CN105636584A - Method for use of vitamin b composition to promote motility of gastrointestinal system - Google Patents

Method for use of vitamin b composition to promote motility of gastrointestinal system Download PDF

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CN105636584A
CN105636584A CN201480039758.4A CN201480039758A CN105636584A CN 105636584 A CN105636584 A CN 105636584A CN 201480039758 A CN201480039758 A CN 201480039758A CN 105636584 A CN105636584 A CN 105636584A
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vitamin
parts
composition
acid
biotin
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周明东
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Zensun Shanghai Science and Technology Ltd
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Zensun Shanghai Science and Technology Ltd
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
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    • A61K31/047Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
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    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41881,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
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    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4415Pyridoxine, i.e. Vitamin B6
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    • A61K31/00Medicinal preparations containing organic active ingredients
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/455Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A61K31/51Thiamines, e.g. vitamin B1
    • AHUMAN NECESSITIES
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/525Isoalloxazines, e.g. riboflavins, vitamin B2
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    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7135Compounds containing heavy metals
    • A61K31/714Cobalamins, e.g. cyanocobalamin, i.e. vitamin B12
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    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
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Abstract

The present invention relates to a vitamin B composition, and in particular to a vitamin B composition promoting motility of the gastrointestinal system. The present composition is suitable for the prevention and/or treatment of conditions or ailments related to deficiencies of gastrointestinal motility.

Description

Method for use of vitamin b composition to promote motility of gastrointestinal system
Promote the method for gastronintestinal system power using vitamin B composition
Technical field
The present invention relates to a kind of vitamin B composition, especially a kind of vitamin B composition of promotion gastronintestinal system power.Said composition is applied to prevention and/or treated and gastroenteritic power deficient related state or disease.Background technology
Now, people's life stress is generally increased, and rhythm of life is accelerated, and increasingly competitive, gastrointestinal distress or upset,gastro-intestinal person are more and more, and its cause is many, and its symptom is also had nothing in common with each other.
Stomach and intestine(Gastrointestinal, GI) power be via digestive system convey nutrients coordination neuromuscular process.It may participate in GERD, gastroparesis(For example, diabetic keratopathy and postoperative gastroparesis), IBS(IBS), intestinal obstruction and constipation(For example, feature or drug-induced constipation)Gastronintestinal system power to weaken be one of maximum health care burden of industrialized country.In view of the foregoing, effectively facilitate gastronintestinal system power be need badly and by as the progress in this area.
Functional dyspepsia FD(Fimctional dyspepsia) and chronic gastritis often have a symptoms such as abdominal fullness sense, epigastric pain, nausea, anorexia, gastrointestinal tract dyskinesis cause gastric emptying to be the major reason that this kind of symptom occurs.And gastrointestinal tract dyskinesis are easily caused IBS.Now the medicine for the treatment of gastroenteritic power has Metoclopramide, domperidone and Itopride.
The medicine for the treatment of gastrointestinal disease was many in the past, but the good effect and person of having no side effect is very few, can especially make long-term care effect, but improve very well gastrointestinal function promote gastroenteritic power and slow down upset,gastro-intestinal symptom medicine or health products it is even more few.
As described above(1) Metoclopramide, the medicine is dopamine receptor blockade medicine, with powerful central town Tuhe intestines and stomach excitation.The medicine can suppress pipe smooth muscle relaxation, gastrointestinal smooth muscle is increased cholinergic reaction, rapid gastric emptying, increase antrum portion phase activity.In addition, the medicine still irritates lactogen release.The more typical lethargic sleep of side effect of Metoclopramide, dysphoria, lassitude, the another medicine is heavy dose of or prolonged application may show as the symptom of parkinsonism because blocking dopamine receptor.(2) domperidone is periphery property dopamine-receptor antagonist, the wriggling and tension force of on the gastrointestinal tract can be promoted to recover normal, promote gastric emptying, increase antrum and duodenum bowel movement, coordinate the contraction of pylorus, while can also strengthen the wriggling of esophagus and the tension force of esophageal sphincter.Because it is poor to the penetration of blood-brain barrier, to intracerebral dopamine receptor almost without antagonism, the external report for thering is vein large bolus injection to cause epileptic attack(The country is without this preparation), but the medicine is a kind of strong lactogen release medicine, may cause menstrual disorder.(3) double action of the retardance of Itopride tool dopamine receptor and acetylcholine ester enzyme level, discharge by irritating endogenous acetylcholine and suppresses its hydrolysis and strengthen stomach and uodenal movement, promote gastric emptying, and have the effect of telling of moderate town.Old or elderly patient uses this medicine with caution.
