TWI787898B - Composition for forming soft capsules, delayed-dissolving soft capsules using the same, and capsule-type human tissue lubricating suppositories - Google Patents

Abstract

The present invention discloses a composition for forming a soft capsule, the composition for forming a soft capsule at least includes: 10 wt% to 50 wt% gelatin; 0.1 wt% to 30 wt% plasticizer; 5 wt% to 50 wt% 0.01wt% to 20wt% thickener; 0.1wt% to 10wt% glidant; 0.1wt% to 10wt% disintegrant; 5wt% to 40wt% water. The soft capsule made by using the soft capsule forming composition can be safely placed in human tissue, and can be completely dissolved within a specified time range in a medium-temperature, high-humidity, acidic environment. Filling the lubricant into the soft capsule can further make a capsule type human tissue lubricating suppository.

Description

Composition for forming soft capsules, delayed-dissolving soft capsules using the same, and capsule-type human tissue lubricating suppositories

The present invention relates to a capsule casing, in particular to a capsule casing for containing lubricant.

Generally speaking, conventionally used lubricants for human skin are contained in cans, bottles or other containers, and the lubricants are taken out from the containers by pouring, squeezing, etc. before use. However, this kind of accommodating method usually has the following problems:

1. When taking out the lubricant for use, if the hands are not clean enough or the taking-out action is repeated, bacteria and viruses may be brought into the human body, thereby causing the risk of infection and causing doubts in terms of hygiene and safety.

2. Since the lubricant is stored in the container, it is inconvenient to carry. In addition, during use, the container may occupy a certain volume, which is visually awkward. In addition, in the use method, it must be taken out before use, which is easy to cause use. A bad impression on the experience.

Among them, the patent TW M544316 of the Ming Dynasty of China is related to a container structure and a pressure container of a water-based composition, which includes a bottle body and a bullet-shaped accommodation space, which is used to accommodate an aloe extract And an aqueous composition of hyaluronic acid, wherein, when the bottle is subjected to a pressure, the aqueous composition flows out of the bottle.

The patent TW M526400 of the Republic of China relates to a dosage form of stomach-disintegrating capsules, which has a stomach-capacity capsule shell; and a natural active peptide powder layer, which is filled in the stomach-soluble capsule shell.

Chinese patent CN103598971A relates to an electric sex toy with lubricating function, which includes a driving part, a lubricating part, a control part and a simulated organ, wherein the driving part can drive the simulated organ to imitate the natural movement of humans, while the lubricating part can effectively store lubricating fluid. The lubricating fluid can be drawn by the pump and then introduced into the simulated organ through the connecting tube. When the human body enters the simulated organ, the lubricating effect can be achieved.

Chinese patent CN104352679A is about a laxative capsule, which includes Chinese herbal medicine extract and gel shell in the capsule. The raw materials and raw material ratio of the gel shell are gelatin: glycerin: ethanol: purified water = 3~5%: 1%~3%: 5~8%: 84~91%. The Runchang Laxative Capsule has a greasy feeling, so it can lubricate the inner wall of the rectum, and the capsule itself is water-soluble.

U.S. Patent US6749557B2 relates to a self-lubricating auxiliary device, which can produce a lubricating effect through the lubricating fluid contained therein, which includes a cavity for loading the lubricating fluid, and a connecting mechanism that connects the cavity to the sexual aid . The sexual aid includes a surface structure for contacting the outer surface and the inner surface of the user, which has one or more holes; the user can make the lubricating fluid in the cavity flow to the human body by controlling the connection mechanism.

US Patent No. 7,858,119B1 relates to a prolonged-release drug, in which the drug is wrapped in a polymer film, and the drug active substance can be gradually released in the gastrointestinal tract and plasma for 12 to 24 hours. The extended-release drug includes a shell, which can be a single-layer or multi-layer polymer film, and it needs to be dissolved in an environment above pH 5. The related patent US7858119B1 further discloses that the shell contains 0.5-30% polyethylene glycol Alcohol plasticizer and 5~55% polymer.

However, none of the above-mentioned related patents can solve the problem that the capsule shell is not corroded by the internal lubricating oil at room temperature.

In view of the above-mentioned known problems, the object of the present invention is to provide a capsule for storing lubricant to solve the problems faced in the prior art.

