JPH09278665A - Pollen extract soft capsule and its production - Google Patents

Abstract

PROBLEM TO BE SOLVED: To prepare a pollen extract soft capsule, capable of preventing deterioration in quality and discoloration and excellent in preservation stability and provide a method for producing the pollen extract soft capsule, containing a pollen extract at a high concentration, readily administrable and stabilized in quality. SOLUTION: This pollen extract soft capsule comprises a pollen extract as an active ingredient. The pollen extract is composed of a water-soluble extract and an oily extract. When the ratio of the water-soluble extract to the oily extract is 20:1, excellent suppressing effects on prostatisms are exhibited. The pollen extract soft capsule is produced by encapsulating the pollen extract as the active ingredient with gelatin.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a pollen extract soft capsule containing a pollen extract effective for prostatitis or benign prostatic hyperplasia as an active ingredient, and a method for producing the same.

[0002]

2. Description of the Related Art Pollen is a particle rich in germ cells and contains important factors related to the fertilizing action of plants. Its chemical composition is protein, amino acid, carbohydrate, hormone,
Physiologically active substances such as vitamins are listed. Therefore,
When this pollen is administered to higher animals, various pharmacological effects are expected, but to date, it has the effects of weight gain, gastrointestinal function regulation, hemoglobin level increase, hemostatic action, anti-inflammatory action, and prostate hypertrophy suppressing action. Are known. In the form of tablets and juice containing pollen, it has been commercialized in Europe and the United States as health foods and pharmaceuticals.

What is called pollen load among pollen is
A bee collects it from a flower, attaches it to the bee's foot along with nectar, and takes it back to the birdhouse, which is used as a nutrition source. Further, this pollen load is easily collected by a person, and pollen foods are usually made from this bee-derived pollen load.

On the other hand, pollen used as a medicine is collected around May to June when a plant is cultivated by human hands. The only pollen formulation used as an agent for prostate disease, "Cernilton tablets (trade name of Fuso Pharmaceutical Co., Ltd.)"
In 1959, the Swedish ask-up mark (A
sk-Upmark) was applied to prostatitis and its usefulness was confirmed, which led to the development of 8 types of pollen, timothy, corn, rye, hazel, pussy willow,
It is a formulation made from cottonwood, chrysanthemum and pine. This product has been launched in many countries around the world, and it is highly evaluated because of its side effects and certainty of its effect. In addition, it is expected that this plant preparation will be used more and more as a base drug due to the advent of an aging society.

[0005]

However, this pollen extract is a mixture of a water-soluble extract obtained by extracting the above pollen mixture with water and an oily extract obtained by extracting with acetone at a ratio of 20: 1. When this is made into a tablet, the surface of the tablet comes into contact with air, and is therefore susceptible to changes due to humidity. On the other hand, various amino acids, sugars,
It contains a large number of ingredients such as vitamins. Therefore, these components deteriorate in quality due to moisture and oxygen in the air, and sugar and amino acid cause Maillard reaction, and the color changes to brown. Therefore, there is a problem that the storage stability of the tablet containing the pollen extract decreases.

[0006] Further, powdered excipients such as lactose, dextrin, and starch are added to the tablet in order to maintain a predetermined shape and suppress discoloration.
It becomes the size of mg. Therefore, considering that the patients with benign prostatic hyperplasia are elderly, they have a drawback that they are very difficult to drink.

The present invention has been made by paying attention to the problems existing in the prior art as described above. An object of the invention is to provide a pollen extract soft capsule capable of preventing deterioration of quality and discoloration and improving storage stability. Another object is to provide a pollen extract soft capsule which is easy to take when ingested. A further object is to include pollen extract in high concentration,
Another object of the present invention is to provide a method for producing a pollen extract soft capsule, which enables easy production of a stable pollen extract soft capsule.

[0008]

In order to achieve the above object, the pollen extract soft capsule of the first invention comprises:
It uses pollen extract as an active ingredient.

According to the pollen extract soft capsule of the second invention, in the first invention, the pollen extract is composed of a water-soluble extract and an oily extract. In the method for producing a soft pollen extract of pollen extract according to the third aspect of the invention, the pollen extract is used as a raw material in the method of producing a soft capsule by mixing the raw materials and then encapsulating with gelatin.

