JPH03161448A - Composition containing oil and fat - Google Patents

Abstract

PURPOSE:To obtain a powdery or granular composition containing oil and fat, free from bleeding of oil and fat even at a high content of oil and fat and keeping sufficiently high strength in a drug-preparation process by using an oil and fat, a base for including oil and fat, a polyol, a base agent for absorbing oil and fat and a binder at specific ratios. CONSTITUTION:The objective composition containing oil and fat is composed of (A) 1-70wt.% of oil and fat such as vegetable oil and pharmaceutical synthetic oil, (B) 30-90wt.% of a base for including oil and fat, e.g. partially hydrolyzed starch, hydrophilic protein or hydrophilic polysaccharide, (C) 1-20wt.% of a polyol, preferably a polyol which is liquid at ordinary temperature, especially glycerol, (D) 1-20wt.% of a base for absorbing oil and fat, preferably light silica and (E) 0.1-15wt.% of a binder, preferably polyvinyl pyrrolidone. Preferable amounts of the components are A<=60%, B=50-80%, C=2-5%, D=5-15% and E=1-5%. Four components other than the component B are uniformly mixed with each other, the component B is uniformly mixed into the mixture and the mixture is granulated and heated at about 60 deg.C for 5min to afford the objective solid composition having high fluidity and containing oil and fat.

Description

DETAILED DESCRIPTION OF THE INVENTION (Industrial Field of Application) The present invention is applicable to the pharmaceutical field, which includes oils and fats, bases for containing oils and fats,
The present invention relates to a fat-and-oil-containing composition having a medicinal ingredient consisting of polyol, a fat-absorbing base, and a binder.

(Prior Art) Since porcelain materials are generally difficult to handle, it is necessary to improve their physical properties. Among these, oil-based substances used as pharmaceuticals, that is, oil-based drugs, require improvements that take into account not only the physical properties but also the absorbability in the gastrointestinal tract. Therefore, as an oil-based drug formulation that satisfies these requirements, a powder formulation with water dispersibility is required.

Conventionally, methods for producing powdered oils and fats include: (1) Freeze-grinding method, in which solid fats with a high melting point are pulverized at low temperatures and pulverized. ■An impregnation method in which oil-impregnated base materials such as modified starch and cellulose are impregnated with fats and oils. (2) There is a spray drying method (Japanese Unexamined Patent Publication No. 150845/1984) in which an oil-in-water emulsion is prepared using a co-emulsifier such as sugar ester, a protein such as casein or gelatin, or starch, and this is spray-dried.

The freeze-grinding method (2) can only be applied to extremely hardened oils with a melting point of 60'C or higher, and the resulting powdered oils and fats melt very slowly and have large variations in solubility, making them generally unsuitable for pharmaceutical use.

In addition, the impregnation method (2) is a method that has been established as a formulation technology and has been commercialized, but the powdered fats and oils obtained by this method have problems such as oozing of fats and oils and a decrease in the fluidity of the powder. Because of this problem, it is limited to low oil and fat contents, so it is not a suitable technique when it is desired to contain a high oil and fat content.

In addition, in the spray drying method (2), since the degree of emulsification is high and the viscosity is high, spray drying cannot be performed unless the water content is increased to about 70 to 90%, and the amount of water that must be evaporated is large, resulting in low energy costs. It becomes huge.

On the other hand, Japanese Patent Application Laid-Open No. 64-27430 is a technology for applying liquid polyols to edible compositions containing fats and oils. This relates to powdered or granular fats and oils containing polyols and their manufacturing method, and is a technology that improves the leaching of fats and oils from powdered fats, but since a slight leaching of fats and oils is unavoidable, , is a difficult technology to apply in the pharmaceutical field.

Conventional methods for filling liquid oil-based drugs include filling soft capsules with the drug, or impregnating an impregnation base with a very small amount of liquid oil-based drug that does not ooze out of the powder. At present, there is no technology for obtaining powdered oils and fats made of drugs that are hard and have good fluidity.

