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Oral Insulin?

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Question:

        are there anything in the market today or in the    research labs to administer insulin orally instead of    through painful injections. if not, is it expected    anytime in the near future? if so, what are the associated    problems of administering orally?

The short form of the answer is no.  The long form is that people are working on alternative routes of insulin administration which include Pulmonary aerosols, vaginal insulin, ophthalmic insulin (by eye), rectal insulin and nasal insulin in addition to oral forms.  Each has big problems.  For example, insulin is a protein and it is the digestive system’s job to break down proteins. Oral insulin has to make it down pretty far in the gut to be absorbed rather than digested.  It is difficult to do that and still have a good absorbtion curve.  If, and it is a big if, oral insulin ever becomes available, it will probably be most used by type II’s looking for a partial basal assist to reduce beta cell production. Sensitivity varies a lot, but improvements in supplies (e.g. 29 ga. needles) and technique should remove most of the pain from the injections.  We all shove the needle through a nerve now and again, OUCH, but most of the time the shots should be fairly painless.  Jet injectors seem to help some people.  The buttock has fewer nerves than the belly.  Your friend may do well to talk to a diabetes educator if shot pain is a problem. Charles Coughran

Response:

Shree, insulin is a protein and will be digested by the stomach if taken orally. FWIW, the injections are not so painful anymore.  They have ultra fine needles that are sharpened exquisitely.  The drug it self doesn’t sting, either. If there are other problems with taking insulin by mouth, I am sure someone will tell you. -=Ben Westheimer

Response:

John Davis said: Yes I know the doctor/CDE ….. told you to use once and

"toss"…. John, this may have been so a few years back.  But I and  most of the CDE’s I know (and I know a lot) now teach safe re-use of syringes and lancets.  And those of us who use syringes and lancets ourselves mostly re-use. Ann S. Williams, MSN, RN, CDE   a diabetic diabetes educator

Response:

Sorry, but Insulin is a protein and would be completely digested.

Actually, work on oral insulin is going on.  The trick is to encapsulate it so that it survives deep into the gut where it is absorbed.  It is a very tricky problem and the utility of it even if it is solved is limited since absorbtion would be slow. One possible use is for Type IIs for a little basal production relief. Charles Coughran

Response:

=       are there anything in the market today or in the =       research labs to administer insulin orally instead of =       through painful injections. if not, is it expected =       anytime in the near future? if so, what are the associated =       problems of administering orally? Yes, I know this is the wrong place in the thread……. I will second what Speaker said here.  Though I’m type II I have to inject insulin too.  And even with a 28ga needle there is rarly any pain to speak of However when I run out of 28ga’s in about six months I’ll switch to 29ga’s (and when I need a boost of "R" that comes from a 30ga now, Now that’s getting small). Likewise you can get 29ga lancets or the finger stick.  Much nicer. Also depending on a few things (ie: age of patient) you might want to consider re-use. ’specially of lancets.  It’s OK as long as it’s NOT SHARED.  I use lancets till they hurt (That takes a while).  I find that the first few tests with a new lance hurt a bit but then, as (This is a guess) the lancet gets a bit "polished" from use (end guess) it quits hurting.  Often with my B-D Ultra Fines and the Soft Touch lancet device I have to LOOK to see if it worked. There is NO SENSATION at all (I will admit to having impared feeling in one hand, however I usually lance the one with full feeling). Syringes I use for about 1 week before tossing (Some studies showed that after about 10 days they may leak around the plunger.  I don’t know if they are right, but the timeing seems about right.  They do get harder to use with each additional use (Plunger gets "Stiffer" and harder to push) so for me 1 week is about right. Yes I know the doctor/CDE (You did take a diabetes class RIGHT?) told you use once and "toss" (Dispose of in a proper "SHARPS" container) but re-use is OK for most people.  I have a few cites on disk if you wish and can E-Mail them (Too long for forum posts) —

Response:

       are there anything in the market today or in the        research labs to administer insulin orally instead of        through painful injections. if not, is it expected        anytime in the near future? if so, what are the associated        problems of administering orally?        thanks,        Shree

Sorry, but Insulin is a protein and would be completely digested.  What is being researched is nasal and suppository forms of administration.  Nasal has certain problems with damage to the nasal tissues and suppositories are not very reliable yet.