Therefore, in the pollen extract soft capsule of the first aspect of the present invention, the pollen extract as an active ingredient is contained in the soft capsule, so that the penetration of water and oxygen into the capsule is blocked. Therefore, it is possible to prevent deterioration of the quality and discoloration of the active ingredient and improve storage stability. Furthermore, since it is not necessary to use a large amount of powdered excipients such as lactose and dextrin, the capsule can be downsized and can be taken easily when ingested.

In the pollen extract soft capsule of the second invention, since the pollen extract is composed of a water-soluble extract and an oily extract, it is possible to exert a suppressing effect particularly on prostatitis and benign prostatic hyperplasia.

According to the third aspect of the method for producing a pollen extract soft capsule, a pollen extract soft capsule containing a high concentration of pollen extract and having a stable quality can be easily produced by an encapsulation method using gelatin.

[0013]

Embodiments of the present invention will be described below in detail. Pollen extract soft capsule
Pollen extract is the active ingredient. The pollen extract may be the pollen cargo itself or an extract of water or an organic solvent. Acetone is used as the organic solvent, but other solvents may be used. The pollen used here is the above-mentioned eight kinds of pollens, that is, those derived from Timothy, corn, hazel, rye, pussy willow, cotton willow, French chrysanthemum and pine, or part thereof, and other pollen. May be.

The pollen extract, which is a mixture of a water-soluble extract and an oily extract, is effective against prostatic diseases such as prostatitis and benign prostatic hyperplasia. When the ratio of the water-soluble extract to the oil-based extract is 20: 1, the optimal pharmacological effect on prostate disease is exerted. When intended for other health foods, the ratio can be changed appropriately. If necessary, a liquid such as an oil or an emulsifier may be added to the pollen extract as described above.

Next, a method for producing the pollen extract soft capsule will be described. The pollen extract soft capsule is produced by wrapping the pollen extract in a gelatin coat. The gelatin coating is prepared by adding 20 to 30 of concentrated glycerin, 1 of titanium oxide, and a small amount of pigment to 100 of gelatin in a weight ratio, and further adding 100 to 120 of water.
The gelatin capsule is used to encapsulate the contents of the pollen extract and, if necessary, an oil as an excipient, an emulsifier and the like.

Specifically, oil and an oily extract are heated and mixed, an emulsifier is added to the mixture, and then a water-soluble extract powder is added to emulsify the mixture. . In order to obtain a stable emulsion, it depends on the type and amount of oil and emulsifier and the nature of the active ingredient, but for the active ingredient 60 mg and oily extract 3 mg, lecithin 30-90 mg, medium-chain fatty acid triglyceride 30-100 mg. , And glycerin fatty acid ester in the range of 10 to 100 mg.

This ratio can be changed depending on the physical properties of the pollen extract as the raw material. In order to maintain the emulsion stability for a longer period, the ranges of lecithin 60 to 80 mg, medium chain fatty acid triglyceride 40 to 60 mg, and glycerin fatty acid ester 10 to 30 mg are preferable.

For example, first, lecithin and medium-chain fatty acid triglyceride are placed in a heating kettle and dissolved with good stirring. Then, the oily extract is added, and the mixture is further mixed and stirred. Next, glycerin fatty acid ester is put and stirred, and water-soluble extract powder is further added to start emulsification. This is wrapped with a gelatin skin and encapsulated. next,
After the drying step, the final packaging, for example, a packaging form in which a capsule is packaged between a transparent film of aluminum and a vinyl chloride resin (PTP packaging), an aluminum metal pack, or the like is used for the product.

According to the pollen extract soft capsule and the method for producing the same as described above, the following effects are exhibited. (1) By wrapping the pollen extract in a gelatin coat, the gelatin coat can block the ingress of water and oxygen into the soft capsule, so that the quality of the active ingredient is stabilized,
Since it is not affected by moisture or the like, the risk of discoloration can be prevented. Therefore, the storage stability of the pollen extract soft capsule is improved. (2) By using an oil or an emulsifier without using a powdered excipient such as lactose or dextrin as an excipient, the pollen extract is wrapped in an oily component and the composition ratio of the active ingredient can be increased. As a result, the capsule can be miniaturized and can be taken easily when ingested. (3) As pollen extract, it is obtained from 8 kinds of pollen, timothy, corn, rye, hazel, pussy willow, cotton willow, france chrysanthemum, and pine, and by containing the water-soluble extract and oily extract in a ratio of 20: 1, In addition, it can exert the effect as an agent for prostate disease. (4) According to the pollen extract soft capsule, in addition to the effect of suppressing prostatitis and the effect of suppressing prostatic hypertrophy, effects such as a weight gain effect, a digestive tract function adjusting effect, a hemostatic effect, and an anti-inflammatory effect can be obtained. (5) The pollen extract soft capsule is useful as a health food for promoting health and improving physical condition. (6) The pollen extract soft capsule is manufactured by the encapsulation method using gelatin, and the pollen extract soft capsule containing the pollen extract in a high concentration and having stable quality can be easily manufactured.

