CN102552247B - Composition of vitamin C and preparation method thereof - Google Patents

Abstract

The invention provides a composition of vitamin C, which is composed of active ingredients and pharmaceutical excipients according to the following weight ratio: (1) active ingredients: vitamin C 5-30%, vitamin C sodium 3.25-19.25%, Calcium pantothenate 0.2-0.8%; (2) Pharmaceutical excipients: lubricant 0.05-0.45%, suspending agent 1-9%, filler 30-80%, adhesive 0.5-4.5%, plasticizer 0.05-2.45% %, flavoring agent 0.2-0.8%, spice 0.2-0.8%, food coloring 0.2-0.8%, coating material 0.05-5.45%. The vitamin C composition of the present invention has a good taste, does not need water or only needs a small amount of water to take, is convenient to carry and use, has good stability, absorbs and takes effect quickly, improves the compliance of taking, and has dual functions of treatment and health care, and is especially suitable for Children or the elderly and some patients with difficulty swallowing. The vitamin C composition of the present invention is superior to the vitamin C sugar-coated tablet in terms of appearance and content. The stability of the vitamin C composition of the present invention is greatly improved. The preparation process of the invention is reasonable, the operation is simple and convenient, and it is suitable for industrial production. It has good clinical effect and great application value.

Description

A composition of vitamin C and its preparation method

technical field

The present invention relates to pharmaceutical preparations. Specifically relates to a vitamin C composition and a preparation method.

Background technique

Vitamin C and dehydrovitamin C form a reversible redox system in the body, which plays an important role in biological oxidation and reduction and cellular respiration. Vitamin C participates in the metabolism of amino acids, the synthesis of neurotransmitters, and the synthesis of collagen and tissue interstitium, which is very important to human health. The main physiological functions of vitamin C: promote the biosynthesis of collagen, facilitate the faster healing of tissue wounds, promote the metabolism of tyrosine and tryptophan in amino acids, prolong the life of the body, improve the utilization of iron, calcium and folic acid, Improve the metabolism of fats and lipids, especially cholesterol, prevent cardiovascular diseases, promote the growth of teeth and bones, prevent gum bleeding, and enhance the body's ability to resist stress and immunity to the external environment. And vitamin C can also block the formation of melanin, enhance skin elasticity, prevent pigmentation, and have cosmetic effects. Sodium vitamin C has been used as a nutritional supplement and antioxidant, and has the advantages of no sour taste, easy solubility in water, and increased stability of vitamin C. At present, vitamin C preparations have various dosage forms such as ordinary tablets, chewable tablets, effervescent tablets, dispersible tablets, buccal tablets, and injections. But all have defects such as easy discoloration, easy degradation, poor stability, inconvenience to carry and use and complex production process (chewable tablet, effervescent tablet, dispersible tablet, injection) to varying degrees. In addition, the sour and astringent taste of vitamin C, when in contact with the taste buds, will transmit the information of the bad stimulus to the cerebral cortex center, resulting in bad taste, resulting in poor compliance of taking, which affects the clinical use of vitamin C. Therefore, people have higher and higher demands for improving the taking and portability of vitamin C preparations. Especially for children or elderly patients and some patients who have difficulty swallowing, granule products that can be swallowed directly are more acceptable. At the same time, it has been the goal of the pharmaceutical industry to cover up the bad taste of drugs and improve patient compliance. However, the present inventors found that the combination of calcium pantothenate and vitamin C produced an unexpected effect. Calcium pantothenate has many effects on human body beauty and fatigue improvement. In addition, it is also clinically used for the prevention and treatment of calcium pantothenate deficiency (such as malabsorption syndrome, tropical sprue, celiac disease, Crohn's disease), and at the same time, it can alleviate pigmentation of spots, freckles, sunburn, and skin inflammation. When vitamin C is combined with calcium pantothenate, it can not only improve the defects of vitamin C preparations, but also increase the uses. Therefore, research into vitamin C composition formulations is a matter of interest.

