WO2016197889A1 - 复合维生素组合物在制备促进胃肠系统动力的药物中的用途 - Google Patents
复合维生素组合物在制备促进胃肠系统动力的药物中的用途 Download PDFInfo
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- WO2016197889A1 WO2016197889A1 PCT/CN2016/084938 CN2016084938W WO2016197889A1 WO 2016197889 A1 WO2016197889 A1 WO 2016197889A1 CN 2016084938 W CN2016084938 W CN 2016084938W WO 2016197889 A1 WO2016197889 A1 WO 2016197889A1
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Definitions
- the present invention relates to a vitamin BC composition, and more particularly to a multivitamin BC composition that promotes gastrointestinal system motility.
- the composition is useful for preventing and/or treating a condition or disease associated with gastrointestinal motility.
- Gastrointestinal motility is a coordinated neuromuscular process that delivers nutrients through the digestive system. May be involved in gastroesophageal reflux disease, gastroparesis (eg, diabetic and postoperative gastroparesis), irritable bowel syndrome (IBS), intestinal obstruction, and constipation (eg, functional or drug-induced constipation)
- gastroparesis eg, diabetic and postoperative gastroparesis
- IBS irritable bowel syndrome
- constipation eg, functional or drug-induced constipation
- gastrointestinal motility disorders are easy to lead to IBS.
- the current drugs for the treatment of gastrointestinal motility are metoclopramide, domperidone and itopride.
- metoclopramide the drug is a dopamine receptor blocker with strong central vomiting and gastrointestinal stimulatory effects.
- the drug can inhibit the relaxation of gastric smooth muscle, increase the response of gastrointestinal smooth muscle to cholinergic, accelerate gastric emptying, and increase the phase activity of gastric antrum.
- the drug also has the effect of stimulating the release of prolactin.
- the side effects of metoclopramide are more common with lethargy, irritability, and fatigue.
- the drug may cause symptoms of Parkinson's disease due to blockade of dopamine receptors in large doses or long-term use.
- Domperidone is a peripheral dopamine receptor antagonist that promotes normal motility and tension of the upper gastrointestinal tract, promotes gastric emptying, increases gastric antrum and duodenal bowel movement, coordinates pyloric contraction, and can also Enhance the peristalsis of the esophagus and the tension of the lower esophageal sphincter. Because of its poor permeability to the blood-brain barrier, it has almost no antagonistic effect on dopamine receptors in the brain. There are reports of seizures caused by large-dose intravenous injections abroad (there is no such preparation in China), but this drug is a powerful prolactin. Hormone release drugs may cause menstrual disorders.
- Itobili has the dual effects of dopamine receptor blockade and acetylcholinesterase inhibition, which enhances gastric and duodenal movement by stimulating endogenous acetylcholine release and inhibiting its hydrolysis, and promotes gastric emptying. Moderate antiemetic effect. This medicine should be used with caution in elderly or elderly patients.
- Vitamin B is a water-soluble vitamin, mostly coenzyme, involved in the metabolism of sugar, protein and fat in the body.
- Vitamin B1 can promote gastrointestinal motility and increase appetite. Vitamin B1 inhibits the hydrolysis of acetylcholine by cholinesterase. When B1 is deficient, the activity of the enzyme is increased, and the hydrolysis of acetylcholine is accelerated. Acetylcholine is an important substance that transmits nerve impulses. When it is lacking, it can cause nerve conduction disorder, especially affecting nerve conduction in the gastrointestinal tract, glands, etc., causing slow gastrointestinal motility, abdominal distension, decreased secretion of digestive glands, and reduced appetite. .
- Vitamin B2 is a component of the luteinase excipients in the body. It can be converted into flavin mononucleotide (FMN) and flavin adenine dinucleotide (FAD), both important coenzymes for tissue respiration, acting as hydrogen in the enzyme system, involved in sugar, protein, fat metabolism, and Can maintain normal visual function.
- vitamin B2 activates vitamin B6, which converts tryptophan to niacin, which may be related to maintaining the integrity of red blood cells. It maintains and improves the health of epithelial tissues such as the digestive tract mucosa.
- the mucosal layer of the human body cavity will have problems, causing mucosal lesions and enhancing the carcinogenic effect of chemical carcinogens. Therefore, vitamin B2 can prevent cancer.