[0020]

EXAMPLES The present invention will be described more specifically with reference to Examples and Test Examples. (Example 1) 700 g of lecithin and 490 g of medium-chain fatty acid triglyceride were mixed and stirred at 50 ° C, and then 30 g of oily extract was added and mixed. To this, 180 g of glycerin fatty acid ester was added and mixed, and further 600 g of the water-soluble extract was added and emulsified. This was wrapped with a gelatin skin and encapsulated to obtain a pollen extract soft capsule. The gelatin coating was prepared using 100 parts by weight of gelatin, 30 parts of concentrated glycerin, 1 part of titanium oxide, and a very small amount of a dye contained in a drug. (Example 2) 300 g of lecithin and 500 g of medium-chain fatty acid triglyceride were mixed and stirred at 50 ° C, and then 30 g of oily extract was added and mixed. To this, 570 g of glycerin fatty acid ester was added and mixed, and further 600 g of the water-soluble extract was added and emulsified. This was wrapped with a gelatin skin and encapsulated to obtain a pollen extract soft capsule. (Example 3) 2 kg of lecithin and 1.4 kg of medium-chain fatty acid triglyceride were mixed and stirred at 50 ° C, and then 86 g of oily extract was added and mixed. To this, 515 g of glycerin fatty acid ester was added and mixed, and 1.72 kg of the water-soluble extract was further added and emulsified. This was wrapped with a gelatin skin and encapsulated to obtain a pollen extract soft capsule. (Test Example 1) In order to confirm the stability of the soft capsule preparation obtained in Example 1, the following test was conducted. The soft capsule was packed in PTP and stored at 25 ° C. for a long time. Test items include properties (appearance, contents), confirmation test, disintegration test,
Quantitation was performed. Exam is 3rd month, 6th month, 12th
The quality was checked on the 18th month, the 18th month, the 24th month, the 30th month, the 36th month and the 39th month.

As a result, the appearance was an orange soft capsule and the content was a dark yellow-green viscous liquid, which did not change during the test period. Ninhydrin color was positive in the confirmation test,
Ultraviolet and visible absorption spectra were also suitable. The disintegration test was also satisfactory for all periods between 9.4 and 11.0 minutes. Furthermore, in the quantitative determination, the water-soluble extract 98.
4 to 101.9%, oil extract 98.2 to 101.8%
And satisfied the standard. (Test Example 2) The following test was performed to confirm the stability of the soft capsule preparation obtained in Example 3 against humidity. Soft capsules are not packaged and are left as is.
The sample was placed in a thermo-hygrostat at 75 ° C. and 75% RH, and the same quality test as in Test Example 1 except for the disintegration test was conducted on the first and second months.
As a control, the Cernilton tablet was taken out from the aluminum package, and the same test was performed with the plain tablet intact.

As a result, the appearance and contents of the pollen extract soft capsule of Example 3 did not change, whereas the surface of the tablets of Cernilton tablets became mottled 2 days after the start of the test, and the parts thereof turned brown. Was.
In the confirmation test and the quantitative test, the pollen extract soft capsule of Example 3 satisfied the standard without any problem.

As described above, it was confirmed that the pollen extract soft capsule was stable against humidity. This is because the content containing pollen extract is covered with a gelatin skin,
Moreover, it is considered that the content composition containing a large amount of oily components can prevent the influence of external moisture. (Test Example 3) The pollen extract soft capsule preparation obtained in Example 3 was tested for the effect of suppressing prostatic hypertrophy by animal pharmacology. The test drug is the pollen extract soft capsule of Example 3,
The control drug was Cernilton tablets (manufactured by Fuso Yakuhin Kogyo Co., Ltd.), which was prepared as a placebo by removing the pollen extract from the pollen extract soft capsule.

