CN101167721A - Compound preparation containing orlistat - Google Patents
Compound preparation containing orlistat Download PDFInfo
- Publication number
- CN101167721A CN101167721A CNA2006101507714A CN200610150771A CN101167721A CN 101167721 A CN101167721 A CN 101167721A CN A2006101507714 A CNA2006101507714 A CN A2006101507714A CN 200610150771 A CN200610150771 A CN 200610150771A CN 101167721 A CN101167721 A CN 101167721A
- Authority
- CN
- China
- Prior art keywords
- orlistat
- preparation
- vitamin
- compound
- fat
- 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
Abstract
The invention belongs to the field of medical technique and relates to a compound fat-reducing containing orlistat. The invention basically contains orlistat and synergistic agent, wherein the synergistic agent is one or several ingredients chosen from pulullan saccharide, chitin, vitamin A, vitamin D, vitamin E, vitamin K and/or beta-carotene. Any solid preparation for oral administration can be made by charging other active component or finding component on the basic components. The invention is characterized in that quick fat reducing can be achieved by inhibiting the absorption of exogenous fat, meanwhile the adsorption action of pulullan saccharide, chitin and other amylase is brought in to effect, the ipidized loose bowel movement, unctuous stool, anal fistula and other side effects of the patient of adiposis are reduced, and fatsoluble vitamin reduced by absorption is complemented.
Description
Technical field
The invention belongs to medical technical field, relate to a kind of compound slimming preparation that contains orlistat.
Background technology
Obesity is a kind of worldwide commonly encountered diseases, and when human body feed heat during more than consumption of calorie, unnecessary heat is stored in the body with the form of fat, causes weight increase, and it is a kind of chronic metabolic disease, and sickness rate increases year by year.The obesity not only bodily form is not beautiful, and has many hidden danger, normal assembles appearance with type ii diabetes, hypertension, dyslipidemia, gout, cholelithiasis, atherosclerosis, coronary heart disease etc., becomes one of important worldwide health problem gradually.Aspect slimming medicine, medicine listings such as sibutramine, orlistat are arranged.Wherein sibutramine is an appetite suppressant, reaches the fat-reducing purpose by appetite-suppressing, minimizing feed.Orlistat is specificity stomach, pancreatic lipase inhibitor; make the lipase inactivation by same stomach, pancreatic lipase irreversible fixation, thereby suppressing fat splitting is absorbable free fatty and monoacylglycerol, the absorption of the middle fat that cuts down one's diet reaches the purpose of fat-reducing.For appetite suppressant class fat-reducing medicine, its mechanism of action is to act on maincenter, causes systemic side effects more, even some serious adverse effects may take place.
The chemical name N-formoxyl of orlistat-L-leucine (s)-1[(2s, 3s) 3-hexyl-4-oxygen base-2-glycidyl methyl] ten diester, be a kind of semisynthetic lipstatin derivant, have potent and optionally suppress the effect of stomach, pancreatic lipase.Orlistat mainly makes enzyme deactivation at gastrointestinal tract by its β lactonic ring and the lipase active position irreversible covalent bond of serine pendant hydroxyl group, suppresses the triacylglycerol hydrolysis, reduces the absorption of monoesters acyl glycerol and free fatty, thus controlling body weight.
Orlistat only plays a role at gastrointestinal tract, and oral about 97% through the feces removing, mainly is the intestinal reaction, untoward reaction such as patient's defecation is eager, oily feces, flatulence.Fat-reducing effect is slow, and patient's 2～3 all body weight of usually need taking medicine just begin to descend, and need take medicine for a long time can reach desirable fat-reducing effect more than 1 year.Take its side effect of orlistat for a long time: untoward reaction such as oily feces, anus leakage of oil influence patient's life of working, and easily cause the picked-up of fat-soluble A, vitamin D, vitamin E, vitamin K and beta-carotene etc. to reduce simultaneously.