- Vitamin B3 constitutes a coenzyme for dehydrogenase in the body. It is the most needed B vitamins in the human body. It is not only a vitamin that maintains the health of the digestive system, but also reduces gastrointestinal disorders. Niacin is converted into nicotinamide in human body. Niacinamide is a component of coenzyme I and coenzyme II, which participates in lipid metabolism in the body, oxidation process of tissue respiration and anaerobic decomposition of carbohydrates. It can promote the health of the digestive system, reduce gastrointestinal disorders, and effectively alleviate constipation symptoms. If it is lacking, it can cause angular cheilitis, glossitis, diarrhea, etc.
- Diarrhea is a typical symptom of this disease. It is often caused by constipation in the early stage, and then due to intestinal wall, digestive gland, intestinal wall and mucosa, atrophy of villi and enteritis. There are often diarrhea, the stool is watery or mushy, the amount is too much and there is stench, but also can bring blood, such as the lesion close to the anus can appear in the rush and then heavy. Diarrhea is often severe and refractory and can be combined with malabsorption.
- vitamin B5 pantothenic acid
- coenzyme A is an acyl carrier in the body and is involved in the metabolism of sugar, fat and protein. They work synergistically to regulate metabolism, maintain skin and muscle health, enhance immune and nervous system function, promote cell growth and division (including promoting red blood cell production and preventing anemia).
- the symptoms of vitamin B5 deficiency are loss of appetite, indigestion, and prone to duodenal ulcer.
- Vitamin B6 includes three kinds of pyridoxine, pyridoxal and pyridoxamine, which can be converted into each other. In vivo, ATP is converted into a coenzyme of various physiologically active enzymes by enzymatic action, thereby participating in various metabolic functions of amino acids and fats. In combination with vitamin B1, it has a strong analgesic effect. Vitamin B12 can enhance the analgesic effect of the combination of both, and alleviate the pain caused by peripheral nerve diseases and spinal cord diseases. Studies have reported that intravenous infusion of vitamin B6 and azithromycin can reduce the side effects of azithromycin on the gastrointestinal tract. Mainly in the body's blood, muscles, nerves, skin and so on.
- Vitamin B 6 deficiency damages cells and affects humoral immune function. Vitamin B6 can increase immunity, reduce carcinogens in the body, and have certain anti-cancer effects.
- Vitamin B7 also known as vitamin H, biotin, coenzyme R, participates in the metabolism of fatty acids and carbohydrates in the body; promotes protein synthesis; also participates in the metabolism of vitamin B12, folic acid and pantothenic acid; promotes urea synthesis and excretion. Enhance the body's immune response and infection resistance, stabilize the lysosomal membrane of normal tissues, maintain the body's humoral immunity, cellular immunity and affect the secretion of a series of cytokines, improve the body's immune function. Reduce the symptoms of perianal eczema and itching.
- the biotin side chain carboxyl group can be attached to the lysine residue of the enzyme via an amide bond. Biotin is a carboxyl carrier and is also involved in the metabolism of vitamin B12, folic acid, and pantothenic acid.
- Vitamin B9 (folic acid), a water-soluble B vitamin consisting of pteridine, p-aminobenzoic acid and glutamic acid residues.
- Tetrahydrofolic acid is a carrier for the transfer of "monocarbon groups" in vivo.
- a "monocarbon group” can be attached to the 5- or 10-position carbon atom of tetrahydrofolate, and is mainly involved in the synthesis and conversion of purine nucleotides and pyrimidine nucleotides.
- folic acid for women are widely noticed by the medical community, and should be supplemented by pregnant and lactating women to prevent rectal cancer and heart disease. It has also been found to prevent free radical damage to chromosomes, and humans such as the lack of folic acid can cause macrocytic anemia and leukopenia.
- Deoxyadenosylcobalamin is a major form of vitamin B12 in the body. It is a red compound containing cobalt. It needs to be converted to methylcobalamin and coenzyme B12 to be active. Vitamin B12 and folic acid play an important role in DNA synthesis. In addition, vitamin B12 also plays an important role in the maturation of red blood cells and the normal maintenance of the nervous system. It is often associated with the action of folic acid. Folic acid has various forms of sputum in cells. Studies have suggested that folic acid can interfere with the occurrence of gastrointestinal cancer. Folic acid can treat atrophic gastritis and improve the pathology of gastric mucosa.
- Hydrocholine tartrate promotes the conversion of phospholipids, accelerates the functioning of fats, and acts as a choleretic agent; inositol promotes cell metabolism, promotes development, and increases appetite.