(Problems to be Solved by the Invention) As a formulation technology for powdering fats and oils, a method has been adopted in which an oil-impregnated base is impregnated with a very small amount of liquid oil-based drug that does not ooze out from the powder. Powdered fats and oils obtained by this impregnation method have low fats and oils content due to problems such as leaching of fats and oils and decreased fluidity of the powder, so it is not possible to obtain the desired powdered fats and oils with a high content using the impregnation method. . Furthermore, the resulting powder becomes soft due to physical properties such as a large specific volume of the oil-containing base, and has the disadvantage of poor fluidity.

In addition, the application technology of liquid polyol to edible compositions containing fats and oils described in the above-mentioned Japanese Patent Application Laid-open No. 64-27430 is as follows:
Although this is a technique for obtaining powder and granules with good fluidity and less oozing of oil and fat by adding a liquid polyol, a slight amount of leaching of the oil and fat from the powdered oil and fat is unavoidable. The oozing of oils and fats in pharmaceuticals suggests a decrease in the content of oil-based drugs, which are crude drugs, in the preparation.
It becomes impossible to administer the prescribed amount of drug to the patient.

■In the case of food products, even if some amount of oil or fat adheres to the packaging material, the impact on the human body is minimal, but in the case of pharmaceuticals, adhesion to the packaging material has the problem of reducing the content of ■. It is inconvenient for patients to take. From the above points, even the slightest leaching of fats and oils makes it extremely difficult to apply in the pharmaceutical field. Therefore, there is a need to establish a technology for producing a formulation that does not seep out even with a high content of fat and oil and has sufficient strength as a powder.

(Means for Solving the Problems) As a result of intensive research to overcome the problems of conventional techniques such as oil seepage, the present inventors have discovered that oils and fats, oil and fat absorption bases,
By creating an oil-containing composition comprising a binder, a base for containing oils and fats, and a polyol, it contains a high content of oils and fats, and furthermore, there is no leaching of oil and a sufficient amount of oil can be maintained even during the formulation process. We have completed a powdered or granular oil with strength.

Preferred composition of powdery or granular fats and oils of the present invention or fats and oils 1
-70% by weight, more preferably up to 60% by weight of fats and oils, 1-20% by weight of fat-absorbing base, more preferably 5-20% by weight
15% by weight, binder 0.1 to 15% by weight, more preferably 1 to 5% by weight, base for fat and oil inclusion 30 to 90% by weight,
More preferably 50 to 80% by weight and 0.0% by weight of polyol.
It is 1 to 10% by weight, more preferably 2 to 5% by weight.

Powdered or granulated products of the above composition are particularly suitable for use as pharmaceuticals because they do not seep out of oil and fat, have strength that can withstand the formulation process, and have good fluidity. No problem.

The base for containing fats and oils in the present invention refers to a base for encapsulating or impregnating fats and oils.

The base for inclusion of fats and oils used in the present invention may be either hydrophilic or hydrophobic substances, and specifically, dextrin (
For example, starch partial hydrolysates such as Pinedex [F] #1, hydrophilic proteins such as gelatin, casein, and albumin, starch, hydrophilic polysaccharides such as carboxymethyl cellulose, and hydrophilic amino acids such as glutamic acid and lysine. or its salts, organic acids such as lactose [M, citric acid, succinic acid, adipic acid, etc., or their salts, and salts commonly used in pharmaceuticals such as sodium chloride, potassium chloride, etc., or any of these two. Examples include a mixture of more than one species, or a pharmaceutical composition containing at least one of them, but among them, dextrin, which is a starch partial hydrolyzate with a low decomposition rate, is preferred.

The shape of the fat/oil inclusion base used in the present invention is not particularly limited, but it is preferably powder-like (spherical), and its preferred particle size is 50 mesh passes or less, more preferably 100 mesh passes or less. . Further, it is preferable that the base does not contain an emulsifying base such as lecithin.

The fats and oils referred to in the present invention are not particularly limited and may be vegetable oils, pharmaceutical oils, solid fats, semi-solid fats, liquid oils, or mixtures of two or more of these. For example, bita ξ
Fat-soluble vitamins and their derivatives such as vitamin A and vitamin E, linoleic acid, linolenic acid, arachidonic acid, EPA,
Examples include lipids such as docosahexaenoic acid, natural or prescribed medicines such as nifedibine, gefarnate, plaunotol, clofibrate, tribenoside, prostaglandin drugs such as ornoprostil, and plant sterols such as soysterol.

