A self-heating gel particle formulation for assisting swallowing of a medicament and a method of preparing the same

Abstract

This invention belongs to the field of pharmaceutical preparations and discloses a self-heating gel granule formulation for assisting in the swallowing of medications. By weight fraction, the raw material components include: calcium chloride: 5%–10%; potassium citrate: 2%–5%; edible gum: 5%–20%; and edible excipients: 65%–82%. The mass ratio of potassium citrate to calcium chloride is 1:1–5. This invention utilizes the exothermic dissolution properties of calcium chloride and potassium citrate to spontaneously provide sufficient heat for the rapid gelation of the gel material. Simultaneously, based on differences in consumer swallowing and taste preferences, it provides gel granule formulations with varying viscosities and flavors to meet diverse market demands.

Description

Technical Field

[0001] This invention belongs to the field of pharmaceutical preparations, specifically relating to a self-heating gel particle formulation for assisting in the swallowing of pharmaceutical agents and its preparation method. Background Technology

[0002] In recent years, with the improvement of people's living standards and the enhancement of health awareness, health foods and dietary supplements have gained widespread acceptance, consumer demand has continued to increase, and the overall market size has shown rapid growth. Health foods and dietary supplements are mainly oral preparations, especially tablets. Due to the influence of age and potential health problems on consumers, coupled with objective factors such as tablet size, shape, coating, and dosage, there are significant differences in swallowing experience among consumers. These factors affect consumer acceptance and adherence. Clinically, there are comprehensive and reasonable measures for the use of medications to treat diseases that severely affect swallowing function, such as stroke, Parkinson's disease, and cerebral palsy. However, for the target population of health foods and dietary supplements, the need is more about improving their consumption (swallowing) experience; many clinical measures used to solve swallowing difficulties are not applicable.

[0003] After dissolving, gel granules have a certain viscosity. When taken with tablets, they can coat the tablets, enhancing their fluidity and reducing the likelihood of them sticking to the mouth or esophagus, thus simplifying swallowing. Furthermore, the addition of fruit powder and flavorings to gel granules can mask unpleasant odors from the nutrients in the tablets, reducing irritation to the mouth and esophagus and improving the consumer's experience. However, since most edible gums require high temperatures and high shear to dissolve and have a slow gelation rate, they are extremely inconvenient for consumers to consume, making their application in daily medication use difficult.

[0004] In addition, commercially available gel matrices can only meet the needs of some drug development. Some active ingredients in drugs will rapidly degrade in liquid form, such as vitamins, making it difficult to exert their functional value. Furthermore, the transportation or storage costs are high. Therefore, many health care products cannot be pre-formed into gel matrices. Summary of the Invention

[0005] To address existing technical problems, this invention provides a self-heating gel granule formulation for assisting in the swallowing of medication and its preparation method. Utilizing the exothermic properties of calcium chloride and potassium citrate dissolving, it spontaneously provides sufficient heat for the rapid gelation of the gel material. Simultaneously, based on differences in consumer swallowing and taste preferences, it offers gel granule formulations with varying viscosities and flavors to meet diverse market demands.

[0006] The main technical solution adopted in this invention is as follows:

[0007] A self-heating gel granule formulation for adjuvant drug ingestion, comprising, by weight fraction:

[0008] Calcium chloride: 5%–10%;

[0009] Potassium citrate: 2%–5%;

[0010] Edible gum: 5%–20%;

[0011] Edible excipients: 65%–82%;

[0012] The mass ratio of potassium citrate to calcium chloride is 1:1-5.

[0013] Preferably, the edible gum is one or more of low-ester pectin, flaxseed gum, konjac gum, or carrageenan.

[0014] Preferably, the edible excipients include one or more of the following: prebiotics, sweeteners, fruit powders, edible flavorings, colorings, or pH adjusters.

[0015] Preferably, the prebiotic includes one or more of resistant dextrin, isomaltooligosaccharide, fructooligosaccharide, galactooligosaccharide or xylooligosaccharide.

