WO2018077310A1 - Vitamin c sodium-containing effervescent tablet and preparation method therefor - Google Patents

Vitamin c sodium-containing effervescent tablet and preparation method therefor Download PDF

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Publication number
WO2018077310A1
WO2018077310A1 PCT/CN2017/114279 CN2017114279W WO2018077310A1 WO 2018077310 A1 WO2018077310 A1 WO 2018077310A1 CN 2017114279 W CN2017114279 W CN 2017114279W WO 2018077310 A1 WO2018077310 A1 WO 2018077310A1
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Prior art keywords
vitamin
sodium
parts
effervescent tablet
sucrose
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PCT/CN2017/114279
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French (fr)
Chinese (zh)
Inventor
黄爱强
钟文
黄爱毅
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广西圣保堂健康产业股份有限公司
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Publication of WO2018077310A1 publication Critical patent/WO2018077310A1/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • A61K31/375Ascorbic acid, i.e. vitamin C; Salts thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0002Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0007Effervescent
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2031Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin

Definitions

  • the invention belongs to the field of medicines, health foods and foods, and relates to a composition preparation and a preparation method thereof, in particular to an effervescent tablet containing vitamin C sodium and a preparation method thereof.
  • Vitamin C is a commonly used drug or nutritional supplement in the clinic. It is one of the antioxidant vitamins. It is involved in the hydroxylation reaction in the body and is necessary for the formation of bone, tooth, connective tissue and non-epithelial cells. The normal function of bones and blood vessels, increase the resistance to disease, and is one of the essential nutrients for the human body. It is widely used in the prevention and treatment of various diseases.
  • Effervescent tablets are a novel tablet developed and applied abroad in recent years. The difference between it and ordinary tablets is that it also contains an effervescent disintegrant.
  • effervescent tablet When the effervescent tablet is placed in drinking water, under the action of the effervescent disintegrant, a large amount of air bubbles are generated immediately, so that the tablet is quickly formed. Disintegration and melting, sometimes the bubbles generated by disintegration also cause the tablets to roll up and down in the water, accelerating their disintegration and melting. The gas generated when the tablet disintegrates is partially dissolved in the drinking water, so that the drinking water has a soda-like beauty when it is drunk in the mouth.
  • Effervescent tablets have the following advantages: easy to store and carry; rapid disintegration, convenient taking, rapid onset; high bioavailability, can improve clinical efficacy; especially suitable for children, the elderly and patients who have difficulty swallowing pills; After the seasoning of the effervescent tablets, the taste is better, the medicine is no longer bitter, so that consumers or patients are more willing to accept.
  • Vitamin C effervescent tablets are included in the second edition of the 2015 Chinese Pharmacopoeia. They are commonly used drugs in clinical practice. Because of the oxidative failure of vitamin C, effervescent tablets are prone to moisture absorption and dampness. Therefore, the use effect of vitamin C effervescent tablets and The shelf life is greatly affected. And the pH value of the aqueous solution of vitamin C is close to 2, and the acidity is large. Oral use is more irritating to the oral cavity, throat esophagus and gastric mucosa. It is not suitable for long-term use, and it is not suitable for taking it with acidic drugs. It is used as a nutrient for daily use or as a nutrient. The treatment or prevention of clinical diseases is limited.
  • Vitamin C sodium is the sodium salt of vitamin C.
  • the pH of the aqueous solution is close to neutral. It has the same effect as vitamin C, but because it is sodium salt, the performance is more stable. At the same time, there is no longer strong acidity of vitamin C.
  • the drug is taken at the same time, which is better than vitamin C.
  • Vitamin C sodium is a vitamin C fortifier widely used at home and abroad and has been gradually replaced by vitamin C. The invention directly forms vitamin C sodium into effervescent tablets, and the preparation is safe and effective through clinical trials. At present, no relevant literature reports have been reported.
  • the invention aims at the problem that the existing vitamin C effervescent tablet has high acidity after dissolution, is irritating to the oral cavity, the throat esophagus and the gastric mucosa, and is not suitable for long-term use, and the vitamin C is easily oxidized and failed during storage, and the effervescent tablet is easy to absorb moisture and damp.
  • the effervescent tablet containing vitamin C sodium and the preparation method thereof solve the problem that the quality of the clinical application of vitamin C is unstable and difficult to be taken for a long time.
  • the effervescent tablet containing vitamin C sodium has simple preparation and stable quality, and can be used for treating scurvy, infectious diseases, purpura, muscle weakness, paralysis, arrhythmia or renal dysfunction, or for malignancy. Prevention and treatment of tumors, cardiovascular and cerebrovascular diseases, infectious diseases or autoimmune diseases; or long-term use as a nutritional supplement.
  • An effervescent tablet containing vitamin C sodium comprising the following components by weight: 200-1120 parts of vitamin C sodium, 560-1300 parts of tartaric acid, 600-1500 parts of sodium hydrogencarbonate, and 200-600 parts of sucrose.
  • the above-mentioned vitamin C sodium-containing effervescent tablet preferably further comprises the following components by weight: 20-50 parts of a sweetener, 0.2-1 part of a pigment, and 2-8 parts of a flavor.
  • the above-mentioned vitamin C sodium-containing effervescent tablet further preferably further comprises 0.5 to 1.0% of trehalose and 0.2 to 0.4% of polyethylene glycol based on the total weight of the above components. 6000.
  • the above-mentioned vitamin C sodium-containing effervescent tablet preferably comprises the following components by weight: 850 parts of vitamin C sodium, 900 parts of tartaric acid, 1000 parts of sodium hydrogencarbonate, 350 parts of sucrose, 35 parts of sweetener,
  • the pigment was 0.6 parts and the fragrance was 5 parts, and further included trehalose which was 0.8% by weight based on the total weight of the above components and polyethylene glycol 6000 which was 0.3% by weight based on the total weight of the above components.
  • the above-mentioned vitamin C sodium-containing effervescent tablet is preferably aspartame, neotame or mogroside.
  • the pigment is preferably lemon yellow, amaranth, and bright blue.
  • the above-mentioned vitamin C sodium-containing effervescent tablet is preferably a sweet orange flavor or a blueberry flavor.
  • the above-mentioned vitamin C sodium-containing effervescent tablets, the acidity measurement and acidity value should preferably meet the following requirements: take the effervescent tablet, add cold water or warm water to disintegrate, make 1g solution per 100ml, to be collapsed After the solution is completely bubble free, the pH is determined to be 4.5 to 6.5; preferably the pH is 5.0 to 6.0.
  • a method for preparing an effervescent tablet containing the above vitamin C sodium comprises the following steps:
  • step S4 Take sodium bicarbonate, add the remaining 30-60% of the syrup pigment solution under step S3, mix, granulate, sieve, dry, and granulate to obtain an alkali agent;
  • drying temperature described in the steps S3 and S4 is preferably 80 ° C or lower, and the obtained particles have a moderate hardness, which is more favorable for tableting and facilitates disintegration; and the steps S3 and S4 are as described below.
  • the screen used for the sieving step is preferably 14-30 mesh.
  • the invention overcomes the problem that the existing vitamin C effervescent tablet has high acidity after dissolution, is irritating to the oral cavity, throat esophagus and gastric mucosa, and is not suitable for long-term use, and the vitamin C is easily oxidized and failed during storage, and the effervescent tablet is easy to absorb moisture and damp.
  • the problem is to make the product more stable and more effective. It is suitable for long-term use by consumers or patients without side effects.
  • the invention can be used for treating diseases such as scurvy, infectious diseases and purpura, such as muscle weakness, paralysis, arrhythmia or renal dysfunction, and can also be used for malignant tumors, cardiovascular and cerebrovascular diseases, infectious diseases and autoimmunity. Prevention and treatment of major and difficult diseases such as sexually transmitted diseases; or long-term use as a nutritional supplement.
  • diseases such as scurvy, infectious diseases and purpura, such as muscle weakness, paralysis, arrhythmia or renal dysfunction
  • malignant tumors such as cardiovascular and cerebrovascular diseases, infectious diseases and autoimmunity.