In addition, Chinese invention patent publication number CN 1373656A discloses a kind of dispersing solid that contains lipase inhibitor, lipase inhibitor is orlistat preferably, this medicine can effectively alleviate the drug induced fatty stool of orlistat just, the generation of untoward reaction such as anus leakage of oil, but its fat-reducing effect is slow.Chinese invention patent CN 1546017A discloses a kind of compound preparation that contains orlistat, L-carnitine, calcium pyruvate, combined effect aspect absorption of inhibition ectogenous fat and acceleration consumption body fat two, reaching the effect of quick weight-lossing, but can not alleviate take fatty stool that this compound preparation causes just, side effect such as anus leakage of oil.Above-mentioned two patents all can not overcome because of taking the minimizing that the orlistat medicine causes that fatsoluble vitamin is ingested in the body for a long time.
Summary of the invention
The object of the present invention is to provide a kind of fat-reducing effect significantly, effectively to alleviate and take the drug induced just generation of untoward reaction such as oil, anus leakage of oil of orlistat, additional because of taking the fatsoluble vitamin that the orlistat medicine causes that minimizing is ingested in the body for a long time.
The present invention contains the compound slimming preparation of orlistat, and ultimate constituent is orlistat and synergist, and wherein synergist is selected from one or more of pulullan, chitin, vitamin A, vitamin D, vitamin E, vitamin K and/or beta-carotene.Synergist can effectively increase the orlistat antiobesity action, alleviate and take the drug induced just generation of untoward reaction such as oil, anus leakage of oil of orlistat, and is additional because of taking the fatsoluble vitamin that the orlistat medicine causes that minimizing is ingested in the body for a long time.Slimming medicine orlistat described in the compound slimming preparation of the present invention also comprises its pharmaceutically useful derivant, trim or prodrug.Pulullan in the synergist comprises pulullan or derivatives thereof, trim, and chitin comprises chitin or derivatives thereof, trim, preferred chitosan.
Pulullan is the linear macromolecule that is formed by connecting by α-1,6 glycosidic bond by the repetitive of maltotriose, and relative molecular mass is generally 5 * 10
4～5 * 10
6Between the Dal, be widely used in aspects such as food, medicine, production in light industry.Be difficult in the pulullan body being digested and absorbing, the obese patient has taken feeling of repletion, can reduce the picked-up of food is had fat-reducing effect; Simultaneously, the also adsorbable obese patient of pulullan takes non-absorbent triglyceride behind the orlistat, reduces side effect such as fat-soluble feces, anus leakage of oil.
Chitin is the polysaccharide that is formed by connecting with β-1,4 glycosidic bond form by N-acetyl-2-amino-2-deoxy-D-glucose.Deacetylation is later on its derivant chitosan, and chitosan has the amino positively charged because of the glucose side chain, can adsorb triacylglycerol hydrolysis free fatty and monoacylglycerol, reduces the picked-up of small intestinal mucosa and has fat-reducing effect; The while chitosan can adsorb the obese patient as high molecular weight polysaccharide takes the non-absorbent triglyceride of orlistat, reduces side effect such as fat-soluble feces, anus leakage of oil.
Replenish fat-soluble A, vitamin D, vitamin E, vitamin K and beta-carotene, increase gastrointestinal and absorb, can reduce the disease that causes because of the fatsoluble vitamin Deficiency of Intake and take place.
Basic composition is of preparation of the present invention: orlistat, synergist and conventional dose adjuvant, prepare various oral solid formulations by conventional method, comprise tablet, granule, capsule, soft capsule, pill or powder, wherein, the conventional dose adjuvant is selected from but is not limited to stabilizing agent, disintegrating agent, antiseptic, antioxidant, emulsifying agent, correctives, coating materials, on this compound slimming preparation basis, also can add other active component or ectogenous fat adsorbent with weight losing function.