Vitamin B is all water soluble vitamin, and majority is coenzyme, participates in the metabolism of sugar, protein and fat in vivo.
Vitamin B1 (thiamine)The effect of cholinesterase activity can be suppressed, be deficient in vitamin B1 when this enzymatic activity it is too high, acetylcholine(One of neurotransmitter)Considerable damage makes nerve conduction be affected, and may involve the secretion of gastrointestinal motility and digestive juice.Thiamines would generally be made as the relatively stable form such as hydrochloride or nitrate to use
(riboflavin 1 constitutes many important coenzyme to vitamin B2, participates in metabolism and releases energy:Help grows.It can maintain and improve The health of epithelial tissue, such as alimentary canal mucous membrane tissue.
Vitamin B3 (nicotinic acid)The coenzyme of dehydrogenase is constituted in vivo, vitamin B3 is the most persons of human body requirement in B family vitamin, it does not maintain the vitamin of digestive system health still, can mitigate gastrointestinal disorders yet.Nicotinic acid is converted into niacinamide in human body, and niacinamide is DPN and DPN I part, participates in HypercholesterolemicRats, the oxidizing process of tissue respiration and the process of carbohydrate anaerobic decomposition.
Vitamin B5 (pantothenic acid)Activity form be coacetylase, be acyl carrier in vivo, the symptom for the B5 that is deficient in vitamin has poor appetite, indigestion, is susceptible to suffer from duodenal ulcer.
Vitamin B6 includes 3 kinds of pyridoxol, pyridoxal and pyridoxamine, can mutual inversion of phases.Studies have reported that vitamin B6 can mitigate azithromycin to gastrointestinal side effect with azithromycin mixing intravenous infusion.
Deoxyadenosyl cobalamin is that vitamin B12 is primarily present form in vivo.The effect of it and folic acid is often interrelated.Folic acid has a variety of auxiliary chest forms in cell, has research prompting folic acid to have intervention effect, folate treatable atrophic gastritis, improvement pathology of gastric mucosa to gastrointestinal cancer.
Biotin side chain carboxyl group can be connected by amido link with the lysine residue of enzyme.Biotin is carboxyl carrier, also participates in vitamin B12, folic acid, the metabolism of pantothenic acid.
Choline bitartrate, which has, promotes phosphatide transformation, the operating for accelerating fat and choleretic effect;Inositol can promote cell metabolism, foster growth, improve a poor appetite.P-aminobenzoic acid(PABA) be actually folic acid a kind of composition, its effect in vivo is coenzyme, and it works to promote the metabolism of protein and the generation of haemocyte together with folic acid.
From mechanism of action, vitamin B would be possible to turn into a kind of medicine or health food of the new promotion gastronintestinal system power with higher-security, but up to the present also prove facilitation of the vitamin B to gastronintestinal system power without factual evidence, particularly under pathological state, treatment and adjustment effect of the vitamin B to gastronintestinal system motility disorder.Additionally, due to vitamin B, family member is numerous, and there is complementary relation, thus vitamin B into component selections and compatibility, treated or the medicine or health food of regulation gastronintestinal system motility disorder are most important for preparing.The content of the invention
A. summary of the invention
The present invention relates to the method for promoting gastronintestinal system power in the object for having this needs, wherein the object suffers from gastrointestinal system disorder(That is, dysfunction caused by deficiency disorder, illness, symptom or medicine or operation).This method includes applying the vitamin B complex composition of therapeutically effective amount to the object for having this needs.Signified vitamin includes its corresponding analog or derivative in the present invention, and such as vitamin B1 refers to thiamine and its analog or derivative;Vitamin B2 refers to riboflavin and its analog or derivative;Vitamin B3 refers to nicotinic acid and its analog or derivative;Vitamin B5 refers to pantothenic acid and its analog or derivative;Vitamin B6 refers to pyridoxol and its analog or derivative;Vitamin B7 is biotin and its analog or biology;Vitamin Β 9 refers to folic acid and its analog or derivative;Vitamin B12 refers to cyanocobalamin and its analog or derivative;Etc..In a preferred embodiment, vitamin Β races composition is to include vitamin B1 (thiamine), (the riboflavin of vitamin Β 2), (the nicotinic acid of vitamin Β 3), (the pantothenic acid of vitamin Β 5), vitamin Β 6, the composition of biotin.In a preferred implementation In scheme, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3
(nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid, biotin, choline bitartrate, the composition of inositol.In another further preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, vitamin B12, folic acid, biotin, choline bitartrate, the composition of inositol and p-aminobenzoic acid.
