CN108175772A - A kind of pharmaceutical composition with antiobesity action and preparation method thereof - Google Patents
A kind of pharmaceutical composition with antiobesity action and preparation method thereof Download PDFInfo
- Publication number
- CN108175772A CN108175772A CN201611123703.9A CN201611123703A CN108175772A CN 108175772 A CN108175772 A CN 108175772A CN 201611123703 A CN201611123703 A CN 201611123703A CN 108175772 A CN108175772 A CN 108175772A
- Authority
- CN
- China
- Prior art keywords
- vitamin
- pharmaceutical composition
- colesevelam
- weight
- silica
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
- A61K31/07—Retinol compounds, e.g. vitamin A
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/255—Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
- A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
- A61K31/355—Tocopherols, e.g. vitamin E
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/74—Synthetic polymeric materials
- A61K31/785—Polymers containing nitrogen
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Emergency Medicine (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention relates to pharmaceutical technology field more particularly to a kind of pharmaceutical compositions and preparation method with antiobesity action.Pharmaceutical composition is prepared by the raw material for including following component：Colesevelam, vitamin E, vitamin A, vitamin K1 and pharmaceutic adjuvant are further prepared by colesevelam, vitamin E, vitamin A, vitamin K1 and microcrystalline cellulose, silica, magnesium stearate.The pharmaceutical composition of the present invention combines colesevelam with vitamin E, vitamin A, vitamin K1, for the treatment of obese patient, cholic acid, serum total cholesterol, serum triglyceride and low density lipoprotein cholesterol can be reduced, also there is antioxidant and anti-aging simultaneously, improve the good result of patients ' life quality.
Description
Technical field
The present invention relates to pharmaceutical technology field more particularly to a kind of pharmaceutical compositions and its preparation side with antiobesity action
Method.
Background technology
With social development, the raising of living standards of the people, adult is because more foods or amount of exercise are fat caused by reducing
Into universal phenomenon.And people pursue U.S., the hope for pursuing health is but very strong always.Therefore various slimming drugs come into being,
While weight-reducing, many adverse reactions can be generated to body.
Most common slimming drugs mainly have three classes currently on the market:One kind is appetite inhibitor, and one kind is that metabolism is accelerated to subtract
Few absorbent, the another kind of preparation for being to aid in consumption fat and heat.Appetite inhibitor drug effect is come in central nervous system
Appetite-suppressing, it is quite big to the side effect of body, it is best；It is to allow the thing eaten not to accelerate metabolism, reduce absorbent drug
It being absorbed by the body or drains as early as possible and absorbed with reducing, the summation for reducing body intake heat achievees the purpose that weight reducing, relative to
Appetite inhibitor risk is smaller, but it is not small to take still hidden danger for a long time；It helps to consume the fatty preparation with heat, you is made to take the photograph daily
The energy entered is identical, but consumption greatly increases, and can naturally also play the role of loss of weight of reducing weight, this is also to act on central nervous system
The drug of system, potential risk are very big.Such as amphetamine (Amphetamine) appetite-suppressing, promote consumption fat and heat.Clothes
With the initial stage of this medicine, excitement, is not desired to sleep at night, and the thing eaten significantly reduces, also peculiar spirit, but with medication time
Extend, it may appear that emotional instability, vainly hope, hallucinate, sleeping there are the mental symptoms such as obstacle.
Clinical test shows that slimming drugs Reductil can increase user and suffer from a heart complaint and the risk of apoplexy, slimming drugs production
Yi Jiangqiche cities of Abbott of the quotient U.S.；Using slimming drugs appetite inhibitor fenfluramine hydrochloride have occur damaged heart valve and
The risk of pulmonary hypertension, fenfluramine hydrochloride have withdrawn from China market (including bulk pharmaceutical chemicals).
Safety currently on the market is also belonged to and is not absorbed substantially in vivo preferably using OTC drugs as orlistat, by
Enteron aisle inhibits fat hydrolase, and body is hindered to reach weight-reducing purpose to the absorption of fat.But also because there may be bad
Reaction obtains the revised comment book warning of FDA：By on December 31st, 2010, national drug adverse reaction monitoring center case
More than 120 example of case report in relation to orlistat, main adverse reaction show as constipation, abdominal pain, diarrhea, head in report database
Dizzy, paramenia, fash etc..On September 1st, 2010, State Food and Drug Administration's publication《About revision orlistat system
The notice of agent specification》(state food medicine prison note [2010] No. 359), required at home to orlistat preparation description into
Row update, adds in relevant warning.
