.96 g Vit C/day). In addition, in vitro experiments were performed in which gastric mucosal cell line (MKN-45 cells) was incubated with ASA or ASA-VitC alone or in combination with H.pylori. Expression of constitutive and inducible NO synthase (cNOS, iNOS) was analyzed by Western blot. Moreover, COX-2 expression was analyzed in gastric biopsies at mRNA and protein level by RT-PCR and Western blot, respectively. In humans, treatment with ASA-VitC induced significantly less gastric mucosal lesions than plain ASA. Furthermore, in comparison to plain ASA, ASA-VitC caused stronger inhibition of cNOS and increase in iNOS expression in the gastric mucosa. In vitro studies demonstrated a significant increase in iNOS expression in MKN-45 cells incubated with Hp. This effect was aggravated by the addition of ASA, but not ASA-VitC, to MKN-45 cells incubated with H.pylori. Both ASA and ASA-VitC stimulated the COX-2 expression in the gastric mucosa. We conclude that ASA-VitC in comparison with ASA induces less gastric mucosal damage and this protective effect may be due to its inhibitory effect on iNOS expression.

    PMID: 17218764
    Remember, believe none of what you hear and half of what you see...





  13. #12
    Proven Member
    Join Date
    Jan 2012
    Posts
    56
    Mentioned
    0 Post(s)
    Tagged
    0 Thread(s)

    Default

    Quote Originally Posted by Benson View Post
    Aliment Pharmacol Ther. 2004 Feb 1;19(3):367-74.
    Effects of buffered and plain acetylsalicylic acid formulations with and without ascorbic acid on gastric mucosa in healthy subjects.
    Dammann HG, Saleki M, Torz M, Schulz HU, Krupp S, Schürer M, Timm J, Gessner U.
    Source

    Klinische Forschung Hamburg, Hamburg, Germany. ammann@kfhh.de
    Abstract
    BACKGROUND:

    The most frequently reported adverse events associated with acetylsalicylic acid intake are minor gastrointestinal complaints. Galenic modifications, such as buffered formulations with or without ascorbic acid, may improve the benefit-risk ratio by decreasing the local mucosal side-effects of acetylsalicylic acid.
    AIM:

    To assess endoscopically-proven gastrointestinal lesions and the amount of gastric microbleeding of four different buffered and plain acetylsalicylic acid formulations, one containing paracetamol.
    METHODS:

    A randomized, four-fold cross-over study was performed in 17 healthy subjects who underwent serial oesophago-gastro-duodenoscopy before and after each course of 4-day dosing. Gastric aspirates were collected for the determination of haemoglobin concentrations to detect microbleeding.
    RESULTS:

    Buffered acetylsalicylic acid plus ascorbic acid yielded the lowest Lanza score, the lowest increase in the number of mucosal petechiae and the lowest increase in the amount of gastric microbleeding. Subjects receiving acetylsalicylic acid plus paracetamol plus caffeine showed the highest Lanza score of all treatments, and a considerably greater sum of petechiae in the oesophagus, stomach and duodenum compared with those receiving buffered acetylsalicylic acid plus ascorbic acid.
    CONCLUSIONS:

    The trial confirms that buffering of acetylsalicylic acid improves local gastric tolerability. Acetylsalicylic acid in combination with ascorbic acid shows significantly fewer gastric lesions and the lowest increase in gastric microbleeding compared with the other tested formulations.

    PMID: 14984384


    J Physiol Pharmacol. 2006 Nov;57 Suppl 5:125-36.
    Ascorbic acid attenuates aspirin-induced gastric damage: role of inducible nitric oxide synthase.
    Konturek PC, Kania J, Hahn EG, Konturek JW.
    Source

    First Department of Medicine, University Erlangen-Nuremberg, Germany. pkonturek@aol.com
    Abstract

    Aspirin (ASA) represents an important risk factor for gastric mucosal injury. Recently, vitamin C releasing aspirin (ASA-VitC) has been shown to reduce gastric toxicity of ASA in animal model of gastric injury. The aim of the present study was to compare the effect of ASA and ASA-VitC on the gastric mucosal damage before and after Helicobacter pylori (Hp) eradication in 10 young healthy Hp-positive volunteers. All subjects underwent endoscopy at day 0 (before ASA or ASA-VitC treatment) and at day 3 following treatment (1.6 g ASA/day or 1.6 g ASA + 0.96 g Vit C/day). In addition, in vitro experiments were performed in which gastric mucosal cell line (MKN-45 cells) was incubated with ASA or ASA-VitC alone or in combination with H.pylori. Expression of constitutive and inducible NO synthase (cNOS, iNOS) was analyzed by Western blot. Moreover, COX-2 expression was analyzed in gastric biopsies at mRNA and protein level by RT-PCR and Western blot, respectively. In humans, treatment with ASA-VitC induced significantly less gastric mucosal lesions than plain ASA. Furthermore, in comparison to plain ASA, ASA-VitC caused stronger inhibition of cNOS and increase in iNOS expression in the gastric mucosa. In vitro studies demonstrated a significant increase in iNOS expression in MKN-45 cells incubated with Hp. This effect was aggravated by the addition of ASA, but not ASA-VitC, to MKN-45 cells incubated with H.pylori. Both ASA and ASA-VitC stimulated the COX-2 expression in the gastric mucosa. We conclude that ASA-VitC in comparison with ASA induces less gastric mucosal damage and this protective effect may be due to its inhibitory effect on iNOS expression.