- Para-aminobenzoic acid (PABA) is actually a component of folic acid. Its role in the body is coenzyme, which works in conjunction with folic acid to promote protein metabolism and blood cell production.
- Vitamin C also known as ascorbic acid, is one of the antioxidant vitamins. It is involved in the hydroxylation reaction in the body and is necessary for the formation of bone, tooth, connective tissue and non-epithelial cells. It can maintain the normal teeth, bones and blood vessels. Function to increase resistance to disease. According to relevant information, vitamin C has different degrees of deficiency in various populations. When there are some minor problems in the body, you should promptly supplement the appropriate amount of vitamins and minerals to improve nutritional deficiencies, especially in middle-aged and elderly people. Vitamins have a preventive effect on many diseases, and many diseases may be more or less related to the lack of vitamin C. In addition, vitamin C can be combined with many other drugs to treat certain diseases. Vitamin C, vitamin C is an antioxidant that protects the body from free radicals.
- Vitamin C is also a coenzyme. Many studies have shown that vitamin C can block the synthesis of carcinogen N-nitroso compounds, preventing the formation of carcinogenic ammonium nitrite in salted, stained and smoked foods containing nitrite (same as bacon and sausage). Cancer, especially for rectal and colon cancer, has a better preventive effect. At the same time, it has the effect of softening the anorectal blood vessels and increasing the anorectal elasticity. VC is easily destroyed by heat or oxidant, especially light, trace heavy metals and fluorescent substances, which promotes its oxidation, which makes VC widely limited in application.
- vitamin C including metal salts of VC, esters of VC and various acids, and compounds of VC and saccharides
- VC instability can overcome the disadvantages of VC instability and better play the role of VC.
- Physiological function include vitamin C (L-ascorbic acid), vitamin C sodium (L-ascorbate), vitamin C phosphate magnesium, vitamin C polyphosphate, vitamin C palmitate, vitamin C stearate, vitamin C glucose. Compounds, etc.
- vitamin B is an important coenzyme involved in human energy metabolism, and vitamin C can promote the body's absorption of vitamin B members.
- Multivitamin BC enhances the body's energy metabolism and provides more energy to the gastrointestinal tract to improve functional dyspepsia caused by gastrointestinal motility. This increase in energy metabolism includes assisting carbohydrates and fats in releasing energy, breaking down amino acids, and delivering nutrient-containing oxygen and energy to the entire body. Multivitamin BC will likely become a new drug or health food with a high safety to promote gastrointestinal system power, but by now So far, there is no evidence to prove the promotion of gastrointestinal motility by vitamin BC, especially in the pathological state, the treatment and regulation of vitamin BC on gastrointestinal motility disorders.
- the selection and compatibility of vitamin B components is essential for the preparation of drugs or health foods for treating or regulating gastrointestinal motility disorders.
- the present invention relates to a method of promoting gastrointestinal system motility in a subject in need thereof, wherein the subject has a gastrointestinal system disorder (i.e., a disorder, a condition, a symptom, or a dysfunction caused by a drug or surgery).
- the method comprises administering to a subject in need thereof a therapeutically effective amount of a vitamin B and vitamin C family composition.
- vitamins referred to in the present invention include their corresponding analogs or derivatives, such as vitamin B1 means thiamine and its analogs or derivatives; vitamin B2 means riboflavin and its analogs or derivatives; vitamin B3 means Niacin and its analogs or derivatives; vitamin B5 means pantothenic acid and analogs or derivatives thereof; vitamin B6 means pyridoxine and its analogues or derivatives; vitamin B7 is biotin and its analogues or derivatives; Vitamin B9 refers to folic acid and analogs or derivatives thereof; vitamin B12 refers to cyanocobalamin and analogs or derivatives thereof; vitamin C refers to ascorbic acid and analogs or derivatives thereof; and the like.
- vitamin B1 means thiamine and its analogs or derivatives
- vitamin B2 means riboflavin and its analogs or derivatives
- vitamin B3 means Niacin and its analogs or derivatives
- vitamin B5 means pantothenic acid and analogs or derivatives thereof
- vitamin B6 means
- the multivitamin BC group composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, biotin, A composition of vitamin C.
- the multivitamin BC composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid , a combination of biotin, vitamin C, hydrogen choline tartrate, inositol.
- the vitamin B group composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, vitamins.
- the invention provides a composition comprising an effective amount of a vitamin B family, a vitamin C family composition, and a pharmaceutically acceptable carrier.