Based on the above purpose, the present invention provides a composition for forming soft capsules, which is characterized in that: it is used to form a soft capsule that can be safely placed in human tissue and can be completely completely within a specified time in a medium-temperature, high-humidity, acidic environment. A dissolved soft capsule, the composition for forming the soft capsule at least includes: 10 wt% to 50 wt% gelatin; 0.1 wt% to 30 wt% plasticizer; 5 wt% to 50 wt% water retaining agent; 0.01 wt% 0.1wt% to 10wt% glidant; 0.1wt% to 10wt% disintegrant; 5wt% to 40wt% water; Among them, the ratio of the total amount of dry product of the plasticizer and the thickener to the weight of the dry product of gelatin is between 0.01 and 5.0; the viscosity of the composition for forming the soft capsule is between 10 and 45 centipoise, The gel strength is between 150 and 2500 Bloom; and the soft capsule obtained after the composition for forming the soft capsule is solidified can be placed in a medium-temperature, high-humidity, acidic environment in human tissue within the range of 5.0 to 15 minutes completely dissolved.

According to one embodiment of the present invention, the plasticizer is selected from glycerin, dicarboxylic acid/tricarboxylic acid esters, adipate, sebacate, maleate benzoate, sulfonate At least one of amides, ethyl acetyl monoglyceride, sanxian gum, citric acid ester and diisononyl cyclohexane-1,2-dicarboxylate.

According to an embodiment of the present invention, the water retaining agent is at least one selected from the group consisting of phosphates, polyols, betaine, NaPCA, hyaluronic acid, magnetite, mucopolysaccharide and panthenol.

According to one embodiment of the present invention, the thickener is selected from inorganic salt thickeners, fatty alcohol thickeners, fatty acid thickeners, alkanolamide thickeners, alkanolamide thickeners , ether thickener, ester thickener, oxidized alcohol amine thickener, cellulose thickener, polyacrylic thickener, polyurethane thickener, polyoxyethylene thickener Thickener, and at least one of natural rubber thickener, hydroxyethyl cellulose and soap thickener; more preferably.

According to one embodiment of the present invention, the glidant is at least one selected from ascorbyl palmitate, calcium palmitate, magnesium stearate, fumed silicon dioxide (colloidal silicon dioxide), starch and lime powder .

According to one embodiment of the present invention, the disintegrant is selected from starch, sodium carboxymethyl starch, low-substituted hydroxypropyl methylcellulose (L-HPC), cross-linked polyvinylpyrrolidone and effervescent disintegrants at least one of them.

According to an embodiment of the present invention, the pH value of the acidic environment with medium temperature and high humidity is between 4-5.8, the temperature is between 30-40° C., and the humidity is between RH60-RH80.

According to an embodiment of the present invention, the human tissue is near the vagina, anus, or rectum.

In addition, the present invention can also provide a time-dissolving soft capsule, which is made from the above-mentioned composition for forming soft capsules by a compression method or a dripping method, and is characterized in that: the time-dissolving soft capsule has a single-layer structure, or Multi-layer structure with more than two layers, the thickness of each single layer is 0.02~1.50mm, and the total thickness is between 0.25~1.50mm; the time-dissolving soft capsule is placed in the human tissue under the condition of medium temperature, high humidity and acidic environment It can be completely dissolved in the range of 5.0 to 15 minutes.

Moreover, the present invention can also provide a capsule-type human tissue lubricating suppository, which is characterized in that: a soft capsule made of the aforementioned composition or a soft capsule made by the aforementioned preparation method is filled with silicon base lubricant or water-based lubricant. The lubricant used in this embodiment at least includes: 42-76wt% cyclopentasiloxane; 18-42wt% dimethiconol; 6-16wt% polydimethylsiloxane. Also, the silicon-based lubricant may further contain 6 wt% to 16 wt% of water.

In addition, the water-based lubricant used in this embodiment preferably contains at least 0.1-2.5wt% Sanxian gum, 0.1-4wt% hydroxyethyl cellulose, 0.1-10wt% glycerin, 0.001-10wt% % hyaluronic acid, 0.01~8wt% water-locking magnet, 0.01~3wt% citric acid, 0.01~4wt% citric acid/sodium hydroxide, 1~8wt% pentylene glycol, and 6~97wt% pure water.

