CN113499314A - Orlistat tablet and preparation method thereof - Google Patents

Abstract

The invention discloses orlistat tablets, which mainly comprise the following components in percentage by weight: 60mg of orlistat (calculated as orlistat), 3-10% (w/w) of disintegrating agent, 3-10% (w/w) of adhesive, 0.1-1% (w/w) of lubricant, and the balance of filler; the invention is prepared by a direct compression method, after raw and auxiliary materials are sieved, orlistat, crospovidone, copovidone, magnesium stearate, sucrose and microcrystalline cellulose in the formula are weighed and placed in a three-dimensional mixing pot, after the materials are mixed for 30min, the mixture is placed on a tablet press for tabletting, and the tablet weight is controlled. The invention adopts a direct compression method for tabletting, effectively reduces the heavy impurities of orlistat tablets, has the characteristics of stable quality and convenient operation, can improve the control of the weight of overweight sick cats, and realizes the aim of the invention.

Description

Orlistat tablet and preparation method thereof

Technical Field

The invention relates to the technical field of animal medicine, in particular to orlistat tablets and a preparation method thereof.

Background

With the development of the pet industry, the health care requirement and the raising level of animals are increasingly improved, and obesity (overweight) becomes a prominent problem troubling pets and is attracting more attention. Especially in cities in developed regions, the problem of obesity (overweight) has become the biggest threat to pet health and animal welfare. Recent survey data show that the problem of obesity (overweight) in pet cats shows a rising trend. According to the american Association of Pet Product Manufacturers (APPMA), the number of pet cats reaches 9630 ten thousand throughout the united states in 2009. In the united states, "national pet obesity promotion date," day 10/13 in 2010, a survey issued by the american pet obesity prevention Association (APOP) indicates that nearly 6000 million american pet cats are either obese or overweight.

The number of overweight pet cats received by the australian royal abuse prevention animal association (RSPCA) has been an increasing trend in recent years. RSPCA first veterinary Mark lawrrie indicated: "there is a survey showing that more than one third of pet cats in australia are overweight. "

The feeding number of pet cats in China is also rapidly increased, and data show that in 2018, the number of people in China towns reaches 7355 thousands, wherein the number of people who feed cats accounts for 30.7%, and more than 4000 thousands of pet cats exist. Although specific survey statistics are not seen in obese (overweight) pet cats in our country, the industry generally believes that the incidence of obesity in pet cats in our country is increasing as in many developed countries, and therefore great attention must be paid to and controlled as soon as possible.

Orlistat is a semisynthetic lipstatin derivative, has a strong selective effect of inhibiting the activity of gastric lipase and pancreatic lipase, is mainly combined with serine residues at the active site of lipase in total, leads to the disappearance of the activity of the lipase, prevents the hydrolysis of triacylglycerol, reduces the intake of monoglyceride and free fatty acid, achieves the purposes of controlling body weight, reducing blood sugar, reducing blood pressure, regulating fat and the like, and improves the state related to obesity. Orlistat can reduce fat absorption by 30%, and reduce cholesterol absorption in small intestine while excreting fat and feces out of body. The oral preparation is rarely absorbed after being taken, can be metabolized and inactivated in intestinal tracts, has metabolic sites on the walls of gastrointestinal tracts, and has an elimination half-life period of about 14-19 hours. About 97% of the product is excreted with feces, and 83% is excreted as it is.

The adhesive commonly used in wet granulation of the traditional tabletting process is starch slurry, the starch slurry has overhigh temperature and is easy to cause the pyrolysis of orlistat, so the produced orlistat tablets have more impurities and poorer quality stability, and are not ideal for controlling the weight of overweight cats.

Disclosure of Invention

The invention aims to provide orlistat tablets and a preparation method thereof, aiming at the defects and shortcomings of the prior art.

In order to achieve the purpose, the invention adopts the technical scheme that: the orlistat tablets have the innovation points that the orlistat tablets mainly comprise the following components in percentage by weight: 60mg of orlistat (calculated as orlistat), 3-10% (w/w) of disintegrating agent, 3-10% (w/w) of adhesive, 0.1-1% (w/w) of lubricant and the balance of filler.

Further, the filler is sucrose and microcrystalline cellulose, and the ratio of the filler to the filler is 1: 1.

Further, the disintegrant is crospovidone.

Further, the binder is copovidone.

Further, the lubricant is magnesium stearate.