    PMID: 17218764
    From those studies it appears to have a protective effect, but Vit C doesn't totally ameliorate the damage. If someone was taking 350-700mg of ASA everyday i imagine there will be lots of damage done, no?

    Also, alka seltzer has Aspirin in it. i was under the impression that it was solely sodium bicarbinate. Does the citric acid and sodium bicarbinate also protect your stomach? If so, Ascorbic Acid + Alka Seltzer could be something to try then. Or would buffered Aspirin + 1g of ascorbic acid be better?

  14. #13
    Senior Member
    Join Date
    Jul 2009
    Posts
    1,726
    Mentioned
    0 Post(s)
    Tagged
    0 Thread(s)

    Default

    I am not quite sure, but I think there is a general misunderstanding of how Aspirin damages the gut... it is not because it is acidic, but because it is anti-inflammatory and thusly inhibits the protective effects of prostaglandins
    J Invest Surg. 2006 Sep-Oct;19(5):283-9.
    Prostaglandin E1 maintains structural integrity of intestinal mucosa and prevents bacterial translocation during experimental obstructive jaundice.
    Gurleyik E, Coskun O, Ustundag N, Ozturk E.
    Source

    Department of Surgery, Abant Izzet Baysal University, Duzce Medical Faculty, Duzce, Turkey. egurleyik@yahoo.com
    Abstract

    The absence of bile in the gut lumen induces mucosal injury and promotes bacterial translocation (BT). Prostaglandin E (PGE) has a protective effect on the mucosal layer of the alimentary tract. We hypothesize that PGE1 may prevent BT by its beneficial action on the mucosa of the small bowel. Thirty Wistar albino rats were divided equally into 3 groups; Group 1 (control) underwent sham laparotomy, group 2 obstructive jaundice (OJ) and group 3 (OJ + PGE1) underwent common bile duct (CBD) ligation and transection. Groups 1 and 2 received; 1 mL normal saline and group 3 received 40 mg of the PGE1 analogue misoprostol dissolved in 1 mL normal saline administered by orogastric tube once daily. After 7 days, laparotomy and collection of samples for laboratory analyses were performed, including bacteriological analysis of intestine, mesenteric lymph nodes (MLNs), and blood, and histopathologic examination of intestinal mucosa to determine mucosal thickness and structural damage. Serum bilirubin and alkaline phosphatase levels confirmed OJ in all animals with CBD transection. The mucosal damage score was significantly reduced in jaundiced animals receiving PGE1 compared to jaundiced controls (2.15 +/- 0.74 vs 5.3 +/- 0.59; p < .00001) and mucosal thickness was greater (607 +/- 59.1 microm vs. 393 +/- 40.3 microm; p < .00001). The incidence of BT to MLNs decreased from 90% to 30% (p < .02) when jaundiced rats received PGE1. PGE1 treatment reduced the detection rate of viable enteric bacteria in the blood from 60% to 10% (p < .057). We conclude that administration of PGE1 provides protection against OJ-induced atrophy and damage of intestinal mucosa, and thereby prevents translocation of enteric bacteria to underlying tissues.

    PMID:
    16966206
    [PubMed - indexed for MEDLINE]
    visit my nutrition & exercise science blog!
    SuppVersity @ SuppVersity.blogspot.com

    As ProfDrAndro, I am also one of the heads behind

    BodyRX Radio @ www.bodyRXRadio.com
    and a frequent guest at Carl Lenore's
    SuperHumanRadio @ www.superhumanradio.com

  15. #14
    Senior Member FunkOdyssey's Avatar
    Join Date
    Aug 2005
    Location
    Manchester, CT
    Posts
    4,167
    Mentioned
    0 Post(s)
    Tagged
    0 Thread(s)

    Default

    Aspirin is going to damage whatever tissue it contacts, it is just an unfriendly caustic substance. You can move the damage from the stomach down to your intestines if you enteric coat it. You can mitigate it to some degree with vitamin C but in my personal experience it has not been nearly as effective as the literature suggests. There may be a difference between taking an aspirin + c compound formulation versus taking them separately that prevents the average person from replicating the studies.

    If you keep taking aspirin some adaptations take place where the mucosa regenerates faster, so on a chronic basis things should not be as bad as in the beginning.
    Last edited by FunkOdyssey; February 5th, 2012 at 05:57 AM.
    "Also, can I rig some sort of enema out of household items?" -Tussman

    "I don't have the stamina for a 3-some, and I am a one-pump chump" -Ubiyca

Thread Information

Users Browsing this Thread

There are currently 1 users browsing this thread. (0 members and 1 guests)

Similar Threads

  1. Sublingual B12
    By Godmode in forum Supplements 101
    Replies: 15
    Last Post: January 25th, 2012, 04:39 PM
  2. Sublingual SAM-e
    By bdog527 in forum Neuroscience/Nootropics
    Replies: 4
    Last Post: November 13th, 2010, 12:21 AM
  3. These new Sublingual's....
    By skigazzi in forum Anabolic Steroids, Prohormones & Other Performance Enhancers
    Replies: 3
    Last Post: June 24th, 2009, 10:41 PM
  4. sublingual sAME
    By oyster in forum Supplements 101
    Replies: 6
    Last Post: July 25th, 2008, 02:37 PM
  5. Sublingual Deprenyl and MAO-A
    By Gill O&#39;Really in forum Neuroscience/Nootropics
    Replies: 9
    Last Post: July 31st, 2007, 03:46 PM

Bookmarks

Posting Permissions

  • You may not post new threads
  • You may not post replies
  • You may not post attachments
  • You may not edit your posts
  •