Response:

=       i couldnt find a FAQ for this newsgroup and maybe the =       answer could be found in that. my cousin has Type I =       diabetes, and it is diagonised to be juvenile diabetes. =       she is on insulin injections. question: = =       are there anything in the market today or in the =       research labs to administer insulin orally instead of =       through painful injections. if not, is it expected =       anytime in the near future? if so, what are the associated =       problems of administering orally? Insulin is a protein, and is broken down by the digestive system if taken orally.  Any attempt at an oral insulin would have to find some way to get the insulin through most of the digestive tract before releasing the insulin.  To do so, you’d almost certainly have to encapsulate it somehow, and variations in the length of time it takes for the capsule to dissolve, combined with variations in the length of time it takes for the capsule to reach a specific point in the digestive tract would very likely make the release of the insulin highly variable. In short:  No, there’s no oral insulin on the market, and there’s not likely to be any time in the forseeable future.  As to the painful injections, it could well bee that th reason for the pain is poor technique in injecting the insulin.  Your cousin should bring the matter up next time she visits her doctor. I  try  very  hard  to say exactly what I mean.  I’d appreciate it if you’d bear that in mind and not try to "interpret"  my  posts  to  fit  your  own preconceived notions if I’m posting in a serious thread.  Remember:  If you throw a strawman into a heated debate, flames are likely to be the result.

Response:

Hi,         i couldnt find a FAQ for this newsgroup and maybe the         answer could be found in that. my cousin has Type I         diabetes, and it is diagonised to be juvenile diabetes.         she is on insulin injections. question:         are there anything in the market today or in the         research labs to administer insulin orally instead of         through painful injections. if not, is it expected         anytime in the near future? if so, what are the associated         problems of administering orally?         thanks,         Shree

Response:

 (3) even : if it was absorbed, much would be metabolized in the first-pass through : the liver — remember all orally absorbed drug must go through the : hepato-portal vein and directly into the liver.   Mmmm, naturally secreted insulin goes directly to the liver, too. So that doesn’t seem to be an objection. What IS an objection, though, seems to be that it’s hard to regulate absorption and since the body is so sensitive to over- and under-doses of insulin, it would be very hard to regulate BGs when absorption is unpredictable. This is one of the reasons why nasal-spray insulin has never been approved. Even shots can be unpredictable in some people. Sincerely, ._c- ._c- ._c- ._c- ._c- ._c- ._c- ._c- ._c- ._c- ._c- ._c- ._c- ._c- ._c- Natalie A. Sera, AKA Dr. Quack, with all her ducks in a row!!!!          ___ Type / 3, MI 4x (3Rs and an N) a year and a half! Proud mother of Josh, age 21                       ._c- ._c- ._c- ._c- ._c- ._c- ._c- ._c- ._c- ._(` ._c- ._c- ._c- ._c- ._c-                                          Can YOU find the Ugly Duckling?

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(Harold Boxenbaum ) writes: I heard speculation that maybe a nasal inhalation type of delievery might be possible.  I would wonder if you could get a good systemic effect that way?

sounds like it would be pretty hard to regulate.  everybody’s lungs are in different shape – i can’t imagine a pack-a-day smoker’s lungs absorbing as much as mine would, so you’d be playing with dangerous stuff.  i’d hate to accidentally get 15 units when my glucose level was only 13.5 mmol/l!!!  :) – jack I ain’t no politician, just worried ’bout the world condition ’cause I’m the doctor of soul and here’s my prescription: Peace, brother, peace. – Mac Rebennack, 1971

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(Harold Boxenbaum ) writes: I can speak on oral insulin.  There are probably three reasons why we will not see an oral insulin in our lifetime: (1) it is degraded by digestive enzymes in the gastrointestinal tract; (2) it has poor permeably through the gastrointestinal epithelial cells; and (3) even if it was absorbed, much would be metabolized in the first-pass through the liver — remember all orally absorbed drug must go through the hepato-portal vein and directly into the liver.  My best guess is that if there is an alternative to the injectables, it will be pulmonary delivery.  Some peptides are sufficiently absorbed orally, e.g., cyclosporin.  But insulin has been an intractable problem so far.  

I heard speculation that maybe a nasal inhalation type of delievery might be possible.  I would wonder if you could get a good systemic effect that way?

Response:

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- Hide quoted text — Show quoted text – There has been much hullabaloo in the media recently about a proprietary preparation of a hormone produced naturally in the body by the adrenal glands – DHEA.       From what I have gleaned from a couple of postings on the internet regarding DHEA, it appears that "naturally" occurring DHEA is ineffective when taken orally because it is broken down in the digestive       tract. This problem has apparently been overcome with the development of Proteusterone which is "an all-natural DHEA precursor complex combined with a proprietary compound(?) to allow for proper absorption by the body.  Recent research indicates that Dioscorea precursors can be converted naturally in the body."