The preparation method of the orlistat tablets has the innovation points that the preparation method comprises the following steps:

s1, sieving: sieving the raw and auxiliary materials with a 60-mesh sieve;

s2, weighing: accurately weighing orlistat, crospovidone, copovidone, magnesium stearate, sucrose and microcrystalline cellulose in the formula amount;

s3, placing the raw and auxiliary materials in a three-dimensional mixing pot according to the prescription amount, and mixing for 30 min;

s4, tabletting: and (3) tabletting the mixed material by a tabletting machine, and controlling the weight of the tablet to be 0.99-1.01 g.

The invention has the beneficial effects that:

the invention adopts a direct compression method for tabletting, effectively reduces the heavy impurities of orlistat tablets, has the characteristics of stable quality and convenient operation, can improve the control of the weight of overweight sick cats, and realizes the aim of the invention.

Detailed Description

The following examples further illustrate the invention.

In order to make the objects, technical solutions and advantages of the present invention more apparent, the present invention is further described in detail with reference to the following embodiments. It should be understood that the detailed description and specific examples, while indicating the invention, are intended for purposes of illustration only and are not intended to limit the scope of the invention.

Example 1

A preparation method of orlistat tablets comprises the following steps:

weighing 60g of orlistat, 70g of crospovidone, 50g of copovidone, 5g of magnesium stearate, 410g of sucrose and 410g of microcrystalline cellulose; and (3) placing the mixture in a three-dimensional mixing pot, mixing the materials for 30min, blanking, removing tablets and tabletting, wherein the weight of the tablets is controlled to be 0.99-1.01 g.

The orlistat tablets prepared by the method are subjected to content measurement of effective components and related substances by a high performance liquid chromatography, wherein the content is 90-110% of the marked amount, the maximum content of a single impurity of the related substance is not more than 0.2%, and the sum of all impurities is not more than 1.0%. In the 5 samples tested, the amount of each impurity is lower than the limit requirement in the related substance detection, the relative retention time of each impurity is in accordance with the regulation, the content is respectively 101.5%, 100.8%, 101.1%, 100.5% and 100.7%, and the results are in accordance with the standard regulation.

And (3) stability test: the product is placed in a stability test box for 24 months, and the detection shows that the property, the content and related substances of the product meet the requirements.

TABLE 1 results of accelerated test on orlistat tablets

Time (moon)	0	1	2	3	6
						Traits	White sheet	White sheet	White sheet	White sheet	White sheet
Related substances	Meets the requirements	Meets the requirements	Meets the requirements	Meets the requirements	Meets the requirements
						Content (%)	100.5	99.8	100.1	98.3	98.6

TABLE 2 Long-term test results of orlistat tablets

Time (moon)	0	3	6	9	12	18	24
								Traits	White sheet	White sheet	White sheet	White sheet	White sheet	White sheet	White sheet
Related substances	Meets the requirements	Meets the requirements	Meets the requirements	Meets the requirements	Meets the requirements	Meets the requirements	Meets the requirements
								Content (%)	100.5	100.1	99.7	100.4	98.1	98.3	99.0

And (4) conclusion: as can be seen from tables 1 and 2, after the product of the invention is placed for 24 months for a long time, the properties, the content and related substances are all qualified, and the product meets the relevant regulations in the orlistat tablet quality standard.

The above description is only for the purpose of illustrating the technical solutions of the present invention and not for the purpose of limiting the same, and other modifications or equivalent substitutions made by those skilled in the art to the technical solutions of the present invention should be covered within the scope of the claims of the present invention without departing from the spirit and scope of the technical solutions of the present invention.

Claims (6)

1. The orlistat tablet is characterized by mainly comprising the following components in percentage by weight: 60mg of orlistat (calculated as orlistat), 3-10% (w/w) of disintegrating agent, 3-10% (w/w) of adhesive, 0.1-1% (w/w) of lubricant and the balance of filler.

2. The orlistat tablet according to claim 1, wherein: the filler is sucrose and microcrystalline cellulose, and the ratio of the filler to the filler is 1: 1.

3. The orlistat tablet according to claim 1, wherein: the disintegrant is crospovidone.

4. The orlistat tablet according to claim 1, wherein: the binder is copovidone.

5. The orlistat tablet according to claim 1, wherein: the lubricant magnesium stearate.

6. A process for preparing orlistat tablets according to claims 1-5, comprising the steps of:

s1, sieving: sieving the raw and auxiliary materials with a 60-mesh sieve;

s2, weighing: accurately weighing orlistat, crospovidone, copovidone, magnesium stearate, sucrose and microcrystalline cellulose in the formula amount;

s3, placing the raw and auxiliary materials in a three-dimensional mixing pot according to the prescription amount, and mixing for 30 min;

s4, tabletting: and (3) tabletting the mixed material by a tabletting machine, and controlling the weight of the tablet to be 0.99-1.01 g.