The oil-absorbing base used in the present invention is preferably one with high oil-retaining properties, such as aluminum compounds such as magnesium metasilicate aldanate, magnesium silicate, magnesium oxide, dry aluminum hydroxide gel, and synthetic aluminum silicate. , magnesium compounds, celluloses such as Avicel, and light silicic anhydride, among which light silicic anhydride is preferred.

Examples of the polyol used in the present invention include non-toxic glycols such as glycerin and propylene glycol, and sugars or sugar alcohols. Among them, polyols that are liquid at room temperature are preferred, and glycerin is more preferred.

Further, the binder used in the present invention may be any pharmaceutically acceptable binder, and specifically, gum arabic, tragacanth, gelatin, starch, methylcellulose, carboxymethylcellulose-Na, HPMC, and polyvinylpyrrolidone are used. Among these, polyvinylpyrrolidone is preferred.

Next, a method for producing powdered or granular fats and oils of the present invention will be explained.

The powdered or granular fat or oil of the present invention comprises 1 to 70% by weight of fat, 1 to 20% by weight of fat-absorbing base, and 0.5% by weight of fat-and-oil absorption base. l~15% by weight
It is obtained by uniformly mixing and stirring a binder, 30 to 90% by weight of a base for inclusion of fat and oil, and 1 to 10% by weight of polyol at a temperature equal to or higher than the melting point of the fat or oil.

Although the method for mixing the above-mentioned raw materials is not particularly limited, it is preferable to uniformly combine the fats and oils, the fat-and-oil absorption base, the binder, and the base for including fats and oils, and then uniformly mix the polyol.

These mixtures are subjected to a granulation process and further heated at around 60°C for 5 minutes to obtain a hard oil-containing composition with good fluidity. In the present invention, the polyol is in a liquid state at the time of mixing. That is, glycols such as glycerin and propylene glycol are kept at a temperature above their melting point, and in the case of aphrodisiacs or sugar alcohols, they are made into an aqueous solution with the highest possible concentration.

The preferred water content at the time of mixing of the raw material composition comprising fats and oils, a fat-absorbing base, a base for containing fats and oils, a binder and a polyol is 15% by weight or less, more preferably 1% by weight or less.
It is 0% by weight or less. The reason for this is that the pulverization phenomenon of the oil- and fat-containing composition due to the polyol does not proceed in a system with a high moisture content.

However, it is also possible to disperse the raw materials in water, spray dry them, and pulverize them.

Furthermore, it is also possible to pulverize a drug dissolved or dispersed in oil or fat at room temperature.

In the present invention, the equipment used to mix and stir the fats and oils, fat-absorbing base, base for containing fats and oils, binder, and liquid polyol is a mixer, a kneader, a granulator, etc. used in normal pharmaceutical manufacturing processes. It can be used without any particular limitation. The mixing time varies depending on the scale and the raw materials used, so it is set appropriately.

In the production of powdery or granular fats and oils of the present invention, if a high-speed stirring granulator, a fluidized bed granulator with stirring blades, etc. are used,
Rice-like or granular fats and oils with a relatively uniform particle size of 1000 μm can be obtained, but depending on the equipment or purpose used, it is possible to use only those in the desired particle size range by sizing after pulverization. .

The important points in producing the powdered or granular fats and oils of the present invention are 1.
~70% by weight of oil, 1 to 20% by weight of fat-absorbing base and 0. 1 to 15% by weight of binder is added together. The purpose of the present invention is to obtain a powder with good fluidity consisting of a high content of fats and oils, and also to avoid oozing of fats and oils. Even if it is obtained, the purpose cannot be achieved due to leaching of oil and fat. However, by adding an oil- or fat-absorbing base and a binder, the oil- or fat-absorbing base with high oil-retaining performance captures the oil and becomes the core of the oil-containing composition, and the binder hardens the core. It is thought that this makes it easier to cover the nucleus. Therefore, the target oil and fat will not seep out.
It seems possible to obtain a powder with good fluidity.

