[acb-diabetics] oral insulin in up-graded study

Patricia LaFrance-Wolf plawolf at earthlink.net
Mon Jun 14 18:09:29 GMT 2010


nsulin Pills Finally in Clinical Trials

 

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This article originally posted 

08 June, 2010

 and appeared in  

Issue 525

Insulin Pills Finally in Clinical Trials

After years of research and anticipation, insulin pills that could make it
easier for millions of patients worldwide to manage their diabetes are
moving

ahead in clinical trials.

...

Advertisement 

Drug manufacturers have tried for years to develop oral insulin without much
success. Insulin is a peptide hormone that people with diabetes currently
take

by injection to bring their blood sugar to within normal levels. But doing
so requires uncomfortable, inconvenient injections that can make patients
reluctant

to use the drug frequently enough to adequately control their blood sugar.
An oral form of insulin could help solve this problem. However, stomach
acids

and enzymes easily destroy insulin and other protein-based drugs. Scientists
have had difficulty finding an effective way to eliminate this problem.

They've responded to this challenge by developing special coatings for
insulin pills that prevent stomach acids from destroying them. Scientists
also are

using additives that make it easier for the intestine to absorb large
molecules like insulin. After years of setbacks, signs of success may be at
hand.

Several insulin pills are now in various stages of clinical trials, and
proof of concept may allow them to move into late-stage and more rigorous
clinical

testing. Only time will tell, however, whether these much-anticipated pills
will make it to the market.

Among developers, India's Biocon is the furthest along, with a technology
acquired in 2006 from now-defunct Nobex. In scientific publications, Biocon
scientists

have described the firm's candidate, IN-105, as an insulin molecule
conjugated to a short-chain polyethylene glycol derivative.

Put in a tablet, IN-105 retains similar activity to insulin alone,
withstands degradation, and is consistently absorbed, according to Biocon.
Results from

a Phase III clinical trial in India are expected in September. In late 2009,
Biocon applied to the U.S. Food & Drug Administration to allow it to start

clinical trials.

Solid oral forms could have efficacy and safety advantages, too. Insulin
delivered this way, unlike injected forms that circulate systemically, is
believed

to behave more like the body's own. Natural insulin is secreted by the
pancreas and taken up by the liver, which stores and metes it out when
needed. Engineered

for release in parts of the small intestine just past the stomach, solid
oral insulin can be taken up from there by the portal vein and delivered to
the

liver.

Getting the insulin

 through the stomach via an enterically coated tablet or capsule, which is
stable under acidic conditions, is the relatively easy first step. The drug
isn't

released until the pill reaches the small intestine and starts to dissolve
at higher pH. Sometimes enzyme inhibitors are added to stave off digestion.

The overall goal is keeping as much insulin as possible intact for eventual
absorption.

The harder second step is getting a large, hydrophilic protein past the
intestinal walls. Although proteins find it hard to diffuse across the
hydrophobic

lipid membrane or through epithelial cells in the wall, they can conceivably
be squeezed between cells. To wedge open tight intercellular junctions,
developers

add permeability or absorption enhancers to formulations.

Enhancers include oils, fatty acids, surfactants, and mucoadhesive or other
polymers. Formulators are loath to give specifics, but they will disclose
that

the materials are typically off-the-shelf and already approved for use as
food additives or in drug formulations. Using physical blends of enhancers
with

a known drug means that the safety profiles of the components are unchanged
for regulatory purposes. In contrast, any chemical modifications create new

entities that have to be tested.

With products

 moving into clinical trials, among the unanswered questions are ones about
the long-term effects of insulin and the accompanying materials. Insulin
induces

cell division, and researchers are concerned that it might be associated
with an increased risk of certain cancers. Companies working in this area
generally

believe that nothing but the drug and enhancers pass through the intestine. 

Results from studies with oral insulins will be presented at the American
Diabetes Association's 70th Scientific Sessions in Orlando, Florida later
this

month.

Chemical & Engineering News June 2010

.  

Diabetes In Control Advertisers 

http://openx.diabetesincontrol.com/www/delivery/ck.php?oaparams=2__bannerid=
41__zoneid=20__cb=c9b49dcced__oadest=http%3A%2F%2Fwww.a1ctest.com

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This article originally posted 08 June, 2010 and appeared in  

Issue 525

 

Insulin Pills Finally in Clinical Trials

 

After years of research and anticipation, insulin pills that could make it
easier for millions of patients worldwide to manage their diabetes are
moving

ahead in clinical trials....