Can not only it lose weight but also good medicine that safe and healthy drug is just dreamed of into people.It is generally believed that overweight people's body
The quantity of fat cell hypertrophy does not increase, and is only showed only as the volume increase of adipocyte.Fat patient generally all especially happinesses
Joyous to eat sweet food or fried based food and heavy, this kind of patient often just causes obesity after adult because of overnutrition,
Therefore also known as Adult Onset obesity.Fat development can be efficiently controlled using weight-reducing by dieting therapy.But obesity is suffered from
It is very universal that person crosses drink overfeeding phenomenon.
Invention content
In order to solve the above technical problem, the present invention provides a kind of pharmaceutical composition with antiobesity action, by wrapping
The raw material for including following component is prepared：Colesevelam, vitamin E, vitamin A, vitamin K1 and pharmaceutic adjuvant.
Preferably, the weight ratio of the colesevelam, vitamin E, vitamin A, vitamin K1 and pharmaceutic adjuvant is 1000：
10-30：1-3：0.1-1：210-415.
Preferably, the colesevelam be carbonic acid colesevelam or colesevelam hydrocholoride, the proportioning meter with other supplementary materials
In calculation in terms of colesevelam.
Preferably, the mixture that the pharmaceutic adjuvant is microcrystalline cellulose, silica and magnesium stearate form.
Further, the weight ratio of microcrystalline cellulose, silica and magnesium stearate is 200- in the pharmaceutic adjuvant
400：10-30：5-15.
The present invention provides a kind of optimization formula of described pharmaceutical composition, by weight, by including following weight
The raw material of part is prepared：
The parts by weight are the unit of weights well known in the art such as μ g, mg, g, kg or are its multiple, such as 1/100,1/10,
10 times, 100 times etc..
It is further preferred that it by weight, is prepared by the raw material for including following parts by weight：
Preferably, pharmaceutical composition of the present invention is the solid pharmaceutical preparations such as ordinary tablet, capsule or granule.
The present invention also provides a kind of methods for preparing aforementioned pharmaceutical compositions, that is, by the vitamin E, vitamin A
After being absorbed with vitamin K1 with silica, it is uniformly mixed with colesevelam, microcrystalline cellulose, silica, magnesium stearate, point
Be packed into capsule to get.
(3) advantageous effect
The above-mentioned technical proposal of the present invention has the advantages that：The pharmaceutical composition of the present invention is by colesevelam with tieing up
Raw element E, vitamin A, vitamin K1 joint, for the treatment of obese patient, while also have anti-aging, improve minimal invasive treatment's matter
The good result of amount.Joined by Pre-clinical animal studies studies have shown that colesevelam and vitamin E, vitamin A, vitamin K1
It closes application to maximize favourable factors and minimize unfavourable ones, shows excellent synergistic effect, dropped in cholic acid and the grease of performance colesevelam absorption enteron aisle
Low blood fat, while reaching fat-reducing effect, cooperation vitamin E, vitamin A, vitamin K1 are taken, and supplement and are adsorbed by colesevelam
Vitamin E, vitamin A, the vitamin K1 of removing play the antioxidation of vitamin E, vitamin A, vitamin K1, prevent
Unrighted acid peroxidating prevents the formation of lipofuscin from reaching and builds up health, the effect of anti-aging.
Specific embodiment
Embodiments of the present invention are described in further detail with reference to embodiment.Following embodiment is used to illustrate this
Invention, but cannot be used for limiting the scope of the invention.
Embodiment 1
A kind of pharmaceutical composition with antiobesity action is present embodiments provided, by the component preparation of following parts by weight
Into：
The present embodiment provides the preparation method of the pharmaceutical composition simultaneously：By the vitamin E, vitamin A, dimension of recipe quantity
Raw element K1 is uniformly mixed after being absorbed with silica with colesevelam, microcrystalline cellulose, silica, magnesium stearate, is distributed into
Capsule to get.
