JP5199508B1 - Easily disintegrating royal jelly-containing tablet and method for producing the same - Google Patents

Abstract

Disclosed is an easily disintegratable royal jelly-containing tablet capable of shortening the disintegration time in a tablet containing royal jelly as a main component, and a method for producing the same.
The easily disintegrating royal jelly-containing tablet of the present invention contains royal jelly as a main component and is described in the 16th revision of the Japanese Pharmacopoeia by changing the three-dimensional structure of the protein in the raw jelly as a raw material. When a disintegration test is performed by the disintegration test method, the disintegration time is defined to be within 30 minutes. Preferably, the change of the three-dimensional structure is performed by heat treatment at 45 ° C. or higher.
[Selection figure] None

Description

  The present invention relates to an easily disintegrating royal jelly-containing tablet having improved tablet disintegration and a method for producing the same.

  Generally, royal jelly is a jelly-like substance made by mixing secretions secreted from the hypopharyngeal gland and the greater vagina by female honeybees 3 to 15 days after emergence, and contains specific proteins, fatty acids, minerals, etc. It is known that RJ is known to have various physiological actions such as blood pressure lowering action, antitumor action, serum cholesterol lowering action, antibacterial action, side effect reducing action of radiation and chemotherapeutic agents, action against chronic diseases and the like. . Therefore, royal jelly has been used not only for health foods with high nutritional value but also for uses such as pharmaceuticals.

  Conventionally, as a form for ingesting royal jelly, a method of filling royal jelly into a soft capsule is known. For example, Patent Document 1 discloses a method of filling royal jelly into a soft capsule together with a filler such as an oil component. However, since soft capsules are usually blended in a liquid state, a sufficient amount cannot be blended as a dry weight, and many oily ingredients and emulsifiers blended as fillers are mixed at a time. There was a problem that the amount to be consumed was limited. There is also a problem that the storage stability is not sufficient. In addition, as a form for ingesting royal jelly, a method of forming a tablet using lyophilized royal jelly is known.

JP 2001-178383 A

  However, tablets produced using lyophilized royal jelly have poor disintegration. For example, when a disintegration test according to the disintegration test method described in the Japanese Pharmacopoeia 16th revision is performed, the disintegration time exceeds 60 minutes. There was a problem that there was a case. This is because the tablet containing the royal jelly absorbs water, whereby the tablet surface gels and prevents the tablet from collapsing.

  This invention is made | formed by discovering that the gelatinization of the tablet surface can be suppressed and the disintegration property of a tablet can be improved by changing the three-dimensional structure of the protein contained in a royal jelly.

  The present invention provides an easily disintegrating royal jelly-containing tablet capable of shortening the disintegration time in a tablet containing royal jelly as a main component and a method for producing the same.

In order to achieve the above object, the easily disintegrating royal jelly-containing tablet of the present invention is an easily disintegrating royal jelly-containing tablet containing 30% by mass or more of royal jelly, and the three-dimensional structure of the protein in the royal jelly as a raw material thereof by varying, in the case of performing the disintegration test according to the disintegration test method described in the Japanese Pharmacopoeia 16th revision, is defined to disintegration time is within 30 minutes, the change in the conformation, raw royal jelly or It is characterized in that the royal jelly dissolved in the solvent was subjected to a heat treatment at 45 ° C. or higher .

The manufacturing method of the easily disintegrating royal jelly-containing tablet of the present invention is a manufacturing method of an easily disintegrating royal jelly-containing tablet containing 30% by mass or more of royal jelly, and the manufacturing method thereof is a raw material royal jelly for the easily disintegrating royal jelly-containing tablet. Ri Na comprise processing step of changing the conformation of the proteins in the processing step of changing the conformation, to royal jelly dissolved in raw royal jelly or solvent, comprising the step of heat treatment above 45 ° C., The easily disintegrating royal jelly-containing tablet is characterized in that, when a disintegration test according to the disintegration test method described in the 16th revision of the Japanese Pharmacopoeia is performed, the disintegration time is specified to be within 30 minutes.

  According to the present invention, the disintegration time can be shortened in a tablet containing royal jelly as a main component.

The electrophoresis photograph of the heat-treated royal jelly in Test Example 2 is shown. (A) A photograph showing the results of Native-PAGE. (B) A photograph showing the results of SDS-PAGE.

