CN106924270B - Orlistat-containing pharmaceutical composition with weight-losing function - Google Patents
Orlistat-containing pharmaceutical composition with weight-losing function Download PDFInfo
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- CN106924270B CN106924270B CN201710141721.8A CN201710141721A CN106924270B CN 106924270 B CN106924270 B CN 106924270B CN 201710141721 A CN201710141721 A CN 201710141721A CN 106924270 B CN106924270 B CN 106924270B
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- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7016—Disaccharides, e.g. lactose, lactulose
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- 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
- A61K31/05—Phenols
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- 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
- A61K31/365—Lactones
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- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/702—Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
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- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
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- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
- A61K31/733—Fructosans, e.g. inulin
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Abstract
The invention relates to a medicinal composition containing orlistat and having a weight-losing function. Wherein the weight ratio of orlistat to resveratrol to oligosaccharide is 1: 0.42-3.75: 0.1-0.6. The invention combines low-dose orlistat (1/3 with conventional dose) and high-dose resveratrol and fructo-oligosaccharide with any dose of high, medium and low for use, thus having remarkable weight-losing effect on nutritional obesity rats, the weight-losing effect is superior to the orlistat with conventional dose, and the incidence rate of gastrointestinal adverse reactions is significantly lower than that of the orlistat with conventional dose. The medicine composition is a healthy weight-losing medicine with low side effect, and meets the requirements of modern people on weight-losing medicines.
Description
Technical Field
The invention belongs to the field of medicines, and particularly relates to a pharmaceutical composition containing orlistat and having a weight-losing function.
Background
With the rapid development of social economy, the living standard of people is continuously improved, the dietary structure of people is also greatly changed, and the obesity problem is more and more serious. Obesity is a metabolic disease caused by imbalance of energy balance of organisms, is a chronic metabolic disease mainly caused by factors such as poor eating habits and living habits of people and environment and heredity, is also a risk factor of various diseases such as hypertension, diabetes, dyslipidemia, coronary heart disease, myocardial infarction and the like, and is evaluated as the fifth major risk factor affecting human health by the world health organization.
In recent years, due to the pressure of life, fast pace and lack of health knowledge, overweight and obesity have become younger, and most children and teenagers have been eagerly obese. It has been found that obesity has severely compromised juvenile growth and development.
Orlistat is known as N-formyl-L-leucine(s) -1[ (2s, 3s) -3-hexyl-4-oxy-2-epoxypropylmethyl ] dodecaester, also known as tetrahydrolipstatin (TH L), is a semisynthetic lipstatin derivative, and has a chemical structural formula shown in the following formula,
orlistat (orlistat) was developed by roche pharmaceutical companies as a lipase inhibitor antiobesity drug, under the trade name Xenical, first marketed in europe and the united states at the end of the nineties of the last century, marketed in china in 2001, and approved by the chinese food and drug administration to be converted to an over-the-counter drug in 2005. Orlistat is used in II crystal capsule and tablet, and after taking the orlistat, 1/3 in the fat is not absorbed and is discharged from intestinal tract, so as to reduce weight. The common dosage is 120mg taken orally once with a meal, the weight can be reduced by 7-10 kg in 3-6 months, orlistat is the only chemical weight-reducing medicine which does not influence appetite and does not act on the central nervous system at home and abroad at present, and the safety characteristic is excellent.
However, because orlistat mainly acts on the digestive tract, long-term use of orlistat can cause a series of adverse gastrointestinal reactions, such as oily spots, gastrointestinal gas with stool, urgent stool feeling, fatty stool, fatty diarrhea, increased stool excretion, fecal incontinence and the like. In addition, the domestic and foreign literatures all believe that orlistat only can reduce the body weight of overweight and obese patients with moderate intensity after being used, and the weight-reducing effect is quite satisfactory. The results of domestic clinical trials show that patients with weight loss degrees of 5% and 10% of the baseline weight after 6 months of administration of 120mg orlistat capsules account for 72.5% and 25.9%, respectively. In addition, the study by pamela morales et al confirmed that the entry of unabsorbed fat into the colon after orlistat administration increases fecal calprotectin (one of the biomarkers of inflammation), increases the oxidative activity of fecal water, and produces a subtle change in colonic flora.
