TWI458502B - Active pellet excluding chemical additives - Google Patents

Description

Active particles without chemical additives

The present invention relates to an active microparticle free of chemical additives.

The method of producing conventional fine particles includes a liquid lamination method, a powder lamination method, and an extrusion spheronization method. In the liquid lamination method, the active ingredient is dissolved in a solvent, a polymer binder is added, and the mucus is adhered to a core by a spray drying method to form a microparticle by lamination. In the powder lamination method, a powder is sprayed with a polymer binder, and particles are also produced in a layered manner. Extrusion spheronization also requires the use of polymeric binders to aid in forming. However, polymer binders are functional chemical additives that do not contribute to the human body.

As for the general active powder, it is usually obtained by extracting and drying the active ingredient. However, the resulting active powders vary in size from about 100 μm. The shape is mostly needle-shaped, lobed, irregular or round. When water vapor is encountered, the active powder easily absorbs moisture to produce viscous and mucus, and is not easy to flow. If you want to carry out subsequent processing, you need to add lubricants (such as talc, magnesium stearate, etc.) to help the powder flow. The lubricant is used to coat the active powder, making it smooth and non-sticky and easy to flow. However, in addition to affecting the disintegration and solubility of the active ingredients in the preparation, the lubricant also imposes a burden on the human body.

In addition to this, in order to improve the properties of the formulation, it is also possible to add other chemical additives. For example, to improve stability, add a preservative. To improve flavor and appearance, flavors, flavors or colors are added. Alternatively, in order to adjust the rate of collapse of the drug, a disintegrating agent is added.

As can be seen from the above, in the process of manufacturing conventional microparticles or preparations, Chemical additives are used. In addition, in order to improve the properties of the formulation, it is also possible to add other chemical additives. However, long-term use of preparations containing chemical additives may have adverse effects on the human body.

Therefore, there is a need for an active microparticle that is processable and free of chemical additives so that it can be processed without a chemical additive.

Accordingly, one aspect of the present invention provides an active particle free of chemical additives comprising a host and a plurality of voids. The body does not contain chemical additives and contains from 50 to 100% by weight of active ingredient.

One aspect of the present invention provides a capsule comprising the above active microparticles and a capsule coated with active microparticles.

One aspect of the present invention provides a tablet comprising the above active fine particles.

One aspect of the present invention provides a granule composed of the above active fine particles.

The above-described embodiments of the present invention have the following advantages over the known prior art:

(1) The active microparticles of the above embodiment of the present invention do not contain a chemical additive, and can reduce the psychological and actual health effects on the user.

(2) The active fine particles of the above embodiment of the present invention can have a higher density and a uniform particle size than a general granule or powder, and have an effect of controlling or delaying release.

(3) The main body of the above embodiment of the present invention may have a round shape and a large particle size, and has good physical fluidity, and thus is processed into a preparation such as a capsule. No lubricant is added during the course of the agent or lozenge.

(4) The main body of the above embodiment of the present invention may have adhesiveness and is suitable for further processing.

(5) The active fine particles of the above embodiment of the present invention contain voids and have preferable disintegration properties.

The Summary of the Invention is intended to provide a simplified summary of the present disclosure in order to provide a basic understanding of the disclosure. This Summary is not an extensive overview of the disclosure, and is not intended to be an The basic spirit of the present invention, as well as the technical means and implementations of the present invention, can be readily understood by those of ordinary skill in the art.

The embodiments of the present invention are disclosed in the following drawings, and the details of However, it should be understood that these practical details are not intended to limit the invention. That is, in some embodiments of the invention, these practical details are not necessary. In addition, some of the conventional structures and elements are shown in the drawings in a simplified schematic manner in order to simplify the drawings.

1A-1B is a schematic cross-sectional view showing the active microparticles 100 according to an embodiment of the present invention. The active microparticles 100 comprise a body 110 and a plurality of voids located in the body 110. In one embodiment, the void is in the honeycomb hole 120 (as shown in Figure 1A). In another embodiment, the voids are textured 140 (as shown in Figure 1B).

The active fine particles 100 can be produced by an extrusion method in combination with a spheronization method. In the extrusion process, the viscosity of the active ingredient can be adjusted by controlling the moisture, the pore size of the die plate, the extrusion stress and the speed, so that no additional chemical additives are required.

