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Related Concept Videos

Oral Hypoglycemic Agents: Glinides01:06

Oral Hypoglycemic Agents: Glinides

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 manages...
Glucagon-like Receptor Agonists01:24

Glucagon-like Receptor Agonists

Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by the...
Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a significant...
Oral Hypoglycemic Agents: Biguanides and Glitazones01:26

Oral Hypoglycemic Agents: Biguanides and Glitazones

Biguanides, particularly metformin (Glucophage), are insulin sensitizers that enhance glucose uptake, thereby reducing insulin resistance. Unlike sulfonylureas, metformin doesn't prompt insulin secretion, which helps to curb hypoglycemia risk. Metformin is beneficial in treating conditions like polycystic ovary syndrome due to its insulin-resistance reduction capability. The drug's primary action involves curtailing hepatic gluconeogenesis, a significant contributor to high blood glucose levels...
Oral Hypoglycemic Agents: α-Glucosidase Inhibitors01:19

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
Acarbose and miglitol are typically...
Oral Hypoglycemic Agents: Sulfonylureas01:17

Oral Hypoglycemic Agents: Sulfonylureas

Sulfonylureas are oral hypoglycemic agents utilized in treating type 2 diabetes. They are characterized by their unique sulfonylurea chemical structure. The family of sulfonylureas is divided into generations. First-generation sulfonylureas, including tolbutamide (Orinase), chlorpropamide (Diabinese), and tolazamide (Tolinase), trigger insulin release from pancreatic β cells and enhance peripheral tissues' insulin sensitivity. The second-generation members, such as glipizide (Glucotrol),...

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Related Experiment Video

Updated: Jun 17, 2026

Preparation of Naringenin Solution for In Vivo Application
08:18

Preparation of Naringenin Solution for In Vivo Application

Published on: August 10, 2021

New solid modifications of nateglinide.

G Bruni1, V Berbenni, C Milanese

  • 1C.S.G.I.-Dipartimento di Chimica Fisica M. Rolla, Università degli Studi di Pavia, Viale Taramelli 16, 27100 Pavia, Italy. giovanna.bruni@unipv.it

Journal of Pharmaceutical and Biomedical Analysis
|December 22, 2009
PubMed
Summary
This summary is machine-generated.

New nateglinide forms, including a hemihydrate and anhydrous polymorph, were identified. These forms exhibit distinct melting points and interconvert under varying storage conditions, impacting the antidiabetic drug's stability.

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Modification and Functionalization of the Guanidine Group by Tailor-made Precursors
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Last Updated: Jun 17, 2026

Preparation of Naringenin Solution for In Vivo Application
08:18

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Published on: August 10, 2021

Modification and Functionalization of the Guanidine Group by Tailor-made Precursors
09:45

Modification and Functionalization of the Guanidine Group by Tailor-made Precursors

Published on: April 27, 2017

Area of Science:

  • Pharmaceutical Chemistry
  • Solid-State Chemistry
  • Materials Science

Background:

  • Nateglinide is a crucial antidiabetic drug.
  • Understanding its solid-state forms is vital for drug formulation and stability.
  • Polymorphism can significantly influence a drug's bioavailability and efficacy.

Purpose of the Study:

  • To identify and characterize novel solid forms of nateglinide.
  • To investigate the interconversion pathways between different nateglinide polymorphs.
  • To establish the thermal behavior and stability profiles of nateglinide modifications.

Main Methods:

  • Thermal analysis (e.g., DSC, TGA) to determine melting points and thermal stability.
  • Vibrational spectroscopy (e.g., FTIR, Raman) for structural elucidation.
  • X-ray powder diffractometry (XRPD) for crystalline phase identification.

Main Results:

  • The final synthesis product is a nateglinide hemihydrate, melting at ~86°C.
  • Dehydration yields a new anhydrous polymorph melting at 102.8°C.
  • The anhydrous form interconverts to H polymorph (room conditions) or reverts to hemihydrate (humid conditions); B polymorph forms via thermal treatment or melt cooling.

Conclusions:

  • Nateglinide exhibits complex polymorphism with distinct anhydrous and hydrated forms.
  • Environmental conditions (humidity, temperature) dictate the stability and interconversion of these forms.
  • Characterization of these polymorphs is essential for controlling nateglinide's solid-state properties and ensuring therapeutic effectiveness.