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ORAL DRUG - H2 DELIVERY

Due to the proven effectiveness of H2B* to both generate and sustain H2 in formulations, as well as serving as a sustained drug delivery system, numerous H2 – proven drug  products are now available for therapeutics - by the oral route. Two examples are provided below:


Example 1: Treatment of Gingivitis with a Good Tasting H2 – Chlorhexidine Formula

It is well known that gingivitis (i.e., gum inflammation) leads to periodontal disease. It is the leading cause of tooth loss in both humans and animals. 


Chlorhexidine has been used in the oral cavity to treat gingivitis. This treatment has been only partially effective. There is a need for both better sustained delivery systems of antimicrobials and for more effective, longer lasting anti-inflammatory therapies. A recent publication attests to the antibacterial activity of H2 water against oral bacteria (1).


Using H2B*, a formula containing 0.12% chlorhexidine gluconate and 22.1% H2 was prepared. A small Phase 1 therapeutic trial was carried out. The product was rubbed into the gums. Overnight, the soreness in the gums was partially relieved. With repeated use, the symptoms of gingivitis were totally relieved.

(1) Lee, S.H., Bach, D.H. (2013) Antibacterial Activity of Hydrogen – Rich Water Against Oral Bacteria. Int. J. Oral Biol. 38 (2), 81-85.


Example 2: Sustained Release of H2 and Bismuth Subsalicylate in the G-I Tract

There are diseases and conditions of the upper G-I tract where sustained delivery of both effective drugs and H2 would have an advantage over current treatments. Conditions such as gastritis,  ulcers, gastroesophageal reflux disease (GERD), Helicobacter pylori infection, bacterial overgrowth, yeast overgrowth - could be better treated. Some of the drugs that could be delivered from H2 – rich H2B* formulations are: misoprostol, H2 receptor antagonists, antibiotics, antifungals, anti-inflammatories, antacids and bismuth subsalicylate.


Using H2B*, a formulation releasing 1.4 ppm H2 and containing 1.1 g./100 mL of bismuth subsalicylate was prepared. It was consumed by a volunteer suffering from GERD. His heartburn was rapidly relieved – with no side effects. The formulation was judged to taste very good.

Bismuth subsalicylate, in combination with 250 mg of metronidazole and 500 mg of tetracycline has been used to eradicate Helicobacter pylori. It is feasible to incorporate both these drugs - along with 1.1 g. bismuth subsalicylate into an H2 generating and sustaining H2B* formulation. The H2B* formulation will spontaneously and rapidly form in the stomach 

–  floating and having a long retention time. Five - to 10 - hour delivery of H2 and the drugs is achievable.