- the composition comprises an effective amount of vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, biotin, Vitamin C and a pharmaceutically acceptable carrier.
- the composition comprises an effective amount of vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid, Biotin, vitamin C, hydrogencholine tartrate, inositol, and a pharmaceutically acceptable carrier.
- the composition comprises an effective amount of vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, vitamins. B12, folic acid, biotin, vitamin C, choline hydrogen tartrate, inositol, p-aminobenzoic acid, and a pharmaceutically acceptable carrier.
- vitamin B1 thiamine
- vitamin B2 riboflavin
- vitamin B3 nicotinic acid
- vitamin B5 pantothenic acid
- vitamins. B12, folic acid, biotin, vitamin C, choline hydrogen tartrate, inositol, p-aminobenzoic acid and a pharmaceutically acceptable carrier.
- the present invention is directed to a composition
- a composition comprising an effective amount of a vitamin B, a C-group composition and an effective amount of a medicament for the treatment and/or prevention of gastrointestinal disorders.
- the composition comprises an effective amount of vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, biotin, Vitamin C and an effective amount of a drug for treating and/or preventing gastrointestinal diseases.
- the composition comprises an effective amount of vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), Vitamin B5 (pantothenic acid), vitamin B6, folic acid, biotin, vitamin C, choline hydrogen tartrate, inositol, and an effective amount of a drug for treating and/or preventing gastrointestinal diseases.
- the composition comprises an effective amount of vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, vitamins. B12, folic acid, biotin, vitamin C, choline hydrogen tartrate, inositol, p-aminobenzoic acid, and an effective amount of a medicament for treating and/or preventing gastrointestinal diseases.
- the present invention is directed to a composition
- a composition comprising an effective amount of a vitamin B, a Group C composition, and other effective amount of a vitamin family compound.
- the composition comprises an effective amount of vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, biotin, Vitamin C and other effective amounts of vitamin compounds.
- the composition comprises an effective amount of vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid, Biotin, vitamin C, choline hydrogen tartrate, inositol, and other effective amounts of vitamin compounds.
- the composition comprises an effective amount of vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, vitamins. B12, folic acid, biotin, vitamin C, choline hydrogen tartrate, inositol, p-aminobenzoic acid and other effective amounts of vitamin compounds.
- the other vitamin compounds include vitamin A, vitamin D, vitamin E, vitamin K, and the like.
- Promoting gastrointestinal motility is used in a method of treating a gastrointestinal dysfunction caused by a drug (for example, an opioid such as morphine-induced intestinal dysfunction or constipation) in a subject in need thereof, the method comprising administering a treatment An effective amount of a vitamin B, C group composition.
- a drug for example, an opioid such as morphine-induced intestinal dysfunction or constipation
- the subject may be using opioid or opioid for postoperative pain management or chronic pain management.
- opioids and opioids include morphine, codeine, oxycodone, hydrocodone, methadone, fentanyl, and anti-inflammatory agents such as acetaminophen or A combination of aspirin).
- the multivitamin BC group composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, biotin, A composition of vitamin C.
- the multivitamin BC composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid , a combination of biotin, vitamin C, hydrogen choline tartrate, inositol.
- the multivitamin BC group composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, A composition of vitamin B12, folic acid, biotin, vitamin C, choline hydrogen tartrate, inositol and p-aminobenzoic acid.
- Promoting gastrointestinal motility can be used to treat gastroparesis in a subject in need thereof by administering a therapeutically effective amount of a vitamin B, C-group composition.
- the multivitamin BC group composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, biotin, A composition of vitamin C.
- the multivitamin BC composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid , a combination of biotin, vitamin C, hydrogen choline tartrate, inositol.
- the multivitamin BC composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), A composition of vitamin B5 (pantothenic acid), vitamin B6, vitamin B12, folic acid, biotin, vitamin C, choline hydrogen tartrate, inositol and p-aminobenzoic acid.
- the method of promoting gastrointestinal motility is used in a method of treating gastroesophageal reflux disease (GERD) in a subject in need thereof, the method comprising administering a therapeutically effective amount of vitamin B, Group C composition.
- the multivitamin BC group composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, biotin, A composition of vitamin C.
- the multivitamin BC composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid , a combination of biotin, vitamin C, hydrogen choline tartrate, inositol.
- the multivitamin BC group composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, A composition of vitamin B12, folic acid, biotin, vitamin C, choline hydrogen tartrate, inositol and p-aminobenzoic acid.