On the other hand, the invention provides a kind of composition, said composition includes the vitamin B complex composition and pharmaceutically acceptable carrier of effective dose.In a preferred embodiment, said composition includes the vitamin B1 (thiamine of effective dose), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, biotin and pharmaceutically acceptable carrier.In a further preferred embodiment, said composition includes the vitamin B1 (thiamine of effective dose), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid, biotin, choline bitartrate, inositol and pharmaceutically acceptable carrier.In another further preferred embodiment, said composition includes the vitamin B1 (thiamine of effective dose), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, vitamin B12, folic acid, biotin, choline bitartrate, inositol, p-aminobenzoic acid and pharmaceutically acceptable carrier.
On the other hand, the present invention relates to a kind of composition, said composition includes the vitamin B complex composition of effective dose and the treatment of effective dose and/or the medicine for preventing gastrointestinal disease.In a preferred embodiment, said composition includes the vitamin B1 (thiamine of effective dose), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, the treatment of biotin and effective dose and/or the medicine for preventing gastrointestinal disease.In a further preferred embodiment, said composition includes the vitamin B1 (thiamine of effective dose), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid, biotin, choline bitartrate, the treatment of inositol and effective dose and/or the medicine for preventing gastrointestinal disease.In another further preferred embodiment, said composition includes vitamin B1 (thiamine), the vitamin B2 (riboflavin of effective dose), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, vitamin B12, folic acid, biotin, choline bitartrate, inositol, the treatment of p-aminobenzoic acid and effective dose and/or the medicine for preventing gastrointestinal disease.
On the other hand, the present invention relates to a kind of composition, said composition includes the vitamin B complex composition of effective dose and the group vitamins compound of other effective dosies.In a preferred embodiment, said composition includes the vitamin B1 (thiamine of effective dose), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, the group vitamins compound of biotin and other effective dosies.In a further preferred embodiment, said composition includes vitamin B1 (thiamine), the vitamin B2 (riboflavin of effective dose), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid, biotin, choline bitartrate, the group vitamins compound of inositol and other effective dosies.In another further preferred embodiment, said composition includes vitamin B1 (thiamine), vitamin B2 (riboflavin), the vitamin B3 (nicotinic acid of effective dose), vitamin B5 (pantothenic acid), vitamin B6, vitamin B12, folic acid, biotin, choline bitartrate, inositol, the group vitamins compound of p-aminobenzoic acid and other effective dosies.Other described group vitamins compounds include compound and its analog or the derivatives such as vitamin eight, vitamin C, vitamin D, vitamin E, vitamin K.
Gastroenteritic power is promoted to be used to treat drug-induced gastrointestinal dysfunction in the object for have this needs(For example, intestinal dysfunction that opioid drug, such as morphine cause or constipation)Method in, this method include apply therapeutically effective amount dimension give birth to Plain B races composition.The object can carry out postoperative pain control using opioids or opioid or chronic ache is controlled.The example of opioids and opioid includes morphine, codeine, Oxycodone, hydrocodone(hydrocod0ne), methadone(Methadone), fentanyl() and itself and antiinflammatory fentanyl(Such as paracetamol or aspirin)Combination.In a preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, the composition of biotin.In a further preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid, biotin, choline bitartrate, the composition of inositol.In another further preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, vitamin B12, folic acid, biotin, choline bitartrate, the composition of inositol and p-aminobenzoic acid.
Gastroenteritic power is promoted to can be used for treating gastroparesis in the object for having this needs, it passes through the vitamin B race composition using therapeutically effective amount.In a preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, the composition of biotin.In a further preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid, biotin, choline bitartrate, the composition of inositol.In another further preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, vitamin B12, folic acid, biotin, choline bitartrate, the composition of inositol and p-aminobenzoic acid.
In another embodiment, gastroenteritic power is promoted to be used in the object for have this needs treat GERD(Gastro esophageal reflux disease, GERD) method in, this method include apply therapeutically effective amount vitamin B complex composition.In a preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, the composition of biotin.In a further preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3
(nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid, biotin, choline bitartrate, the composition of inositol.In another further preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2
(riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, vitamin B12, folic acid, biotin, choline bitartrate, the composition of inositol and p-aminobenzoic acid.In a specific embodiment, the GERD is nocturnal gastroesophageal reflux disease.