  • Prevention and treatment of major and difficult diseases such as sexually transmitted diseases; or long-term use as a nutritional supplement.
  • the effervescent tablet containing vitamin C sodium of the invention has simple preparation, good fluidity of the particles, and the tablet is not sticky, and the prepared tablet has a smooth surface, is not easy to absorb moisture, has uniform effervescent gas production, and has short disintegration time. After disintegration, the solution is transparent and clear, the taste is sweet, the quality is stable, and the carrying is convenient. It has the characteristics of solid preparation and liquid preparation, especially suitable for children, the elderly and patients who cannot swallow solid preparations, with high bioavailability and safer use. effective.
  • the word "preferred" and variants refers to embodiments of the invention that are capable of providing a particular benefit in a particular environment. However, other embodiments may be preferred under the same or other circumstances. In addition, the detailed description of one or more preferred embodiments does not indicate that other embodiments are useless and are not intended to exclude other embodiments from the scope of the invention.
  • the acid sources commonly used in effervescent tablets are tartaric acid, citric acid, fumaric acid, adipic acid, malic acid, etc.; alkali sources include sodium hydrogencarbonate, potassium carbonate, potassium hydrogencarbonate, calcium carbonate and the like.
  • the effervescent tablet prepared by using sodium hydrogencarbonate as an alkali source can rapidly disintegrate in water, and the pH of the effervescent solution is suitable for the stabilization of vitamin C sodium, so the alkali source of the present invention selects sodium hydrogencarbonate.
  • the fixed alkali source is sodium bicarbonate
  • the selection of tartaric acid, citric acid, fumaric acid, malic acid, adipic acid was tested to determine the best source of acid in the effervescent tablet.
  • the present invention uses tartaric acid mixed with vitamin C sodium, sodium hydrogencarbonate and sucrose to form granules, has a short disintegration time, clarifies the solution, and has a good mouthfeel, but has a sticking phenomenon when tableting.
  • the acid source of the present invention selects tartaric acid
  • the alkali source selects sodium hydrogencarbonate.
  • the invention compares the dry pressing tablet, the wet granulation and the re-pulling, the dry pressing tablet adopts the ordinary tableting machine has a poor effect and has high requirements on the equipment, so the invention adopts the wet granulation and the tableting.
  • 30% starch slurry, 40% sucrose syrup, 5% hypromellose aqueous solution, and 85% ethanol were used as binders. The results are shown in Table 2.
  • Vitamin C sodium is the sodium salt of vitamin C, which is more stable than vitamin C, but is prepared as an effervescent tablet in an acid agent.
  • the effects of alkaline agents, other excipients, and moisture and oxidation in the air must ensure that the quality of the product is stable during the shelf life, or that stabilizers need to be added.
  • 0.02% EDTA disodium, 1% trehalose, and 0.2% sodium sulfite were compared.
  • the samples prepared by the above stabilizers were respectively packaged with aluminum-plastic composite film, and the stability was accelerated in the test chamber: temperature: 40 ⁇ 2°C, relative humidity: 75 ⁇ 5%, accelerated test for 3 months, the test results are shown in Table 4.
  • the material of the invention before the tableting has acid agent, vitamin C sodium, essence, alkali agent, material particle size and texture unevenness, poor particle flowability when tableting, and easy sticking when tableting.
  • the other formulas except the lubricant are the same.
  • the different amounts of dodecyl magnesium sulfate, polyethylene glycol 6000, mannitol are specifically compared, and the above lubricants are respectively used.
  • the prepared samples were packaged with aluminum-plastic composite film respectively, and the stability test was accelerated in the test chamber: temperature: 40 ⁇ 2°C, relative humidity: 75 ⁇ 5%, accelerated test for 3 months, and the results are shown in Table 6.
  • the effervescent tablet After the effervescent tablet disintegrates, it is a beverage-like liquid. Therefore, the flavor and taste are very important.
  • the effervescent tablet is small in volume, the sample loading is small, and the sweetness of simple sucrose is not enough.
  • the following sweeteners are compared: stevia, licorice Acid disodium, aspartame, sodium saccharin, sodium cyclamate, mogroside, neotame, and alitame, the results show that: the above sweeteners are aspartame, mogroside, neotame In the range of the components of the "sweetener 20-50 parts", the taste is good, the sweetness is moderate, and there is no discomfort, and the aspartame tastes best. Therefore, the present invention selects aspartame, mogroside, and neotame as sweeteners, and the amount thereof is 20-50 parts.
  • the preparation method of the effervescent tablet containing vitamin C sodium includes the following steps:
  • step S3 Take tartaric acid, 12kg of sucrose and neotame in step S2, mix well, add appropriate 30% syrup pigment solution obtained under step S2, mix, granulate, pass 14 mesh sieve, dry at 80 °C, Whole grain, acidifier;
  • step S4 Take sodium bicarbonate, add the remaining 30% syrup pigment solution under step S3, mix well, then add the appropriate amount of 60% Ethanol granulation, passing through a 14 mesh sieve, drying at 80 ° C, granules, to obtain an alkali agent;
  • the preparation method of the effervescent tablet containing vitamin C sodium includes the following steps:
  • step S3 Take tartaric acid, 10kg of sucrose, and sucrose glycosides under step S2, mix well, add appropriate amount of 60% syrup pigment solution obtained under step S2, mix, granulate, pass 30 mesh sieve, dry at 100 °C , whole grain, acidifier;
  • step S4 Take sodium bicarbonate, add the remaining 60% syrup pigment solution under step S3, mix well, then add appropriate amount of 100% ethanol granules, pass through a 30 mesh sieve, dry at 60 ° C, and granulate to obtain an alkali agent;
  • the preparation method of the effervescent tablet containing vitamin C sodium includes the following steps:
  • step S3 Take tartaric acid, 20kg of sucrose and aspartame under step S2, mix well, add 40% syrup pigment solution obtained under step S2, mix, granulate, pass 20 mesh sieve, dry at 70 °C , whole grain, acidifier;
  • step S4 Take sodium bicarbonate, add the remaining 40% syrup pigment solution under step S3, mix well, then add appropriate amount of 60% ethanol granules, pass 20 mesh sieve, dry at 70 ° C, whole granules, get alkali agent;
  • the samples of the above Examples 1-3 were respectively packaged with an aluminum-plastic composite film, and the stability was accelerated in the test chamber: temperature: 40 ⁇ 2° C., relative humidity: 75 ⁇ 5%, accelerated test for 3 months, and the results were as follows.
  • the appearance characteristics, moisture, effervescence reaction time, solution pH value, main component content and other stability of the 1-3 samples were compared with the results of the samples at 0, and there was no significant change, the sweetness was moderate, and the taste of the taste did not change.
  • the sample of the embodiment 1-3 of the invention is relatively stable in quality and can meet the stability requirements of storage, transportation and use.
  • the test results are shown in Table 7.

Abstract

Disclosed is a vitamin C sodium-containing effervescent tablet, comprising the following components in parts by weight: 200-1120 parts of vitamin C sodium, 560-1300 parts of tartaric acid, 600-1500 parts of sodium bicarbonate, and 200-600 parts of sucrose. The present invention targets problems such as existing vitamin C effervescent tablets having high acidity after dissolving, irritating the mouth, throat, oesophagus and gastric mucosa, being unsuitable for long-term use, losing efficacy during storage due to the vitamin C oxidizing easily, and being susceptible to moisture absorption. The vitamin C sodium-containing effervescent tablet is a simple preparation, and has a stable mass.

Description

一种含维生素C钠的泡腾片及其制备方法Effervescent tablet containing vitamin C sodium and preparation method thereof 技术领域Technical field
本发明属于药品、保健食品、食品领域,涉及一种组合物制剂及其制备方法,特别是涉及一种含维生素C钠的泡腾片及其制备方法。The invention belongs to the field of medicines, health foods and foods, and relates to a composition preparation and a preparation method thereof, in particular to an effervescent tablet containing vitamin C sodium and a preparation method thereof.