In one embodiment, the body 110 is shaped like a circular particle. The body 110 has a particle size of about 100 to 1800 μm and can be adjusted according to application requirements. For example, the particle size of the active microparticles 100 can be designed in accordance with the disintegration of the active microparticles 100 and the required release rate. In addition, since the bulk density of the main body 110 is higher than that of the general active powder, and the particle diameter is uniform, the effect of controlled release is obtained.

The above-mentioned circular-like granular shape means that the main body 110 can be a sphere, an elliptical sphere, or a nearly spherical or elliptical sphere. And because its shape is easy to roll, and it is not easy to be affected by moisture, it produces mucus, so it can show better fluidity during processing without additional lubricant.

In one embodiment, the body 110 comprises a fine powder 112, that is, the body 110 comprises a continuous or discontinuous structure. The fine powder 112 can be obtained by subjecting the active ingredient to extraction drying and then passing through a pulverization process. The fine powder 112 may have a particle diameter of 20 to 160 μm and a circular shape, a fixed shape or an irregular shape.

In one embodiment, the width D1 of the honeycomb-shaped aperture 120 (as shown in FIG. 1A) is about 0.1-100 μm. In another embodiment, the width D2 of the texture 140 (as shown in FIG. 1B) is about 0.1-100 μm. The texture 140 may be in the form of a honeycomb or an ice. The texture of the honeycomb pattern is usually in the form of a lattice. The ice-like lines are usually linear, such as the state in which the cracks appear when the ice cubes are split. The above-described textures 140 can be connected to each other. Due to active particles 100 There is a void in the middle, so the disintegration is preferred. For example, internal stress generated during extrusion and spheronization can be utilized to cause voids in the active fine particles 100.

In one embodiment, the active microparticles 100 further comprise a liquid 114 in the void. As shown in Figures 1A-1B, the liquid 114 is located in the honeycomb hole 120 or in the vein 140. The liquid 114 may be an active ingredient in a liquid state, such as a oleaginous substance having a pharmacological action.

The cladding layer 130 is located on the surface of the body 110. The cover layer 130 serves to protect the body 110 to enhance the stability of the active particles 100 or to control the release rate of the active ingredients. The cover layer 130 can be in the form of a sugar coating or a film coat.

Additionally, the active microparticles 100 can be processed into a formulation. The form of the preparation may be, for example, capsule 200, tablet 300 or granule 400.

2 is a schematic cross-sectional view showing a capsule according to an embodiment of the present invention. Capsule 200 comprises active microparticles 210 and capsules 250. In the present embodiment, the active particles 210 have a grain 240 therein. Since the main body 110 of the active fine particles 100 has a round granular shape and does not generate mucus by absorbing moisture, it is not necessary to add a lubricant when the active fine particles 100 are filled into the capsule 250.

3 is a schematic cross-sectional view showing a tablet according to an embodiment of the present invention. In the present embodiment, the tablet is produced by a wet granulation method. First, the active fine particles 100 are first mixed with water or alcohol, followed by a drying process, and then ingot to form a tablet. Since the active microparticles 100 have preferred compressive physical properties, no excipients need to be added during the manufacturing process.

4 is a schematic cross-sectional view showing a granule according to an embodiment of the present invention. In the present embodiment, the granule 400 includes The active particles 410 of the honeycomb hole 420 and the active particles 510 having the grain 540. Moreover, both active particles comprise a coating layer 530. For example, the active particles 410, 510 can be formed into a strip or round-like granule 400 having a diameter of 300 to 1800 μm by extrusion or granulation.

From the above, it is understood that in the process of producing the capsules 200 containing the active fine particles, the tablet 300, and the granules 400, it is not necessary to add a chemical additive. Further, the above preparation has the advantages of delayed release, improved storage or bio-stability with respect to general granules or powders.

Composition of the main body of the active particles

In one embodiment, the body 110 is composed entirely of active ingredient (100%) and is free of chemical additives. The above chemical additive means a substance which is synthesized by a chemical process and which has some specific functions. The chemical additives may, for example, be excipients, binders, disintegrating agents, diluents, glidants, lubricants, flavoring agents, emulsifiers, preservatives, perfumes or pigments.

The above active ingredient may be an active ingredient applied to foods or medicines. According to the activity, it can be divided into an active substance or an auxiliary active substance. The active substance may be an organic acid, a fatty acid, a polypeptide or a protein, a probiotic, a fungus, an alga, an alkaloid, a flavonoid, a mineral or a chemical compound. The auxiliary active substance may be a polysaccharide, a saccharide or a cellulose.