[0016] Preferably, the sweetener is a natural sweetener, including one or more of xylitol, erythritol, sorbitol, maltitol, isomaltitol, glucose, steviol glycosides, and mogrosides.

[0017] Preferably, the pigment is a natural pigment, including one or more of grape skin red, sweet potato purple, natural amaranth, curcumin, gardenia blue, gardenia yellow, and beetroot red.

[0018] Preferably, the pH adjuster is one or more of citric acid, tartaric acid, malic acid, ascorbic acid, lactic acid, and gluconic acid.

[0019] A method for preparing a self-heating gel granule formulation for adjuvant drug ingestion, the specific preparation steps are as follows:

[0020] S1: Weigh each component material according to the product formula;

[0021] S2: Mix the pigment at a certain stirring speed for 3-5 minutes, then disperse it evenly with the prebiotics at a weight ratio of 1:10 and pass it through a 60-mesh sieve.

[0022] S3: Add the sweetener to the mixed powder obtained in step S2, disperse it evenly, and then add it to the mixer;

[0023] S4: Add the remaining edible ingredients, potassium citrate, calcium chloride and edible gum to the mixer and mix at a certain stirring speed for 5-10 minutes;

[0024] S5: Transfer the mixed material into a dry pellet mill for pelleting, wherein the roller pressure is 80KN, the roller speed is 8rpm, and the feeding speed is 50rpm.

[0025] S6: Use a granule packaging machine for packaging and sealing.

[0026] Preferably, in S2 and S4, the mixing speed is 11 rpm.

[0027] Beneficial effects: This invention provides a self-heating gel granule formulation for assisting in the swallowing of medicines and its preparation method, which has the following advantages:

[0028] (1) In this invention, the exothermic reaction of calcium chloride and potassium citrate is used to promote the dissolution of edible gum and accelerate gel formation, thereby obtaining a self-heating gel particle preparation, which improves the convenience of using the gel preparation.

[0029] (2) The gel particles in this invention have a certain viscosity after rapid dissolution. When taken with tablets, they can coat the tablets, enhance tablet fluidity, reduce the possibility of tablets adhering to the mouth or esophagus, and reduce the difficulty of swallowing.

[0030] (3) In this invention, by adding appropriate amounts of gel matrix, fruit powder, edible flavoring, sweetener, etc., the viscosity and flavor are adjusted, masking the unpleasant odors brought by the nutrients in the tablets, reducing the irritation to the mouth and esophagus, and improving the consumer's experience. Detailed Implementation

[0031] To enable those skilled in the art to better understand the technical solutions in this application, the technical solutions in the embodiments of this application are clearly and completely described below. Obviously, the described embodiments are only some embodiments of this application, and not all embodiments. Based on the embodiments in this application, all other embodiments obtained by those skilled in the art without creative effort should fall within the scope of protection of this application.

[0032] Example 1

[0033] A self-heating gel granule formulation for oral administration of an orange-flavored adjuvant is prepared in 10g / packet specifications, with the specific formula as follows:

[0034]

[0035]

[0036] The preparation method of Example 1 is as follows:

[0037] S1: Accurately weigh each component of the formula according to a batch size of 1000 packages;

[0038] S2: Mix gardenia yellow and beet red 11 rpm for 3 min, then disperse evenly with resistant dextrin (weight ratio 1:10) and pass through a 60 mesh sieve;

[0039] S3: Add sucralose and erythritol to the mixed powder in step S2, disperse them evenly, and then put them into the mixer;

[0040] S4: Add the remaining resistant dextrin, calcium chloride, potassium citrate, konjac powder, carrageenan, citric acid, orange powder and orange flavoring to the mixer and mix at 11 rpm for 6 minutes.

[0041] S5: Transfer the mixed material into a dry granulator for granulation. The process parameters are: roller pressure 80KN, roller speed 8rpm, and feeding speed 50rpm.

[0042] S6: Use a granule packaging machine for packaging and sealing.