Based on the above, the capsule for storing lubricants of the present invention has the characteristics that the capsule shell will dissolve when it meets the range of the dissolution pH value, the dissolution temperature range, and the dissolution humidity range, so that the capsules contained in the capsule shell Lubricants can act on the human body to produce a lubricating effect.

In the following, various specific embodiments are listed for the implementation of the present invention and described and illustrated in more detail so as to make the spirit and content of the present invention more complete and easy to understand; however, those with ordinary knowledge in this art should It is understood that the present invention is of course not limited to these examples, and other same or equivalent functions and step sequences can also be used to achieve the present invention.

In this document, the meanings of scientific and technical terms used herein are the same as those understood and commonly used by those skilled in the art to which the present invention belongs. In addition, the singular nouns used in this specification include the plural forms of the nouns, and the plural nouns used also include the singular forms of the nouns, unless the context conflicts with the context.

In this article, for the numerical values and parameters used to define the scope of the present invention, the standard deviations caused by individual test methods are inevitably included in nature, so most of them are expressed in approximate numerical values, but in the specific examples The relevant numerical values are presented as precisely as possible. In this article, "about" usually depends on the consideration of those with ordinary knowledge in the technical field of the present invention, and generally means that the actual value falls within the acceptable standard error of the mean, for example, the actual value is within a Within ±10%, ±5%, ±1%, or ±0.5% of a specified value or range.

Please refer to Fig. 1, which is a schematic diagram of the capsule-type human tissue lubricating suppository of the present invention. As shown in Figure 1, the capsule type human tissue lubricating suppository 100 includes a soft capsule 110, the soft capsule 110 is a hollow shell, and a lubricant 120 is housed inside it; the capsule type human tissue lubricating suppository of the present invention The suppository 100 can be safely placed in human tissue, and can be completely dissolved within a specified time range in a medium-temperature, high-humidity, acidic environment. The soft capsule 110 is made by using a composition for forming a soft capsule by a compression method or a dropping method. The composition for forming a soft capsule at least includes: 10 wt% to 50 wt% gelatin; 0.1 wt% to 30 wt% plasticizer; 5wt% to 50wt% water retaining agent; 0.01wt% to 20wt% thickener; 0.1wt% to 10wt% glidant; 0.1wt% to 10wt% disintegrant; 5 wt% to 40 wt% water. Also, the viscosity of the soft capsule forming composition is between 10-45 centipoise.

According to the technical idea of the present invention, the plasticizer is selected from glycerin, dicarboxylic acid/tricarboxylic acid esters, adipate esters, sebacate esters, sanxian gum, maleic acid ester benzoate At least one of triglycerides, sulfonamides, ethyl acetyl monoglyceride, citrate and diisononyl cyclohexane-1,2-dicarboxylate; preferably selected from glycerol, dicarboxylic acid/ At least one of tricarboxylic acid esters, adipate esters, sebacic acid esters, maleic acid esters, benzoic acid esters, sulfonamides, and ethyl acetyl monoglyceride; more preferably At least one selected from glycerin, dicarboxylic acid/tricarboxylic acid esters, adipate, sebacic acid ester, and maleic acid ester benzoate; optimally selected from glycerin, dicarboxylic acid /At least one of tricarboxylic acid esters and adipate esters.

According to the technical idea of the present invention, the water-retaining agent is selected from phosphates, polyols, betaine, sodium rolidone carboxylate (NaPCA, Sodium Pyrrolidone Carboxylate), hyaluronic acid, water-locking magnets, mucopolysaccharides and panthenol. At least one; preferably at least one selected from phosphates, polyols, betaines, and sodium rolidone carboxylate (NaPCA, Sodium Pyrrolidone Carboxylate); more preferably selected from phosphates, polyols, and at least one of betaines.