If the amount of the fat-absorbing base is outside this range, the fluidity of the granulated product will be poor due to its large specific volume, and furthermore, the fats and oils will seep out, so that the objective cannot be achieved. Furthermore, what is important in the present invention is to uniformly disperse 0.1 to 10% by weight of the liquid polyol into the other raw materials. The polyol is uniformly separated, and after the granulation process, 60'
By heating around C for 5 minutes, the desired hard oil-containing composition can be obtained.

In particular, when dispersing a highly viscous liquid such as glycerin or a highly concentrated sugar alcohol aqueous solution, heating and spraying is extremely effective.

The reason why fats and oils can be easily powdered by the above production method and the reason why the powdered or granular fats and oils of the present invention quickly separates fats and oils when water is added are not necessarily clear, but are speculated as follows.

That is, by mixing the oil, fat-absorbing base, and binder, a solid core containing oil and fat is formed. moreover,
The core is covered with a base for containing fats and oils, and by uniformly mixing and stirring with liquid polyol, the polyol crosslinks between the primary particles of the hydrophilic base for containing fats and oils, resulting in granulation (three-dimensional structure). It is thought that oils and fats are included in the voids between the primary particles while forming (forming) the primary particles. Therefore, it is presumed that when water is added, the hydrophilic structure consisting of the hydrophilic base for containing fats and oils and the polyol dissolves, and the fats and oils inside are released.

(Effects of the Invention) The oil-containing Mi prefecture of the present invention has the following excellent characteristics.

1) Compared to powdered fats and oils obtained by normal impregnation methods, leaching of fats and oils is extremely small. In particular, there is no leaching of fats and oils even at high fat and oil contents of 30% or more, and even 50% or more. Therefore, the powder has very good fluidity.

2) It is possible to produce granules containing high oil and fat content up to 70% by weight.

3) By adding a liquid polyol, a hard powder with good dispersibility can be obtained, with quick separation of fats and oils when water is added.

4) Odor and unpleasant taste can be avoided due to the fat and oil inclusion effect of the liquid polyol.

5) No drying process is required, and the manufacturing method is extremely simple and economical.

6) It can be applied to any oil such as liquid oil-based drugs and solid fat, and the resulting powdered oil has a wide range of uses.

7) Gastrointestinal absorption is promoted by the coexistence of fats and oils After dispersing and suspending the drug in fats and oils, it is also possible to make a powdered preparation.

8) It is also possible to disperse and suspend a drug that easily decomposes on contact with water in oil and fat, and then stabilize it as a powdered preparation.

The following experimental examples demonstrate the effects of the present invention in more detail. Prescriptions 1 to 7 show the respective prescriptions of the samples used in the study. Formulation 1 to Formulation 6 have an oil content of 35% by weight, Formulation 7 has an oil content of 60% by weight, and Formulation 6 and 7 are the compositions of the present invention.

Manufacturing method: After uniformly mixing and stirring the bases shown in each formulation example below, a powder was obtained by heating at around 60°C for 5 minutes through a granulation process.

<Experimental example> Formulation 1 Light anhydrous silicic acid 65 parts by weight Soybean oil
35 parts by weight Formula 2 Light silicic anhydride 63 parts by weight Polyvinylpyrrolidone (K-90) 2 parts by weight Soybean oil
35 parts by weight Formulation 3 Pine Denks [F] #1 (DE・8) 65 parts by weight Soybean oil 35 parts by weight Glycerin 3 parts by weight Formulation 4 Pine Denks #1 (DE・8) Polyvinylpyrrolidone (K-90) Soybean oil glycerin prescription 5 Pine Index [F] # 1 (DE=8) Light anhydrous polyvinyl pyrrolidone silicate (K-90) Soybean oil formulation 6 Pine Index # 1 (DE/8) Light polyvinyl pyrrolidone silicate anhydride (K-90) Large Soybean oil glycerin formulation 7 Pine Index #1 (DE・8) Light anhydrous polyvinylpyrrolidone silicate (K-90) Soybean oil 65 parts by weight 2 parts by weight 35 parts by weight 53 parts by weight 10 parts by weight 2 parts by weight 35 parts by weight Part 53 parts by weight 10 parts by weight 2 parts by weight 35 parts by weight 3 parts by weight 33 parts by weight 30 parts by weight 2 parts by weight 99 parts by weight Glycerin 3 parts by weight The measurement results are shown. Each evaluation method is described below.