- the gastroesophageal reflux disease is nocturnal gastroesophageal reflux disease.
- the invention also provides a method of promoting gastrointestinal motility to treat irritable bowel syndrome (IBS) in a subject in need thereof by administering a therapeutically effective amount of a vitamin B, C-group composition.
- the multivitamin BC group composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, biotin, A composition of vitamin C.
- the multivitamin BC composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid , a combination of biotin, vitamin C, hydrogen choline tartrate, inositol.
- the multivitamin BC group composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, A composition of vitamin B12, folic acid, biotin, vitamin C, choline hydrogen tartrate, inositol and p-aminobenzoic acid.
- the irritable bowel syndrome may be constipation-type irritable bowel syndrome or constipation/diarrhea alternating irritable bowel syndrome.
- the invention also provides a method of promoting gastrointestinal motility to treat constipation in a subject in need thereof by administering a therapeutically effective amount of a vitamin B, C-group composition.
- the constipation includes functional (bad habits, eating habits, senile and other constipation without organic causes) and drug-induced constipation.
- the multivitamin BC group composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, biotin, A composition of vitamin C.
- the multivitamin BC group composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, vitamins. B12, a composition of folic acid, biotin, vitamin C, hydrogencholine tartrate, inositol.
- the multivitamin BC group composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, A composition of folic acid, biotin, vitamin C, choline hydrogen tartrate, inositol and p-aminobenzoic acid.
- the method of promoting gastrointestinal motility is used in the treatment of a gastrointestinal dysfunction caused by surgery or related to gastrointestinal dysfunction (eg, post-operative bowel movement slowing) in a subject in need thereof, the method comprising administering the therapeutically effective A quantity of vitamin B, C group composition.
- the multivitamin BC group composition comprises vitamin B1 (thiamine), A composition of vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, biotin, and vitamin C.
- the multivitamin BC composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid , a combination of biotin, vitamin C, hydrogen choline tartrate, inositol.
- the multivitamin BC group composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, A composition of vitamin B12, folic acid, biotin, vitamin C, choline hydrogen tartrate, inositol and p-aminobenzoic acid.
- a preferred multivitamin BC group composition is a composition comprising vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, biotin, vitamin C. .
- a more preferred multivitamin BC group composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid, biotin, vitamin C. , a composition of choline hydrogen tartrate, inositol.
- the multivitamin BC group composition comprises vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, A composition of vitamin B12, folic acid, biotin, vitamin C, choline hydrogen tartrate, inositol and p-aminobenzoic acid.
- the dosage form of the multivitamin BC group composition of the present invention may be a chewable tablet, but is not limited thereto, and the composition of the present invention may also be added with various conventional excipients required for preparing different dosage forms, such as a disintegrating agent, a lubricant, and a sticking agent.
- a pharmaceutical carrier such as a mixture, an antioxidant, a complexing agent or the like can be prepared into any of the commonly used oral dosage forms, such as dispersible tablets, granules, capsules, oral liquids, and the like, by a conventional preparation method.
- the multivitamin BC group composition of the present invention has various weight ratios of the components, and each of them has a corresponding promoting effect on the gastrointestinal system kinetics.
- it may comprise the following components by weight: 5-10 parts of vitamin B1, 10-15 parts of vitamin B2, 6-25 parts of vitamin B3, 10-110 parts of vitamin B5, 5-10 parts Vitamin B6, 5-10 parts biotin, 0.1-0.5 parts folic acid, 0.001-0.030 parts vitamin B12, 100-300 parts choline heavy tartrate, 50-500 parts vitamin C.
- the vitamin B group composition comprises the following components by weight: 10 parts of vitamin B1, 15 parts of vitamin B2, 25 parts of vitamin B3, 110 parts of vitamin B5, 10 parts of vitamin B6 and 9 parts of biotin.
- the vitamin B group composition comprises the following components by weight: 10 parts of vitamin B1, 15 parts of vitamin B2, 25 parts of vitamin B3, 110 parts of vitamin B5, 10 parts of vitamin B6, 9 parts Biotin, 0.4 parts folic acid, 250 parts of choline hydrogen tartrate, 150 parts of vitamin C and 250 parts of inositol.
- the vitamin B family composition comprises the following components by weight: 10 parts of vitamin B1, 15 parts of vitamin B2, 25 parts of vitamin B3, 110 parts of vitamin B5, 10 parts of vitamin B6, 9 Biotin, 0.4 parts folic acid, 250 parts of choline hydrogen tartrate, 150 parts of vitamin C, 250 parts of inositol, 0.025 parts of vitamin B12 and 50 parts of p-aminobenzoic acid.
