Zydis absorption

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kugel

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Who can tell me if there is any decent evidence that the olanzapine in a Zydis orally-disintegrating tablets is absorbed to any significant degree through the oral mucosa. I know there is some evidence that Zydis and IM olanzapine have less weight gain than regular tablets and suggest this as evidence of mucosal absorption, but that's specious. Having people drink dissolved Zydis produces a plasma concentration about as fast as permitting sublingual dissolution - so that's not clear evidence of true mucosal absorption.

I can't find a good article via search engines to answer this.

Anybody know of good evidence of mucosal absorption separate from swallowing the olanzapine dissolved in saliva?

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Thanks!

http://jclinpharm.highwire.org/cgi/content/abstract/46/2/164

This study shows that there was no difference in time to plasma concentration when you allow the pill to dissolve sublingually vs swallowing the saliva with olanzapine dissolved in it. Suggesting, that IF there is oral mucosal absorption, it does not reduce time to plasma concentration - but not addressing the question directly.


http://www.ncbi.nlm.nih.gov/pubmed/...med_ResultsPanel.Pubmed_RVDocSum&ordinalpos=6

This study from 1998 was more direct (and one I did not find on my own - THANKS!). It states: "The saliva containing the dissolved or dispersed medicament is then swallowed and the drug is absorbed in the normal way."

If these two pieces of evidence are correct, then there is no signif. absorption from oral mucosa and hype about using Zydis to avoid hepatic first-pass effect is bunk.

But I'd like more than just these two small pieces of evidence.
If anyone has more, I'd sure appreciate it.
 
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http://books.google.com/books?hl=en...vo6Gj-bgWR3o#v=onepage&q=zydis mucosa&f=false

This book mentions that in some cases, it is absorbed through the oral mucosa

Thanks! I didn't have that either.
On pg 198, it mentions that some medications can be absorbed through mucosa when provided in the Zydis orally dissolving tablet form, but it mentions selegiline, apomorphine, buspirone, midazolam, and timolol as examples of drugs which can be absorbed to a significant degree through the mucosa. Interestingly, it does NOT mention olanzapine as one of them.
 
I really have not seen this as a clinically meaningful difference, nothing like f.ex. Lorazepam with PTSD flashbacks. The only benefit I see is with patients who have difficult swallowing or tend to spit out pills. So we really are talking MR, Autism and such. And that is a population that I am not eager to use Zyprexa in.

If you think it is hard to get a "regular" patient to exercise and do portion control, then you do not want to try it in this population.

I really don't see much use outside of PRN with unruly, lower-functioning patients.
 
I really have not seen this as a clinically meaningful difference, nothing like f.ex. Lorazepam with PTSD flashbacks. The only benefit I see is with patients who have difficult swallowing or tend to spit out pills. So we really are talking MR, Autism and such. And that is a population that I am not eager to use Zyprexa in.

If you think it is hard to get a "regular" patient to exercise and do portion control, then you do not want to try it in this population.

I really don't see much use outside of PRN with unruly, lower-functioning patients.

All true. I just had a curiosity about the mucosal absorption question.

Time to seek out a Lilly rep and make a "clinical science" request for "evidence of clinically significant mucosal absorption."
I don't have access to reps here. Anyone got one I can contact?
Send me a PM.
 
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