Embodiment 2
A kind of pharmaceutical composition with antiobesity action is present embodiments provided, by the component preparation of following parts by weight
Into：
Test example 1
High lipid food feeding " nutritive obesity in rats mould is established according to literature method to the weight of nutritive obesity in rats
Type " observes compound preparation of the present invention to the weight of the nutritive obesity rat, Lee's indexes, blood fat, Serum Vitamin
E, the influence of vitamin A, vitamin K1 level and serum lipofuscin (LPO).
High lipid food feeding ablactation rat causes rat auxotype obese model after 12 weeks.The present invention is significantly inhibiting
Rat body weight increases, and while reducing blood fat, and can improve Serum Vitamin E, vitamin A, vitamin K1 level, reduce serum
Lipofuscin is horizontal, and weight-reducing plays antioxidant and anti-aging effect again simultaneously.
The colesevelam hydrocholoride (Colesevelam) of the present invention is one of the common drugmaker's exploitation of Japan one or three non-absorbing
Property bile acid sequestrant class fat-reducing medicament, it with the cholic acid in enteron aisle can be combined and be substantially reduced the re-absorption of the latter, as drink
The complementary therapy of food and kinesiatrics.Colesevelam hydrocholoride in enteron aisle by, with cholic acid Irreversible binding, making cholic acid in enteron aisle
Interior resorption is received to reduce to be increased with the cholic acid that excrement is discharged from enteron aisle, liver cell is promoted to increase the synthesis of cholic acid, due to cholic acid
Exhaustion can improve the balance that cholesterol is converted into cholic acid, therefore can be used for reducing cholesterol concentration, while stimulate by feedback mechanism
Liver cell accelerates the synthesis of ldl receptor, and the combination of LDL increases in blood, so as to make the content of LDL and T-CHOL in blood
It reduces.And pass through the level of the formation increase HDL-C of HDL-C in enteron aisle.Colesevelam hydrocholoride is suitable for except homozygote familial
Any kind of hypercholesterolemia other than hypercholesterolemia is unknown to any kind of hypertriglyceridemia effect
It is aobvious.The treatment of all raised combined hyperlipidemia to Triglycerides in Serum and cholesterol, must be with other kinds of reducing blood lipid
Medicine is combined.
Colesevelam has nonabsorbable, the characteristics of can absorbing and degrade to avoid gastrointestinal tract.Indication：Norcholesterol：
Colesevelam hydrocholoride can independent medication or be aided with statins drug combination keep on a diet reduced with moderate exercise it is primary
Property hypercholesterolemia.In addition, colesevelam hydrocholoride piece and suspension are used for 10~17 years old boy of heterozygosis heritable hyperlipidemic
With girl after menarche.It is hypoglycemic：Colesevelam hydrocholoride can also be with melbine, sulfonylurea hypoglycemic agent or insulin combination
Medication is aided with to keep on a diet and improves the glycemic control to diabetes B adult patient with moderate exercise.
A large amount of clinical trial show colesevelam hydrocholoride be applied alone the LDL-C that can significantly lower patient it is horizontal (15%~
18%), raising HDL-C is horizontal (3%), but the influence to triglycerides is smaller.(atropic cuts down him to colesevelam hydrocholoride with Statins
Spit of fland, Lovastatin and Simvastatin) combination, lower the horizontal of LDL-C more significantly (individually additionally reduces with Statins compared with
16%) it is, less relative to Statins adverse reaction, relative to the level that colesevelam hydrocholoride is applied alone to be obviously improved lipid.
Vitamin E (Vitamin E) is a kind of liposoluble vitamin, also known as tocopherol, be most important antioxidant it
One.It is not soluble in water, it is dissolved in the organic solvents such as fatty and ethyl alcohol, heat, acid is stablized, it is unstable to alkali, it is sensitive to oxygen, to heat not
Sensitivity, but vitamin E, vitamin A, vitamin K1 activity are substantially reduced during frying.Recently it has also been found that vitamin E, vitamin A,
Vitamin K1 can inhibit the peroxidization in ocular lens body, expand small blood vessels, improve blood circulation, pre- myopia prevention hair
Raw and development.
