Heartburn, indigestion, ulcers and other gastric disorders affect 1 in every 20 people, and U.S. patients fork over more money for treatment -- about $13 billion every year for prescription drugs -- than for almost any other type of medication.
But easing the symptoms can take time. The pills' thick coatings -- necessary so the medication isn't destroyed by the stomach's powerful acids -- delay the drugs' absorption until they get to the intestine.
Now a low-tech discovery happened upon by a university pharmacologist has led to the reformulation of some of the gastric reflux drugs with baking soda. Not only does the new formula appear to dramatically improve the performance of the acid-suppressing medications, it also makes them take effect much faster.
"If this is marketed appropriately, it could revolutionize what people take for acid reflux," said Dr. Rudolph Bedford, staff gastroenterologist at Santa Monica-UCLA Hospital. "It's potentially a winner for these types of drugs ... and it might overtake what's out their now, if the price is right."
Jeffrey Phillips, director of research at the University of Missouri-Columbia Department of Surgery, was trying to figure out how to help trauma patients with tubes in their throats ingest acid-reflux drugs such as Prevacid, Nexium and Prilosec.
Although intensive-care unit patients are prone to bleeding from stress ulcers, the acid-reflux drugs (called proton pump inhibitors) can't be given intravenously. Breaking the caplets into pieces small enough to be swallowed wouldn't work because the drugs would be destroyed by stomach acids.
Knowing that baking soda, or sodium bicarbonate, was a potent antacid, Phillips gave it to the patients as a buffer to first neutralize stomach acids. Then the crushed drugs were washed down the tube with additional baking soda and water. This protected the drugs from the stomach acids and allowed them to be absorbed more quickly, reaching peak blood levels in 30 minutes versus 1 1/2 to 3 hours.
Over-the-counter medications -- histamine 2 drugs Tagamet, Zantac, Axid and Pepcid, and antacids Tums and Rolaids -- are faster-acting than the proton pump inhibitors, but their effects are not as potent or as long lasting.
In administering the baking soda, Phillips learned something crucial about the little cells -- or pumps -- in the stomach that make the acid and that the drugs are designed to turn off. "To get the most effect, we had to turn the little acid pumps on first. It sounds crazy; why would we want to have more on? But you can only inhibit the ones that are on ... and our buffer tricked the acid pumps to turn on first." Then the drug shut them all down at once. "So the more you can turn on, the better."
Only a few of these pumps would have been on without adding the sodium bicarbonate.
Dr. Michael Metzler, who was the trauma unit chief at the University of Missouri-Columbia Hospital when the reformulated drugs were tested, said the reformulation represents more than a slight change. "It makes [the drugs] a lot more effective," said Metzler, who now directs the trauma center at Sunrise Hospital in Las Vegas.
San Diego-based Santarus Inc. received FDA approval in June to market omeprazole (the key ingredient in Prilosec) using Phillips' formulation. The 20-milligram powder form will be known as Zegerid. Santarus expects it to be available by the end of the year. (Studies are underway for capsule and chewable tablet versions using sodium bicarbonate or other buffers.)
Other drug makers are interested too. Tap Pharmaceutical Products Inc. has sublicensed the reformulation to use in its acid-reflux treatment blockbuster, Prevacid, which uses the ingredient lansoprazole. Among those expected to benefit from the powdered medication are children, who might have difficulty swallowing pills.
Because these anti-reflux medications are among the top-selling drugs in the world, both Phillips and the University of Missouri stand to reap millions from the formulations.