Present invention also offers promote gastroenteritic power in the object for having this needs to treat IBS(Irritable bowel syndrome, IBS) method, it is realized by applying the vitamin B complex composition of therapeutically effective amount.In a preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3
(nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, the composition of biotin.In a further preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid, biotin, choline bitartrate, the composition of inositol.In another further preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin)、 Vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, vitamin B12, folic acid, biotin, choline bitartrate, the composition of inositol and p-aminobenzoic acid.The IBS can be constipation-predominant of irritable bowel syndrome or constipation/diarrhoea alternate type IBS.
Present invention also offers method of the gastroenteritic power to treat constipation is promoted in the object for having this needs, it is realized by applying the vitamin B complex composition of therapeutically effective amount.The constipation includes feature(Bad life habits, eating habit, senile constipation of the grade without organic cause)With drug-induced constipation.In a preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, the composition of biotin.In a further preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, vitamin B12, folic acid, biotin, choline bitartrate, the composition of inositol.In another further preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid, biotin, choline bitartrate, the composition of inositol and p-aminobenzoic acid.
In one embodiment, promotion gastroenteritic power be used to treat in the object for have this needs is caused or related gastrointestinal dysfunction by operation(For example postoperative intestine is wriggled and slowed down)Method in, this method include apply therapeutically effective amount vitamin B race composition.In a preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, the composition of biotin.In a further preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid, biotin, choline bitartrate, the composition of inositol.In another further preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, vitamin B12, folic acid, biotin, choline bitartrate, the composition of inositol and p-aminobenzoic acid.
It is preferred that vitamin B complex composition be include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, the composition of biotin.Preferred vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, folic acid, biotin, choline bitartrate, the composition of inositol.In another further preferred embodiment, vitamin B complex composition is to include vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6, vitamin B12, folic acid, biotin, choline bitartrate, the composition of inositol and p-aminobenzoic acid.
The formulation of the vitamin B complex composition of the present invention can be chewable tablet, but not limited to this, the present composition can also add various customary adjuvants required when preparing different dosage forms, such as disintegrant, lubricant, adhesive, antioxidant, complexing agent pharmaceutical carrier, any conventional peroral dosage form, such as other formulations of dispersible tablet, granule, capsule, oral liquid are made with conventional formulation method.
The vitamin B complex composition of the present invention, the weight proportion of its each component can have multiple choices, and it has corresponding facilitation to gastronintestinal system power.In certain embodiments, it can include the component of following weight proportion:10 parts of vitamin B l, 10-15 parts of vitamin B2s, 6-25 parts of vitamin B3s, 10-100 parts of vitamin B5s, 5-10 parts of vitamin B6s and 0.01-0.1 parts of biotins.In a preferred embodiment, vitamin B complex composition includes the component of following weight proportion:10 parts of vitamin B l, 15 parts of vitamin B2s, 25 parts of vitamin B3s, 100 parts of vitamin B5s, 10 parts of vitamin B6s and 0.1 part of biotin.In a further preferred embodiment, vitamin B complex composition includes the component of following weight proportion:10 parts of vitamin B l, 15 parts of vitamin B2s, 25 parts of vitamin B3s, 100 parts of vitamin B5s, 10 parts of vitamin B6s, 0.1 part of biotin, 0.4 part of folic acid, 250 parts of choline bitartrates and 250 parts of inositols.In another further preferred embodiment, vitamin B complex composition includes the component of following weight proportion:10 parts of vitamin B l, 15 parts of vitamin B2s, 25 parts of vitamin B3s, 100 parts of vitamin B5s, 10 parts of vitamin B6s, 0.1 part of biotin, 0.4 part of folic acid, 250 parts of choline bitartrates, 250 parts of inositols, 0.025 part of vitamin B12 and 50 parts of p-aminobenzoic acid.
B. define
Except as otherwise definition, all scientific and technical terminologies used herein understand that implication is identical with general technical staff of the technical field of the invention.All patent documents, Patent Application Publication, disclosed patent document and other publications are as reference.This section illustrate definition with above-mentioned bibliography as described in definition it is inconsistent or opposite when, be defined by the definition that this section is illustrated.
Unless clearly indicated that within a context, " one " as used herein means " at least one " or " one or more than one ".
Term " part ", more particularly to one given amount, refers to amount of the positive and negative deviation within 10%.Term used herein " is included(Comprises) ", " include(Comprising) ", " include(Includes) ", " include(Including) ", " contain(Contains),, " contain(Containing) " and its any variant is intended to non-monopolistic inclusion, for example including, include or contain the composition of process, method, converted products or the material of a kind of element or the element of a list not only includes intrinsic other elements that those elements are also possible that the composition of the do not list clearly or process, method, converted products or material.Terminology used herein " vitamin B complex composition " includes all vitamin B compounds, its analog or derivative, such as vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid)With vitamin B6 etc..Terminology used herein " analog " refers to that structure is roughly the same and has identical bioactivity but can have different degrees of active any two above molecule or wherein fragment.Term " derivative " used refers to that hydrogen atom or atomic group in compound are replaced and derivative more complicated compound by other atoms or atomic group.