Vitamin A (Vitamin A) is also known as retinol (its aldehyde derivatives retinene) or antiophthalmic factor, is a tool
There is the unsaturated monohydric alcohol of alicyclic ring, two kinds of the retinol1 including animal food source, A2 are a kind of with retinol biology
The substance of activity.Retinol1 is stored in the liver of mammal and saltwater fish more, and dehydroretinol is often stored in the liver of fresh-water fishes
In.Since the expression activitiy of dehydroretinol is low, so usually said vitamin A refers to retinol1.The function of vitamin A：
1. having effects that adjust epidermis and cuticula being metabolic, can wrinkle be gone with anti-aging.2. seborrhea can be reduced and make skin
Skin is flexible, while Kohakuhi, soft and moist skin.3. helping to protect epidermis, mucous membrane is not by bacterial infestation, healthy skin, in advance
Anti- cutaneum carcinoma.4. preventing yctalopia, the blurring of image treats various eye illnesses, woman's bright eyes is made to be apt to hide.5. promote bone growth, side
Dental growth is helped, is regenerated.6. effective pre- preventing obesity, the stature for keeping women slender.7. it can help to prevention alopecia.
Necessary material of the vitamin K1 for synthesis factor in liver, blood coagulation disorders can be caused when shortage.When in blood
During prothrombin deficiency, it is slow that the solidification of blood just will appear, and at this moment, supplementing suitable vitamin K1 can promote liver synthesis solidifying
Hemase is former, plays the role of hemostasis.Vitamin K1 is as pharmaceutical preparation, clinically applied to the too low disease of fibrin ferment, vitamin
Bleeding caused by K1 deficiency diseases, the prevention of newborn's nature haemorrhage and obstructive jaundice, leak, chronic diarrhea etc., cumarin
Hypoprothrombinemia caused by class, sodium salicylate etc..Vitamin also has the function of analgesia, alleviates bronchial spasm, internally
Angina caused by dirty smooth muscle angina, cholepathia spastica, enterospasm has obvious effects on.Vitamin K1 can be also used for multidimensional food
With the additive of poultry and livestock feed.
We have found in zoopery, give colesevelam gavage to renal insufficiency rat model, rat serium inorganic phosphorus drop
While low, cholic acid, triglycerides, low density lipoprotein cholesterol, liposoluble vitamin level also reduce, and enlighten us, mouth
Take gavage give rat colesevelam can with lipid-loweringing, lose weight, but liposoluble vitamin level needed by human simultaneously decline.For
This experiment finds that we devise various dose, the colesevelam of different ratio and vitamin and take orally again gives rat, observes
The variations such as its weight, apparent condition, behavior and blood fat, vitamin level.It has been found through experiments that colesevelam with vitamin most
The composition of good proportioning can reduce rat appetite, rat body weight is inhibited to increase, and reduce rat fat and its liposoluble vitamin
Level is held essentially constant, and rat spirit is good, and behavior is normal.
The embodiment of the present invention provides for the sake of example and description, and is not exhaustively or by this to send out
It is bright to be limited to disclosed form.Many modifications and variations are obvious for the ordinary skill in the art.Choosing
It is to more preferably illustrate the principle of the present invention and practical application to select and describe embodiment, and makes those of ordinary skill in the art
It will be appreciated that the present invention is so as to design the various embodiments with various modifications suitable for special-purpose.
Claims (9)
1. a kind of pharmaceutical composition with antiobesity action, which is characterized in that be prepared by the raw material for including following component：It examines
To tie up logical sequence, vitamin E, vitamin A, vitamin K1 and pharmaceutic adjuvant.
2. pharmaceutical composition according to claim 1, which is characterized in that the colesevelam, vitamin E, vitamin A,
The weight ratio of vitamin K1 and pharmaceutic adjuvant is 1000：10-30：1-3：0.1-1：210-415.
3. pharmaceutical composition according to claim 1 or 2, which is characterized in that the colesevelam is carbonic acid colesevelam
Or colesevelam hydrocholoride, in being calculated with the proportioning of other supplementary materials in terms of colesevelam.
4. according to claims 1 to 3 any one of them pharmaceutical composition, which is characterized in that the pharmaceutic adjuvant is fine for crystallite
The mixture of dimension element, silica and magnesium stearate composition.