In a test using rats, it is impossible to administer the drug as it is. Therefore, the test drug and placebo are soft capsule contents, and the control drug is powdered, each containing 1% HCO-60 (Japan Surfactant Co., Ltd. (Trade name) manufactured by (1) Suspended in physiological saline solution. The dose was determined to be effective in the literature. Animals are 4 weeks old SD
Male rats (CLEA Japan, Inc.) and Japanese white male rabbits with a body weight of 2 kg (SEIKEN Material Co., Ltd.) were preliminarily bred for 1 week and rabbits for 1 month, and then subjected to the experiment. The rats used for the "effect on prostate hypertrophy" were castrated the day after arrival and the subsequent 1 week was used as the preliminary breeding period.

[0025] For "action on prostate hypertrophy" and "action on granulation growth", rats were divided into 10 groups and 10 groups. In the "effect on urination pressure", 8 rabbits were used repeatedly 4 times in total, and 1 test was conducted with 2 animals in each of the 4 groups, and the same sample was given to the same animal during a drug holiday of about 10 days. Not to be administered.

1) Action on Prostatic Hypertrophy Ito et al. (Applied Pharmacology, 31: 1-11, 1986)
Was carried out according to the method described above. The dose is 630 mg / kg,
Oral administration was carried out once a day for 7 days. The prostate abdominal lobe and dorsal lobe weights are shown in Tables 1 and 2.

[0027]

[Table 1]

[0028]

[Table 2] As shown in Tables 1 and 2, the control group showed a significant increase in prostate weight in both abdominal lobe and dorsal lobe weights versus the untreated group that was castrated only and not treated with testosterone propionate. In contrast to this change, no significant effect was observed on the abdominal lobe weight in the test drug and control drug administration groups, but there was a significant effect of 19.3 and 17.3% to the increase in the back lobe weight, respectively. A suppressive effect was observed.

2) Effect on granulation proliferation Ito et al. (Applied Pharmacology, 28, 55-65, 1985)
Year). The dose is 1260mg / k
It was orally administered once a day for 7 days. Table 3 shows the dry weight of the granulation of each experimental group.

[0030]

[Table 3] As shown in Table 3, in the test drug and control drug administration groups, 16.0 and 18.8, respectively, with respect to the control group.
%, A significant inhibitory effect was observed. On the other hand, the placebo-administered group of the study drug showed no difference from the control group, but the study-drug-administered group showed a significant inhibitory effect on the placebo-administered group.

3) Effect on urination pressure Nakaarai and Sonoda (Bulletin of Urology, Vol. 18, 501-515)
Page, 1972). The dose was 6 capsules or 6 tablets, and was orally administered once a day for 2 days.

[0032]

[Table 4] As shown in Table 4, the urination pressure of each experimental group is shown in Table 4.
Significant enhancing effects of 47.9% and 49.3% were observed in the test drug and control drug administration groups as compared with the control group, respectively. On the other hand, no difference was observed in the placebo-administered group of the study drug from the control group, but the study drug-administered group showed a significant enhancing effect over the placebo-administered group.

From the above results, the pollen extract soft capsules of each Example exhibit the same action as that of Cernilton tablets,
It was found that there was no difference between the two formulations. (Test Example 4) Using the pollen extract soft capsule of Example 2, an open clinical test was conducted for patients with chronic prostatitis and patients with early stage prostatic hypertrophy, and the effect was confirmed.
The dosage was 2 capsules orally twice a day. As a general rule, the administration period was 14 days. The survey items are 1) patient background, 2) clinical findings (difficulty in urination, urination, residual urine, painful urination, urinary fineness, perineal discomfort) 3) clinical examination (physiological function, hematology) Tests, blood biochemical tests, urinalysis) 4) Adverse effects were evaluated as 1) improvement by symptoms, 2) general improvement, 3) side effects, and 4) usefulness.
The number of cases was 40 at 3 locations.

As a result, in terms of clinical findings, each item was investigated 3 days, 7 days, 14 days after administration, and at the time of termination, but all showed a stepwise improvement. "Slightly improved" or higher in the degree of improvement by symptom at the end of the test, 95% (38/40) of dysuria and 95% (38/4) of frequent urination
0), 95% of residual urine (38/40), 95% of urination pain (3
8/40), 90% of urinary fineness (36/40) and 95% of perineal discomfort (38/40).

