Writing in its European patent application, Zensun Shanghai Sci & Tech said its blend, made from nine B vitamin components and vitamin C, can treat and prevent a number of conditions associated with insufficient GI motility, including irritable bowel syndrome (IBS), constipation, and gastroparesis.
Zensun said impaired GI motility is “one of the largest health care burdens of industrialized nations”.
“Nowadays, the pressure of people's life is generally increasing, the pace of life is accelerating, and the competition is fiercer day by day. More and more patients are suffering from gastrointestinal disorders or gastrointestinal discomfort. The pathogeny thereof is extensive and the symptoms thereof are also different,” it wrote in its patent filing.
The company said that whilst there are a range of pharmaceutical drugs to treat gastrointestinal diseases, including metoclopramide, domperidone and itopride, few have good curative effects without side effects. In addition, it said products that provided long-term improvements to gastrointestinal function are rare.
An alternative way to effectively stimulate motility of the gastrointestinal system is therefore “highly desirable and would be an advance in the art”, the company said.
Improved energy metabolism
Zensun said its multivitamin B-C blend is made using a careful selection of vitamin B components, each chosen for a particular function, both individually and in combination with other compounds.
The blend contains: vitamin B1 (thiamine), B2 (riboflavin), B3 (niacin), B5 (pantothenic acid), B6, B7 (biotin), B9 (folic acid), B12, and choline bitartrate (from B4) – all of which play different roles towards the end goal of stimulating GI motility.
“Due to the large number of family members of B vitamins and their independent relationship, component selection and compatibility of the B vitamins are very important for preparation of drugs or health food for the treatment or regulation of motility disorders of the gastrointestinal system,” the company wrote.
Most importantly, it said the B vitamins had to be combined with vitamin C to create an effective composition in the treatment of gastrointestinal disorders.
“From the perspective of mechanism of action, vitamin B is an important coenzyme involved in energy metabolism of the human body, and vitamin C can promote the body's absorption of members of B vitamins. Multivitamin B-C is used to improve the energy metabolism of the human body and provide more energy for the gastrointestinal tract to improve the functional dyspepsia caused by inadequate gastrointestinal motility.”
The multivitamin blend works, it said, by assisting carbohydrates and fat in releasing energy, decomposing amino acids and transporting nutrient-containing oxygen and energy through the body.
The company said depending on what disorder the blend is used to treat, different compositions could be developed to include, for example, additional vitamin compounds like vitamin A, D, E and K or inositol (B8) and para-aminobenzoic acid (PABA). The dosage can be delivered in chewable tablet form, it said, or mixed with carriers to create dispersible tablets, granules, capsules or liquids.
Zensun said its multivitamin B-C has great potential to become a new supplementary health food, or drug, used to promote motility of the gastrointestinal system, although for the time being evidence is needed to prove its therapeutic and regulatory effects – an aspect it is trying to address through its mouse study.
In its patent, Zensun outlines methods and results of a mouse study conducted to test the efficacy of its multivitamin in varying doses on the small intestinal propulsive rate in mice with loperamide-induced constipation.
Using a powder form of its multivitamin B-C on 40 female mice, aged 9 weeks, it tested three dosages: a high dosage blend containing 1.317g of the combination of B vitamins; a moderate dosage blend with 0.439g; and a low dosage blend containing 0.132g of B vitamins.
The animals were divided into five groups using the random number table method and three groups were administered the multivitamin at different doses, the remaining two 'model' and 'control' groups were given CarboxyMethyl cellulose sodium (CMC-Na).
Each group was administered 20ml/kg of the blend (or CMC-Na) followed by a subcutaneous injection of loperamide after 30 minutes, except the control group which was given Tween 80 (polysorbate 80). At 60 minutes the animals were administered a charcoal solution which, at the end, enabled Zensun to measure the total length of the small intestine and propulsive distance of the charcoal solution.
A final small intestinal propulsive rate (%) was determined by diving the propulsive distance by the total length of the small intestine and multiplying it by 100.
Findings showed that the high, moderate and low dose compositions could all “significantly improve the small intestinal propulsive rate (%) in the loperamide-induced constipation mouse model”, with improvements being dose-dependent – increasing with higher dosage. A repeated test, following the same study model, confirmed these findings.
Combined results showed the higher dose gave a small intestinal propulsive rate of between 30-34%; the moderate dose between 23.2-25%; and the low dose between 17-21.3% - comparatively higher than three drugs tested in a later study - itopride hydrochloride, mosapride citrte and domperidone. Nalaxone was the one drug that showed a strong effect compared to the multivitamin blend.
Source: WIPO European Patent No. EP3308787
Published: April 18, 2018. Filed: June 6, 2016.
Title: “Use of composition of vitamin complex in preparing drug for stimulating gastrointestinal system motility”
Authors: Zensun Shanghai Science & Tech Co. Ltd.