The above organic acid may be citric acid, malic acid, lactic acid, grain ferment, fruit ferment or other organic acid that can be applied to foods.

The above fatty acid may be an unsaturated fatty acid having a carbon chain of less than 50 carbon atoms. For example, Omega 3 fatty acids, Omega 6 fatty acids, Omega 9 fats Fatty acid, lecithin or phosphoserine.

The above polypeptide or protein may be a polypeptide or protein having physiological regulation.

The probiotic may be Lactobacillus, Bifidobacterium, Bacillus, Bacillus subtilis, Streptococcus, Enterococcus or Yeast.

The fungus may be an edible or medicinal fungal hyphae, an edible or medicinal fungal fruiting body, an ascomycete fungus or a monosarcoma fungus. For example, the fungal material may be Antrodia camphorata, Cordyceps sinensis, Ganoderma lucidum, Cordyceps militaris, Honeycomb or F.

The above algae may be edible or medicinal algae, including cyanobacteria, grape algae, green algae, red algae, nuclear algae, cryptophyta, dulgrass, purple red algae, and spirulina.

The above alkaloids may be extracts of plants, animals or fungi that can be applied to food additives. For example, piperine, fenugreek, theophylline and caffeine, resveratrol, serotonin, ergot and its derivatives, carnitine or choline.

The flavonoids may be flavonoids derived from fruits, vegetables, tea, wine, seeds or plant roots, or other flavonoids that may be applied to food additives. For example, the flavonoids may be rutin, hesperidin, quercetin, green tea polyphenols, red wine polyphenols or olive polyphenols.

The above minerals may be minerals that are edible or applied to food additives, including sodium salts, calcium salts, chromium salts, zinc salts, iron salts, magnesium salts, selenium salts.

The above cellulose may be derived from ginger, turmeric, pepper, garlic, scutellaria, bamboo leaves, mangosteen shell, orange peel, rambutan peel, yam, tea and other fibers.

In one embodiment, the active ingredient is a natural fiber that is sparse Releases the function of bonding, so no thinner or adhesive is used in the process.

In another embodiment, the composition of the body 110 of the active microparticles 100 comprises an active ingredient and an auxiliary starting material. Auxiliary materials include natural diluents, binders, and humectants.

Natural diluents do not contain active pharmacological effects, which are used to increase the weight and volume of the body, which is advantageous for molding and dispensing. Natural diluents are, for example, lactose, sucrose, glucose, calcium carbonate, calcium phosphate, starch, microcrystalline cellulose, ginger, turmeric, lycopene, sweet potato skin, potato peel, bagasse dried powder or combinations thereof.

Adhesives do not contain active pharmacological agents. They are used to aggregate non-viscous or less viscous components into granules or to compress into a viscous solid powder or viscous liquid. The binder is, for example, a sugar, a starch, an acacia, a cellulose derivative or a combination thereof.

The humectant moisturizes the main component and other excipients to produce a sufficient strength to form microparticles. The humectant itself is not very viscous, but after contact with the wet material (generally referred to as the processed material, here refers to the active ingredient plus the auxiliary material), it can induce its own viscosity, so that it can coalesce into a soft material and Further made into particles. Wetting agents are used in the process and are not present in the product. In one embodiment, the humectant is water.

In several embodiments, the proportion of active ingredient in the body is from 50 to 100%, the ratio of natural diluent is from 0 to 40%, and the proportion of binder is from 0 to 10%.

Method for producing active particles

The active particles can be produced by different methods. Classified by process, it may include powder lamination, liquid lamination, and extrusion spheronization. In several embodiments, the extrusion method is used in conjunction with the spheronization method as the main process or the sole process.

First, choose different material combinations based on material properties. In one embodiment, the active ingredient is selected from natural fibers having pharmacological activity. When the natural fiber is added to a suitable water, it has sufficient viscosity to be molded, and the extrusion spheronization process can be directly used to maintain the circular appearance of the produced active particles and maintain the strength of the structure after drying. Therefore, in the present embodiment, the active ingredient (i.e., natural fiber) has a function of dilution and adhesion without adding a diluent and a binder.

In another embodiment, if an active ingredient that does not conform to the requirements is selected, additional ingredients such as a natural diluent or/and a binder are required.