- Figure 1 Different concentrations of multivitamin B, 9 components + VC for the first trial of loperamide-induced constipation in mice after administration of ink in mice Intestinal propulsion rate (%) change
- Figure 2 Changes in the rate of adduction of ink in the small intestine of mice after repeated trials of loperamide-induced constipation in different concentrations of multivitamin B, 9 components + VC
- Figure 3 Changes in ink penetration rate (%) of mice in mice after administration of 2.5 mg/kg loperamide-induced constipation mice with complex VB, 9 components + VC and positive control
- Multivitamin B 9 components + VC
- the experimental animals were randomly divided into 5 groups, 8 in each group.
- the specific grouping and dosage were shown in Table 1 and Table 2.
- Tween-80 saline accurately measure 40 mL of normal saline into a 50 mL centrifuge tube, using a pipette Measure 400 ⁇ L of Tween-80, add to the centrifuge tube, vortex and mix, and set aside at room temperature.
- Composite VB, 9-component + VC high-dose group accurately weighed composite VB, 9 parts of 1.317g were added to 3 VCs, and after grinding, add 0.5% CMC-Na 20ml, shake and mix to form a stable suspension. .
- Composite VB, 9 components + VC medium dose group accurately weighed composite VB, 9 parts 0.439g added 3 pieces of VC, after grinding, add 0.5% CMC-Na 20ml, shake and mix to form a stable suspension .
- Composite VB, 9-component + VC low-dose group accurately weighed composite VB, 9 parts of 0.132g added 3 pieces of VC, after grinding, add 0.5% CMC-Na 20ml, shake and mix to form a stable suspension .
- Loperamide Accurately weigh 5.0 mg of loperamide, add 20 mL of physiological saline solution containing 1.0% Tween 80, shake and mix for at least 5 min, and use it now.
- each group was administered at a dose of 20 ml/kg.
- the model group and the normal group were intragastrically administered with 0.5% CMC-Na solution at the same dose; After 30 minutes, the normal group was subcutaneously injected with a physiological saline solution containing 1.0% Tween 80, and the other groups were subcutaneously injected with loperamide solution at a volume of 10 ml/kg. After subcutaneous injection for 30 minutes, the ink was administered by intragastric administration at a dose of 10 ml/kg [1, 2, 3] .
- the animals were sacrificed by cervical dislocation. Immediately open the abdominal cavity to separate the mesentery. The upper end of the intestine from the pylorus and the lower end to the ileocecal area was cut and placed on the tray. Be careful not to involve the small intestine and gently put the small intestine into a straight line. The total length of the small intestine was measured, and the ink advancement length was calculated from the pylorus to the ink front, and the intestinal ink propulsion rate (%) was calculated.
- test data were expressed by X ⁇ S, and one-way ANOVA was performed using SPSS software.
- the LSD test was used for comparison between groups.
- the results of the first trial showed that the small intestine propulsion rate (%) of the model group was significantly lower than that of the normal group (48.6 ⁇ 0.0VS16.1 ⁇ 0.0), indicating that the mouse constipation model was successfully prepared; compared with the model group, high and medium In the low-concentration group, the ink propelling distance and the small intestine propulsion rate (%) were significantly increased (p ⁇ 0.05); the high-middle-low concentration group had a significant dose-effect relationship in improving the small intestine propulsion rate (%). 34.0 ⁇ 0.1, 25.0 ⁇ 0.0 & 21.3 ⁇ 0.1).
- the VB, 9 component + VC high, medium and low dose groups can significantly improve the intestinal propulsion rate (%) of the loperamide-induced constipation mouse model, and there are high, medium and low concentration groups. Significant dose-effect relationship.
- Multivitamin B 9 components + VC
- the experimental animals were randomly divided into 8 groups, 8 in each group.
- the specific grouping and dosage were shown in Table 1 and Table 2.
- 1% Tween-80 saline accurately measure 40 mL of normal saline into a 50 mL centrifuge tube, measure 400 ⁇ L Tween-80 with a pipette, add to a centrifuge tube, vortex and mix, and set aside at room temperature. .
- 5% ink accurately weigh 100g of gum arabic, add water 800ml, boil until the solution is transparent, weigh 50g of activated carbon powder into the above solution and boil for 3 times. After the solution is cooled, add water to make up to 1000ml.