背景技术Background technique
维生素C是临床基本常用药物或营养补充剂,是抗氧化维生素当中的一种,它参与体内羟化反应,为形成骨骼、牙齿、结缔组织及非上皮组织细胞间粘物所必需,可维持牙齿、骨骼、血管的正常功能,增加对疾病的抵抗能力,为人体必需的营养元素之一,广泛应用于多种疾病预防和治疗。Vitamin C is a commonly used drug or nutritional supplement in the clinic. It is one of the antioxidant vitamins. It is involved in the hydroxylation reaction in the body and is necessary for the formation of bone, tooth, connective tissue and non-epithelial cells. The normal function of bones and blood vessels, increase the resistance to disease, and is one of the essential nutrients for the human body. It is widely used in the prevention and treatment of various diseases.
泡腾片是近年来国外开发应用的一种新颖片剂。它与普通片剂的不同之处,就在于它还含有泡腾崩解剂,当泡腾片放入饮水中之后,在泡腾崩解剂的作用下,即刻产生大量气泡,使片剂迅速崩解和融化,有时崩解产生的气泡还会使药片在水中上下翻滚,加速其崩解和融化。片剂崩解时产生的气体部分溶解于饮水中,使饮水喝入口中时有汽水般的美感。泡腾片有如下的优点:便于保存和携带;崩解快速、服用方便、起效迅速;生物利用度高,能提高临床疗效;特别适用于儿童、老年人以及吞服药丸困难的患者;经过调味后的泡腾片,口味更佳,良药不再苦口,使消费者或病人更乐于接受。Effervescent tablets are a novel tablet developed and applied abroad in recent years. The difference between it and ordinary tablets is that it also contains an effervescent disintegrant. When the effervescent tablet is placed in drinking water, under the action of the effervescent disintegrant, a large amount of air bubbles are generated immediately, so that the tablet is quickly formed. Disintegration and melting, sometimes the bubbles generated by disintegration also cause the tablets to roll up and down in the water, accelerating their disintegration and melting. The gas generated when the tablet disintegrates is partially dissolved in the drinking water, so that the drinking water has a soda-like beauty when it is drunk in the mouth. Effervescent tablets have the following advantages: easy to store and carry; rapid disintegration, convenient taking, rapid onset; high bioavailability, can improve clinical efficacy; especially suitable for children, the elderly and patients who have difficulty swallowing pills; After the seasoning of the effervescent tablets, the taste is better, the medicine is no longer bitter, so that consumers or patients are more willing to accept.
维生素C泡腾片收载于2015年版《中国药典》第二部,为临床常用药物,由于维生素C易氧化失效,泡腾片易吸湿受潮等问题,因此,维生素C泡腾片的使用效果及保质期受到很大影响。且维生素C水溶液pH值接近2左右,酸性较大,口服使用对口腔、咽喉食道以及胃粘膜刺激较大,不宜长期服用,也不适合与酸性药物同时服用,在日常作为营养剂的使用或作为临床疾病的治疗或预防应用均受到一定限制。Vitamin C effervescent tablets are included in the second edition of the 2015 Chinese Pharmacopoeia. They are commonly used drugs in clinical practice. Because of the oxidative failure of vitamin C, effervescent tablets are prone to moisture absorption and dampness. Therefore, the use effect of vitamin C effervescent tablets and The shelf life is greatly affected. And the pH value of the aqueous solution of vitamin C is close to 2, and the acidity is large. Oral use is more irritating to the oral cavity, throat esophagus and gastric mucosa. It is not suitable for long-term use, and it is not suitable for taking it with acidic drugs. It is used as a nutrient for daily use or as a nutrient. The treatment or prevention of clinical diseases is limited.
维生素C钠是维生素C的钠盐,水溶液pH值接近中性,它的作用与维生素C相同,但由于是钠盐,所以性能更稳定,同时不再有维生素C的强酸性,可以长期与多种药物同时服用,更优于维生素C。维生素C钠属于国内外广泛使用的维生素C强化剂,已逐步替代维生素C使用。本发明直接将维生素C钠制成泡腾片,经临床试用,制剂安全有效,目前,尚未见有相关文献报道。Vitamin C sodium is the sodium salt of vitamin C. The pH of the aqueous solution is close to neutral. It has the same effect as vitamin C, but because it is sodium salt, the performance is more stable. At the same time, there is no longer strong acidity of vitamin C. The drug is taken at the same time, which is better than vitamin C. Vitamin C sodium is a vitamin C fortifier widely used at home and abroad and has been gradually replaced by vitamin C. The invention directly forms vitamin C sodium into effervescent tablets, and the preparation is safe and effective through clinical trials. At present, no relevant literature reports have been reported.
发明内容Summary of the invention
本发明针对现有维生素C泡腾片溶解后酸性大、对口腔、咽喉食道以及胃粘膜刺激较大、不宜长期服用,及存储过程中维生素C容易氧化失效、泡腾片易吸湿受潮等问题,提供一种 含维生素C钠的泡腾片及其制备方法,解决了临床上应用维生素C存在的质量不稳定、不易长期服用的问题。本发明含维生素C钠的泡腾片,制剂简便,质量稳定,可长期用于治疗坏血病、传染性疾病、紫癜兼有肌肉无力、瘫痪、心律失常或肾功能障碍疾病,或用于恶性肿瘤、心脑血管疾病、感染性疾病或自身免疫性疾病等的防治和辅助治疗;或作为营养补充剂长期服用。The invention aims at the problem that the existing vitamin C effervescent tablet has high acidity after dissolution, is irritating to the oral cavity, the throat esophagus and the gastric mucosa, and is not suitable for long-term use, and the vitamin C is easily oxidized and failed during storage, and the effervescent tablet is easy to absorb moisture and damp. Provide a kind The effervescent tablet containing vitamin C sodium and the preparation method thereof solve the problem that the quality of the clinical application of vitamin C is unstable and difficult to be taken for a long time. The effervescent tablet containing vitamin C sodium has simple preparation and stable quality, and can be used for treating scurvy, infectious diseases, purpura, muscle weakness, paralysis, arrhythmia or renal dysfunction, or for malignancy. Prevention and treatment of tumors, cardiovascular and cerebrovascular diseases, infectious diseases or autoimmune diseases; or long-term use as a nutritional supplement.
为解决上述技术问题,本发明是通过以下技术方案实现的:In order to solve the above technical problems, the present invention is achieved by the following technical solutions:
一种含维生素C钠的泡腾片,包括以下重量份的组分:维生素C钠200-1120份、酒石酸560-1300份、碳酸氢钠600-1500份、蔗糖200-600份。An effervescent tablet containing vitamin C sodium, comprising the following components by weight: 200-1120 parts of vitamin C sodium, 560-1300 parts of tartaric acid, 600-1500 parts of sodium hydrogencarbonate, and 200-600 parts of sucrose.
以上所述的含维生素C钠的泡腾片,优选还包括以下重量份的组分:甜味剂20-50份、色素0.2-1份、香精2-8份。The above-mentioned vitamin C sodium-containing effervescent tablet preferably further comprises the following components by weight: 20-50 parts of a sweetener, 0.2-1 part of a pigment, and 2-8 parts of a flavor.
以上所述的含维生素C钠的泡腾片,进一步优选还包括占以上所述组分总重量0.5-1.0%的海藻糖及占以上所述组分总重量0.2-0.4%的聚乙二醇6000。The above-mentioned vitamin C sodium-containing effervescent tablet further preferably further comprises 0.5 to 1.0% of trehalose and 0.2 to 0.4% of polyethylene glycol based on the total weight of the above components. 6000.
以上所述的含维生素C钠的泡腾片,最佳优选包括以下重量份的组分:维生素C钠850份、酒石酸900份、碳酸氢钠1000份、蔗糖350份、甜味剂35份、色素0.6份、香精5份,还包括占以上所述组分总重量0.8%的海藻糖及占以上所述组分总重量0.3%的聚乙二醇6000。The above-mentioned vitamin C sodium-containing effervescent tablet preferably comprises the following components by weight: 850 parts of vitamin C sodium, 900 parts of tartaric acid, 1000 parts of sodium hydrogencarbonate, 350 parts of sucrose, 35 parts of sweetener, The pigment was 0.6 parts and the fragrance was 5 parts, and further included trehalose which was 0.8% by weight based on the total weight of the above components and polyethylene glycol 6000 which was 0.3% by weight based on the total weight of the above components.
