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Apriso - A Novel Medication in the Treatment of Ulcerative Colitis

In October, 2008 after getting the FDA approval, Salix Pharmaceuticals Company introduced its novel medication, called Apriso, to treat patients with ulcerative colitis (UC). Well, telling the truth, the medication is not “novel” in the full meaning of this word, because mesalamine, which is the main working ingredient of Apriso, is widely used today in other UC prescription medications, such as Pentasa, Rowasa, and Asacol; besides, it is also available in the generic form.

However, there is still one feature of Apriso, which grants an advantage to Apriso over the analogue medications. What is really new in Apriso is its unique combination of delayed and extended release technology of mesalamine delivery, which made Apriso the first and the only for the time being once-daily medication, indicated for the maintenance of ulcerative colitis (UC) remission in adults.

The point is that ulcerative colitis, which is a chronic inflammatory condition of the bowel, affects mainly colon or large intestine. And the main challenge for scientists is to deliver anti-inflammatory medication right to the affected area without having it destroyed by gastric acid in the stomach and small intestines. To reach this goal mesalamine medications (Asacol, Pentasa and others) are usually made in the form of delayed-release tablets, which start to dissolve only after passing the stomach.

Unlike its close rivals, Apriso features not only delayed-release technology, but the extended release as well. As the result of the prolonged and gradual release of its active ingredient, Apriso provides long-term effect on the colon, thus helping to keep ulcerative colitis symptoms in remission.

In general, the pattern of Apriso mode of action is as follows:

-         first, the medication gel outer layer is dissolved in the stomach and the microgranules with the active ingredient are dispersed into digestive tract;

-         then the coating of the microgranules starts to dissolve at pH 6.0 or higher and the release of mesalamine begins; - the particular level of pH is used to “tell” the medication that it has already reached the colon and it is time to start working (by the way, it is said that other analogue medications start to dissolve only at pH 7.0 or higher, while many people never reach that level of pH in their large intestine);

-         finally, the special polymer matrix core of Apriso controls the extended release of mesalamine to provide the distribution of main working substance throughout all the affected areas.

As the result of new delivery mechanism implementation patients can take Apriso only once per whole day (in the amount of 1.5 g, which is 4 capsules), usually in the morning with or without food. For comparison, Asacol is usually taken 3 times a day, and Pentasa is recommended twice a day.

So, from the point of view of users’ convenience only Lialda (another recently approved once-day UC treatment) may compete with Apriso. However, the recommended dosage of Lialda is 2.4 g per day versus 1.5 g of Apriso. On one hand, this may translate into lower side effects associated with Apriso, but on the other hand it may also mean lower effectiveness.

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Anyway, since the working ingredient is the same in all the mentioned medications, it may only be a matter of trying different products to define the one, which suits your therapeutic expectations best.

 
Nick
 

P.S. Taking Apriso along with antacids is not the best idea, because antacids influence pH level, which may bring to nothing all the efforts of highly-sophisticated Apriso technology of delivering mesalamine right where it is needed.


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