- Composite VB, 9 components + VC (5X) group Take 1 composite VB, 9 components + VC tablets, add 0.5% CMC-Na 19.5ml after grinding, shake and mix to form a stable suspension. . Now available.
- Compound VB, 9 components + VC (1X) group Take 5 times the dose of compound VB, 9 parts + VC suspension 2ml, add 0.5% CMC-Na 8ml, shake and mix to form a stable suspension liquid. Now available.
- the morphine group 1 tablet of morphine was taken, and after grinding, 0.5% CMC-Na 32.52 ml was added, and the mixture was shaken to form a stable suspension. Now available.
- Mosapride citrate group 1 tablet of mosapride citrate was added, and 0.5% CMC-Na 32.52 ml was added after grinding, and the mixture was shaken to form a stable suspension.
- Itopride hydrochloride group 1 tablet of itopride hydrochloride was taken, and 0.5% CMC-Na 32.52 ml was added after grinding, and the mixture was shaken to form a stable suspension. Now available.
- Naloxone group Take 1 bottle (0.8 mg) of naloxone hydrochloride for injection, add 0.5 ml of 0.5% CMC-Na, shake and mix. A clear solution is formed. Now available.
- Loperamide Accurately weigh 5.0 mg of loperamide, add 20 mL of physiological saline solution containing 1.0% Tween 80, shake and mix for at least 5 min, and use it now.
- each group was administered at a dose of 20 ml/kg.
- the model group and the normal group were intragastrically administered with 0.5% CMC-Na solution at the same dose; After 30 minutes, the normal group was subcutaneously injected with a physiological saline solution containing 1.0% Tween 80, and the other groups were subcutaneously injected with loperamide solution at a volume of 10 ml/kg. After subcutaneous injection for 30 minutes, the ink was administered by intragastric administration at a dose of 10 ml/kg [1, 2, 3] .
- the animals were sacrificed by cervical dislocation. Immediately open the abdominal cavity to separate the mesentery. The upper end of the intestine from the pylorus and the lower end to the ileocecal area was cut and placed on the tray. Be careful not to involve the small intestine and gently put the small intestine into a straight line. The total length of the small intestine was measured, and the ink advancement length was calculated from the pylorus to the ink front, and the intestinal ink propulsion rate (%) was calculated.
- test data were expressed by X ⁇ S, and one-way ANOVA was performed using SPSS software.
- the LSD test was used for comparison between groups.
- test group VB, 9 components + VC (5 times dose) group can significantly improve the intestinal propulsion rate (%) of loperamide-induced constipation mouse model, and the positive control naloxone also has significant intestinal propulsion.
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Abstract
Description
Claims (10)
- 一种复合维生素B、C族组合物,其可用于预防和/或治疗与胃肠系统动力匮乏相关的状态或疾病。
- 根据权利要求1所述的组合物,其中所述复合维生素B、C组合物包括维生素B族组合物或其类似物或衍生物和维生素C或其类似物或衍生物。
- 根据权利要求2所述的组合物,其中所述维生素B族组合物或其类似物或衍生物选自维生素B1(硫胺素)、维生素B2(核黄素)、维生素B3(烟酸)、维生素B5(泛酸)、维生素B6和维生素B7(生物素)、维生素B9(叶酸)、维生素B12等。
- 根据权利要求2所述的组合物,其中所述维生素C或其类似物或衍生物选自维生素C(L-抗坏血酸)、维生素C钠(L-抗坏血酸钠)、维生素C磷酸酯镁、维生素C多磷酸酯、维生素C棕榈酸酯、维生素C硬脂酸酯、维生素C葡萄糖化合物等。
- 根据权利要求1或2所述的组合物,其中所述复合维生素B、C族组合物还包括酒石酸氢胆碱。
- 根据权利要求1或2所述的组合物,其中所述复合维生素BC族组合物还包括肌醇或对氨基苯甲酸。
- 根据权利要求2所述的组合物,其特征在于其包含如下重量配比的组份:10份维生素B1,15份维生素B2,25份维生素B3,110份维生素B5,10份维生素B6,0.1份维生素B7,0.4份维生素B9,0.025份维生素B12和150份维生素C。
- 根据权利要求2所述的组合物,其特征在于其包含如下重量配比的组份:10份维生素B1,15份维生素B2,25份维生素B3,110份维生素B5,10份维生素B6,0.1份维生素B7,0.4份维生素B9,0.025份维生素B12,250份酒石酸氢胆碱和150份维生素C。