[0043] Example 2

[0044] A pineapple-flavored, self-heating gel granule formulation for oral administration, prepared in 10g / packet specifications, with the following specific formula:

[0045]

[0046]

[0047] The preparation method of Example 2 is as follows:

[0048] S1: Accurately weigh each component of the formula according to a batch size of 1000 packages;

[0049] S2: Mix gardenia yellow at 11 rpm for 3 minutes, then disperse it evenly with galactooligosaccharides (weight ratio 1:10) and pass it through a 60-mesh sieve;

[0050] S3: Steviol glycosides and isomaltitol are added to the mixed powder in step S2, dispersed evenly, and then fed into a mixer;

[0051] S4: Add the remaining galactooligosaccharides, resistant dextrin, potassium citrate, calcium chloride, low-fat pectin, flaxseed gum, carrageenan, citric acid, pineapple fruit powder and pineapple flavor to the mixer and mix at 11 rpm for 8 minutes.

[0052] S5: Transfer the mixed materials into a dry granulator for granulation. The process parameters are: roller pressure 80KN, roller speed 8rpm, and feeding speed 50rpm.

[0053] S6: Use a granule packaging machine for packaging and sealing.

[0054] Example 3

[0055] A strawberry-flavored self-heating gel granule formulation for swallowing medication, prepared in 10g / packet specifications, with the following specific formula:

[0056]

[0057]

[0058] The specific preparation method of Example 3 is as follows:

[0059] S1: Accurately weigh each component of the formula according to a batch size of 1000 packages;

[0060] S2: Mix gardenia yellow and grape skin red 11 rpm for 3 min, then disperse evenly with oligofructose (weight ratio 1:10) and pass through a 60 mesh sieve;

[0061] S3: Add mogrosides, isomaltitol, and steviol glycosides to the mixed powder in step S1, disperse them evenly, and then put them into a mixer;

[0062] S4: Add the remaining fructooligosaccharides, potassium citrate, calcium chloride, flaxseed gum, xylooligosaccharides, citric acid, strawberry fruit powder, and strawberry flavoring to the mixer and mix at 11 rpm for 8 minutes.

[0063] S5: Transfer the mixed material into a dry granulator for granulation. The process parameters are: roller pressure 80KN, roller speed 8rpm, and feeding speed 50rpm.

[0064] S6: Use a granule packaging machine for packaging and sealing.

[0065] Comparative Example 1

[0066] A gel particle formulation, compared with Example 1, removes the self-heating materials (calcium chloride and potassium citrate), while retaining the same raw materials and preparation method as in Example 1. The specific formulation is as follows:

[0067]

[0068] (1) Comparative test of gelation formation

[0069] Take 10g of the self-heating gel particle formulations prepared in Examples 1-3 and the gel particle formulation prepared in Comparative Example 1, respectively, and pour them into 250mL of purified water. Stir gently with a small spoon for 10-20 seconds to ensure that the gel particles are fully in contact with the water. Record the gelation time, gel state, and taste evaluation of the gel particles after dissolution in Examples 1-3 and Comparative Example 1, respectively. The test results are shown in Table 1.

[0070] Table 1. Dissolution and gelation time, gel state, and taste evaluation of each gel particle.

[0071]

[0072]

[0073] As can be seen from the comparison of the test results of Example 1 and Comparative Example 1 in Table 1, the addition of calcium chloride and potassium citrate in Example 1 can promote the rapid dissolution and uniform dispersion of the gel.

[0074] As can be seen from Table 1, the self-heating gel granule formulations prepared in Examples 1-3 have good dissolution rate, gel quality, and taste, which can meet customers' different taste requirements.

[0075] (2) Gel particle formulation assisted swallowing drug test

[0076] Using the self-heating gel granules prepared in Example 1 as the test subject, two different sizes of tablets were selected, and the assisted swallowing effect was evaluated by different testers (numbered NO.1 to NO.5). The results are shown in Table 2.