In the compound preparation of the present invention, be by weight percentage: contain orlistat 0.1%～99.9% in this compound slimming preparation, preferred 10.0%～80.0%, first-selected 20.0%～30.0%; Synergist 0.1%～99.9%, preferred 20.0%～90.0%, first-selected 30.0%～60.0%.
The specific embodiment
Following embodiment is for the present invention being described better, can not limiting the present invention.
Embodiment 1
The tablet prescription 1 of orlistat compound preparation of the present invention
In the preparation process of tablet, with above-mentioned prescription compound preparation and a certain amount of starch disaggregation, the mixing starch slurry is granulated together.Dried particles is mixed with magnesium stearate and remaining starch, this mixture is suppressed forming then in tablet machine.
Embodiment 2
The tablet prescription 2 of orlistat compound preparation of the present invention
In the preparation process of tablet, with above-mentioned prescription compound preparation and a certain amount of starch disaggregation, the mixing starch slurry is granulated together.Dried particles is mixed with magnesium stearate and remaining starch, this mixture is suppressed forming then in tablet machine.
Embodiment 3
The capsule prescription of orlistat compound preparation of the present invention
In the preparation process of capsule, with above-mentioned prescription compound preparation, lactose, microcrystalline Cellulose disaggregation.Then this mixture is incapsulated and make.
Embodiment 4
The granule prescription 1 of orlistat compound preparation of the present invention
In the preparation process of granule, above-mentioned prescription compound preparation, starch, lactose disaggregation and combination drying are made.
Embodiment 5
The granule prescription 2 of orlistat compound preparation of the present invention
In the preparation process of granule, above-mentioned prescription compound preparation, lactose, microcrystalline Cellulose disaggregation and combination drying are made.
The experimentation data
The antiobesity action of 3 pairs of obese rats of the embodiment of the invention
1 experiment material and method
1.1 experiment material
1.1.1 laboratory animal
Select Wistar children rat for use, age in days is about 30 days, body weight 70～90g, totally 50, male and female half and half.
1.1.2 rat feed
Normal diet; High lipid food (fat content accounts for 30%).
1.1.3 experiment medicine
Make test group with embodiment 3, simple orlistat matched group does not contain synergist, all is prepared into capsule according to conventional method.
1.2 experimental technique
1.2.1 grouping and processing method
Get 50 rats, with the rat random packet, 10 of A groups are fed normal diet, as the normal control group, remain 40 modelings, feed 5 weeks of high lipid food, weigh, and choose modeling success animal, are divided into three groups of B, C, D at random, 10 every group.
Preceding 5 weeks of A group normal control group are fed normal diet, 5 weeks of back continue to feed normal diet and irritate stomach with normal saline
B organizes preceding 5 weeks of fat matched group and feeds high lipid food, 5 weeks of back continues to feed normal diet and irritates stomach with normal saline
Preceding 5 weeks of C group test group are fed high lipid food, 5 weeks of back continue to feed normal diet and irritate stomach with the embodiment of the invention 3
D organizes preceding 5 weeks of simple orlistat matched group and feeds high lipid food, 5 weeks of back continues to feed normal diet and irritates stomach with simple Ao Sita
1.2.2 drug dose
Test group and simple orlistat matched group are made into orlistat 6mg/mL, and rat body weight is pressed 1mL/kg and irritated stomach, every day three times.
1.3 experimental index and observational technique
1.3.1 experimental index
The fat-reducing index: experiment is body weight just, and the experiment opisthosoma is heavy long with body, the obesity index (cubic root of LI=body weight * 10
3/ height).
The lipid metabolism observed value: fat index (g/100g body weight) and plasma high density lipoprotein level, T-CHOL, content of triglyceride are measured.
Side effect: oiliness feces whether, add up oiliness feces number of times the 6th thoughtful the tenth every day at weekend.