- 一种复合维生素B、C族组合物在制备治疗和/或预防与胃肠系统动力匮乏相关的胃肠状态或疾病的药物或保健食品中的用途。
- 根据权利要求9所述的用途,其中所述复合维生素B、C组合物包括维生素B族组合物或其类似物或衍生物和维生素C或其类似物或衍生物。
Priority Applications (6)
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AU2016276482A AU2016276482A1 (en) | 2015-06-12 | 2016-06-06 | Use of composition of vitamin complex in preparing drug for stimulating gastrointestinal system motility |
US15/735,568 US10881639B2 (en) | 2015-06-12 | 2016-06-06 | Use of composition of multivitamin in preparing drug for stimulating gastrointestinal system motility |
CA2989214A CA2989214A1 (en) | 2015-06-12 | 2016-06-06 | Use of composition of multivitamin in preparing drug for stimulating gastrointestinal system motility |
JP2017564367A JP2018521031A (ja) | 2015-06-12 | 2016-06-06 | 胃腸系運動を刺激するための薬物の製造におけるマルチビタミン組成物の使用 |
EP16806787.4A EP3308787A4 (en) | 2015-06-12 | 2016-06-06 | USE OF A VITAMIN COMPLEX COMPOSITION FOR THE PREPARATION OF A MEDICAMENT FOR STIMULATING THE MOTILITY OF THE GASTROINTESTINAL SYSTEM |
BR112017026834-5A BR112017026834A2 (zh) | 2015-06-12 | 2016-06-06 | [Use of the inventive name established by ISA under Rule 37.2] The use of a complex vitamin composition for the preparation of a medicament for promoting gastrointestinal motility |
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CN201510321294.2A CN106265696A (zh) | 2015-06-12 | 2015-06-12 | 使用复合维生素b、c组合物促进胃肠系统动力的方法 |
CN201510321294.2 | 2015-06-12 |
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US (1) | US10881639B2 (zh) |
EP (1) | EP3308787A4 (zh) |
JP (1) | JP2018521031A (zh) |
CN (2) | CN111803514A (zh) |
AU (1) | AU2016276482A1 (zh) |
BR (1) | BR112017026834A2 (zh) |
CA (1) | CA2989214A1 (zh) |
WO (1) | WO2016197889A1 (zh) |
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US20210393531A1 (en) * | 2018-04-28 | 2021-12-23 | Zensun (Shanghai) Science & Technology, Co., Ltd. | Composition of multivitamin for stimulating gastrointestinal system motility and preparation method therefor |
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CN108079008A (zh) * | 2016-11-23 | 2018-05-29 | 上海泽生科技开发股份有限公司 | 促进胃肠系统动力的复合维生素组合物 |
CN108567792A (zh) | 2017-03-07 | 2018-09-25 | 上海泽生科技开发股份有限公司 | 一种治疗阿尔茨海默病的复合维生素组合物 |
EP3801498A1 (en) * | 2018-06-08 | 2021-04-14 | DSM IP Assets B.V. | Methods and compositions to support the growth or maintenance of oxygen-sensitive bacteria in the gastrointestinal tract |
US20220023303A1 (en) * | 2018-12-11 | 2022-01-27 | Dsm Ip Assets B.V. | Use of riboflavin to benefit bowel health |
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US20080213395A1 (en) * | 2004-10-14 | 2008-09-04 | Adventures Plus Pty Ltd | Method for the Treatment of Gastrointestinal and Other Disorders with an Admixture of Vitamins |
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CN104337813A (zh) * | 2013-07-23 | 2015-02-11 | 上海泽生科技开发有限公司 | 使用维生素b组合物促进胃肠系统动力的方法 |
CN104256652A (zh) * | 2014-10-08 | 2015-01-07 | 李明刚 | 一种口服复合维生素纳米脂质体 |
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CN111803514A (zh) | 2020-10-23 |
AU2016276482A1 (en) | 2018-01-18 |
EP3308787A1 (en) | 2018-04-18 |
JP2018521031A (ja) | 2018-08-02 |
BR112017026834A2 (zh) | 2018-08-14 |
EP3308787A4 (en) | 2019-01-16 |
CN106265696A (zh) | 2017-01-04 |
CA2989214A1 (en) | 2016-12-15 |
US10881639B2 (en) | 2021-01-05 |
US20180353469A1 (en) | 2018-12-13 |
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