Disclosure of Invention
In view of the gastrointestinal reaction risk of orlistat taken alone and the insignificant weight-reducing effect, the invention provides a pharmaceutical composition containing orlistat, which improves the weight-reducing effect of commercially available orlistat products and reduces the gastrointestinal adverse reactions of the orlistat products.
The invention provides a medicinal composition containing orlistat and having a weight-losing function, and the medicinal composition contains orlistat, resveratrol and oligosaccharide.
Further, the weight ratio of orlistat, resveratrol and oligosaccharide is 1: 0.42-3.75: 0.1-0.6.
Preferably, the weight ratio of orlistat, resveratrol and oligosaccharide is 1: 0.5-1.5: 0.1-0.3.
Furthermore, the oligosaccharide is at least one of fructo-oligosaccharide, xylo-oligosaccharide and soybean oligosaccharide.
Further, the pharmaceutical compositions can be prepared by methods known in the art of pharmaceutical formulation, for example, see the treford headquartend, pharmaceutics (7 th edition) (published by the national institutes of health), incorporated herein by reference. In particular, orlistat, resveratrol and oligosaccharides may be mixed with at least one pharmaceutically acceptable excipient, such as citric acid or dicalcium phosphate, or: (a) fillers or extenders, for example, starch, lactose, sucrose, glucose, mannitol, and silicic acid; (b) binders, for example, cellulose derivatives, starch, alginates, gelatin, polyvinylpyrrolidone, sucrose and acacia; (c) disintegrating agents, for example, agar-agar, calcium carbonate, potato or tapioca starch, alginic acid, croscarmellose sodium, complex silicates and sodium carbonate; (d) solution retarders, e.g., paraffin; (e) absorption accelerators, such as quaternary ammonium compounds; (f) wetting agents, for example, cetyl alcohol and glyceryl monostearate, magnesium stearate, and the like; (g) adsorbents such as kaolin and bentonite; and (h) lubricants, for example, talc, calcium stearate, magnesium stearate, solid polyglycols, sodium lauryl sulfate or mixtures thereof. In the case of capsules, tablets and pills, the dosage forms also include buffering agents.
Preferably, the pharmaceutical composition is an oral solid preparation.
More preferably, the pharmaceutical composition is a capsule.
Experiments show that the orlistat-containing pharmaceutical composition with the weight-losing function can obviously reduce the weight of rats, has obvious difference (P <0.05) compared with a pure feeding nutritional feed group (a model group), and can obviously reduce the incidence rate (P <0.05) of grease appearing on the hair of the rats by feeding the pharmaceutical composition provided by the invention compared with the nutritional feed group which is only fed with orlistat, so that the pharmaceutical composition provided by the invention has an obvious weight-losing effect, can reduce the gastrointestinal adverse reaction of orlistat, is a healthy weight-losing medicine with low side effect, and meets the requirements of modern people on weight-losing medicines.
Compared with the prior art, the invention has the advantages that:
a large number of experiments show that the orlistat, resveratrol and oligosaccharide combination achieves unexpected effects when applied to treating or preventing obesity, and animal experiment results show that the orlistat composition can generate remarkable weight-reducing effect on nutritional obesity rats by combining low-dose orlistat (1/3 with a conventional dose) with high-dose resveratrol and combining with fructo-oligosaccharide with high, medium and low doses for use, and the weight-reducing effect is superior to that of orlistat with a conventional dose, while the incidence of gastrointestinal adverse reactions is significantly lower than that of orlistat with a conventional dose.
In addition, the orlistat, resveratrol and oligosaccharide are combined for use, so that the medication compliance of overweight and obese patients is improved.
Detailed Description
The present invention will be further described below by way of specific embodiments, but the present invention is not limited to only the following examples.
