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Related Concept Videos

Insulin Formulations: Types and Delivery01:27

Insulin Formulations: Types and Delivery

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Insulin preparations are categorized by their duration of action into short-acting and long-acting types. Two strategies are used to modify insulin's absorption and pharmacokinetic profile: slowing the absorption post-subcutaneous injection, or altering human insulin's amino acid sequence or protein structure. These changes retain the insulin's ability to bind to the insulin receptor, but alter its behavior in solution or after injection.
Short-acting insulins are divided into...
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Insulin: Dosing Regimen and Adverse Effects01:16

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Insulin-replacement therapy usually includes both long-acting insulin (basal) and short-acting insulin (to cater to postprandial needs). In a diverse group of type 1 diabetes patients, the average daily insulin dose is typically 0.5-0.7 units/kg body weight. However, obese patients and pubertal adolescents may need more due to insulin resistance.
The basal dose constitutes about 40%-50% of the total daily dose, with the rest as premeal insulin. The mealtime insulin dose should mirror...
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Insulin: Biosynthesis, Chemistry, and Preparation01:25

Insulin: Biosynthesis, Chemistry, and Preparation

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The endoplasmic reticulum (ER) of pancreatic β-cells synthesizes preproinsulin, which consists of a signal peptide, A and B chains, and a C-peptide. Preproinsulin is then cleaved and folded into proinsulin, which translocates to the Golgi apparatus for sorting and packaging into secretory granules. In these granules, enzymatic clipping generates insulin and C-peptide.
Damage or functional impairment of β-cells inhibits insulin production, leading to diabetes. Diabetes treatment...
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Production of Pharmaceuticals01:30

Production of Pharmaceuticals

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Industrial insulin production uses genetically engineered E. coli expressing a proinsulin gene controlled by a tryptophan promoter and containing a methionine linker for later cleavage. The cells also carry ampicillin resistance for selective growth. Seed cultures are stored at −80 °C and production begins by thawing a small amount to inoculate starter cultures, which are progressively scaled to a 50,000-L bioreactor. In the bioreactor, E. coli grow in nutrient-rich media under...
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Oral Hypoglycemic Agents: Glinides01:06

Oral Hypoglycemic Agents: Glinides

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Repaglinide (Prandin) and Nateglinide (Starlix), known as glinides, are oral insulin secretagogues that stimulate insulin release from pancreatic β cells by closing the ATP-sensitive potassium channels (KATP channel). Repaglinide controls insulin release from pancreatic β cells by managing potassium efflux. It shares two binding sites with sulfonylureas and also has a unique site, indicating overlapping mechanisms of action. With a rapid onset and a 4-7 hour duration, it effectively...
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One-Compartment Open Model for IV Bolus Administration: General Considerations01:19

One-Compartment Open Model for IV Bolus Administration: General Considerations

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The one-compartment model is a pharmacokinetic tool that models the body as a single, uniform compartment, facilitating the understanding of drug distribution and elimination. This model is particularly beneficial for intravenous (IV) bolus administration, where the drug rapidly circulates throughout the body.
The drug's presence in the body is defined by an equation representing the difference between the rates of drug entry and exit. Key parameters—elimination rate constant,...
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Intra-Omental Islet Transplantation Using h-Omental Matrix Islet filliNG hOMING
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Oral insulin reloaded: a structured approach.

Eric Zijlstra1, Lutz Heinemann2, Leona Plum-Mörschel2

  • 1Profil, Neuss, Germany eric.zijlstra@profil.com.

Journal of Diabetes Science and Technology
|May 31, 2014
PubMed
Summary

Developing an oral insulin pill remains a significant challenge in diabetes management. While research is increasing, most studies focus on preclinical development, with few recent clinical trials published for oral insulin formulations.

Keywords:
bioavailabilitydiabetesenteral absorptionglycemic controloral deliveryoral insulin

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Area of Science:

  • Pharmaceutical Sciences
  • Endocrinology
  • Drug Delivery

Background:

  • Optimal insulin coverage is crucial for diabetes mellitus management.
  • Needle-free and more physiological insulin delivery drives research into alternative administration routes.
  • Despite decades of effort, an orally available insulin formulation is not yet commercially available.

Purpose of the Study:

  • To systematically update recent developments in orally available insulin formulations.
  • To focus on data from clinical-experimental and clinical studies.
  • To assess the current landscape of oral insulin research and development.

Main Methods:

  • Identification of companies developing oral insulin formulations.
  • Analysis of published clinical trial results within the past five years.
  • Review of the proportion of clinical data relative to overall publications on oral insulin development.

Main Results:

  • Thirteen companies are reportedly developing oral insulin formulations.
  • Only six companies published new clinical trial results in the last five years.
  • Clinical data constitutes only 4% of the total publications on oral insulin development in this period.

Conclusions:

  • Research interest in orally bioavailable insulin formulations is rising.
  • The majority of research efforts for oral insulin remain in the preclinical stages.
  • Significant challenges persist in translating preclinical findings to clinical success for oral insulin.