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Enemacort Properties:
Enemacort is retention enema that is effective in the managements of acute cases of ulcerative colitis.
Enemacort has unique formulation by which the drug is delivered directly to the affected site.
   
Enemacort has unique formulation by which the drug is delivered directly to the affected site.
 
Composition:
Enemacort contain 2.3mg budesonide of dispersible tablet soluble in 115ml, isotonic aqueous vehicle of carboxy methyl cellulose.
Enemacort has to be reconstituted directly before use and the reconstituted enema will contain 0.02mg /ml in the form of micronized suspension.
Chemical and Pharmacology Properties:
The active ingredient in Enemacort is Budesonide. A glucocorticosteroid that modified to have powerful local anti-inflammatory activity, with low systemic effect.
Very low intestinal absorption (only <10%)
This little fraction of the absorbed budesonide is extensively biotransformed in the liver (first pass metabolism 90%).
The isotonic aqueous vehicle contains carboxymethyl cellulose.
The surface active properties of that vehicle distinguish this product from other drugs used by the same route of administration.
 
  • By virtue of its surface activity, carboxymethyl cellulose ensures rapid spread ability of the retention enema and helps carrying the microniszed particles of the budesonide against gravity to reach higher lesions in the colon.
Carboxymethyl cellulose provides muco-adhesive character to the drug.
 
  • And directing the active ingredient to adhere to the ulcerated mucosa.
  • Maximizing the retention of the drug on the affected site even with expulsion of the liquid phase.
Mode of Action:
The aim is to target the local activity to the site of inflammation.
Budesonide is designed for topical use and can generate a 100-fold or even higher intrinsic activity compared to systemically acting classic primary glucocorticoids.
Due to its modified chemical structure budesonide is highly lipophilic and has relatively high receptor binding affinity (11 times higher than that of dexamethasone;) and thus shows higher topical activity combined with high extra hepatic metabolic stability.
These specific properties have been well documented, especially for budesonide as a representative of the glucocorticoid group.
 
In This Page :
- Enemacort Properties
- Chemical Pharmacology Properties
- Mode of Action
 
 
 
 
 
 
 
 
 
 
 

 

 

 

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