Such a breakthrough, if  legitimately demonstrated, would have no problem getting published in a peer-reviewed journal such as the "Journal of Endocrinology" I keep up on the current literature pretty well, I can’t imagine such a monumental discovery slipping by without me knowing of it. Where was it published?  Perhaps in the "Journal of Complete and Utter Bullshit?" PA

Response:

There has been much hullabaloo in the media recently about a proprietary preparation of a hormone produced naturally in the body by the adrenal glands – DHEA.       From what I have gleaned from a couple of postings on the internet regarding DHEA, it appears that "naturally" occurring DHEA is ineffective when taken orally because it is broken down in the digestive       tract. This problem has apparently been overcome with the development of Proteusterone which is "an all-natural DHEA precursor complex combined with a proprietary compound(?) to allow for proper absorption by the body.  Recent research indicates that Dioscorea precursors can be converted naturally in the body." Given that the source for DHEA is " natural" Wild Yam (Dioscorea villosa L.), how effective would the ingestion of Wild Yam be? If Wild Yam were to contain the necessary precursors (and not necessarily the hormone itself) for the body to produce its own DHEA would the outcome be any different?  That is, would the mechanism for the production of DHEA from the ingestion of Wild Yam be unimpeded by the environment of the gut?  Is this the case? If so, is the ability of hormonal precursors to be effectively converted to their related hormones in the body peculiar to the DHEA hormonal mechanism? Can the knowledge from the development of Proteusterone be adapted to enable the production of other hormonal precursor complexes other than for DHEA? How about "oral insulin"? Any informed comment? With Thanks Michael P.S. 1 – apparently Proteusterone is a component of "numerous" products distributed by Emprise International, Inc. of Grand Prairie, Texas. What are these products and can anyone explain the rationale for the inclusion of Proteusterone in any of them? P.S. 2 – another aside to this debate is the claim that "the body can use DHEA to produce many of the other hormones(?) it requires." Does this include insulin?  If so, to what extent?

Response:

Michael, I can speak on oral insulin.  There are probably three reasons why we will not see an oral insulin in our lifetime: (1) it is degraded by digestive enzymes in the gastrointestinal tract; (2) it has poor permeably through the gastrointestinal epithelial cells; and (3) even if it was absorbed, much would be metabolized in the first-pass through the liver — remember all orally absorbed drug must go through the hepato-portal vein and directly into the liver.  My best guess is that if there is an alternative to the injectables, it will be pulmonary delivery.  Some peptides are sufficiently absorbed orally, e.g., cyclosporin.  But insulin has been an intractable problem so far.   Harold.   – Hide quoted text — Show quoted text -(Michael O’Day) writes: There has been much hullabaloo in the media recently about a proprietary preparation of a hormone produced naturally in the body by the adrenal glands – DHEA.       From what I have gleaned from a couple of postings on the internet regarding DHEA, it appears that "naturally" occurring DHEA is ineffective when taken orally because it is broken down in the digestive       tract. This problem has apparently been overcome with the development of Proteusterone which is "an all-natural DHEA precursor complex combined with a proprietary compound(?) to allow for proper absorption by the body.  Recent research indicates that Dioscorea precursors can be converted naturally in the body." Given that the source for DHEA is " natural" Wild Yam (Dioscorea villosa L.), how effective would the ingestion of Wild Yam be? If Wild Yam were to contain the necessary precursors (and not necessarily the hormone itself) for the body to produce its own DHEA would the outcome be any different?  That is, would the mechanism for the production of DHEA from the ingestion of Wild Yam be unimpeded by the environment of the gut?  Is this the case? If so, is the ability of hormonal precursors to be effectively converted to their related hormones in the body peculiar to the DHEA hormonal mechanism? Can the knowledge from the development of Proteusterone be adapted to enable the production of other hormonal precursor complexes other than for DHEA? How about "oral insulin"? Any informed comment? With Thanks Michael P.S. 1 – apparently Proteusterone is a component of "numerous" products distributed by Emprise International, Inc. of Grand Prairie, Texas. What are these products and can anyone explain the rationale for the inclusion of Proteusterone in any of them? P.S. 2 – another aside to this debate is the claim that "the body can use DHEA to produce many of the other hormones(?) it requires." Does this include insulin?  If so, to what extent?

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