There were no cases in which the symptoms were aggravated. Regarding the feeling of taking it, it was very easy to take, but it was 20%. Regarding the overall improvement degree, 38 cases (95%) out of all 40 cases showed a slight improvement or more. No side effects were observed in any case, and no problem in taking the drug was observed. The clinical test values were all within the normal range of the individual, and no change due to administration was observed.

When the degree of usefulness was judged based on the degree of overall improvement and the like, 38 cases (95%) out of 40 cases were evaluated as slightly more than useful. As described above, the pollen extract soft capsule of the present invention has high clinical utility and satisfies market demands because of its ease of administration.

The technical idea understood from the above embodiment will be described below. (1) The pollen extract is made from timothy, corn, rye, hazel, pussy willow, cotton willow, chrysanthemum and pine as raw materials.
Pollen extract soft capsule described in.

With such a constitution, the pollen extract soft capsule can exert the effect of suppressing prostatic hypertrophy and can be used as an agent for prostate disease. (2) The weight ratio of water-soluble extract to oil-based extract is 2
The pollen extract soft capsule according to claim 2, wherein the ratio is 0: 1. With this constitution, the pollen extract soft capsule has high stability of the active ingredient and is most effective against benign prostatic hyperplasia and prostatitis. (3) The pollen extract soft capsule as described in (2) above, wherein the pollen extract is made from timothy, corn, rye, hazel, pussy willow, cotton willow, chrysanthemum, and pine.

This pollen extract soft capsule shows excellent quality stability and prostatic hypertrophy suppressing effect. (4) The pollen extract soft capsule according to claim 2 or (2), which contains an oil and an emulsifier.

Since this pollen extract soft capsule contains an oily component as its content component, it is unlikely to be affected by moisture and the like, and a homogeneous dispersion liquid can be obtained with an emulsifier,
The quality of the active ingredient is stabilized. (5) The pollen extract soft capsule of claim 1 or 2, which is used for medicinal purposes.

According to this pollen extract soft capsule, it is possible to obtain effects such as a weight gain effect, a digestive tract function adjusting effect, a hemostatic effect, an anti-inflammatory effect, and a prostate hypertrophy suppressing effect. (6) The pollen extract soft capsule according to claim 1 or 2, which is used for prostate disease.

This pollen extract soft capsule is effective for suppressing prostatitis and prostatic hypertrophy. (7) A method for producing a pollen extract soft capsule, which comprises adding an excipient to the pollen oil extract, adding a pollen water-soluble extract powder, and then encapsulating with gelatin.

According to this production method, since the excipient is added to and mixed with the pollen extract, a homogeneous pollen extract soft capsule can be produced. (8) The method for producing a pollen extract soft capsule according to the above (7), wherein the excipient is an oil or an emulsifier.

According to this production method, an oil or an emulsifier is added to and mixed with pollen extracts having different properties, so that a pollen extract soft capsule having a more stable quality can be produced.

[0045]

As described above in detail, according to the present invention, the following effects can be obtained. According to the pollen extract soft capsule of the first invention, since the pollen extract is contained in the soft capsule as an active ingredient, deterioration of the quality and discoloration of the active ingredient can be prevented and storage stability can be improved. Moreover, since it is not necessary to use a large amount of powdered excipient such as lactose or dextrin, the capsule can be downsized and can be easily taken when ingested.

According to the pollen extract soft capsule of the second invention, since the pollen extract is composed of a water-soluble extract and an oily extract, it is possible to exert a suppressing effect particularly on prostatitis and benign prostatic hyperplasia.

According to the method for producing the pollen extract soft capsule of the third invention, the pollen extract soft capsule containing the pollen extract at a high concentration and having stable quality can be easily produced by the encapsulation method using gelatin.

Therefore, this pollen extract soft capsule is useful as a medicine, health food and the like.

 ─────────────────────────────────────────────────── ─── Continuation of the front page (72) Inventor Takashi Nonogaki 1-1, Kano Sakurada-cho, Gifu City Api Stock Company

Claims (3)

[Claims] 1. A pollen extract soft capsule containing a pollen extract as an active ingredient. 2. The pollen extract soft capsule according to claim 1, wherein the pollen extract is composed of a water-soluble extract and an oily extract. 3. A method for producing a soft capsule, which comprises using pollen extract as a raw material in a method for producing a soft capsule by encapsulating with gelatin after mixing the raw materials.