Embodiment
The vitamin B complex composition specific formula of embodiment 1 Vitamin B complex composite formula 1 includes the component of following weight proportion:10 parts of vitamin B l, 15 parts of vitamin B2s, 25 parts of vitamin B3s, 100 parts of vitamin B5s, 10 parts of vitamin B6s and 0.1 part of biotin.Vitamin B complex composite formula 2 includes the component of following weight proportion:10 parts of vitamin B l, 15 parts of vitamin B2s, 25 parts of vitamin B3s, 100 parts of vitamin B5s, 10 parts of vitamin B6s, 0.1 part of biotin, 0.4 part of folic acid, 250 parts of choline bitartrates and 250 parts of inositols.Vitamin B complex composite formula 3 includes the component of following weight proportion:10 parts of vitamin B l, 15 parts of vitamin B2s, 25 parts of vitamin B3s, 100 parts of vitamin B5s, 10 parts of vitamin B6s, 0.1 part of biotin, 0.4 part of folic acid, 250 parts of choline bitartrates, 250 parts of inositols, 0.025 part of vitamin B12 and 50 parts of p-aminobenzoic acid.Vitamin B complex composite formula 4 includes the component of following weight proportion:10 parts of vitamin B1s, 15 parts of vitamin B2s, 25 parts of vitamin B3s, 100 parts of vitamin B5s, 10 parts of vitamin B6s, 0.1 part of biotin, 0.4 part of folic acid, 250 parts of choline bitartrates, 250 parts of inositols and 0.025 part of vitamin B12.
The vitamin B complex composition of embodiment 2 causes the therapeutic action of mice with constipation to Loperamide
1. experiment material
1.1 medicine
Vitamin B complex composition(VB 1) is formulated, 2 and formula 3 are formulated
Loperamide(Loperamide):Sigma companies, lot number: 109K1107V
Naloxone:Beijing Sihuan Pharmaceutical Co., Ltd, lot number: 20110505
1.2 animal
C57BL/6 mouse, female, 18 ~ 22g of body weight
2. experimental method
The preparation of 2.1 prepared Chinese ink:
Arabic gum 100g accurately is weighed, add water 800ml, boil transparent to solution, weighed activated carbon powder 50g and add and boiled 3 times in above-mentioned solution, the constant volume that added water after solution is cool is to 1000ml.
2.2 Loperamides cause Constipated mice to prepare
Loperamide is with 1% Tween 80 physiological saline solution, and mouse was to fasting before Loperamide 24 hours(It can't help water)Afterwards, it is disposable that the Loperamide for giving that dosage is 5mg/kg is subcutaneously injected.After 30 minutes, gavage gives prepared Chinese ink.Administered volume is 10ml/kg.2.3 packets and administration
To 60 minutes before prepared Chinese ink, administration group gavage gave VB, and positive controls gavage gives naloxone, and other groups are given physiological saline. Administered volume is 20ml/kg body weight.
Control group:Gavage gives normal saline
Model group:Gavage gives normal saline
Naloxone group:Gavage gives naloxone 50mg/kg
Each dosage group:Gavage is given (is converted into the amount of mouse according to formula 1-3)
2.4 observation item
After gavage gives prepared Chinese ink 20 minutes, de- cervical vertebra puts to death animal, abdominal cavity separation mesenterium is opened immediately, intestinal tube of the clip upper end from pylorus, lower end to ileocecus, it is placed on pallet, small intestine is gently pulled into straight line, measures total small intestinal length, length is promoted from pylorus to prepared Chinese ink forward position for prepared Chinese ink, small intestine ink progradation is calculated.