以上所述的含维生素C钠的泡腾片,所述甜味剂优选为阿斯巴甜、纽甜或罗汉果甜苷。The above-mentioned vitamin C sodium-containing effervescent tablet is preferably aspartame, neotame or mogroside.
以上所述的含维生素C钠的泡腾片,所述色素优选为柠檬黄、苋菜红、亮蓝。In the above-mentioned effervescent tablet containing vitamin C sodium, the pigment is preferably lemon yellow, amaranth, and bright blue.
以上所述的含维生素C钠的泡腾片,所述香精优选为甜橙香精、蓝莓香精。The above-mentioned vitamin C sodium-containing effervescent tablet is preferably a sweet orange flavor or a blueberry flavor.
以上所述的含维生素C钠的泡腾片,其酸度的测定及酸度值优选应符合以下规定:取泡腾片,加冷水或温水使崩解,制成每100ml含1g的溶液,待崩解完全无气泡后,测定pH值为4.5-6.5;优选pH值为5.0-6.0。The above-mentioned vitamin C sodium-containing effervescent tablets, the acidity measurement and acidity value should preferably meet the following requirements: take the effervescent tablet, add cold water or warm water to disintegrate, make 1g solution per 100ml, to be collapsed After the solution is completely bubble free, the pH is determined to be 4.5 to 6.5; preferably the pH is 5.0 to 6.0.
一种以上所述含维生素C钠的泡腾片的制备方法,包括如下步骤:A method for preparing an effervescent tablet containing the above vitamin C sodium comprises the following steps:
S1.称取以下重量份的组分:维生素C钠200-1120份、酒石酸560-1300份、碳酸氢钠600-1500份、蔗糖200-600份、甜味剂20-50份、色素0.2-1份、香精2-8份;再称取占以上所述组分总重量0.5-1.0%的海藻糖及占以上所述组分总重量0.2-0.4%的聚乙二醇6000;S1. Weigh the following parts by weight: vitamin C sodium 200-1120 parts, tartaric acid 560-1300 parts, sodium bicarbonate 600-1500 parts, sucrose 200-600 parts, sweetener 20-50 parts, pigment 0.2- 1 part, 2-8 parts of flavor; further weigh 0.5-1.0% of the total weight of the above components of trehalose and 0.2-0.4% of the total weight of the above components of polyethylene glycol 6000;
S2.将水煮沸,加入海藻糖及上述部分称量好的蔗糖,搅拌使其溶解,继续加热至100℃,滤过,得滤液,在滤液中再加入水、上述称量好的色素,混匀,得含蔗糖重量百分比为30-60%的糖浆色素溶液;S2. Boiling the water, adding trehalose and the above-mentioned part of the weighed sucrose, stirring to dissolve, continuing to heat to 100 ° C, filtering, to obtain a filtrate, adding water to the filtrate, the above-mentioned weighed pigment, mixed Evenly, a syrup pigment solution containing 30-60% by weight of sucrose;
S3.取酒石酸、步骤S2项下余下蔗糖、甜味剂,混匀,加入步骤S2项下得到的30-60%的糖浆色素溶液,混匀,制粒,过筛,干燥,整粒,得酸剂; S3. Take tartaric acid, the remaining sucrose and sweetener under step S2, mix, add 30-60% syrup pigment solution obtained under step S2, mix, granulate, sieve, dry, and granulate. Acid agent
S4.取碳酸氢钠,加入步骤S3项下余下的30-60%的糖浆色素溶液,混匀,制粒,过筛,干燥,整粒,得碱剂;S4. Take sodium bicarbonate, add the remaining 30-60% of the syrup pigment solution under step S3, mix, granulate, sieve, dry, and granulate to obtain an alkali agent;
S5.取酸剂、维生素C钠、香精,混匀,再加入碱剂、聚乙二醇6000,混匀,压片,即得。S5. Take acid, vitamin C sodium, essence, mix, add alkali agent, polyethylene glycol 6000, mix, tablet, that is.
进一步的,步骤S3、步骤S4项下所述的干燥的温度优选为80℃以下,这样得到的颗粒硬度适中,更有利于压片,同时利于崩解;所述步骤S3、S4项下所述的过筛步骤所用的筛网优选为14-30目。Further, the drying temperature described in the steps S3 and S4 is preferably 80 ° C or lower, and the obtained particles have a moderate hardness, which is more favorable for tableting and facilitates disintegration; and the steps S3 and S4 are as described below. The screen used for the sieving step is preferably 14-30 mesh.
本发明的有益效果是:The beneficial effects of the invention are:
1.本发明克服现有维生素C泡腾片溶解后酸性大、对口腔、咽喉食道以及胃粘膜刺激较大、不宜长期服用,及存储过程中维生素C容易氧化失效、泡腾片易吸湿受潮等问题,使产品稳定性更好,疗效更确切,适用于消费者或患者长期服用,无副作用。1. The invention overcomes the problem that the existing vitamin C effervescent tablet has high acidity after dissolution, is irritating to the oral cavity, throat esophagus and gastric mucosa, and is not suitable for long-term use, and the vitamin C is easily oxidized and failed during storage, and the effervescent tablet is easy to absorb moisture and damp. The problem is to make the product more stable and more effective. It is suitable for long-term use by consumers or patients without side effects.
2.本发明可用于治疗坏血病、传染性疾病、紫癜等兼有肌肉无力、瘫痪、心律失常或肾功能障碍等疾病,也可用于恶性肿瘤、心脑血管疾病、感染性疾病、自身免疫性疾病等重大疑难病症防治和辅助治疗;或作为营养补充剂长期服用。2. The invention can be used for treating diseases such as scurvy, infectious diseases and purpura, such as muscle weakness, paralysis, arrhythmia or renal dysfunction, and can also be used for malignant tumors, cardiovascular and cerebrovascular diseases, infectious diseases and autoimmunity. Prevention and treatment of major and difficult diseases such as sexually transmitted diseases; or long-term use as a nutritional supplement.
3.本发明含维生素C钠的泡腾片,制剂简便,颗粒流动性好,压片不粘冲,所制得的片剂表面光滑,不易吸湿,泡腾产气均匀,崩解时间短,崩解后溶液透明澄清,口感香甜,质量稳定,携带方便,兼具了固体制剂和液体制剂的特点,尤其适用于儿童、老年人和不能吞咽固体制剂的患者,生物利用度高,使用更安全有效。3. The effervescent tablet containing vitamin C sodium of the invention has simple preparation, good fluidity of the particles, and the tablet is not sticky, and the prepared tablet has a smooth surface, is not easy to absorb moisture, has uniform effervescent gas production, and has short disintegration time. After disintegration, the solution is transparent and clear, the taste is sweet, the quality is stable, and the carrying is convenient. It has the characteristics of solid preparation and liquid preparation, especially suitable for children, the elderly and patients who cannot swallow solid preparations, with high bioavailability and safer use. effective.
具体实施方式detailed description
虽然本说明书通过特别指出并清楚要求保护本发明的权利要求书作出结论,但应该相信下列说明将更好地理解本发明。While the specification concludes with particular reference to the claims of the invention, it is believed that
如本文所用,单词“优选”及变体是指在特定环境下能够提供特定有益效果的本发明的实施方案。然而,其它的实施方案在相同或其它的环境下也可以是优选的。此外,一个或多个优选实施方案的详述并不表示其它实施方案是无用的,并且不旨在从本发明的范畴排除其它的实施方案。As used herein, the word "preferred" and variants refers to embodiments of the invention that are capable of providing a particular benefit in a particular environment. However, other embodiments may be preferred under the same or other circumstances. In addition, the detailed description of one or more preferred embodiments does not indicate that other embodiments are useless and are not intended to exclude other embodiments from the scope of the invention.