According to the technical idea of the present invention, the thickener is selected from inorganic salt thickeners, fatty alcohol thickeners, fatty acid thickeners, alkanolamide thickeners, alkanolamide thickeners, Ether thickener, ester thickener, amine oxide thickener, cellulose thickener, polyacrylic thickener, polyurethane thickener, polyoxyethylene thickener At least one of thickeners, hydroxyethyl cellulose and natural gum thickeners, soap thickeners; preferably selected from inorganic salt thickeners, fatty alcohol thickeners, fatty acid thickeners, Alkanolamide thickeners, alkanolamide thickeners, ether thickeners, ester thickeners, oxidized alcohol amine thickeners, cellulose thickeners, polyacrylic acid thickeners, At least one of polyurethane thickeners and natural rubber thickeners; more preferably selected from inorganic salt thickeners, fatty alcohol thickeners, fatty acid thickeners, alkanolamides thickeners, ester thickeners, amine oxide thickeners, cellulose thickeners, polyacrylic thickeners, polyurethane thickeners, and natural rubber thickeners At least one of them; optimally selected from inorganic salt thickeners, fatty alcohol thickeners, fatty acid thickeners, ester thickeners, cellulose thickeners, polyacrylic thickeners, And at least one of natural rubber thickeners.

According to the technical idea of the present invention, the glidant is at least one selected from ascorbyl palmitate, calcium palmitate, magnesium stearate, fumed silicon dioxide (colloidal silicon dioxide), starch and lime powder; Preferably at least one selected from ascorbyl palmitate, calcium palmitate, magnesium stearate, fumed silicon dioxide (colloidal silicon dioxide), and starch; preferably selected from magnesium stearate, fumed At least one of phase silicon dioxide (colloidal silicon dioxide), and starch; preferably selected from ascorbyl palmitate, calcium palmitate, magnesium stearate, and fumed silicon dioxide (colloidal silicon dioxide ) at least one of them.

According to the technical idea of the present invention, the disintegrant is selected from starch, sodium carboxymethyl starch, low-substituted hydroxypropyl methylcellulose (L-HPC), cross-linked polyvinylpyrrolidone and effervescent disintegrants. At least one; preferably at least one selected from starch, sodium starch glycolate, and low-substituted hydroxypropylmethylcellulose (L-HPC).

Furthermore, in the composition for forming soft capsules, the ratio of the total dry weight of the plasticizer and thickener to the weight of the dry gelatin is generally between 0.01 and 5.0; preferably between 0.01 and 4.0 between; more preferably between 0.01 and 3.0; most preferably between 0.01 and 1.0; thereby, the soft capsule obtained after the soft capsule forming composition is solidified is placed in the human tissue at a high temperature It can be controlled to completely dissolve within a specified time range of 5.0 to 15 minutes under an acidic humidity environment, and the dissolution rate of the soft capsule can be controlled within a range of 0.1 g/min to 2.0 g/min.

The time-dissolving soft capsule shown in Figure 1 is a single-layer structure, but it is not limited to this. The time-dissolving soft capsule of the present invention can also be a multi-layer structure with more than two layers, and each single-layer thickness is 0.02~ 1.50mm, the total thickness is between 0.25~1.50mm.

In addition, the lubricant 120 filled in the soft capsule 110 at least includes 42-76wt% cyclopentasiloxane; 18-42wt% dimethylsiloxane alcohol; 6-16wt% polydimethylsiloxane alkyl. The lubricant 120 can be stably stored in the capsule shell 110 by the raw materials and the ratio of the raw materials. Since the lubricant contains water, if the proportion of water is too high, the capsule shell 110 will be softened, thereby reducing the water content to a minimum. degree, the minimum degree here refers to the need to take into account the somatosensory effect and function of the lubricant 120, rather than simply requiring a minimum water content ratio. Therefore, generally speaking, the lubricant 120 also contains 1 wt% to 16 wt% of water.

When the capsule 100 for preserving lubricant of the present invention is actually used, it is placed in a specific tissue of the human body, such as near the vagina, anus, or rectum, and the pH value and temperature of the capsule shell 110 at the location And when the humidity meets the range of dissolution pH value, dissolution temperature range and dissolution humidity range, the capsule shell 110 will start to dissolve, and the lubricant 120 contained in the capsule shell 110 will flow out from the capsule shell 110 to exert its Lubricating effect.

It is worth mentioning that the capsule shell can be dissolved in the human body under conditions that meet the dissolution temperature range and dissolution humidity range through the raw materials and raw material ratio of the capsule shell 110. On the other hand, it can also be achieved in the storage environment. It will not dissolve naturally but can be stored stably.