1.3.2 observational technique
Every rat is observed rat feces every day, and record oiliness feces number of times is weighed weekly once, handle corresponding laboratory animal group for the tenth weekend respectively: claim rat body weight on an empty stomach, with 2.0% pentobarbital sodium 50mg/kg intraperitoneal injection of anesthesia, eyeball is got blood, surveys body long (nose is to anus length).The dislocation of Mus cervical vertebra is put to death, separate the whole fat of genitals on every side, claim fat heavy.In addition obtained blood is isolated serum immediately, survey triglyceride (using acetylacetone method) and T-CHOL (using the phosphoric acid iron processes).
1.3.3 statistical method
Use t check carrying out significance test.
2 experimental results and analysis see Table 1 and table 2.
Table 1 rat growth indexes measured value
Annotate: compare with the B group,
1)There is the significance meaning P＜0.01, difference; Compare with the D group,
2)There is the significance meaning P＜0.01, difference
Table 2 body fat weight (testis and perinephric fat pad)
Annotate: compare with the B group,
1)There is the significance meaning P＜0.01, difference; Compare with the D group,
2)There is the significance meaning P＜0.01, difference; Compare with the D group,
3)There is the significance meaning P＜0.05, difference
Oiliness feces number of times: C group totally 281 times, D group totally 126 times.
The result shows: orlistat compound preparation of the present invention and orlistat folk prescription reference substance all can reduce obese rat body weight, fat index, T-CHOL, triglyceride concentration, but orlistat compound preparation of the present invention has more obvious advantage, significantly is better than simple orlistat group.Orlistat compound preparation oiliness feces number of times of the present invention is less than the orlistat matched group, and side effect is littler.
Claims (8)
1. compound slimming preparation that contains orlistat, it is characterized in that: the main component of this compound preparation is orlistat and synergist, and wherein synergist is selected from one or more of pulullan, chitin, vitamin A, vitamin D, vitamin E, vitamin K and/or beta-carotene.
2. the compound slimming preparation of claim 1, it is characterized in that: orlistat comprises orlistat or its pharmaceutically useful derivant, trim or prodrug.
3. the compound slimming preparation of claim 1, it is characterized in that: pulullan comprises pulullan or derivatives thereof, trim, chitin comprises chitin or derivatives thereof, trim, preferred chitosan.
4. the arbitrary described compound slimming preparation of claim 1 to 3, it is characterized in that, basic composition is of preparation: orlistat, synergist and conventional dose adjuvant, be prepared into various oral solid formulations by conventional method, comprise tablet, granule, capsule, soft capsule, pill or powder, wherein, the conventional dose adjuvant is selected from but is not limited to stabilizing agent, disintegrating agent, antiseptic, antioxidant, emulsifying agent, correctives, coating materials.
5. the described compound slimming preparation of claim 4 is characterized in that: by weight percentage, contain orlistat 0.1%～99.9% in this compound preparation, synergist 0.1%～99.9%.
6. the described compound slimming preparation of claim 4 is characterized in that, by weight percentage, contains orlistat 10.0%～80.0% in this compound preparation, first-selected 20.0%～30.0%.
7. the described compound slimming preparation of claim 4 is characterized in that, by weight percentage, contains synergist 20.0%～90.0% in this compound preparation, first-selected 30.0%～60.0%.