Evaluation method ■ To measure the leaching of fats and oils, place approximately 1 g of a 32-mesh sample that has passed through a 28-mesh sieve on a filter paper, then cover the filter paper and place 200 g as a weight. Determine the residual rate after 3 hours, and 0% indicates no seepage.
Calculate the oil seepage as .

■ The angle of repose is determined by powder desk calculation based on the residual cone method.
Product name: Konishi FK type angle of repose measuring device].

The particle size of the measurement sample was 32 after passing through a 28 mesh sieve.
Use 15 g of sample on the mesh.

■ The hardness of the powder is measured by the percentage remaining on the sieve after passing the sample through a 32-mesh sieve after the oil and fat leaching test.

Table 1 Leaching of fats and oils, angle of repose and hardness measurement From the results in Table 1, formulations 6 and 7 of the present invention have almost no leaching of fats and oils. The angle of repose also shows good values for a powder. Although the hardness of the granular oil and fat is slightly inferior to Formulas 3 and 4, it is considered that the hardness is significantly improved compared to the conventional impregnation method (Formulation 1). From the results of Formulation 7, it was found that granular fats and oils with a fat content of 60% by weight could be produced satisfactorily. Therefore, it was observed that the powder of the present invention did not seep out of oil and fat and had good fluidity as a powder or granule.

To summarize the above, the granular fats and oils obtained by the present invention have a composition and structure that easily disintegrates with water, so separation of the fats and oils occurs quickly when water is added, and therefore, environments where rapid release is desired. Good release (immediate release) is expected at lower temperatures.

In addition, compared to powdered fats and oils obtained by normal impregnation methods,
It has a high oil and fat content, and has high fluidity because it produces hard powder and granules without leaching of oil and fat. Moreover, liquid oil
It can be applied to any type of fat or oil, including solid fats, and has the advantage of being versatile. The high oil and fat content can be expected to be applied to reduce the dosage of pharmaceuticals, that is, to miniaturize capsules and the like.

Furthermore, by pulverizing a liquid oil-based drug, the ease of filling and handling the drug is greatly improved, making dispensing within a hospital and administering it to a patient less complicated and easier to operate.

In addition to powdering liquid oil-based drugs, powdered oils and fats can be used as intermediate raw materials for solid preparations such as tablets and capsules.

(Examples) Examples of the present invention are shown below, but the present invention is not limited to these Examples.

Example 1 Vitagon E 35 parts by weight Light silicic anhydride 10 parts by weight Polyvinylpyrrolidone (
K-90) 2 parts by weight Pine Index [F] #1
53 parts by weight Glycerin 3 parts by weight Production method 35 parts by weight of Vitamin C, 10 parts by weight of light silicic acid anhydride, 2 parts by weight of polyvinylpyrrolidone (K~90) and 53 parts by weight of binder index [F] #l After sufficiently kneading, 3 parts by weight of glycerin was further added and stirred to make the mixture uniform. After the granulation process, the mixture was heated at 60° C. for 5 minutes to obtain powder.

The angle of repose of the obtained granular material was 44°, there was no seepage of oil or fat, and the hardness of the granular material was good at 91.7%.

Further, when the powdered oil and fat were added to water, the oil and fat were quickly separated.

The following manufacturing methods are also used in Examples 2 to 14.

Example 2 Gefarnate 35 parts by weight Light silicic anhydride IO Parts by weight Polyvinylpyrrolidone (
K-90) 2 parts by weight Pine Denks [F] #1
(DE・8) 53 parts by weight glycerin
The angle of repose of the granular material obtained at 3 parts by weight was 46°, there was no seepage of oil or fat, and the hardness of the granular material was good at 89.7%. Further, when the powdered oil and fat were added to water, the oil and fat were quickly separated.

Example 3 Linoleic acid 35 parts by weight Light silicic anhydride 10 parts by weight Polyvinylpyrrolidone (K
-90) 2 parts by weight Pine Denox ■#1 (D
E.8) 53 parts by weight glycerin
The angle of repose of the powder obtained at 3 parts by weight was 42°, there was no seepage of oil and fat, and the hardness of the powder was good at 84.7%. Further, when the powdered oil and fat were added to water, the oil and fat were quickly separated.