Contents of the invention

The technical problem to be solved by the present invention is to overcome the above disadvantages, research and design a vitamin C composition that is easy to carry and take, fast to absorb and take effect, good in stability, and easy to carry.

A vitamin C composition according to the present invention, said composition is composed of active ingredients and pharmaceutical excipients according to the following weight ratio:

(1) Active ingredients:

Vitamin C 5～30%

Sodium vitamin C 3.25～19.25%

Calcium pantothenate 0.2～0.8%

;

(2) Pharmaceutical excipients

Preferably, a vitamin C composition of the present invention, said composition is composed of the following components by weight ratio: 2000g/1000 bags

The composition of the present invention is granule, 1-3g (per bag).

The function of each component in the composition of the present invention is as follows:

The active ingredients include: vitamin C, sodium vitamin C and calcium pantothenate. Among them, sodium vitamin C has the functions of antioxidant and vitamin C; calcium pantothenate has many effects on human body beauty and fatigue improvement, and can relieve pigmentation of spots, freckles, sunburn, and skin inflammation.

The pharmaceutical auxiliary materials include lubricants, suspending agents, fillers, binders, plasticizers,

Flavoring agents, spices, food coloring, coating materials.

Lubricants: including but not limited to magnesium stearate, calcium stearate, glyceryl monostearate, polyethylene glycol, hydrogenated vegetable oil, sodium lauryl sulfate, magnesium lauryl sulfate, talc, etc. Can be used alone or in combination. It can improve the fluidity of raw materials, eliminate electrostatic adsorption, and facilitate the smooth progress of crushing and taste-masking coating.

Taste-masking granules: taste-masking coated with coated polymer materials.

Coating materials: including but not limited to acrylic resin L-100, ethyl cellulose, hypromellose, polyvinylpyrrolidone, methyl cellulose, gelatin, gum arabic, zein, sodium alginate, chitosan, etc. , can be used alone or in combination. Prepared as water or ethanol solution coating, to achieve the purpose of taste masking.

Flavor granules: Suspensions, fillers and the above granules are granulated with a binder solution (including flavors, plasticizers, spices, and pigments) through fluidized bed technology.

Suspension: including but not limited to microcrystalline cellulose-sodium carboxymethyl starch (RC-591), sodium carboxymethyl cellulose (sodium CMC), polyvinylpyrrolidone (PVP), xanthan collagen, sodium carboxymethyl starch (CMS sodium), hydroxypropyl methylcellulose (HPMC), etc., can be used alone or in combination. Acts as a suspension stabilizer in the granules.

Fillers: including but not limited to mannitol, sorbitol, maltose, microcrystalline cellulose, glucose, sucrose, lactose, dextrin, etc., which can be used alone or in combination.

Binder: including but not limited to hydroxypropyl cellulose (HPC-L), HPMC, PVP, starch, dextrin, methylcellulose, alginic acid and alginate, etc., which can be used alone or in combination. According to the needs of the process, it can be prepared as a water or ethanol solution as a binder for granulation.

Flavoring agents: including but not limited to sodium saccharin, aspartame, lactose, fructose, sucrose, stevia, mannitol, xylitol, etc., which can be used alone or in combination. On the basis of taste masking, it plays a role of flavor correction.

Plasticizers: including but not limited to polyethylene glycol 6000 (PEG6000), polyethylene glycol 4000 (PEG4000), triethyl citrate, cetyl alcohol, etc., which can be used alone or in combination. Play a role in improving the appearance of particles.

Spices: including but not limited to essence, mint, vanillin, ethyl vanillin, etc., which can be used alone or in combination. Play a role in improving the sense of smell and making it easier for people to accept.

Pigments: natural or synthetic pigments acceptable in the pharmaceutical and food industries, including but not limited to tartrazine, sunset yellow, carotene, curcumin, etc., which can be used alone or in combination to improve the appearance of granules . It can make the appearance of particles more beautiful and more acceptable.

Another object of the present invention is to provide a method for preparing a vitamin C composition.