一、制剂条件筛选First, the screening of preparation conditions
1.酸源和碱源的选择1. Selection of acid source and alkali source
泡腾片中常用的酸源有酒石酸、柠檬酸、富马酸、己二酸、苹果酸等;碱源有碳酸氢钠、碳酸钾、碳酸氢钾、碳酸钙等。用碳酸氢钠作为碱源制成的泡腾片在水中能迅速崩解,且泡腾溶液的pH值适宜维生素C钠的稳定,故本发明碱源选择碳酸氢钠。在固定碱源为碳酸氢钠 的基础上,按下表1中的配方对酒石酸、柠檬酸、富马酸、苹果酸、己二酸进行选择试验,以确定泡腾片中最佳的酸源种类。The acid sources commonly used in effervescent tablets are tartaric acid, citric acid, fumaric acid, adipic acid, malic acid, etc.; alkali sources include sodium hydrogencarbonate, potassium carbonate, potassium hydrogencarbonate, calcium carbonate and the like. The effervescent tablet prepared by using sodium hydrogencarbonate as an alkali source can rapidly disintegrate in water, and the pH of the effervescent solution is suitable for the stabilization of vitamin C sodium, so the alkali source of the present invention selects sodium hydrogencarbonate. The fixed alkali source is sodium bicarbonate On the basis of the following formula, the selection of tartaric acid, citric acid, fumaric acid, malic acid, adipic acid was tested to determine the best source of acid in the effervescent tablet.
表1 酸源和碱源优选试验Table 1 Preferred test of acid source and alkali source
序号Serial number 维生素C钠(g)Vitamin C sodium (g) 蔗糖(g)Sucrose (g) 酸源(g)Acid source (g) 试验结果test results
11 100100 3030 酒石酸tartaric acid 制粒效果好、压片粘冲,泡腾崩解时间短,溶液澄清,口感好The granulation effect is good, the tablet is sticky, the effervescence disintegration time is short, the solution is clear, and the taste is good.
22 100100 3030 柠檬酸Citric acid 制粒困难、压片粘冲,泡腾崩解时间短,溶液澄清,口感好Difficulty in granulation, tableting and blunting, short effervescent disintegration time, clear solution, good taste
33 100100 3030 富马酸Fumaric acid 制粒、压片效果好,泡腾崩解时间长,溶液混浊Granulation, tableting effect, effervescent disintegration time, solution turbidity
44 100100 3030 苹果酸Malic acid 制粒困难、压片粘冲,泡腾崩解时间短,溶液澄清,口感好Difficulty in granulation, tableting and blunting, short effervescent disintegration time, clear solution, good taste
55 100100 3030 己二酸Adipic acid 制粒、压片效果较好,泡腾崩解时间长Good granulation and tableting, long effervescent disintegration
从表1中的试验结果可知:本发明使用酒石酸与维生素C钠、碳酸氢钠、蔗糖混和,好制粒,腾崩解时间短,溶液澄清,口感好,只是压片时有粘冲现象,相比其他酸源最好,故本发明酸源选择酒石酸,碱源选择碳酸氢钠。It can be seen from the test results in Table 1 that the present invention uses tartaric acid mixed with vitamin C sodium, sodium hydrogencarbonate and sucrose to form granules, has a short disintegration time, clarifies the solution, and has a good mouthfeel, but has a sticking phenomenon when tableting. Compared with other acid sources, the acid source of the present invention selects tartaric acid, and the alkali source selects sodium hydrogencarbonate.
2.粘合剂选择2. Adhesive selection
本发明对比了干法压片、湿法制粒再压片,干法压片采用普通压片机效果不好,对设备要求高,故本发明采用湿法制粒再压片。试验中对比了30%淀粉浆、40%蔗糖糖浆、5%羟丙甲纤维素水溶液、85%乙醇做粘合剂,结果见表2。The invention compares the dry pressing tablet, the wet granulation and the re-pulling, the dry pressing tablet adopts the ordinary tableting machine has a poor effect and has high requirements on the equipment, so the invention adopts the wet granulation and the tableting. In the test, 30% starch slurry, 40% sucrose syrup, 5% hypromellose aqueous solution, and 85% ethanol were used as binders. The results are shown in Table 2.
表2 粘合剂考察结果表Table 2 Adhesive inspection results table
Figure PCTCN2017114279-appb-000001
Figure PCTCN2017114279-appb-000001
从表2中的试验结果可知:本发明使用40%蔗糖糖浆制粒情况及泡腾效果最好,故本发明粘合剂选择蔗糖糖浆。为进一步优化糖浆浓度,本发明继续优化蔗糖糖浆浓度,试验结果见表3。It can be seen from the test results in Table 2 that the granulation effect and the effervescence effect of the 40% sucrose syrup of the present invention are the best, and the sucrose syrup is selected as the binder of the present invention. In order to further optimize the syrup concentration, the present invention continues to optimize the sucrose syrup concentration, and the test results are shown in Table 3.
表3 糖浆浓度考察结果表Table 3 Table of results of syrup concentration investigation
序号Serial number 粘合剂Adhesive 制粒情况Granulation 颗粒外观Particle appearance 泡腾效果Effervescent effect
11 20%蔗糖糖浆20% sugar syrup 不成团,制粒困难Not in a group, difficult to pelletize 颗粒松Granular pine 泡腾崩解时间3分钟,溶液澄清Effervescent disintegration time 3 minutes, solution clarification
22 30%蔗糖糖浆30% sugar syrup 成团,制粒不结块In a cluster, granulation does not agglomerate 颗粒松紧合适Suitable for loose particles 泡腾崩解时间3分钟,溶液澄清Effervescent disintegration time 3 minutes, solution clarification
33 50%蔗糖糖浆50% syrup syrup 成团,制粒不结块In a cluster, granulation does not agglomerate 颗粒松紧合适Suitable for loose particles 泡腾崩解时间3.5分钟,溶液澄清Effervescent disintegration time 3.5 minutes, solution clarification
44 60%蔗糖糖浆60% sugar syrup 成团,制粒不结块In a cluster, granulation does not agglomerate 颗粒松紧合适Suitable for loose particles 泡腾崩解时间3.5分钟,溶液澄清Effervescent disintegration time 3.5 minutes, solution clarification
55 70%蔗糖糖浆70% sugar syrup 成团,制粒不结块In a cluster, granulation does not agglomerate 颗粒松紧合适Suitable for loose particles 泡腾崩解时间5.5分钟,溶液澄清Effervescent disintegration time 5.5 minutes, solution clarification
从表3中的试验结果可知:本发明使用30%-60%蔗糖糖浆制粒情况及泡腾效果较好,浓度低太松,浓度太高影响泡腾时间,故本发明粘合剂选择30%-60%蔗糖糖浆。It can be seen from the test results in Table 3 that the granulation of 30%-60% sucrose syrup and the effervescence effect of the present invention are better, the concentration is too low, and the concentration is too high, which affects the effervescence time, so the adhesive of the present invention is selected 30 %-60% sucrose syrup.
3.稳定剂的选择3. Selection of stabilizers
维生素C钠是维生素C的钠盐,性能较维生素C更稳定,但制备成泡腾片剂,在酸剂、 碱剂、其他辅料及空气中水分及氧化等的影响,要在保质期内保证产品的质量稳定,还是需要加入稳定剂。试验中对比了0.02%EDTA二钠、1%海藻糖、0.2%亚硫酸钠,将分别用上述稳定剂制成的样品,分别用铝塑复合膜包装好,置稳定性加速试验箱内试验:温度:40±2℃,相对湿度:75±5%,加速试验3个月,试验结果见表4。Vitamin C sodium is the sodium salt of vitamin C, which is more stable than vitamin C, but is prepared as an effervescent tablet in an acid agent. The effects of alkaline agents, other excipients, and moisture and oxidation in the air must ensure that the quality of the product is stable during the shelf life, or that stabilizers need to be added. In the test, 0.02% EDTA disodium, 1% trehalose, and 0.2% sodium sulfite were compared. The samples prepared by the above stabilizers were respectively packaged with aluminum-plastic composite film, and the stability was accelerated in the test chamber: temperature: 40±2°C, relative humidity: 75±5%, accelerated test for 3 months, the test results are shown in Table 4.