Example 4 Linolenic acid 35 parts by weight Light silicic anhydride 10 parts by weight Polyvinylpyrrolidone (K
-90) 2 parts by weight Paindex [F] #1
(DE・8) 53 parts by weight glycerin
The angle of repose of the powder obtained at 3 parts by weight was 43°, there was no seepage of oil and fat, and the hardness of the powder was good at 90.7%. Further, when the powdered oil and fat were added to water, the oil and fat were quickly separated.

Example 5 Arachidonic acid 35 parts by weight Light silicic anhydride 10 parts by weight Polyvinylpyrrolidone (K
-90) 2 parts by weight Paindex [F] #1
(DE・8) 53 parts by weight glycerin
The angle of repose of the powder obtained in 3 parts by weight was 43°, there was no oozing of oil and fat, and the hardness of the powder was good at 85.1%. Further, when the powdered oil and fat were added to water, the oil and fat were quickly separated.

Example 6 Docosahexaenoic acid 35 parts by weight Light silicic anhydride 10 parts by weight Polyvinylpyrrolidone (K
-90) 2 parts by weight Paindex [F] #1
(DE・8) 53 parts by weight glycerin
The angle of repose of the powder obtained at 3 parts by weight was 40', there was no seepage of oil and fat, and the hardness of the powder was good at 83.9%. Further, when the powdered oil and fat were added to water, the oil and fat were quickly separated.

Example 7 Peppermint oil 35 parts by weight Light silicic anhydride 10 parts by weight Polyvinylpyrrolidone (K
-90) 2 parts by weight Pinedenox■#l (D
H・8) 53 parts by weight glycerin
The angle of repose of the powder obtained at 3 parts by weight was 46°, there was no seepage of oil and fat, and the hardness of the powder was good at 89.0%. Further, when the powdered oil and fat were added to water, the oil and fat were quickly separated.

Example 8 Vitamin 8 oil 35 parts by weight Light silicic anhydride 10 parts by weight Polyvinylpyrrolidone (K
-90) 2 parts by weight Vitamin C
53 parts by weight Glycerin 3 parts by weight The angle of repose of the obtained powder was 45°, there was no oozing of oil and fat, and the hardness of the powder was good at 86.4%.

Further, when the powdered oil and fat were added to water, the oil and fat were quickly separated.

Example 9 Soysterol 35 parts by weight Light silicic anhydride 10 parts by weight Polyvinylpyrrolidone (K
-90) 2 parts by weight Pine Index ■#1 (D
E=87 5 3 parts by weight glycerin
The angle of repose of the powder obtained in 3 parts by weight was 46°, there was no oozing of oil and fat, and the hardness of the powder was good at 87.2%. Further, when the powdered oil and fat were added to water, the oil and fat were quickly separated.

Example 10 EPA 3 5 parts by weight Light silicic anhydride 10 parts by weight Polyvinylpyrrolidone (K-90) 2 mm parts Pa index ■#
1 (DE・8) 53 parts by weight glycerin
The angle of repose of the powder and granules obtained in 3 parts by weight was 44°, there was no seepage of oil and fat, and the hardness of the powder and granules was 84.9.
%, which was good. Also, when the powdered oil is added to water,
The fat and oil separated quickly.

Example 11 Tribenoside 35 parts by weight Light silicic anhydride io Parts by weight Polyvinylpyrrolidone (K
-90) 2 parts by weight Pine Denks ■#1 (D
E.8) 53 parts by weight glycerin
The angle of repose of the granular material obtained at 3 parts by weight was 46°, there was no seepage of oil or fat, and the hardness of the granular material was good at 82.4%. Further, when the powdered oil and fat were added to water, the oil and fat were quickly separated.

Example 12 Ornobrostil 35 parts by weight Light silicic anhydride IO Parts by weight Polyvinylpyrrolidone (K
-90) 2 parts by weight Pine index [F] #l
([lE=8) 5 3 parts by weight glycerin
The angle of repose of the powder and granules obtained in 3 parts by weight was 40°, there was no clarification of fat and oil, and the hardness of the powder and granules was 80.1.
%, which was good. Also, when the powdered oil is added to water,
The fat and oil separated quickly.