[0077] Table 2 Evaluation of the effect of self-heating gel particles on assisted swallowing

[0078]

[0079]

[0080] As can be seen from Table 2, for people with difficulty swallowing tablets, the self-heating gel granule formulation prepared in Example 1 can significantly improve their swallowing experience and increase their medication compliance. At the same time, the gel granule formulation can mask odors and improve the user experience.

[0081] The above description is only a preferred embodiment of the present invention. It should be noted that for those skilled in the art, several improvements and modifications can be made without departing from the principle of the present invention, and these improvements and modifications should also be considered within the scope of protection of the present invention.

Claims

1. A self-heating gel particle formulation for assisting the swallowing of a medicament, characterised in that, The raw material components include, by weight fraction: Calcium chloride: 5% to 10%; Potassium citrate: 2% to 5%; Edible gum: 5% to 20%; Edible auxiliary materials: 65% to 82%; The mass ratio of potassium citrate: calcium chloride satisfies 1:1-5, and the edible gum is one or more of low-ester pectin, flaxseed gum, konjac gum, or carrageenan; The edible auxiliary materials include one or more of prebiotics, sweeteners, fruit powder, edible essence, pigments, or pH value regulators; The specific preparation steps are as follows: S1: weigh each component material according to the product formula; S2: mix the pigments at a certain stirring speed for 3-5 min, and then uniformly disperse the prebiotics at a weight ratio of 1:10 through a 60-mesh sieve; S3: add the sweeteners to the mixed powder obtained in step S2, uniformly disperse, and then add to the mixer; S4: add the remaining edible auxiliary materials, potassium citrate, calcium chloride, and edible gum to the mixer, and mix at a certain stirring speed for 5-10 min; S5: transfer the mixed material to a dry granulator for granulation, wherein the roller pressure is 80 KN, the roller speed is 8 rpm, and the feeding speed is 50 rpm; S6: use a granule packaging machine for packaging and sealing.

2. The self-heat gel pellet formulation for assisting the ingestion of a medicinal agent according to claim 1, characterized by, The prebiotics include one or more of resistant dextrin, isomalto-oligosaccharide, fructo-oligosaccharide, galacto-oligosaccharide, or xylo-oligosaccharide.

3. The self-heat gel pellet formulation for assisting the ingestion of a medicinal agent according to claim 1, wherein The sweeteners are natural sweeteners, including one or more of xylitol, erythritol, sorbitol, maltitol, isomalt, glucose, stevioside, and mogroside.

4. The self-heat gel pellet formulation for assisting the ingestion of a medicinal agent according to claim 1, wherein The pigments are natural pigments, including one or more of grape skin red, sweet potato purple, natural amaranth red, curcumin, gardenia blue, gardenia yellow, and beetroot red.

5. The self-heat gel pellet formulation for assisting the ingestion of a medicinal agent according to claim 1, wherein The pH value regulators are one or more of citric acid, tartaric acid, malic acid, ascorbic acid, lactic acid, and gluconic acid.

6. A process for the preparation of a self-heating gel granule formulation for the administration of an auxiliary agent according to any one of claims 1 to 5, characterized in that, The specific preparation steps are as follows: S1: weigh each component material according to the product formula; S2: mix the pigments at a certain stirring speed for 3-5 min, and then uniformly disperse the prebiotics at a weight ratio of 1:10 through a 60-mesh sieve; S3: add the sweeteners to the mixed powder obtained in step S2, uniformly disperse, and then add to the mixer; S4: add the remaining edible auxiliary materials, potassium citrate, calcium chloride, and edible gum to the mixer, and mix at a certain stirring speed for 5-10 min; S5: transfer the mixed material to a dry granulator for granulation, wherein the roller pressure is 80 KN, the roller speed is 8 rpm, and the feeding speed is 50 rpm; S6: use a granule packaging machine for packaging and sealing.

7. The method for preparing a self-heating gel particle formulation for adjuvant drug ingestion according to claim 6, characterized in that, In S2 and S4, the mixing and stirring speeds are both 11 rpm.

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