Hereinafter, an embodiment of an easily disintegrating royal jelly-containing tablet embodying the present invention will be described.
Royal jelly (hereinafter referred to as “RJ”) contained as a main component in an easily disintegrating royal jelly-containing tablet is raw RJ and raw RJ powder as raw materials dried by freeze-drying or the like (FD-RJ) ) Can be used. The production area of raw RJ and dry RJ used in the present embodiment is not particularly limited. For example, any of Asian countries such as China, Taiwan and Japan, European countries, North American countries, South American countries such as Brazil, and Oceania countries But you can.

  Here, containing RJ as a main component means that a component having a high abundance ratio (% by mass) in the tablet is RJ. And it is preferable that content of RJ in a tablet is 30 mass% or more, and 60 mass% or more is more preferable. When the RJ content in the tablet is 30% by mass or more, the intake or blending amount of RJ can be increased. Moreover, you may contain additives, such as an excipient | filler and a functional material, as components other than RJ.

  The easily disintegrating RJ-containing tablet of the present embodiment is subjected to a disintegration test according to the disintegration test method described in the 16th revision of the Japanese Pharmacopoeia by changing the three-dimensional structure of the protein in RJ as a raw material. It is specified that the decay time is within 30 minutes.

  Here, changing the three-dimensional structure of the protein in RJ indicates a state in which only the three-dimensional structure is changed while maintaining the primary structure of the protein. As a method for changing the three-dimensional structure of the protein in RJ, a known method is appropriately employed. For example, heating, alkali treatment, ionizing radiation treatment and the like can be mentioned. Among these, heat treatment is preferable from the viewpoints of ease of treatment, uniform treatment, and easy disintegration.

  When heat treatment is performed as a change in the three-dimensional structure, the heating temperature is preferably 45 ° C. or higher. When heating temperature is 45 degreeC or more, the three-dimensional structure of the protein in RJ can be changed easily and easy disintegration can be improved. Although the upper limit of the heating temperature is not particularly defined, it is generally performed at a temperature at which the protein is not carbonized.

  The heating time is appropriately set depending on the heating temperature, but the three-dimensional structure of the protein can be changed by heat treatment for several hours. For example, it is preferably 180 minutes or longer at 50 ° C., 30 minutes or longer at 60 ° C., and 15 minutes or longer at 70 ° C., respectively.

  The disintegration test method is performed in accordance with the 6.09 disintegration test method described in the general test method of the 16th revision of the Japanese Pharmacopoeia. When such a disintegration test is performed, the easily disintegratable RJ-containing tablet of this embodiment is specified to have a disintegration time of 30 minutes or less, more preferably 25 minutes or less, and even more preferably 20 minutes. By defining the disintegration time within 30 minutes, when the tablet is ingested, the disintegration of the tablet is accelerated and the absorption can be accelerated. In addition, it complies with the provision of 2.1 immediate release formulation (within 30 minutes of uncoated tablet) of the 6.09 disintegration test method of the 16th revision of the Japanese Pharmacopoeia.

Next, the manufacturing method of the easily disintegratable RJ containing tablet comprised as mentioned above is demonstrated.
In the production method of the easily disintegratable RJ-containing tablet of the present embodiment, first, a processing step is performed in which the three-dimensional structure of the protein in raw RJ or FD-RJ is changed as a raw material. For example, when heat treatment is performed, raw RJ or FD-RJ may be directly heat-treated, and after dissolving raw RJ or FD-RJ in a solvent such as water, buffer, and organic solvent, together with the solvent Heat treatment may be performed. Among these, the method of heat-treating after dissolving in a solvent is preferable from the viewpoint of uniformity of heating.

  After the treatment for changing the three-dimensional structure of the protein in RJ is performed, the modified treatment RJ is dried and molded into a tablet using a tableting machine. The form of the modification treatment RJ at the time of molding into a tablet is not particularly limited, and may be a powder or a granule having a predetermined particle size.