Example 13 Docosahexaenoic acid 35 parts by weight Light silicic anhydride 10 parts by weight Polyvinylpyrrolidone (K
-90) 2 parts by weight Pine Index ■#1 (D
E.8) 53 parts by weight glycerin
The angle of repose of the rice granules obtained at 3 parts by weight was 43°, there was no oozing of oil and fat, and the hardness of the granules was good at 88.9%. Further, when the powdered oil and fat were added to water, the oil and fat were quickly separated.

Example 14 Clofibrate 35 parts by weight Light silicic anhydride 10 parts by weight Polyvinylpyrrolidone (K
-90) 2 parts by weight Pine index [F] #l
(DE・8) 53 parts by weight glycerin
The angle of repose of the granules obtained in 3 parts by weight was 46°, there was no oozing of oil and fat, and the hardness of the rice granules was as good as 89.5%. Further, when the powdered oil and fat were added to water, the oil and fat were quickly separated.

Example 15 N4-valmitoyl-β-D-arabinofuranosylcytosine 1 heavy mm sesame oil 3
5 parts by weight Light silicic anhydride 10 parts by weight Polyvinylpyrrolidone (K-90) 2 parts by weight Pine Index #1 (DE=8) 5 3 parts by weight Glycerin 3 parts by weight Manufacturing method 7 parts by weight N4-Valmitoy B-β After dispersing and suspending -D-arabinofuranosylcytosine and 35 parts by weight of sesame oil, 10 parts by weight of light silicic anhydride, 2 parts by weight of polyvinylpyrrolidone (K-90) and 53 parts by weight of pinde nox. [F] Add #1 and mix thoroughly, then add 3
Parts by weight of glycerin were added, stirred to make it uniform, and after the granulation process, a powder was obtained by heating for 60"05 minutes.The angle of repose of the obtained powder was 43 degrees, There was no seepage of oil or fat, and the hardness of the powder was good at 87.7%.

Similar manufacturing methods were used in Examples 16 to 19 below.

Example 16 Nifedipine 2.8 parts by weight Soybean oil
35 parts by weight light silicic anhydride
10 parts by weight polyvinylpyrrolidone (K-90)
2 parts by weight Pine Denks [F] #1 (DE・8)
53 parts by weight Glycerin 3 parts by weight The angle of repose of the obtained powder was 43°, there was no oozing of oil and fat, and the hardness of the powder was good at 88.1%.

Example 17 Vitamin K2 15 parts by weight Soybean oil
35 parts by weight light silicic anhydride
10 parts by weight polyvinylpyrrolidone (K-90)
2 parts by weight Vitamin ξ C 53 parts by weight Glycerin 3 parts by weight The angle of repose of the obtained powder was 41°, and there was no seepage of oil or fat.
The hardness of the powder was also good at 91.3%.

Example 18 Vitamin D2 15 parts by weight soybean oil
35 parts by weight light silicic anhydride
10 parts by weight polyvinylpyrrolidone (K-90)
'2 parts by weight Vitamin C 53 parts by weight Glycerin 3 parts by weight The angle of repose of the obtained powder was 46°, and there was no seepage of oil or fat.
The hardness of the powder was also good at 88.1%.

Example 19 Amphotericin-8 7 parts by weight Sodium dioxygol 5. 6
Parts by weight Soybean oil 35 parts Light silicic anhydride 10 parts by weight Polyvinylpyrrolidone (K-90) 2 parts by weight Pine index [F]#
1 (DE・8) 53 parts by weight glycerin
The angle of repose of the powder and granules obtained in 3 parts by weight was 46°, there was no seepage of oil and fat, and the hardness of the powder and granules was 86.7.
%, which was good.

(other names)

Claims (1)

[Claims] 1-70% by weight of fats and oils, 30-90% by weight of base for fat and oil inclusion, 0.1-10% by weight of polyol, 1-20% by weight of fat-absorbing base and 0.1-15% by weight of binding. An oil- and fat-containing composition consisting of an agent.