表4 稳定剂试验结果表Table 4 Stabilizer test results table
Figure PCTCN2017114279-appb-000002
Figure PCTCN2017114279-appb-000002
从表4中的试验结果可知:采用EDTA二钠及亚硫酸钠作为稳定剂,含水量变化较大,容易造成酸剂碱剂内部反应,溶液pH降低及加速氧化,导致维生素C钠含量降低。以1%海藻糖为稳定剂,加速试验后,水分变化不大,外观、泡腾反应时间、溶液pH及维生素C钠含量变化小,故本发明使用1%海藻糖作为稳定剂,为此,进一步考察海藻糖的加入量并将所得样品进行加速试验,试验方法同表4,结果详见表5。It can be seen from the test results in Table 4 that the use of disodium EDTA and sodium sulfite as a stabilizer has a large change in water content, which tends to cause an internal reaction of the acid agent alkali, a decrease in the pH of the solution and an accelerated oxidation, resulting in a decrease in the vitamin C content. With 1% trehalose as a stabilizer, after the accelerated test, the moisture does not change much, and the appearance, effervescence reaction time, solution pH and vitamin C sodium content change little, so the present invention uses 1% trehalose as a stabilizer, for which, The amount of trehalose added was further investigated and the obtained sample was subjected to an accelerated test. The test method was the same as in Table 4, and the results are shown in Table 5.
表5 海藻糖的加入量试验结果表Table 5 Test results of the amount of trehalose added
Figure PCTCN2017114279-appb-000003
Figure PCTCN2017114279-appb-000003
Figure PCTCN2017114279-appb-000004
Figure PCTCN2017114279-appb-000004
从表4中的试验结果可知:加入0.2-0.4%海藻糖后泡腾片的水分、外观、泡腾反应时间、溶液pH及维生素C钠含量变化均较大;而含0.5-1.0%海藻糖的泡腾片各项理化指标在3个月的加速时间内变化小,质量稳定;含1.2-1.5%海藻糖的泡腾片在3个月的加速时间内外观、pH值、含量指标变化不大,3个月加速时间内质量仍稳定,但水分、泡腾反应时间变化超出质量标准规定。故本发明控制海藻糖的加入量为0.5-1.0%。From the test results in Table 4, it can be seen that the moisture, appearance, effervescence reaction time, solution pH and vitamin C sodium content of the effervescent tablet are changed after adding 0.2-0.4% trehalose; and 0.5-1.0% trehalose is contained. The physical and chemical indicators of the effervescent tablets changed little during the acceleration period of 3 months, and the quality was stable. The appearance, pH value and content index of the effervescent tablets containing 1.2-1.5% trehalose did not change during the acceleration period of 3 months. Large, the quality is still stable during the 3 months acceleration period, but the change of water and effervescence reaction time exceeds the quality standard. Therefore, the amount of trehalose controlled by the present invention is 0.5-1.0%.
4.润滑剂的选择4. Selection of lubricants
本发明在压片前的物料有酸剂、维生素C钠、香精、碱剂,物料颗粒大小、质地不均,压片时出现颗粒流动性差、压片时易粘冲等现象。本发明试验中除润滑剂外其余配方相同,经初步试验确定可用比例后,具体对比了不同加入量的十二烷基硫酸镁、聚乙二醇6000、甘露醇,并将分别用上述润滑剂制成的样品,分别用铝塑复合膜包装好,置稳定性加速试验箱内试验:温度:40±2℃,相对湿度:75±5%,加速试验3个月,结果见表6。The material of the invention before the tableting has acid agent, vitamin C sodium, essence, alkali agent, material particle size and texture unevenness, poor particle flowability when tableting, and easy sticking when tableting. In the test of the present invention, the other formulas except the lubricant are the same. After the preliminary test determines the available ratio, the different amounts of dodecyl magnesium sulfate, polyethylene glycol 6000, mannitol are specifically compared, and the above lubricants are respectively used. The prepared samples were packaged with aluminum-plastic composite film respectively, and the stability test was accelerated in the test chamber: temperature: 40±2°C, relative humidity: 75±5%, accelerated test for 3 months, and the results are shown in Table 6.
表6 润滑剂试用结果表Table 6 Lubricant Trial Results Table
Figure PCTCN2017114279-appb-000005
Figure PCTCN2017114279-appb-000005
Figure PCTCN2017114279-appb-000006
Figure PCTCN2017114279-appb-000006
从表4中的试验结果可知:加入0.2-0.5%聚乙二醇6000的流动性好,且压片不粘冲,片面光滑美观,但加速试验发现,加入聚乙二醇6000量增加,含水量增加,泡腾反应时间也增加很多,不符合泡腾剂崩解时间要求,故本发明选用0.2-0.4%的聚乙二醇6000作为润滑剂。From the test results in Table 4, it is known that the flowability of adding 0.2-0.5% polyethylene glycol 6000 is good, and the tableting is not sticky, and the sheet surface is smooth and beautiful, but the accelerated test found that the amount of 6000 added polyethylene glycol increased, including As the amount of water increases, the effervescent reaction time also increases a lot, which does not meet the requirements for the disintegration time of the effervescent agent. Therefore, the present invention selects 0.2-0.4% of polyethylene glycol 6000 as a lubricant.
5.甜味剂的选择5. Selection of sweeteners
泡腾片崩解后为类似饮料的液体,因此,风味、口感非常重要,泡腾片体积小,载样量小,单纯蔗糖的甜度不够,试验中对比如下甜味剂:甜菊糖、甘草酸二钠、阿斯巴甜、、糖精钠、环己基氨基磺酸钠、罗汉果甜苷、纽甜、阿力甜,结果表明:上述甜味剂中阿斯巴甜、罗汉果甜苷、纽甜,在组分中比例为“甜味剂20-50份”的范围内,口感风味好,甜度适中,没有不适感,其中阿斯巴甜口感最佳。故本发明选用阿斯巴甜、罗汉果甜苷、纽甜为甜味剂,并规定其加入量为20—50份。After the effervescent tablet disintegrates, it is a beverage-like liquid. Therefore, the flavor and taste are very important. The effervescent tablet is small in volume, the sample loading is small, and the sweetness of simple sucrose is not enough. In the test, the following sweeteners are compared: stevia, licorice Acid disodium, aspartame, sodium saccharin, sodium cyclamate, mogroside, neotame, and alitame, the results show that: the above sweeteners are aspartame, mogroside, neotame In the range of the components of the "sweetener 20-50 parts", the taste is good, the sweetness is moderate, and there is no discomfort, and the aspartame tastes best. Therefore, the present invention selects aspartame, mogroside, and neotame as sweeteners, and the amount thereof is 20-50 parts.