8. the described compound slimming preparation of claim 4, it is characterized in that, on the basic composition basis of preparation, add active component or the ectogenous fat adsorbent that weight losing function is arranged, be prepared into various oral solid formulations by conventional method, comprise tablet, granule, capsule, soft capsule, pill or powder.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2006101507714A CN101167721A (en) | 2006-10-26 | 2006-10-26 | Compound preparation containing orlistat |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2006101507714A CN101167721A (en) | 2006-10-26 | 2006-10-26 | Compound preparation containing orlistat |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101167721A true CN101167721A (en) | 2008-04-30 |
Family
ID=39388571
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2006101507714A Pending CN101167721A (en) | 2006-10-26 | 2006-10-26 | Compound preparation containing orlistat |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101167721A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102552409A (en) * | 2012-01-02 | 2012-07-11 | 西北农林科技大学 | Compound orlistat nano-emulsion oral liquid and preparation method thereof |
| CN105520947A (en) * | 2015-12-24 | 2016-04-27 | 广东药学院 | Pharmaceutical composition containing glucosamine and having weight reducing function |
| CN105985941A (en) * | 2015-12-20 | 2016-10-05 | 山东建筑大学 | Liquid alpha-amylase composite heat stabilizer |
-
2006
- 2006-10-26 CN CNA2006101507714A patent/CN101167721A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102552409A (en) * | 2012-01-02 | 2012-07-11 | 西北农林科技大学 | Compound orlistat nano-emulsion oral liquid and preparation method thereof |
| CN105985941A (en) * | 2015-12-20 | 2016-10-05 | 山东建筑大学 | Liquid alpha-amylase composite heat stabilizer |
| CN105985941B (en) * | 2015-12-20 | 2019-04-05 | 山东建筑大学 | A kind of liquid alpha-amylase composite thermal stabilizer |
| CN105520947A (en) * | 2015-12-24 | 2016-04-27 | 广东药学院 | Pharmaceutical composition containing glucosamine and having weight reducing function |
| CN105520947B (en) * | 2015-12-24 | 2018-05-01 | 广东药科大学 | A kind of pharmaceutical composition with weight losing function containing Glucosamine |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US8343543B2 (en) | Lipase inhibiting composition | |
| KR100877600B1 (en) | Pharmaceutical composition comprising metadoxine and garlic oil for preventing and treating alcohol-induced fatty liver and steatohepatitis | |
| US10342797B2 (en) | Solubility of therapeutic agents | |
| CN101309688A (en) | Compositions and methods for the sustained release of beta-alanine | |
| US20030232097A1 (en) | Oily wax matrix suspension formulation comprising ibuprofen free acid and potassium salt of ibuprofen | |
| JP3285410B2 (en) | Oral pharmaceutical composition containing anthocyanosides | |
| JP4009642B2 (en) | Composition for improving obesity | |
| WO2006111085A1 (en) | A method, formulation and use thereor with improved oral absorption of drugs or nutrients | |
| AU2273899A (en) | Therapeutic agents | |
| AU2002257817A1 (en) | Pharmaceutical composition comprising a lipase inhibitor and a sucrose fatty acid ester | |
| US11602510B2 (en) | Agent for use in the treatment of dyslipidemia | |
| AU742460B2 (en) | Fatty acids as a diet supplement | |
| CN101167721A (en) | Compound preparation containing orlistat | |
| ES2861023T3 (en) | Reducing composition of fat in the blood and its application | |
| CN108542903A (en) | A kind of pharmaceutical composition containing orlistat Yu plant origin lipase inhibitor | |
| JP2005187405A (en) | Uric acid value inhibitor and purine body adsorbent | |
| WO2001012200A1 (en) | An oral composition comprising coenzyme a for treating hyperlipemia, the preparation method and the use thereof | |
| EP1187606A1 (en) | Pharmaceutical composition containing sibutramine and orlistat | |
| US20210346471A1 (en) | Superoxide dismutase compositions and methods | |
| JP2009196972A (en) | Medicinal composition | |
| TW202002996A (en) | Peptide-containing formulations | |
| KR100771322B1 (en) | Antiobesity agent and health food | |
| CN109663123A (en) | Capsule for improving liver injury and body fatigue and preparation method thereof | |
| EP4353241A1 (en) | Fine silicon particle-containing preventive or therapeutic agent for diseases | |
| TWI292315B (en) | Composition for decreasing lipids in blood |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C12 | Rejection of a patent application after its publication | ||
| RJ01 | Rejection of invention patent application after publication |
Open date: 20080430 |