Example 1 preparation of orlistat-containing pharmaceutical composition capsule having weight-losing effect
Prescription design (1000 granules):
the preparation method comprises the following steps:
sodium Dodecyl Sulfate (SDS), polyvidone K30, carboxymethyl starch sodium, microcrystalline cellulose, orlistat powder, resveratrol, and fructo-oligosaccharide by sieving with 80 mesh sieve. Weighing sodium dodecyl sulfate, povidone K30, carboxymethyl starch sodium, microcrystalline cellulose, orlistat powder, resveratrol and fructo-oligosaccharide according to the prescription amount, uniformly mixing small amount of sodium dodecyl sulfate, povidone K30 and carboxymethyl starch sodium, adding microcrystalline cellulose, orlistat, resveratrol and fructo-oligosaccharide, uniformly mixing, and sieving with a 80-mesh sieve twice. Slowly adding 50% ethanol solution containing 10% polyvidone K30 into the mixed powder, making soft mass, extruding and sieving with 20 mesh sieve to obtain wet granule, oven drying the wet granule in a blast drying oven at 30 deg.C for 6 hr, taking out and sieving with 20 mesh sieve, and packaging into capsule shell.
Example 2 preparation of orlistat-containing pharmaceutical composition capsule having weight-losing effect
Prescription design (1000 granules):
the preparation method comprises the following steps:
sodium Dodecyl Sulfate (SDS), polyvidone K30, carboxymethyl starch sodium, microcrystalline cellulose, orlistat powder, resveratrol, and xylooligosaccharide by sieving with 80 mesh sieve. Weighing sodium dodecyl sulfate, povidone K30, carboxymethyl starch sodium, microcrystalline cellulose, orlistat powder, resveratrol and xylo-oligosaccharide according to the prescription amount, uniformly mixing small amount of sodium dodecyl sulfate, povidone K30 and carboxymethyl starch sodium, adding microcrystalline cellulose, orlistat, resveratrol and xylo-oligosaccharide, uniformly mixing, and sieving with a 80-mesh sieve twice. Slowly adding 50% ethanol solution containing 10% polyvidone K30 into the mixed powder, making soft mass, extruding and sieving with 20 mesh sieve to obtain wet granule, oven drying the wet granule in a blast drying oven at 30 deg.C for 6 hr, taking out and sieving with 20 mesh sieve, and packaging into capsule shell.
Example 3 preparation of orlistat-containing pharmaceutical composition capsule having weight-losing effect
Prescription design (1000 granules):
the preparation method comprises the following steps:
sodium Dodecyl Sulfate (SDS), polyvidone K30, carboxymethyl starch sodium, microcrystalline cellulose, orlistat powder, resveratrol, and soybean oligosaccharide by sieving with 80 mesh sieve. Weighing sodium dodecyl sulfate, povidone K30, carboxymethyl starch sodium, microcrystalline cellulose, orlistat powder, resveratrol and soybean oligosaccharide according to the prescription amount, uniformly mixing small amount of sodium dodecyl sulfate, povidone K30 and carboxymethyl starch sodium, adding microcrystalline cellulose, orlistat, resveratrol and soybean oligosaccharide, uniformly mixing, and sieving twice with a 80-mesh sieve. Slowly adding 50% ethanol solution containing 10% polyvidone K30 into the mixed powder, making soft mass, extruding and sieving with 20 mesh sieve to obtain wet granule, oven drying the wet granule in a blast drying oven at 30 deg.C for 6 hr, taking out and sieving with 20 mesh sieve, and packaging into capsule shell.
Example 4 weight-loss Effect of orlistat-containing pharmaceutical composition having weight-loss function on nutritionally obese rats
1 Material
1.1 medicaments
120mg orlistat capsules (Zhongshan Wanhan medical science and technology Co., Ltd.) all the capsules containing orlistat as a pharmaceutical composition having a weight-losing effect were taken out just before use, and each capsule was dissolved in 40m L0.5.5% sodium carboxymethylcellulose solution.
1.2 animal and feed
The male cleaning grade SD rat is provided by the experimental animal center of Zhongshan university, has the license number of SCXK (Guangdong) 2015-. The general feed and nutritional type were provided by the laboratory animal center of Zhongshan university, and the composition of both is shown in the following table.