The pre-treatment is then carried out on the materials selected. In one embodiment, the material is formed into a product having a honeycomb-like pore structure. For example, a natural diluent (such as ginger fiber) is first added to the appropriate water to mix and stir, and if necessary, a binder is added. After agitation, a loose structure filled with voids is formed, and then the active ingredient is added to form a product having a honeycomb-like pore.

In one embodiment, the material is formed into a product having a texture. For example, a natural diluent (such as ginger fiber) is first mixed with an active ingredient and added to a suitable water, and a binder is added as necessary. The strip process is formed by an extrusion process. The number of times of extrusion is not limited here, and the structural strength of the particles can be adjusted.

The extruder can be a single screw or a twin screw. A circular orifice plate is provided at the front end of the extruder, or a curved orifice plate is provided on both sides of the extruder. As the spiral advances forward and on both sides, the material is squeezed out of the hole in the orifice (pressure relief).

In one embodiment, the screw advances the material at a pressure of about 2000-30000 psi through the orifice to form the strands. This pressure is related to the aperture of the circular hole on the orifice plate and the opening ratio. The higher the pressure, the higher the density of extruded particles, and the less the amount of natural diluent and binder required.

In one embodiment, the aperture is between 0.2 and 1.8 mm. The smaller the pore size, the greater the extrusion pressure, and the less the amount of natural diluent and binder.

Then, the spheronization process is performed using the centrifugal dial and the attachment device to cut the strip-shaped particles, and the particles or particles collide with the inner wall of the machine table in a centrifugal state to form round-like particles. In the spheronization method, the appearance of the active particles can also be improved by controlling the speed and time of the spheronization and the cutting plate of the additional machine.

Finally, the drying process is carried out to obtain the active particles having the texture.

Active microparticles can be used for both physiological and pharmacological applications. For example, it can be applied to modulate physiological changes or indications caused by physiological disorders. Such as sleep disorders, including insomnia, shallow sleep, anxiety, etc.; environmental pollution, including heavy metals, environmental hormones, pesticides, sacrotoxin and other intake and absorption; gastrointestinal physiology disorders, including constipation, flatulence, diarrhea, etc.; metabolic syndrome Including obesity, hyperlipidemia, fatty liver, diabetes and so on.

Instance Example one

For the composition of Comparative Example 1, Comparative Example 2, Experimental Example 1 and Experimental Example 2, refer to Table 1. In Comparative Example 1, the main component with a total weight of 500 grams was weighed and diluted. The release agent was uniformly mixed, and about 150 mL of an aqueous solution (5%) of hydroxypropylmethylcellulose (HPMC) was added. Then, the long pellets were extruded at a single screw of 1.0 mm, spheronized at a rotational speed of 500 rpm for 30 seconds, and the pellets were oven-dried at 60 ° C for 3 hours to obtain active fine particles.

Comparative Example 2, Experimental Example 1 and Experimental Example 2 were also prepared by the above procedure with different material compositions to prepare active fine particles.

The diluent content of Comparative Example 1 is low, and although the extrusion and spheronization processes can be performed, the density of the active particles is low and the structure is loose. In the process of filling the particles (automatic filling), the loss rate is about 20% higher (easy to become powder). And the average filling amount of capsule No. 0 is about 400 mg (generally 500 mg), which means that the structure is loose and is not suitable for further processing into microcapsules.

The diluent of Comparative Example 2 has a high content, and although it can be extruded, the formability of the particles is not good, and it is revealed that lactose is not a good particulate diluent, and the reason may be that Lactose dissolves when it absorbs water and does not form a stable structure.

In Experimental Example 1 and Experimental Example 2, in the particle sorting (particle yield, 1.0 mm stencil extrusion, between 0.81 and 0.9 mm diameter), the yield was up to 90%, and the average filling amount of capsule No. 0 was about 500 mg, and the filling loss was Less than 5% means that the fluidity and structural hardness are appropriate and are suitable.

Another ginger fiber (the powder which is dried and pulverized after the ginger juice is extruded) has suitable formability for the microparticle preparation, and the moldability is not bad compared with the conventional microparticle diluent (for example, crystalline cellulose). Natural products, not manufactured by chemical processes.