Next, the present invention is described below with specific examples. "Examples 1 to 5"

First, mix gelatin and water with the weight shown in Table 1 and obtain the capsule matrix after uniform stirring; then, glycerin, betaine, methylcellulose, magnesium stearate, magnesium stearate, and starch are sequentially added into the capsule base agent, and stirred at a temperature of 50° C. until the components are uniformly dispersed, and then the compositions S1 to S5 for forming soft capsules of the present invention can be obtained. The viscosities and strengths of the compositions S1 to S5 for forming soft capsules were tested with a viscometer and a gel strength meter, and the values were recorded in Table 1.

Next, the compositions S1 to S5 for forming soft capsules are evenly coated on a flat plate surface, and then heated at a temperature of about 90° C. to evaporate the moisture on the surface to form a soft film. The film is made into a capsule shell, and a lubricant composition for the human body is filled into the capsule shell, thereby making soft capsules M1 to M5. The lubricant composition for the human body can use silicon-based lubricants or water-based lubricants. The silicon-based lubricant used in this embodiment preferably contains at least 42~7wt% of cyclopentasiloxane (Cyclopentasiloxane), 18~42wt% of dimethylsiloxane alcohol (Dimethiconol), 6~ 16% polydimethylsiloxane (Dimethicone); and, may further include 6 wt% to 16 wt% of water.

In addition, the water-based lubricant used in this embodiment preferably contains at least 0.1-2.5wt% Sanxian gum, 0.1-4wt% hydroxyethyl cellulose, 0.1-10wt% glycerin, 0.001-10wt% % hyaluronic acid, 0.01~8wt% water-locking magnet, 0.01~3wt% citric acid, 0.01~4wt% citric acid/sodium hydroxide, 1~8wt% pentylene glycol, and 6~97wt% pure water.

Then, the in vitro dissolution test of the soft capsules M1 to M5 was carried out.

Prepare 500ml of phosphate buffer solution with a concentration of 50mM, adjust the pH value to 4.0, and adjust the solution temperature to 37°C to simulate the human vaginal environment. Next, using a fully automatic 8-tank dissolution system (Agilent Technologies 708-DS Dissolution Apparatus), place the soft capsules M1 to M5 in phosphate buffer solution respectively, observe the shell dissolution time of the soft capsules M1 to M5, and convert their dissolution rate.

As can be seen from the results in Table 1 above, the viscosities of compositions S1 to S5 for forming soft capsules are 10 centipoise, 18 centipoise, 26 centipoise, 34 centipoise, and 45 centipoise, and the gel strengths are 150 Bloom, Bloom, and S5 in sequence. 350Bloom, 878Bloom, 1954Bloom, 2500Bloom; moreover, the dissolution time of soft capsules M1 to M5 is 5.8 minutes, 6.4 minutes, 7.6 minutes, 10.7 minutes, 11.3 minutes, and the dissolution rate is 0.207g/min, 0.188g/min min, 0.158g/min, 0.112g/min, 0.106g/min, showing that the soft capsule M1 prepared from the soft capsule forming composition S1 in Example 1 has the fastest dissolution rate.

In addition, in Examples 1 to 5, the ratio of the total amount of dry product of glycerin (plasticizer) and methylcellulose (thickener) relative to the weight of gelatin dry product is 0.014, 0.192, 0.705, 0.813, 0.838, showing that when the ratio of the total amount of dry product of plasticizer and thickener to the weight of gelatin dry product is smaller, the dissolution rate of the soft capsule prepared by the composition for forming a soft capsule is faster, which can be obtained by controlling the increase The ratio of the total amount of dry product of plasticizer and thickener to the weight of gelatin dry product controls the dissolution time and speed of the soft capsule. "Example 6"

In this example, the composition S1 for forming soft capsules obtained in Example 1 was used to make soft capsules with different shell thicknesses, and the dissolution time of soft capsules with different shell thicknesses was analyzed. The analysis method was the same as that of Examples 1 to 5 above. Same, the obtained results are shown in Table 2.

Table 2 Experiment items (n) sample name capsule shell rupture time 1 Capsules for storing lubricants (thickness 5.2~9mm) 19 minutes and 58 seconds 25 minutes and 31 seconds 28 minutes and 10 seconds 2 Capsules for storing lubricants (thickness 2.2~4.6mm) 17 minutes and 07 seconds 18 minutes and 38 seconds 19 minutes and 10 seconds 3 Capsules for storing lubricants (thickness 0.28~1.4mm) 09 minutes 40 seconds 12 minutes and 25 seconds 13 minutes and 20 seconds

From the results in Table 2 above, we can see that the rupture time of the capsule shell will increase with the thickness of the shell, so the thickness of the shell can also be adjusted according to the needs to achieve the best use effect.