Next, the operation of the easily disintegratable RJ-containing tablet configured as described above will be described.
The easily disintegrating RJ-containing tablet of this embodiment is subjected to a treatment for changing the three-dimensional structure of the protein in the raw material RJ. Thereby, when a disintegration test by the disintegration test method described in the 16th revision of the Japanese Pharmacopoeia is performed, the disintegration time is specified to be within 30 minutes. Usually, a tablet manufactured using freeze-dried RJ may cause gelation of the tablet surface due to water absorption of the tablet containing RJ, thereby preventing disintegration of the tablet. By performing the treatment for changing the three-dimensional structure of the protein in the RJ as a raw material, only the three-dimensional structure is changed while the primary structure of the protein is maintained. Thereby, when the modified RJ is molded into a tablet, the disintegration property of the RJ-containing tablet in water can be improved.

According to the easily disintegratable RJ-containing tablet of the above embodiment, the following effects can be obtained.
(1) The easy-disintegrating RJ-containing tablet of the above embodiment is described in the 16th revision of the Japanese Pharmacopoeia by containing RJ as a main component and changing the three-dimensional structure of the protein in RJ as a raw material. When a disintegration test is performed by the disintegration test method, it is specified that the disintegration time is within 30 minutes. Therefore, when the easily disintegratable RJ-containing tablet is ingested, the disintegration property in the digestive organ can be improved.

(2) Preferably, the heat treatment is performed at 45 ° C. or higher. Therefore, the change process of the three-dimensional structure of the protein in RJ can be easily performed.
In addition, you may change the said embodiment as follows.

  -As a specific blending form of the easily disintegrating RJ-containing tablet of the present embodiment, it may be applied as a pharmaceutical intended for taking the tablet, a quasi-drug, a food, a health food, a food for specified health use, etc. it can.

  -The easily disintegratable RJ-containing tablet of this embodiment is preferably provided in the form of an uncoated tablet from the viewpoint of disintegration. However, a coating treatment such as sugar coating may be performed from the viewpoint of improving moisture absorption resistance, improvement in feeling of taking, suppression of changes in properties and appearance, and the like within a range that does not impair the effects of the present invention.

  -An additive may be mix | blended in an easily disintegrating RJ containing tablet within the range which does not inhibit the effect of this invention. As an additive, a well-known additive is suitably selected according to the administration purpose of an easily disintegrating RJ containing tablet. Examples of additives include excipients, functional materials, binders, bases, stabilizers, sugars, fragrances, sweeteners, fats and oils, base materials, food additives, auxiliary materials, and bulking agents. Moreover, as an excipient | filler, a well-known thing is employ | adopted suitably, For example, crystalline cellulose, saccharides, starch, a stearate etc. are mentioned. Examples of the functional material include minerals such as Ca and Mg, vitamins, polyphenols such as isoflavones, and propolis.

-The easily disintegratable RJ containing tablet of this embodiment contains RJ as a main component. Therefore, the easily disintegrating RJ-containing tablet may contain only the RJ without containing an additive.
-The shape of the easily disintegrating RJ-containing tablet of the present embodiment is not particularly limited, and may be, for example, a circle, a circle, a long shape, a polygon, or the like.

  -RJ contained in the easily disintegratable RJ-containing tablet of the present embodiment may be partially decomposed by a proteolytic enzyme within the range that does not inhibit the effect of the present invention, but is improved in moisture absorption resistance and handling properties. From the viewpoint, it is preferable that the proteolytic enzyme treatment is not performed.

Although the test example is given below and the embodiment is described more specifically, the present invention is not limited to these.
(Test Example 1: Examination of heating conditions)
(1) Preparation of RJ-containing tablets 244 g of Chinese-produced RJ (solid content 32.8% (w / w)) was added to 156 g of water as a solvent, and stirred at room temperature (about 25 ° C.) for about 1 hour. Dissolved. Next, this solution was used as a comparative example at 40 ° C. (8, 16, 24 hours), and as examples, 50 ° C. (3,4, 8, 16 hours), 60 ° C. (30 minutes, 1, 4 hours), 70 ° C. (15, 30 minutes, 1, 4 hours), 80 ° C. (15, 30 minutes, 1 hour), 90 ° C. (15, 30 minutes, 1 hour) at each treatment temperature and time, protein The process which changes the three-dimensional structure of was implemented. In addition, FD-RJ which was not heat-processed was used as control (comparative example 1). The resulting treated solution was lyophilized to obtain a powder. In each example, 62.15% by mass of the obtained powder and the remainder were added with additives (porosified starch (manufactured by Nissho Chemical Co., Ltd., Long Food OWP) 33.65 parts by mass, powdered cellulose (manufactured by Nippon Paper Chemicals Co., Ltd., KC Flock W-50) 3 parts by mass and 1.2 parts by mass of calcium stearate (setty) 1.2), and using a single tableting machine (SSP-10A, manufactured by Shimadzu Corporation) Each tablet was obtained using a scissors. In Comparative Example 2, 50% by mass of FD-RJ that was not heat-treated and the balance containing an additive composed of the same components as above were used. In Comparative Example 3, 40% by mass of FD-RJ that was not heat-treated and the balance containing an additive composed of the same components as described above were used. The comparative example 4 used what mix | blended the additive which consists of a component similar to the above in 30 mass% and FD-RJ which is not heat-processed in the remainder.