Example two

Refer to Table 2 for the composition of the experimental examples 1 to 4 and the extrusion process conditions. Firstly, a total of 500 g of the main component and the diluent were uniformly mixed, and then a binder HPMC aqueous solution (5%), an HPMC aqueous solution (1%) or water of about 150 mL was added. The strips were then extruded in a single screw extruder at 1.0 mm or 0.4 mm. In the spheronization process, each was extruded in a 1.0 mm orifice plate at a speed of 500 rpm for 30 seconds, and was spheronized for 30 seconds by extruding with a 0.4 mm orifice at a speed of 500 rpm. The spheronized granules were dried in an oven at 60 ° C for 3 hours.

The microparticles produced in Experimental Example 3 and Experimental Example 4 (0.4 mm stencil extrusion, between 0.3 and 0.4 mm in diameter) were approximately circular in shape and uniform in size, and were also qualified particles. The average filling amount of No. 0 capsule is about 500 mg, and the filling loss is less than 5%, which means that the fluidity and structural hardness are appropriate, which is suitable for the side. In other words, a smaller aperture and a lower unit density orifice plate can form suitable particles without the need for a binder or a less viscous composition.

Example three

Refer to Table 3 for the composition of the experimental examples 5 to 8 and the conditions of the previous stage. In Example 3, a total of 500 grams of the main component (powder or fine particles) and the diluent were weighed. Then, the front-end process and the back-end process are sequentially performed.

The first stage of the experimental example 5 was to mix the high-viscosity main component green tea extract powder (EGCG content 70%, Mino) with microcrystalline cellulose 150g. Evenly, add 150 ml of a binder HPMC aqueous solution (2.5%).

In the first stage of the experiment 6, 150 g of microcrystalline cellulose and 150 ml of a binder HPMC aqueous solution (2.5%) were first mixed, allowed to stand for 30 minutes, and then a highly viscous main component green tea extract powder (EGCG content 70%, Mino) was added. ) 350g simple mixing.

In Experimental Example 7, green tea extract microparticles were prepared first, followed by a anterior stage process. The microparticles were prepared by mixing a diluent, a binder and 150 ml of water, allowing to stand for 30 minutes, and then adding a highly viscous main component for simple mixing. Then, a high-viscosity main component and 500 g of ginger fiber were extruded and spheronized in a 0.4 mm orifice plate (porosity of about 1%). The resulting microparticles were then dried to form microparticles having a diameter of about 0.4 mm (EGCG content of about 49%). Then, 150 g of microcrystalline cellulose and 150 ml of an aqueous solution of HPMC (2.5%) were uniformly mixed, and then 350 g of fine particles were added.

In Experimental Example 8, green tea extract particles were prepared first, and then the front stage process was carried out. The preparation of the microparticles is carried out by first mixing a diluent, a binder and 150 ml of water, allowing to stand for 30 minutes, and then adding a highly viscous main component for simple mixing. Then, a high-viscosity main component and 500 g of ginger fiber were extruded and spheronized in a 0.4 mm orifice plate (porosity of about 1%). The resulting microparticles were then dried to form microparticles having a diameter of about 0.4 mm (EGCG content of about 49%). Then, 150 g of ginger fiber powder and 150 ml of an aqueous solution of HPMC (2.5%) were uniformly mixed, and then 350 g of fine particles were added.

After the end of the previous process, the above products are sequentially extruded and spheronized. The spheronized granules were dried in an oven at 60 ° C for 3 hours.

Experimental Example 5 Long strips of pellets were extruded in a single screw extruder of 1.0 mm orifice plate, and spheronized for 30 seconds at a rotation speed of 800 rpm to form fine particles and then dried. The obtained microparticles are strip-shaped rather than round, and the size is not uniform. The main reason for the estimation is that the viscosity of the mixture in the front stage process is too high, although it can be extruded but cannot be rounded.

Experimental Example 6 Long strips of pellets were extruded in a single screw extruder of 1.0 mm orifice plate, and spheronized for 30 seconds at a rotation speed of 800 rpm to form fine particles and then dried. The obtained microparticles were round and uniform, and the average was also better than that of Experimental Example 5, but the yield (0.9mm~1.0mm) was still less than 70%. The main reason for the estimation was that the viscosity of the mixture in the previous stage was more appropriate, although the prescription and experimental examples. 5 is the same, but the process is different, and its process helps to reduce the viscosity.