 

Advertisement 

 

Click here to find out more! frame

 

Flash movie start

Flash movie end

Click here to find out more! frame end

 

Drug manufacturers have tried for years to develop oral insulin without much
success. Insulin is a peptide hormone that people with diabetes currently
take

by injection to bring their blood sugar to within normal levels. But doing
so requires uncomfortable, inconvenient injections that can make patients
reluctant

to use the drug frequently enough to adequately control their blood sugar.
An oral form of insulin could help solve this problem. However, stomach
acids

and enzymes easily destroy insulin and other protein-based drugs. Scientists
have had difficulty finding an effective way to eliminate this problem.

 

They've responded to this challenge by developing special coatings for
insulin pills that prevent stomach acids from destroying them. Scientists
also are

using additives that make it easier for the intestine to absorb large
molecules like insulin. After years of setbacks, signs of success may be at
hand.

Several insulin pills are now in various stages of clinical trials, and
proof of concept may allow them to move into late-stage and more rigorous
clinical

testing. Only time will tell, however, whether these much-anticipated pills
will make it to the market.

 

Among developers, India's Biocon is the furthest along, with a technology
acquired in 2006 from now-defunct Nobex. In scientific publications, Biocon
scientists

have described the firm's candidate, IN-105, as an insulin molecule
conjugated to a short-chain polyethylene glycol derivative.

 

Put in a tablet, IN-105 retains similar activity to insulin alone,
withstands degradation, and is consistently absorbed, according to Biocon.
Results from

a Phase III clinical trial in India are expected in September. In late 2009,
Biocon applied to the U.S. Food & Drug Administration to allow it to start

clinical trials.

 

Solid oral forms could have efficacy and safety advantages, too. Insulin
delivered this way, unlike injected forms that circulate systemically, is
believed

to behave more like the body's own. Natural insulin is secreted by the
pancreas and taken up by the liver, which stores and metes it out when
needed. Engineered

for release in parts of the small intestine just past the stomach, solid
oral insulin can be taken up from there by the portal vein and delivered to
the

liver.

 

Getting the insulin through the stomach via an enterically coated tablet or
capsule, which is stable under acidic conditions, is the relatively easy
first

step. The drug isn't released until the pill reaches the small intestine and
starts to dissolve at higher pH. Sometimes enzyme inhibitors are added to

stave off digestion. The overall goal is keeping as much insulin as possible
intact for eventual absorption.

 

The harder second step is getting a large, hydrophilic protein past the
intestinal walls. Although proteins find it hard to diffuse across the
hydrophobic

lipid membrane or through epithelial cells in the wall, they can conceivably
be squeezed between cells. To wedge open tight intercellular junctions,
developers

add permeability or absorption enhancers to formulations.

 

Enhancers include oils, fatty acids, surfactants, and mucoadhesive or other
polymers. Formulators are loath to give specifics, but they will disclose
that

the materials are typically off-the-shelf and already approved for use as
food additives or in drug formulations. Using physical blends of enhancers
with

a known drug means that the safety profiles of the components are unchanged
for regulatory purposes. In contrast, any chemical modifications create new

entities that have to be tested.

 

With products moving into clinical trials, among the unanswered questions
are ones about the long-term effects of insulin and the accompanying
materials.

Insulin induces cell division, and researchers are concerned that it might
be associated with an increased risk of certain cancers. Companies working
in

this area generally believe that nothing but the drug and enhancers pass
through the intestine. 

 

Results from studies with oral insulins will be presented at the American
Diabetes Association's 70th Scientific Sessions in Orlando, Florida later
this

month.

 

Chemical & Engineering News June 2010. Issue 525

Insulin Pills Finally in Clinical Trials

After years of research and anticipation, insulin pills that could make it
easier for millions of patients worldwide to manage their diabetes are
moving

ahead in clinical trials.

...

Advertisement 

Drug manufacturers have tried for years to develop oral insulin without much
success. Insulin is a peptide hormone that people with diabetes currently
take

by injection to bring their blood sugar to within normal levels. But doing
so requires uncomfortable, inconvenient injections that can make patients
reluctant

to use the drug frequently enough to adequately control their blood sugar.
An oral form of insulin could help solve this problem. However, stomach
acids

and enzymes easily destroy insulin and other protein-based drugs. Scientists
have had difficulty finding an effective way to eliminate this problem.