3. experimental result
Each formulation data is as follows:
Group body weight (g) small intestinal length (cm) prepared Chinese ink advance distance (cm) Intestinal propulsive rate (%) model group(n=8) 16.5±0.7 19.3±1.6 5.7±0.7 29.9±5.5
Naloxone group(n=8) 16.1±0.4 16.8±1.5** 7.6±1.7* 44.8±8.1** It is formulated 3 30.8mg/kg (n=8) 16.3 ± 07 19.8,41.9 ± 5.7** of ± 1.2 8.3 ± 1.0**
It is formulated 3 153.8mg^g (n=8) 16.4 ± 0.3 19.9,42.6 ± 9.2** of ± 1.7 9.2 ± 2.1**
It is formulated 3 768.7mg kg (n=8) 16.3 ± 0.9 20.1,43.8 ± 10.5** of ± 1.3 9.6 ± 2.2**
Normal group(n=8) 16.3±0.7 19.3±1.8 11.8±2.7** 61.2±11.3**
*:Compared with model group, P<0.05; **:Compared with model group, PO.01
It can be seen that from data above, formula 1-3 has corresponding facilitation to the gastroenteritic power of mouse, and be in increasing trend with the increase of application dosage.The vitamin Β race's compositions of embodiment 3 cause the influence of mice with constipation bowel relaxing functions to Loperamide
1. experiment material
1.1 medicine
Vitamin Β races composition(VB 3) are formulated
Loperamide(Loperamide):Sigma companies, lot number:The animals of 109K1107V 1.2
C57BL/6 mouse, male, the 24g of body weight 18
2. experimental method
Influence of 2.1 vitamin B compounds to normal mouse bowel relaxing functions
Mouse is randomly divided into four groups, and administration group gavage gives compound VB formulas 3, and other groups are given drinking water.Administered volume is 20ml/kg body weight.
Vitamin B compound group low dose group(A groups):Normal mouse gavage gives VB formula 3 153.8mg/kg (n=14) vitamin B compound group middle dose groups(B groups):Normal mouse gavage gives VB formula 3 768.7mg/kg (n=14) vitamin B compound group middle dose groups(C groups):Normal mouse gavage gives VB formula 3 3843.7mg/kg (n=14) normal groups(D groups):Normal mouse gavage gives equivalent drinking water(n=14)
Administration terminates to start after timing, timing 7hl5min, takes off cervical vertebra and puts to death animal, records body weight, body weight at the end of experiment, 7hl5min defecation quantity and defecation dry weight before every mouse administration(60°C,6h).
2.2 vitamin B compounds cause the influence of mice with constipation bowel relaxing functions to normal mouse and Loperamide
Mouse is randomly divided into three groups, and administration group gavage gives compound VB formulas 3, and other groups are given drinking water.Administered volume is 20ml/kg body weight.
Model group(A groups):Mice with constipation gavage gives equivalent drinking water(n=10)
Vitamin B compound group(B groups):Mice with constipation gavage gives VB and is formulated 3 768.7mg/kg (n=10)
Control group(C groups):Normal mouse gavage gives equivalent drinking water(n=10)
It is administered after 60min and uses Loperamide gavage modeling.Loperamide drinking water dissolves, and gavage gives dosage for 4mg/kg, administration Volume is 10ml/kg.After modeling 15 minutes, start timing, mouse single cage word is supported, and water is can't help in fasting.After timing 6h, take off cervical vertebra and put to death animal, record body weight, body weight at the end of experiment, 6h defecation quantity and defecation dry weight (60 before every mouse administration.C, 6h).
3. experimental result
Influence of 3.1 vitamin B compounds to normal mouse bowel relaxing functions
A groups are compared with D groups, and defecation grain number is not significantly different, and there were significant differences for defecation dry weight(P<0.05), show that low dosage is combined VB and can dramatically increase the defecation dry weight of mouse, but defecation grain number can not be significantly increased;B groups, C groups are compared with D groups, and there were significant differences for defecation grain number and defecation dry weight(P<0.01, P<0.01 ; P<0.01 , P<0.01), show that compound VB middle dosages and high dose can dramatically increase the defecation quantity and defecation dry weight in normal mouse 7M5min.Germicidal efficacy also found that the appearance of high dose mouse is just dilute simultaneously, thus it is speculated that be probably the toxic side effect for medicine occur.Result data is as follows:
Influence of the various dose vitamin B compound to normal mouse bowel relaxing functions
*:Compared with normal group, PO.05: **:Compared with normal group, PO.01
3.2 vitamin B compounds cause the influence of mice with constipation bowel relaxing functions to normal mouse and Loperamide(For the first time)
C groups are compared with A groups, and there were significant differences for defecation grain number and defecation dry weight(P<0.01, P<0.01), show that Constipated mice is successfully prepared;B groups are compared with A groups, and there were significant differences for defecation grain number and defecation dry weight(PO.01 , P<0.05), show that compound VB can dramatically increase Loperamide and cause defecation quantity and defecation dry weight in mice with constipation 6 hours.Result data is as follows:
*:Compared with model group, Ρ<0.05; **:Compared with model group, Ρ<0.01
