• #LGM Pharma is a Budesonide CAS# 51333-22-3 API supplier distributor based in the USA. Inquire about DMF, cGMP, price, availability, delivery, purity, and more.
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  • #LGM Pharma offers this active ingredient but not the finished dosage forms.

Product Details:

  • CAS No: 51333-22-3
  • AHFC code: 52:08.08 68:04.00
  • Synonyms:
  • ATC Code: A07EA06 D07AC09 R01AD05 R03BA02
  • Chemical Formula: C6H12N2O4Pt
  • Molecular Weight: 430.5339
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB01222 (APRD00442)
  • SMILES: [H][C,,]12C[C,H]3OC(CCC)O[C,,]3(C(=O)CO)[C,,]1(C)C[C,H](O)[C,,]1([H])[C,,]2([H])CCC2=CC(=O)C=C[C,]12C
  • InChl: VOVIALXJUBGFJZ-KWVAZRHASA-N
  • PubChem: 63006
  • IUPAC: (1S,2S,4R,8S,9S,11S,12S,13R)-11-hydroxy-8-(2-hydroxyacetyl)-9,13-dimethyl-6-propyl-5,7-dioxapentacyclo[10.8.0.0^{2,9}.0^{4,8}.0^{13,18}]icosa-14,17-dien-16-one

Additional Details

Indication:
For the treatment of mild to moderate active Crohn’s disease. Also for the treatment of asthma, non-infectious rhinitis (including hay fever and other allergies), and for treatment and prevention of nasal polyposis.
Pharmacodynamics:
Budesonide is a synthetic corticosteroid used in Crohn’s disease to decrease the symptoms and inflammation associated with the disease, especially at times of flare up. Budesonide has a high topical glucocorticosteroid (GCS) activity and a substantial first pass elimination. The formulation contains granules which are coated to protect dissolution in gastric juice, but which dissolve at pH >5.5, ie, normally when the granules reach the duodenum. Thereafter, a matrix of ethylcellulose with budesonide controls the release of the drug into the intestinal lumen in a time-dependent manner.
Mode of Action:
The exact mechanism of action of budesonide in the treatment of Crohn’s disease is not fully understood. However, being a glucocorticosteroid, budesonide has a high local anti-inflammatory effect.
Metabolism:
Following absorption, budesonide is subject to high first pass metabolism (80-90%). In vitro experiments in human liver microsomes demonstrate that budesonide is rapidly and extensively biotransformed, mainly by CYP3A4, to its 2 major metabolites, 6b-hydroxy budesonide and 16a- hydroxy prednisolone. The glucocorticoid activity of these metabolites is negligible (
Toxicity:
Single oral doses of 200 and 400 mg/kg were lethal in female and male mice, respectively. The signs of acute toxicity were decreased motor activity, piloerection and generalized edema.
General Reference:
Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

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