They've responded to this challenge by developing special coatings for
insulin pills that prevent stomach acids from destroying them. Scientists
also are

using additives that make it easier for the intestine to absorb large
molecules like insulin. After years of setbacks, signs of success may be at
hand.

Several insulin pills are now in various stages of clinical trials, and
proof of concept may allow them to move into late-stage and more rigorous
clinical

testing. Only time will tell, however, whether these much-anticipated pills
will make it to the market.

Among developers, India's Biocon is the furthest along, with a technology
acquired in 2006 from now-defunct Nobex. In scientific publications, Biocon
scientists

have described the firm's candidate, IN-105, as an insulin molecule
conjugated to a short-chain polyethylene glycol derivative.

Put in a tablet, IN-105 retains similar activity to insulin alone,
withstands degradation, and is consistently absorbed, according to Biocon.
Results from

a Phase III clinical trial in India are expected in September. In late 2009,
Biocon applied to the U.S. Food & Drug Administration to allow it to start

clinical trials.

Solid oral forms could have efficacy and safety advantages, too. Insulin
delivered this way, unlike injected forms that circulate systemically, is
believed

to behave more like the body's own. Natural insulin is secreted by the
pancreas and taken up by the liver, which stores and metes it out when
needed. Engineered

for release in parts of the small intestine just past the stomach, solid
oral insulin can be taken up from there by the portal vein and delivered to
the

liver.

Getting the insulin

 through the stomach via an enterically coated tablet or capsule, which is
stable under acidic conditions, is the relatively easy first step. The drug
isn't

released until the pill reaches the small intestine and starts to dissolve
at higher pH. Sometimes enzyme inhibitors are added to stave off digestion.

The overall goal is keeping as much insulin as possible intact for eventual
absorption.

The harder second step is getting a large, hydrophilic protein past the
intestinal walls. Although proteins find it hard to diffuse across the
hydrophobic

lipid membrane or through epithelial cells in the wall, they can conceivably
be squeezed between cells. To wedge open tight intercellular junctions,
developers

add permeability or absorption enhancers to formulations.

Enhancers include oils, fatty acids, surfactants, and mucoadhesive or other
polymers. Formulators are loath to give specifics, but they will disclose
that

the materials are typically off-the-shelf and already approved for use as
food additives or in drug formulations. Using physical blends of enhancers
with

a known drug means that the safety profiles of the components are unchanged
for regulatory purposes. In contrast, any chemical modifications create new

entities that have to be tested.

With products

 moving into clinical trials, among the unanswered questions are ones about
the long-term effects of insulin and the accompanying materials. Insulin
induces

cell division, and researchers are concerned that it might be associated
with an increased risk of certain cancers. Companies working in this area
generally

believe that nothing but the drug and enhancers pass through the intestine. 

Results from studies with oral insulins will be presented at the American
Diabetes Association's 70th Scientific Sessions in Orlando, Florida later
this

month.

Chemical & Engineering News June 2010

.  

Diabetes In Control Advertisers 

http://openx.diabetesincontrol.com/www/delivery/ck.php?oaparams=2__bannerid=
41__zoneid=20__cb=c9b49dcced__oadest=http%3A%2F%2Fwww.a1ctest.com

Flash movie end

Sign up for our FREE Weekly Newsletter 

Current Issue

Past Issue 

images/butnsignup  /

News and Information for Medical Professionals 

Search Diabetes In Control 

 

  

throwaway     

 

list of 10 items

Articles 

list of 5 items nesting level 1

Newsflash 

Diabetes News 

Features 

Feature Writers 

Past Newsletters 

list end nesting level 1

Tools 

list of 3 items nesting level 1

Continuing Education 

Test Your Knowledge 

Tools for your Practice 

list end nesting level 1

CE/CME 

Jobs 

Special Products 

list of 3 items nesting level 1

Current Spotlight Newsletter 

Previous Spotlight Newsletter 

Spotlight Product Review 

list end nesting level 1

Special Issues 

list of 5 items nesting level 1

Top Tools 

Best of 2009 

Byetta Special Edition 

ISMP Interview 

Primary Care Providers 

list end nesting level 1

Advertiser Profiles 

Studies 

list of 2 items nesting level 1

Current Studies 

Previous Studies 

list end nesting level 1

Links 

About us 

list of 3 items nesting level 1

About Us 

Contact Us 

Advertising 

list end nesting level 1

list end

  