二、含维生素C钠的泡腾片的制备方法2. Preparation method of effervescent tablet containing vitamin C sodium
实施例1Example 1
含维生素C钠的泡腾片的制备方法,包括如下步骤:The preparation method of the effervescent tablet containing vitamin C sodium includes the following steps:
S1.分别称取以下重量的组分:维生素C钠56kg、酒石酸56kg、碳酸氢钠60kg、蔗糖20kg、纽甜2kg、柠檬黄0.02kg、甜橙香精0.2kg,再称取占以上所述组分总重量0.5%的海藻糖9.7g及占以上所述组分总重量0.2%的聚乙二醇6000388g;S1. Weigh the following components: vitamin C sodium 56 kg, tartaric acid 56 kg, sodium bicarbonate 60 kg, sucrose 20 kg, neotame 2 kg, lemon yellow 0.02 kg, sweet orange flavor 0.2 kg, and then weighed the above group 9.7 g of trehalose having a total weight of 0.5% and 6000388 g of polyethylene glycol accounting for 0.2% of the total weight of the above components;
S2.将水煮沸,加入海藻糖,再从上述称量好的蔗糖中取8kg加入沸水中,搅拌使其溶解,继续加热至100℃,滤过,得滤液,在滤液中再加入适量水及上述称量好的柠檬黄,混匀,得含蔗糖重量百分比为30%的糖浆色素溶液;S2. boil the water, add trehalose, and then add 8kg from the above weighed sucrose to the boiling water, stir to dissolve, continue to heat to 100 ° C, filter, obtain the filtrate, add the appropriate amount of water in the filtrate and The above-mentioned weighed lemon yellow is mixed and obtained a syrup pigment solution containing 30% by weight of sucrose;
S3.取酒石酸、步骤S2项下余下蔗糖12kg、纽甜,混匀,加入适量步骤S2项下得到的30%的糖浆色素溶液,混匀,制粒,过14目筛,80℃下干燥,整粒,得酸剂;S3. Take tartaric acid, 12kg of sucrose and neotame in step S2, mix well, add appropriate 30% syrup pigment solution obtained under step S2, mix, granulate, pass 14 mesh sieve, dry at 80 °C, Whole grain, acidifier;
S4.取碳酸氢钠,加入步骤S3项下余下的30%的糖浆色素溶液,混匀,再加入适量60% 乙醇制粒,过14目筛,80℃下干燥,整粒,得碱剂;S4. Take sodium bicarbonate, add the remaining 30% syrup pigment solution under step S3, mix well, then add the appropriate amount of 60% Ethanol granulation, passing through a 14 mesh sieve, drying at 80 ° C, granules, to obtain an alkali agent;
S5.取酸剂、维生素C钠、甜橙香精,混匀,再加入碱剂、聚乙二醇6000,混匀,压片,即得。S5. Take acid, vitamin C sodium, sweet orange flavor, mix, add alkali agent, polyethylene glycol 6000, mix, tablet, that is.
实施例2Example 2
含维生素C钠的泡腾片的制备方法,包括如下步骤:The preparation method of the effervescent tablet containing vitamin C sodium includes the following steps:
S1.分别称取以下重量的组分:维生素C钠112kg、酒石酸130kg、碳酸氢钠150kg、蔗糖50kg、罗汉果甜苷5kg、苋菜红0.1kg、蓝莓香精0.8kg,再称取占以上所述组分总重量1.0%的海藻糖4421g及占以上所述组分总重量0.4%的聚乙二醇60001768g;S1. Weigh the following components: vitamin C sodium 112 kg, tartaric acid 130 kg, sodium bicarbonate 150 kg, sucrose 50 kg, mogroside 5 kg, amaranth 0.1 kg, blueberry flavor 0.8 kg, and then weighed the above group The total weight of 1.0% of trehalose 4421g and the total weight of the above components of 0.4% of polyethylene glycol 60001768g;
S2.将水煮沸,加入海藻糖,再从上述称量好的蔗糖中取40kg加入沸水中,搅拌使其溶解,继续加热至100℃,滤过,得滤液,在滤液中再加入适量水及上述称量好的苋菜红,混匀,得含蔗糖重量百分比为60%的糖浆色素溶液;S2. The water is boiled, trehalose is added, and 40 kg of the above weighed sucrose is added to the boiling water, stirred to dissolve, and the mixture is further heated to 100 ° C, filtered to obtain a filtrate, and an appropriate amount of water is added to the filtrate. The above-mentioned weighed amaranth is mixed, and a syrup pigment solution containing 60% by weight of sucrose is obtained;
S3.取酒石酸、步骤S2项下余下蔗糖10kg、罗汉果甜苷,混匀,加入适量步骤S2项下得到的60%的糖浆色素溶液,混匀,制粒,过30目筛,100℃下干燥,整粒,得酸剂;S3. Take tartaric acid, 10kg of sucrose, and sucrose glycosides under step S2, mix well, add appropriate amount of 60% syrup pigment solution obtained under step S2, mix, granulate, pass 30 mesh sieve, dry at 100 °C , whole grain, acidifier;
S4.取碳酸氢钠,加入步骤S3项下余下的60%的糖浆色素溶液,混匀,再加入适量100%乙醇制粒,过30目筛,60℃下干燥,整粒,得碱剂;S4. Take sodium bicarbonate, add the remaining 60% syrup pigment solution under step S3, mix well, then add appropriate amount of 100% ethanol granules, pass through a 30 mesh sieve, dry at 60 ° C, and granulate to obtain an alkali agent;
S5.取酸剂、维生素C钠、蓝莓香精,混匀,再加入碱剂、聚乙二醇6000,混匀,压片,即得。S5. Take acid, vitamin C sodium, blueberry flavor, mix, add alkali agent, polyethylene glycol 6000, mix, tablet, that is.
实施例3Example 3
含维生素C钠的泡腾片的制备方法,包括如下步骤:The preparation method of the effervescent tablet containing vitamin C sodium includes the following steps:
S1.分别称取以下重量的组分:维生素C钠85kg、酒石酸90kg、碳酸氢钠100kg、蔗糖35kg、阿斯巴甜3.5kg、亮蓝0.06kg、蓝莓香精0.5kg,再称取占以上所述组分总重量0.8%的海藻糖2512g及占以上所述组分总重量0.3%的聚乙二醇6000942g;S1. Weigh the following components: vitamin C sodium 85kg, tartaric acid 90kg, sodium bicarbonate 100kg, sucrose 35kg, aspartame 3.5kg, bright blue 0.06kg, blueberry flavor 0.5kg, and then weighed above 2512g of trehalose having a total weight of 0.8% of the component and 6000942g of polyethylene glycol accounting for 0.3% of the total weight of the above components;
S2.将水煮沸,加入海藻糖,再从上述称量好的蔗糖中取15kg加入沸水中,搅拌使其溶解,继续加热至100℃,滤过,得滤液,在滤液中再加入适量水及上述称量好的亮蓝,混匀,得含蔗糖重量百分比为40%的糖浆色素溶液;S2. boil the water, add trehalose, and then add 15kg from the above weighed sucrose to the boiling water, stir to dissolve, continue to heat to 100 ° C, filter, obtain the filtrate, add the appropriate amount of water in the filtrate and The above-mentioned weighed bright blue is mixed and obtained a syrup pigment solution containing 40% by weight of sucrose;
S3.取酒石酸、步骤S2项下余下蔗糖20kg、阿斯巴甜,混匀,加入步骤S2项下得到的40%的糖浆色素溶液,混匀,制粒,过20目筛,70℃下干燥,整粒,得酸剂;S3. Take tartaric acid, 20kg of sucrose and aspartame under step S2, mix well, add 40% syrup pigment solution obtained under step S2, mix, granulate, pass 20 mesh sieve, dry at 70 °C , whole grain, acidifier;
S4.取碳酸氢钠,加入步骤S3项下余下的40%的糖浆色素溶液,混匀,再加入适量60%乙醇制粒,过20目筛,70℃下干燥,整粒,得碱剂;S4. Take sodium bicarbonate, add the remaining 40% syrup pigment solution under step S3, mix well, then add appropriate amount of 60% ethanol granules, pass 20 mesh sieve, dry at 70 ° C, whole granules, get alkali agent;
S5.取酸剂、维生素C钠、蓝莓香精,混匀,再加入碱剂、聚乙二醇6000,混匀,压片, 即得。S5. Take acid, vitamin C sodium, blueberry flavor, mix, add alkali agent, polyethylene glycol 6000, mix, tablet, That is.
三、稳定性试验Third, the stability test
将上述实施例1-3样品分别用铝塑复合膜包装好,置稳定性加速试验箱内试验:温度:40±2℃,相对湿度:75±5%,加速试验3个月,结果实施例1-3样品的外观性状、水分、泡腾反应时间、溶液pH值、主要成分含量等稳定性重点考察指标与0时样品测定结果比较,均无明显变化,甜度适中,口感风味也没有变化,说明本发明实施例1-3样品质量较为稳定,可满足贮存、运输、使用的稳定性要求。试验结果见表7。The samples of the above Examples 1-3 were respectively packaged with an aluminum-plastic composite film, and the stability was accelerated in the test chamber: temperature: 40±2° C., relative humidity: 75±5%, accelerated test for 3 months, and the results were as follows. The appearance characteristics, moisture, effervescence reaction time, solution pH value, main component content and other stability of the 1-3 samples were compared with the results of the samples at 0, and there was no significant change, the sweetness was moderate, and the taste of the taste did not change. It is to be noted that the sample of the embodiment 1-3 of the invention is relatively stable in quality and can meet the stability requirements of storage, transportation and use. The test results are shown in Table 7.