2 method
2.1 Molding, grouping and administration
According to the pharmacodynamics research and evaluation method of obesity in traditional Chinese medicine pharmacodynamics research and evaluation, a model method for preventing obesity is adopted, 240 SD rats are selected as test animals and are randomly divided into 30 groups according to body weight, each group of n is 8, the feed and treatment dosage of each group are shown in the table, the corresponding feed is provided for each group of animals at 9 am every day, the food is taken away at 7 pm, the feed is quantitatively administered every day (the feed dosage is adjusted every day on the basis of the principle that most animals eat the feed completely), the drug treatment group is perfused with a solution of the corresponding drug dissolved in 0.5% sodium carboxymethylcellulose twice at 9 am every day and 3 pm every day in a dosage of 10m L/kg, and all the animals are fed in a single cage for 7 weeks.
2.2 evaluation index
Weighing the body weight once a week; observing and counting the number of animals with oil (visible light) on hair every day, and performing comprehensive statistics according to week
3 results
3.1 weight Change
3.2 number of rats with oil distribution on hair
The results show that compared with the simple feeding nutritional feed group (model group), the orlistat-containing pharmaceutical composition with the weight-losing function can significantly reduce the weight of rats (P < 0.05). The combination of the orlistat with low dose (1/3 with conventional dose) and the resveratrol with high dose is combined with fructo-oligosaccharide with high, medium and low dose for use, so that the weight-losing effect on the nutritional obesity rat is remarkable, and the weight-losing effect is superior to that of the orlistat with conventional dose. Meanwhile, the dosage of orlistat in the composition is reduced, so that the risk of gastrointestinal discomfort caused by orlistat is greatly reduced, and the probability of grease generation on rat hair proves that the pharmaceutical composition containing orlistat and having the weight-reducing function can reduce the probability of grease generation on rat hair, and has significant difference (P <0.05) compared with the orlistat group which is only given with conventional dosage. The pharmaceutical composition provided by the invention is a healthy weight-losing medicine with low side effect, and meets the requirements of modern people on weight-losing medicines.
The above is only a preferred embodiment of the present invention, and it should be noted that the above preferred embodiment should not be considered as limiting the present invention, and the protection scope of the present invention should be subject to the scope defined by the claims. It will be apparent to those skilled in the art that various modifications and adaptations can be made without departing from the spirit and scope of the invention, and these modifications and adaptations should be considered within the scope of the invention.
Claims (3)
1. A pharmaceutical composition containing orlistat and having a weight-losing function is characterized in that the pharmaceutical composition contains orlistat, resveratrol and oligosaccharide;
the weight ratio of orlistat to resveratrol to oligosaccharide is 1:0.42: 0.13;
the oligosaccharide is selected from fructo-oligosaccharide.
2. The orlistat-containing pharmaceutical composition with a weight-losing function according to claim 1, wherein the pharmaceutical composition is an oral solid preparation.
3. The orlistat-containing pharmaceutical composition with a weight-losing function according to claim 2, wherein the pharmaceutical composition is a capsule.
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| CN201710141721.8A CN106924270B (en) | 2017-03-10 | 2017-03-10 | Orlistat-containing pharmaceutical composition with weight-losing function |
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| CN106924270A CN106924270A (en) | 2017-07-07 |
| CN106924270B true CN106924270B (en) | 2020-07-31 |
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| CN108524495B (en) * | 2018-07-10 | 2019-02-26 | 中山万汉制药有限公司 | Purposes of the orlistat in the drug of preparation treatment constipation |
| CN112294798A (en) * | 2020-10-31 | 2021-02-02 | 中山万汉制药有限公司 | Composition for reducing absorption of lipase inhibitor in digestive tract |
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| WO2009049105A2 (en) * | 2007-10-09 | 2009-04-16 | Gelesis, Inc. | Methods for inducing satiation |
| CN102613456B (en) * | 2012-03-05 | 2014-07-23 | 陈功 | Xylo-oligosaccharide composition with lipase activity inhibition effect and application of xylo-oligosaccharide composition |
| CN103142457B (en) * | 2013-01-17 | 2015-01-21 | 西安电子科技大学 | Resveratrol nanometer-preparation preparation method |
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