5. pharmaceutical composition according to claim 4, which is characterized in that microcrystalline cellulose, dioxy in the pharmaceutic adjuvant
SiClx and the weight ratio of magnesium stearate are 200-400：10-30：5-15.
6. according to Claims 1 to 5 any one of them pharmaceutical composition, which is characterized in that by weight, as follows by including
The raw material of parts by weight is prepared：
7. pharmaceutical composition according to claim 6, which is characterized in that by weight, by including following parts by weight
Raw material is prepared：
8. according to claim 1~7 any one of them pharmaceutical composition, which is characterized in that described pharmaceutical composition is common
Piece, capsule or granule.
A kind of 9. method for preparing any one of claim 1~8 described pharmaceutical composition, which is characterized in that give birth to the dimension
After plain E, vitamin A and vitamin K1 are absorbed with silica, with colesevelam, microcrystalline cellulose, silica, magnesium stearate
Be uniformly mixed, be distributed into capsule to get.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611123703.9A CN108175772A (en) | 2016-12-08 | 2016-12-08 | A kind of pharmaceutical composition with antiobesity action and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611123703.9A CN108175772A (en) | 2016-12-08 | 2016-12-08 | A kind of pharmaceutical composition with antiobesity action and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN108175772A true CN108175772A (en) | 2018-06-19 |
Family
ID=62544915
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201611123703.9A Pending CN108175772A (en) | 2016-12-08 | 2016-12-08 | A kind of pharmaceutical composition with antiobesity action and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN108175772A (en) |
-
2016
- 2016-12-08 CN CN201611123703.9A patent/CN108175772A/en active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US20080268066A1 (en) | Synergistic Formulation for Preventing and/or Treating Diabetes | |
| CN102670864B (en) | Medicine composition with antioxidant function for treating cardiovascular and cerebrovascular diseases and sugar diabetes | |
| CN1956734A (en) | Multi-vitamin and mineral nutritional supplements | |
| CN101715913B (en) | Capsule for regulating blood fat and production process thereof | |
| RU2559784C2 (en) | Composition for mitigating fatigue, formulation and using them | |
| JP5596704B2 (en) | Composition containing fucoxanthin extract | |
| CN104208695A (en) | Multifunctional composition, and preparation method and application thereof | |
| CN105079309B (en) | Composition for relaxing bowel | |
| CN101278928A (en) | Medicament composition containing levocarnitine or its derivatives and use thereof | |
| JP5537151B2 (en) | Tranquilizers and functional foods | |
| CN109125315A (en) | Composition and purposes with hypoglycemic, reducing blood lipid and hypotensive activity | |
| TW201225966A (en) | Use of djulis in manufacturing a drug or health food for reducing blood lipids | |
| JP2003113089A (en) | Chitosan-containing formulation having action to inhibit lipid accumulation and reduce cholesterol and food and drink | |
| CN105101817B (en) | Edible composition and preparation method thereof and the food comprising said composition | |
| CN101208351A (en) | Compounds for the treatment of non-autoimmune type 2 diabetes mellitus and/or syndrome x | |
| JP3433917B2 (en) | Nutritional composition for enhancing body protein accumulation efficiency | |
| CN109965072A (en) | A kind of pressed candy and the preparation method and application thereof conserving liver | |
| CN106727480B (en) | Fex-3 is preparing the application in anti-obesity drug | |
| CN109381455A (en) | With the composition for adjusting blood glucose, blood lipid and blood pressure function | |
| CN108175772A (en) | A kind of pharmaceutical composition with antiobesity action and preparation method thereof | |
| US6506420B2 (en) | Combinations of psyllium and chitosan for synergistic adsorption of triglyceride | |
| CN108186670A (en) | It is a kind of to be used to treat fat pharmaceutical composition and preparation method thereof | |
| JP2010168399A (en) | Pharmaceutical for controlling elevation of blood sugar | |
| CN105995980A (en) | Composition with weight management function and preparation method thereof | |
| JP2009062348A (en) | Hypoglycemic action and blood sugar level elevation-suppressive action by seed ingredient of kenafs (kenaf and roselle) |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20180619 |
|
| WD01 | Invention patent application deemed withdrawn after publication |