3.3 B B-complex Β cause the influence of mice with constipation bowel relaxing functions to normal mouse and Loperamide(Second) C groups are compared with A groups, and there were significant differences for defecation grain number and defecation dry weight(P<0.01, P<0.01), show that Constipated mice is successfully prepared;B groups are compared with A groups, and there were significant differences for defecation grain number and defecation dry weight(P<0.05, P<0.05), show that compound VB can dramatically increase Loperamide and cause defecation quantity and defecation dry weight in mice with constipation 6 hours.Result data is as follows:
Vitamin B compound causes the influence of mice with constipation bowel relaxing functions to Loperamide(Second)
*:Compared with model group, P<0.05 ; **:Compared with model group, PO.01
As can be seen here, 3 pairs of normal mouses of vitamin B compound formula and Loperamide cause mice with constipation bowel relaxing functions to have significant facilitation.The vitamin B complex composite formula 3 of embodiment 4 and 4 pairs of Loperamides cause the therapeutic action of mice with constipation to compare
1. experiment material
1.1 medicine
Vitamin B complex composition(VB) formula 3 and formula 4
Loperamide(Loperamide):Sigma companies, lot number: 109K1107V
Naloxone:Beijing Sihuan Pharmaceutical Co., Ltd, lot number: 20110505
1.2 animal
C57BL/6 mouse, female, the g of body weight 17 20
2. experimental method
The preparation of 2.1 prepared Chinese ink:
Arabic gum 100g accurately is weighed, add water 800ml, boil transparent to solution, weighed activated carbon powder 50g and add and boiled 3 times in above-mentioned solution, the constant volume that added water after solution is cool is to 1000ml.
2.2 Loperamides cause Constipated mice to prepare
Loperamide is with 1% Tween 80 physiological saline solution, and mouse was to fasting before Loperamide 24 hours(It can't help water)Afterwards, it is disposable that the Loperamide for giving that dosage is 5mg/kg is subcutaneously injected.After 30 minutes, gavage gives prepared Chinese ink.Administered volume is 10ml/kg.2.3 packets and administration
To 60 minutes before prepared Chinese ink, administration group gavage gave VB, and positive controls gavage gives naloxone, and other groups are given physiological saline.Administered volume is 20ml/kg body weight.
Control group:Gavage gives normal saline Model group:Gavage gives normal saline
Naloxone group:Gavage gives the mg/kg of naloxone 50
Each dosage group:Gavage is given (is converted into the amount of mouse according to formula 3-4)
2.4 observation item
After gavage gives prepared Chinese ink 20 minutes, de- cervical vertebra puts to death animal, abdominal cavity separation mesenterium is opened immediately, intestinal tube of the clip upper end from pylorus, lower end to ileocecus, it is placed on pallet, small intestine is gently pulled into straight line, measures total small intestinal length, length is promoted from pylorus to prepared Chinese ink forward position for prepared Chinese ink, i calculates small intestine ink progradation.
3. experimental result
Each formulation data is as follows:
Various dose VB formulas cause the influence of mice with constipation Intestinal propulsive rate to Loperamide
*:Compared with model group, PO.05; **:Compared with model group, P<0.01 result is shown:Compared with normal group, the Intestinal propulsive rate (%) of model group is significantly reduced(46.9 ± 7.3 VS 15.5 ± 2.8), show that Constipated mice is successfully prepared;Compared with model group, the prepared Chinese ink advance distance and Intestinal propulsive rate (%) of each administration group dramatically increase (p<0.01);It is basically identical that compound VB is formulated 3 and compound VB, 4 action effects in terms of mouse small intestine propulsion rate (%) is improved of formula(25.9±4.5VS24.9±3.7).
Conclusion:Test sample vitamin B compound formula 3 and vitamin B compound formula 4 can significantly improve the Intestinal propulsive rate (%) of the mice with constipation model of Loperamide induction, and the action effect of the two is basically identical.In order to more clearly describe and understand the present invention, the present invention is described in detail in we by way of example, but it will be apparent that those of ordinary skill can make appropriate be altered or modified on the premise of without departing substantially from spirit and scope by the claims to the present invention in the art.

Claims (25)

  1. Claims
    1. a kind of vitamin B complex composition, it can be used for prevention and/or treats and gastronintestinal system power deficient related state or disease.
    2. composition according to claim 1, wherein the vitamin B complex composition includes vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6 and biotin.
    3. composition according to claim 1 or 2, wherein the vitamin B complex composition also includes folic acid, choline bitartrate and inositol.
    4. any combination thing according to claim 1-3, wherein the vitamin B complex composition also includes vitamin B12 and/or p-aminobenzoic acid.