To sum up, the content of the present invention has been specifically described by way of examples in the above-listed embodiments, but the present invention is not limited to these embodiments. Those skilled in the technical field of the present invention should understand that various changes and modifications can be made without departing from the spirit and scope of the present invention; Changes can be made into new embodiments, and these embodiments should of course also be regarded as the content of the present invention. Therefore, the scope of protection in this case also includes the scope of the patent application and the scope defined thereafter.

100: Capsule type human tissue lubricating suppository 110: soft capsule 120: lubricant

Fig. 1 is a schematic diagram showing the capsule type human tissue lubricating suppository of the present invention.

100: Capsule type human tissue lubricating suppository

110: soft capsule

120: lubricant

Claims (5)

A composition for forming a soft capsule, characterized in that: it is used to form a soft capsule that can be safely placed in human tissue and can be completely dissolved within a specified time range in a medium-temperature, high-humidity, acidic environment, the soft capsule The forming composition at least includes: 10wt% to 50wt% gelatin; 0.1wt% to 30wt% plasticizer, the plasticizer is glycerin; 5wt% to 50wt% water retaining agent, the water retaining agent is phosphate, Polyols other than glycerin, and at least one of betaine; 0.01wt% to 20wt% of thickeners selected from cellulose thickeners; 0.1wt% to 10wt% of glidants , the glidant is at least one selected from ascorbyl palmitate, calcium palmitate, magnesium stearate, and fumed silicon dioxide (colloidal silicon dioxide); 0.1wt% to 10wt% of disintegrants , the disintegrating agent is at least one selected from starch, sodium carboxymethyl starch, and low-substituted hydroxypropylmethylcellulose (L-HPC); 5wt% to 40wt% of water; wherein the soft capsule is formed In the composition, the ratio of the total amount of dry product of the plasticizer and the thickener to the weight of the dry product of gelatin is between 0.01 and 5.0; the viscosity of the composition for forming the soft capsule is between 10 and 45 centipoise between; and the strength of the soft capsule obtained after curing the composition for forming the soft capsule is 150~2500Bloom, and it can be completely in the range of 5.0 to 15min when placed in the human tissue in a medium-temperature, high-humidity, acidic environment. dissolve. The composition for forming soft capsules as described in Claim 1, wherein the pH value of the medium-temperature, high-humidity acidic environment is between 4 and 5.8, the temperature is between 30 and 40°C, and the humidity is between RH60 and RH80 between. The composition for forming a soft capsule according to claim 1, wherein the human tissue is around the vagina, anus, or rectum. A time-dissolving soft capsule, which is made of the soft capsule-forming composition as described in any one of claims 1 to 3 by a compression method or a dripping method, characterized in that: the time-dissolving soft capsule is Single-layer structure, or multi-layer structure of more than two layers, the thickness of each single layer is 0.02~1.50mm, and the total thickness is between 0.25~1.50mm; the time-dissolving soft capsule is placed in the medium temperature and high humidity of human tissue It can be completely dissolved in the range of 5.0 to 15 minutes under acidic environmental conditions. A capsule-type human tissue lubricating suppository, characterized in that: it is contained in a soft capsule made of the composition as described in any one of claim items 1 to 3, or is dissolved in a timed manner as described in claim item 4 A silicon-based lubricant or a water-based lubricant is filled in the type soft capsule, wherein the silicon-based lubricant at least includes: 42-76wt% cyclopentasiloxane, 18-42wt% dimethylsiloxanol, and 6 ~16wt% polydimethylsiloxane; the water-based lubricant at least includes: 0.1~2.5wt% Sanxian gum, 0.1~4wt% hydroxyethyl cellulose, 0.1~10wt% glycerin, 0.001~10wt% % hyaluronic acid, 0.01~8wt% water-locking magnet, 0.01~3wt% citric acid, 0.01~4wt% citric acid/sodium hydroxide, 1~8wt% pentylene glycol, and 6~97wt% pure water.

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