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About Zinc Carnosine

Zinc L-carnosine (beta-alanyl-L-histidinato zinc) (N-(3-aminopropionyl)-L-histidinato zinc), often simply called zinc carnosine, and also known as polaprezinc, is a mucosal protective chelate compound of zinc and L-carnosine.

It is a quadridentate 1:1 complex of a polymeric nature.It contains 23% zinc and 77% L-carnosine by mass.

Zinc is an essential trace element which plays an important role in the body, for example at the active centers of over 300 enzymes.

L-Carnosine composed of amino acids histidine and β-alanine.

Pharmacological properties of zinc carnosine

  • Strengthens the stomach mucosa
  • Adheres to the stomach wall
  • Acts as an anti-inflammatory
  • Acts as an antioxidant
  • Inhibits Helicobacter pylori.
  • Maintains homeostasis of the mucosa and promotes the repair of damaged tissues by wound healing action

Unique antiulcer properties

  • Stable in acidic pH of stomach
  • Adheres and bind to ulcer site
  • Slow dissociation on the ulcer site
  • Increases production of insulin-like growth factor-1 (IGF-1)
  • Promotes gastric epithelial wound repair

Anti-inflammatory effect

  • Inhibits production of pro-inflammatory cytokines i.e. Interleukin-8 
  • Reduces the activation of Nuclear factor kappa beta

Penetration of Zinc Carnosine

Being a chelate, Zinc carnosine is not destroyed in the acidic pH of stomach.
On administration, zinc carnosine adheres and bind to ulcer site.
Via the stage of the mixed ligand complex, L-carnosine and zinc which have anti-oxidant and wound healing properties are released on the ulcer lesion.

Zinc carnosine has a slow dissociation rate because of which it is not easily removed from the ulcer site. Slow dissociation rate of zinc carnosine DUE ITS POLYMERIC CHARACTER ensures prolonged existence at the ulcer site.

CHEMISTRY

Molecular formula5: C9H12N4O3Zn

Molecular mass5: 289.61

Structural formula:

MECHANISM OF ACTION OF ZINC CARNOSINE

healing of ulcers:

  • Increases production of insulin like growth factor-1 (IGF-1).
  • Promotes epithelial wound repair.

Anti- inflammatory effect:

  • Inhibits production of pro –inflammatory interleukin-8.
  • Prevents inflammatory white blood cells from adhering to epithelial cells.

Antioxidant effect:

  • Minimizes stress due to free radicals.

Advantages of chelate form of Zinc and L-Carnosine

Zinc binds quickly to stomach tissue if taken on an empty stomach. If taken on an empty stomach, it causes severe stomach pain and gastritis. It has been theorized that zinc ions are highly soluble in stomach acid and have corrosive, antimicrobial, and immune-stimulating properties that irritate the stomach tissue because of the direct absorption of the zinc ions. The chelation slows down the absorption and elimination of zinc from the stomach. Zinc is then able to repair the stomach and intestinal tissue directly without irritating it. Zinc carnosine may be taken on an empty stomach as needed. Zinc carnosine also protects the stomach lining from opportunistic H. pylori infection, and NSAIDs damage that cause ulcers that come from long-term use of the medication.

Zinc Carnosine and Diseases/Disorders:

Acid-Peptic Disorders (APD):

One of the most common gastrointestinal disorders encountered in day to day practice.
Heterogeneous group of disorders involving the gastrointestinal tract and result from an imbalance between the aggressive forces of gastric acid and pepsin and the defensive mechanism of gastric mucosa.

  • DEFENSIVE FACTORS
  • Mucus
  • Bicarbonate
  • Prostaglandins
  • Mucosal blood flow
  • Nitric oxide
  • DAGGRESSIVE FACTORS
  • Acid
  • Pepsin
  • NSAIDs
  • Oxidative stress
  • These are result of distinctive, but overlapping pathogenic mechanisms leading to either excessive acid secretion or diminished mucosal defense.Helitobacterpyloriis one of the most common causes of acid peptic disorders .H.pylori is found in half the population of the world.

Its prevalence is highly variable- high in developing countries.

Zinc Carnosine acts as a scavenger of monochloramine, released by H. pylori which contributes to injury to the stomach’s lining and thus protects the lining of stomach

NSAID induced mucosal damage:

  • NSAIDs- most commonly prescribed drugs for acute and chronic musculoskeletal inflammatory conditions.
  • Gastrointestinal toxicity is a common adverse effect of traditional NSAIDs.
  • NSAIDS present a further problem for individuals at risk for peptic ulcers. Since, by nature, these drugs dampen pain sensations, a person on long-term NSAID therapy may not notice ulcer-related pain, thus allowing the disease process to progress far further.

Inflammatory Bowel Diseases:

Inflammatory bowel disease (IBD) is a group of inflammatory conditions of the colon and small intestine. Crohn's disease and ulcerative colitis are the principal types of inflammatory bowel disease.

Zinc Carnosine salt and complex as an active ingredient has excellent inhibiting or suppressing functions against the bleeding and ulcer of colonic mucosa, hyperplasia of the colon and the leukocyte humidity, and exhibit extremely low toxicity and weak side-effect. Hence, is very useful for the prevention and treatment of IBD.

Zinc Carnosineaccelerates ulcer healing through actions such as prostaglandin-independent cytoprotection and antioxidative activity.

Salient points of Zinc Carnosine

Chemistry

Chemistry

Mechanism of action

Mechanism of action

Pharmacokinetics

Pharmacokinetics

Safety

Safety

Comparisons

Comparisons

Regulatory status

Regulatory status

Zinc and L-Carnosine

Zinc and L-Carnosine

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