表7 维生素C钠的泡腾片稳定性试验结果表Table 7 Table of results of stability test of effervescent tablets of sodium vitamin C
Figure PCTCN2017114279-appb-000007
Figure PCTCN2017114279-appb-000007

Claims (12)

  1. 一种含维生素C钠的泡腾片,其特征在于,包括以下重量份的组分:维生素C钠200-1120份、酒石酸560-1300份、碳酸氢钠600-1500份、蔗糖200-600份。An effervescent tablet containing vitamin C sodium, comprising the following components by weight: 200-1120 parts of vitamin C sodium, 560-1300 parts of tartaric acid, 600-1500 parts of sodium hydrogencarbonate, 200-600 parts of sucrose .
  2. 如权利要求1所述的含维生素C钠的泡腾片,其特征在于,还包括以下重量份的组分:甜味剂20-50份、色素0.2-1份、香精2-8份。The vitamin C-containing effervescent tablet according to claim 1, which further comprises the following components by weight: 20-50 parts of a sweetener, 0.2-1 part of a pigment, and 2-8 parts of a flavor.
  3. 如权利要求2所述的含维生素C钠的泡腾片,其特征在于,还包括占以上所述组分总重量0.5-1.0%的海藻糖及占以上所述组分总重量0.2-0.4%的聚乙二醇6000。The vitamin C sodium-containing effervescent tablet according to claim 2, which further comprises 0.5 to 1.0% of trehalose based on the total weight of the above components and 0.2 to 0.4% by weight based on the total weight of said components. Polyethylene glycol 6000.
  4. 如权利要求3所述的含维生素C钠的泡腾片,其特征在于,包括以下重量份的组分:维生素C钠850份、酒石酸900份、碳酸氢钠1000份、蔗糖350份、甜味剂35份、色素0.6份、香精5份,还包括占以上所述组分总重量0.8%的海藻糖及占以上所述组分总重量0.3%的聚乙二醇6000。The vitamin C sodium-containing effervescent tablet according to claim 3, which comprises the following components by weight: 850 parts of vitamin C sodium, 900 parts of tartaric acid, 1000 parts of sodium hydrogencarbonate, 350 parts of sucrose, and sweetness. 35 parts of the agent, 0.6 parts of the pigment, and 5 parts of the essence also included trehalose in an amount of 0.8% by weight based on the total weight of the above components and polyethylene glycol 6000 in an amount of 0.3% based on the total weight of the above components.
  5. 如权利要求2或4所述的含维生素C钠的泡腾片,其特征在于,所述甜味剂为阿斯巴甜、纽甜、罗汉果甜苷。The vitamin C sodium-containing effervescent tablet according to claim 2 or 4, wherein the sweetener is aspartame, neotame, and mogroside.
  6. 如权利要求2或4所述的含维生素C钠的泡腾片,其特征在于,所述色素为柠檬黄、苋菜红、亮蓝。The vitamin C sodium-containing effervescent tablet according to claim 2 or 4, wherein the pigment is lemon yellow, amaranth, and bright blue.
  7. 如权利要求2或4所述的含维生素C钠的泡腾片,其特征在于,所述香精为甜橙香精、蓝莓香精。The vitamin C sodium-containing effervescent tablet according to claim 2 or 4, wherein the flavor is a sweet orange flavor and a blueberry flavor.
  8. 如权利要求1-7中任一所述的含维生素C钠的泡腾片,其特征在于:取泡腾片,加冷水或温水使崩解,制成每100ml含1g的溶液,待崩解完全无气泡后,测定pH值为4.5-6.5。The effervescent tablet containing vitamin C sodium according to any one of claims 1 to 7, which is characterized in that an effervescent tablet is taken, and cold water or warm water is added to disintegrate to prepare a solution containing 1 g per 100 ml to be disintegrated. After completely no bubbles, the pH was determined to be 4.5-6.5.
  9. 如权利要求1-7中任一所述的含维生素C钠的泡腾片,其特征在于:取泡腾片,加冷水或温水的水使崩解,制成每100ml含1g的溶液,待崩解完全无气泡后,测定pH值为5.0-6.0。The effervescent tablet containing vitamin C sodium according to any one of claims 1 to 7, which is characterized in that an effervescent tablet is taken, and cold water or warm water is added to disintegrate, and a solution containing 1 g per 100 ml is prepared. After the disintegration was completely free of bubbles, the pH was measured to be 5.0 to 6.0.
  10. 一种如权利要求3所述含维生素C钠的泡腾片的制备方法,其特征在于,包括如下步骤:A method for preparing a vitamin C sodium-containing effervescent tablet according to claim 3, comprising the steps of:
    S1.分别称取以下重量份的组分:维生素C钠200-1120份、酒石酸560-1300份、碳酸氢钠600-1500份、蔗糖200-600份、甜味剂20-50份、色素0.2-1份、香精2-8份,再称取占以上所述组分总重量0.5-1.0%的海藻糖及占以上所述组分总重量0.2-0.4%的聚乙二醇6000;S1. Weigh the following parts by weight: 200-1120 parts of vitamin C sodium, 560-1300 parts of tartaric acid, 600-1500 parts of sodium bicarbonate, 200-600 parts of sucrose, 20-50 parts of sweetener, 0.2 coloring agent 1 part, 2-8 parts of flavor, further weigh 0.5-1.0% of the total weight of the above components of trehalose and 0.2-0.4% of the total weight of the above components of polyethylene glycol 6000;
    S2.将水煮沸,加入海藻糖及上述部分称量好的蔗糖,搅拌使其溶解,继续加热至100℃,滤过,得滤液,在滤液中再加入水、上述称量好的色素,混匀,得含蔗糖重量百分比为30-60%的糖浆色素溶液;S2. Boiling the water, adding trehalose and the above-mentioned part of the weighed sucrose, stirring to dissolve, continuing to heat to 100 ° C, filtering, to obtain a filtrate, adding water to the filtrate, the above-mentioned weighed pigment, mixed Evenly, a syrup pigment solution containing 30-60% by weight of sucrose;
    S3.取酒石酸、步骤S2项下余下蔗糖、甜味剂,混匀,加入步骤S2项下得到的30-60%的 糖浆色素溶液,混匀,制粒,过筛,干燥,整粒,得酸剂;S3. Take tartaric acid, the remaining sucrose and sweetener under step S2, mix and add 30-60% of the obtained under step S2. Syrup pigment solution, mixing, granulating, sieving, drying, granulating, acidifying agent;
    S4.取碳酸氢钠,加入步骤S3项下余下的30-60%的糖浆色素溶液,混匀,制粒,过筛,干燥,整粒,得碱剂;S4. Take sodium bicarbonate, add the remaining 30-60% of the syrup pigment solution under step S3, mix, granulate, sieve, dry, and granulate to obtain an alkali agent;
    S5.取酸剂、维生素C钠、香精,混匀,再加入碱剂、聚乙二醇6000,混匀,压片,即得。S5. Take acid, vitamin C sodium, essence, mix, add alkali agent, polyethylene glycol 6000, mix, tablet, that is.
  11. 如权利要求8所述含维生素C钠的泡腾片的制备方法,其特征在于,步骤S3、步骤S4项下所述的干燥的温度为80℃以下。The method for producing a vitamin C-containing effervescent tablet according to claim 8, wherein the drying temperature in the step S3 and the step S4 is 80 ° C or lower.
  12. 如权利要求8所述含维生素C钠的泡腾片的制备方法,其特征在于,步骤S3、S4项下所述的过筛步骤所用的筛网为14-30目。 The method for producing a vitamin C sodium-containing effervescent tablet according to claim 8, wherein the sieve used in the sieving step described in the steps S3 and S4 is 14 to 30 mesh.
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