(2) Disintegration test A disintegration test was performed using each tablet obtained in (1) above. The disintegration test was performed according to the 6.09 disintegration test method described in the General Test Method of the 16th revision of the Japanese Pharmacopoeia, and finally the disintegration time of the tablets was measured. HC-1 manufactured by Yazawa Science Co., Ltd. was used as a disintegration tester. Six tablets were used in each example, and the average disintegration time is shown in Tables 1 and 2.

As shown in Tables 1 and 2, shortening of the disintegration time was recognized under the temperature condition of 50 ° C. or higher. On the other hand, under the heating condition of 40 ° C., the action of shortening the disintegration time was not recognized even when the heating time was increased. It was suggested that shortening of the disintegration time may be observed in the temperature condition between 40 ° C and 50 ° C.

(Test Example 2: Change in the three-dimensional structure of the protein in RJ)
Native-PAGE and SDS-PAGE were performed to examine changes in the three-dimensional structure of the protein in the RJ when the RJ was heat-treated. For Native-PAGE, a gel for 7.5% → 15% Native-PAGE was used. For SDS-PAGE, a gel concentration of 7.5% → 15% SDS-PAGE was used.

  As the samples, molecular weight markers, untreated raw RJ (control), untreated FD-RJ (control), 70 ° C. for 1 hour heat treatment RJ, and 70 ° C. for 4 hours heat treatment RJ were used from the left in FIG. A sample of Native-PAGE was prepared by suspending 30 mg of each RJ (100 mg of raw RJ) in 1 mL of loading buffer and diluting 8 times with the same solution, and then applying 10 μL / 1 lane. For SDS-PAGE samples, 20 mg of each RJ (100 mg of raw RJ) is suspended in 1 mL of SDS sample buffer, heat-treated at 95 ° C. for 3 minutes, and then appropriately diluted with SDS sample buffer to give a protein amount of 5 μg / lane. Applied. The results are shown in FIG.

  As shown in FIG. 1, there was no change in the detection band pattern of SDS-PAGE due to the heat treatment of RJ. On the other hand, in Native-PAGE, it was confirmed that the band appearing in the untreated RJ disappeared by the heat treatment of RJ. That is, it was confirmed that the disintegration time of the RJ-containing tablet can be shortened by changing only the three-dimensional structure while maintaining the primary structure of the protein.

Claims (2)

An easily disintegrating royal jelly-containing tablet containing 30% by mass or more of royal jelly ,
By changing the conformation of the protein in royal jelly which is a raw material, when subjected to disintegration test according to the disintegration test method described in the Japanese Pharmacopoeia 16th revision, such that the disintegration time is within 30 minutes provisions In addition , the three-dimensional structure change is carried out by subjecting raw royal jelly or royal jelly dissolved in a solvent to a heat treatment at 45 ° C. or higher, and an easily disintegrating royal jelly-containing tablet. A method for producing an easily disintegrating royal jelly-containing tablet comprising 30% by mass or more of royal jelly,
The production method, Ri Na comprise processing step of changing the conformation of the protein in the feed royal jelly of the easily disintegratable royal jelly-containing tablets,
The treatment step for changing the three-dimensional structure includes a step of heat treatment at 45 ° C. or higher for raw royal jelly or royal jelly dissolved in a solvent,
The easy-disintegrating royal jelly-containing tablet is specified to have a disintegration time of 30 minutes or less when subjected to a disintegration test according to the disintegration test method described in the 16th revision of the Japanese Pharmacopoeia. A method for producing a disintegrating royal jelly-containing tablet.