Bookmark and Share  

| 

Print | 

Category | 

Home 

Previous | 

All Articles This Week | 

Next 

This article originally posted 08 June, 2010 and appeared in  

Issue 525

 

Insulin Pills Finally in Clinical Trials

 

After years of research and anticipation, insulin pills that could make it
easier for millions of patients worldwide to manage their diabetes are
moving

ahead in clinical trials....

 

Advertisement 

 

Click here to find out more! frame

 

Flash movie start

Flash movie end

Click here to find out more! frame end

 

Drug manufacturers have tried for years to develop oral insulin without much
success. Insulin is a peptide hormone that people with diabetes currently
take

by injection to bring their blood sugar to within normal levels. But doing
so requires uncomfortable, inconvenient injections that can make patients
reluctant

to use the drug frequently enough to adequately control their blood sugar.
An oral form of insulin could help solve this problem. However, stomach
acids

and enzymes easily destroy insulin and other protein-based drugs. Scientists
have had difficulty finding an effective way to eliminate this problem.

 

They've responded to this challenge by developing special coatings for
insulin pills that prevent stomach acids from destroying them. Scientists
also are

using additives that make it easier for the intestine to absorb large
molecules like insulin. After years of setbacks, signs of success may be at
hand.

Several insulin pills are now in various stages of clinical trials, and
proof of concept may allow them to move into late-stage and more rigorous
clinical

testing. Only time will tell, however, whether these much-anticipated pills
will make it to the market.

 

Among developers, India's Biocon is the furthest along, with a technology
acquired in 2006 from now-defunct Nobex. In scientific publications, Biocon
scientists

have described the firm's candidate, IN-105, as an insulin molecule
conjugated to a short-chain polyethylene glycol derivative.

 

Put in a tablet, IN-105 retains similar activity to insulin alone,
withstands degradation, and is consistently absorbed, according to Biocon.
Results from

a Phase III clinical trial in India are expected in September. In late 2009,
Biocon applied to the U.S. Food & Drug Administration to allow it to start

clinical trials.

 

Solid oral forms could have efficacy and safety advantages, too. Insulin
delivered this way, unlike injected forms that circulate systemically, is
believed

to behave more like the body's own. Natural insulin is secreted by the
pancreas and taken up by the liver, which stores and metes it out when
needed. Engineered

for release in parts of the small intestine just past the stomach, solid
oral insulin can be taken up from there by the portal vein and delivered to
the

liver.

 

Getting the insulin through the stomach via an enterically coated tablet or
capsule, which is stable under acidic conditions, is the relatively easy
first

step. The drug isn't released until the pill reaches the small intestine and
starts to dissolve at higher pH. Sometimes enzyme inhibitors are added to

stave off digestion. The overall goal is keeping as much insulin as possible
intact for eventual absorption.

 

The harder second step is getting a large, hydrophilic protein past the
intestinal walls. Although proteins find it hard to diffuse across the
hydrophobic

lipid membrane or through epithelial cells in the wall, they can conceivably
be squeezed between cells. To wedge open tight intercellular junctions,
developers

add permeability or absorption enhancers to formulations.

 

Enhancers include oils, fatty acids, surfactants, and mucoadhesive or other
polymers. Formulators are loath to give specifics, but they will disclose
that

the materials are typically off-the-shelf and already approved for use as
food additives or in drug formulations. Using physical blends of enhancers
with

a known drug means that the safety profiles of the components are unchanged
for regulatory purposes. In contrast, any chemical modifications create new

entities that have to be tested.

 

With products moving into clinical trials, among the unanswered questions
are ones about the long-term effects of insulin and the accompanying
materials.

Insulin induces cell division, and researchers are concerned that it might
be associated with an increased risk of certain cancers. Companies working
in

this area generally believe that nothing but the drug and enhancers pass
through the intestine. 

 

Results from studies with oral insulins will be presented at the American
Diabetes Association's 70th Scientific Sessions in Orlando, Florida later
this

month.

 

Chemical & Engineering News June 2010. 

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