Experimental Example 7 Long strips of pellets were extruded in a single screw extruder of 1.0 mm orifice plate, and spheronized for 30 seconds at a number of revolutions of 800 rpm to form fine particles and then dried. The obtained microparticles were round in shape, and the average was better than that of Experimental Example 6 and the yield (0.9 mm to 1.0 mm) was higher than 90%. The main reason for the estimation was that the viscosity of the mixture in the latter stage was appropriate and similar to that of the general particles. The green tea extract is mixed with water after being made into fine particles, and does not produce high viscosity for a short period of time.

Experimental Example 8 Long strips of pellets were extruded in a single screw extruder of 1.0 mm orifice plate, and spheronized by spinning at 800 rpm for 30 seconds to form fine particles and then dried. The obtained microparticles have a circularity uniformity similar to that of Experimental Example 7, but are better than Experimental Example 6 and the yield (0.9 mm to 1.0 mm) is higher than 90%, which means that the viscosity of the mixture in the latter stage process is appropriate, similar to the characteristics of general particles. . The green tea extract is mixed with water after being made into fine particles, and does not produce high viscosity for a short period of time. In addition, the ginger fiber powder has the same function as the microcrystalline cellulose.

It can be seen from the above that through different processes, the substances which do not conform to the demand can be made into active particles containing no chemical additives, and the processing properties are changed. In other words, when the aforementioned active fine particles are mixed with other substances such as natural diluent or water, high viscosity is less likely to occur. Therefore, this active particle can be widely used. In the manufacture of various preparations, and without the use of any chemical additives in the process, the harm to the human body can be greatly reduced.

Although the present invention has been disclosed in the above embodiments, it is not intended to limit the present invention, and the present invention can be modified and modified without departing from the spirit and scope of the present invention. The scope is subject to the definition of the scope of the patent application attached.

100, 210, 310, 410, 510‧‧‧active particles

110‧‧‧ Subject

112‧‧‧fine powder

114‧‧‧Liquid

120, 320, 420‧‧‧ honeycomb holes

130, 430, 530‧‧ ‧ coating

140, 240, 540‧‧‧ lines

200‧‧‧Capsules

250‧‧‧ capsules

300‧‧‧Lozenges

400‧‧‧ granules

D1‧‧‧The width of the honeycomb hole

D2‧‧‧ width of the grain

The above and other objects, features, advantages and embodiments of the present invention will become more <RTIgt; </ RTI> <RTIgt; </ RTI> <RTIgt; </ RTI> <RTIgt; Schematic diagram of the section structure.

2 is a schematic cross-sectional view showing a capsule according to an embodiment of the present invention.

3 is a schematic cross-sectional view showing a tablet according to an embodiment of the present invention.

4 is a schematic cross-sectional view showing a granule according to an embodiment of the present invention.

100‧‧‧active particles

110‧‧‧ Subject

112‧‧‧fine powder

114‧‧‧Liquid

120‧‧‧Hive-shaped holes

130‧‧‧Cladding

D1‧‧‧The width of the honeycomb hole

Claims (10)

An active microparticle comprising no chemical additive, comprising: a main body consisting essentially of 50 to 85 wt% of an active ingredient and 15 to 50 wt% of a natural diluent, the natural diluent being a material selected from the group consisting of ginger, turmeric, and pepper a group consisting of garlic, scutellaria, bamboo leaves, mangosteen shell, yam, sweet potato skin, potato skin, dried bagasse powder, and combinations thereof; and a plurality of voids located in the body. The active microparticles according to claim 1, wherein the main body has a shape of a circular particle. The active microparticles according to claim 1, wherein the host has a particle diameter of about 300 to 400 μm. The active microparticles of claim 1 further comprising a coating layer on the surface of the body. The active microparticles of claim 1, wherein the natural diluent comprises the ginger fiber. A capsule comprising: the active microparticles according to any one of claims 1 to 5; and a capsule coated with the active microparticles. A lozenge comprising the active microparticles according to any one of claims 1 to 5. A granule comprising the active microparticles according to any one of claims 1 to 5. A composition comprising no active particles of a chemical additive consisting essentially of 50 to 85 wt% of an active ingredient and 15 to 50 wt% of a natural diluent selected from the group consisting of ginger, turmeric, pepper, and garlic. , a group of yellow scorpion, bamboo leaves, mangosteen shell, yam, sweet potato skin, potato skin, dried bagasse powder and combinations thereof. The composition of the active microparticles of claim 9, wherein the natural diluent comprises the ginger fiber.