    5. composition according to claim 1, wherein the gastronintestinal system power scarcity is due to using caused by opioid.
    6. composition according to claim 5, wherein the opioid is selected from morphine, codeine, Oxycodone, Hydromorphone, hydrocodone, methadone and fentanyl.
    7. composition according to claim 1, wherein the state or disease include feature or drug-induced constipation, the gastroparesis related to diabetes or idiopathic gastroparesis, GERD, IBS or postoperative intestine are wriggled and slowed down.
    8. any combination thing according to claim 14, it is characterised in that it includes the vitamin B complex composition and pharmaceutically acceptable carrier of effective dose.
    9. any combination thing according to claim 14, it is characterised in that its medicine for including the vitamin B complex composition of effective dose and the treatment of effective dose and/or preventing gastrointestinal disease.
    10. any combination thing according to claim 1-4, it is characterised in that it includes the vitamin B complex composition of effective dose and the vitamin compound of other effective dosies.
    11. any combination thing according to claim 10, wherein described vitamin compound is selected from vitamin A, C, D, E and K one or more.
    12. any combination thing according to claim 1-4, it is characterised in that formulation is chewable tablet.
    13. any combination thing according to claim 1-4, it is characterised in that formulation can also be dispersible tablet, granule, capsule and oral liquid.
    14. composition according to claim 2, it is characterised in that it includes the component of following weight proportion:10 parts of vitamin B1s, 15 parts of 2,25 parts of vitamin Β, 3,100 parts of vitamin Β vitamin Β, 5,10 parts of vitamin Β 6 and 0.1 part of biotin.
    15. composition according to claim 3, it is characterised in that it includes the component of following weight proportion:10 parts of vitamin B1s, 15 parts of 2,25 parts of vitamin Β, 3,100 parts of vitamin Β, 5,10 parts of vitamin Β, 6,0.1 part of vitamin Β biotins, 0.4 part of folic acid, 250 parts of choline bitartrates and 250 parts of inositols.
    16. composition according to claim 4, it is characterised in that it includes the component of following weight proportion:10 parts of vitamin B1s, 15 parts of vitamin B2s, 25 parts of vitamin B3s, 100 parts of vitamin B5s, 10 parts of vitamin B6s, 0.1 part of biotin, 0.4 part of folic acid, 250 parts of choline bitartrates, 250 parts of inositols, 0.025 part of vitamin B12.
    17. composition according to claim 4, it is characterised in that it includes the component of following weight proportion:10 parts of vitamin B1s, 15 parts of vitamin B2s, 25 parts of vitamin B3s, 100 parts of vitamin B5s, 10 parts of vitamin B6s, 0.1 part of biotin, 0.4 part of folic acid, 250 parts of choline bitartrates, 250 parts of inositols, 0.025 part of vitamin B12 and 50 parts of p-aminobenzoic acid.
    18. a kind of vitamin B complex composition is preparing treatment and/or prevented and the purposes in the deficient related gastrointestinal condition of gastronintestinal system power or the medicine or health food of disease.
    19. purposes according to claim 18, wherein the vitamin B complex composition includes vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (nicotinic acid), vitamin B5 (pantothenic acid), vitamin B6 and biotin.
    20. the purposes according to claim 18 or 19, wherein the vitamin B complex composition also includes folic acid, choline bitartrate and inositol.
    21. any purposes according to claim 18-20, wherein the vitamin B complex composition also includes vitamin B12 and p-aminobenzoic acid.
    22. purposes according to claim 18, wherein the gastronintestinal system power scarcity is due to using caused by opioid.
    23. purposes according to claim 22, wherein the opioid is selected from morphine, codeine, Oxycodone, Hydromorphone, hydrocodone, methadone and fentanyl.
    24. purposes according to claim 18, wherein the state or disease include feature or drug-induced constipation, the gastroparesis related to diabetes or idiopathic gastroparesis, GERD, IBS or postoperative intestine are wriggled and slowed down.
    25. purposes according to claim 18, wherein described medicine or health food its subject are people.
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CN113498862A (en) * 2021-08-27 2021-10-15 上海英库商务咨询有限公司 Diet formula capable of preventing beriberi, herpes and corner inflammation and losing weight
CN115105514A (en) * 2022-06-14 2022-09-27 邯郸制药股份有限公司 Pharmaceutical composition for protecting gastric mucosa and treating gastric ulcer and preparation method and application thereof
CN115105514B (en) * 2022-06-14 2024-03-15 邯郸制药股份有限公司 Pharmaceutical composition for protecting gastric mucosa and treating gastric ulcer as well as preparation method and application thereof

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