The method of the present invention comprises preparation of core granules, preparation of taste-masking granules and preparation of flavor-correcting granules, specifically comprising the following steps:

(1) Preparation of core particles:

Fully mix vitamin C, vitamin C sodium, calcium pantothenate and lubricant, and then crush the mixture to a particle size of 25-50um to make core particles;

(2) Preparation of taste-masking granules:

The core granules of (1) are placed in a fluidized bed coating machine, continuously sprayed with an anhydrous ethanol solution (concentration 5-10%) prepared by a polymer coating material, and the coated granules are passed through an 80-mesh sieve. Make taste-masking granules; set the spray volume at 10g/min, the spray pressure at 0.5MPa, the air intake volume at 1m ³ /min, and the air intake temperature at 80°C; and dry at 50°C for 15min after coating.

(3) Preparation of flavoring granules

Mix the taste-masking granules of (2) with suspending agents and fillers and place them in a fluidized bed; in addition, dissolve binders, plasticizers, flavoring agents, spices and pigments in water or ethanol to make 3-9 % solution, continuous spraying, drying in hot air at 40-50°C after spraying, discharging, passing through a 20-mesh sieve to obtain flavoring granules.

According to the specifications required for taking, it can be packed in aluminum-plastic composite bags (the weight of each bag is 1-3g).

In the present invention, the composition of vitamin C, vitamin C sodium and calcium pantothenate is made into granules, and core granules, taste-masking granules and flavor-correcting granules are prepared step by step, which has good effect. In the present invention, vitamin C and vitamin C sodium are first made into core particles, which can prevent the stability of vitamin C from being affected by oxygen and moisture, and significantly improve the stability of the vitamin C composition. The polymer coating material is further coated on the surface of the bad-tasting drug particles, thereby reducing the dissolution of the drug in the oral cavity and achieving the purpose of taste masking. Finally, flavor-correcting granules are made, so that the granules of the present invention have good taste and mouthfeel and accurate dosage. In addition, the granules of the present invention are easy to carry and take, do not need water or only need a small amount of water, do not need to chew, and can enter the stomach with the help of swallowing power, and the vitamin C, sodium vitamin C and calcium pantothenate in the composition form a highly dispersed The fine particles improve bioavailability. Because the composition of the invention has good taste and fast absorption, it is beneficial for patients to take and increase compliance. At the same time, it also has the functions of beauty and health care such as treating calcium pantothenate deficiency and relieving pigmentation of spots, freckles, sunburn, and skin inflammation. There is no relevant report on the composition and granule dosage form of the present invention.

The vitamin C composition of the present invention can be used to prevent and treat diseases caused by vitamin C deficiency (such as scurvy, bleeding gums, nosebleeds), and can also be used to enhance the body's resistance, prevent cardiovascular and cerebrovascular diseases, and treat wounds during the healing period. , Physical fatigue, pregnancy, breast-feeding period, recovery period after illness and other low physical strength and habitual abortion, infertility and skin pigmentation, etc. adjuvant treatment. The invention is a granule, which overcomes the defects of the existing formulations of vitamin C. The preparation process of the invention is reasonable, the operation is simple and convenient, and it is suitable for industrial production. It has good clinical effect and great application value.

Detailed ways

In order to better illustrate the vitamin C composition and preparation method of the present invention, further description will be made in conjunction with examples.

Example 1

Preparation:

1) Thoroughly mix vitamin C, vitamin C-Na, and calcium stearate evenly, and grind to a particle size of 25-50um to obtain core granules.

2) Put the core particles of 1) in a fluidized bed coating machine (equipment model SFP-01), prepare an 8% ethanol solution as a slurry with acrylic resin L100 and absolute ethanol 316.25 g, and spray coating continuously; The fixed spray volume is 10g/min, the spray pressure is 0.5MPa, the air intake volume is 1m ³ /min, and the air intake temperature is 80°C; after coating, it is dried at 50°C for 15min.

3) passing 2) the coated granules through an 80-mesh sieve to obtain taste-masked granules;

4) Mix 3) granules with microcrystalline cellulose, microcrystalline cellulose-carboxymethyl cellulose sodium and place them in a fluidized bed (equipment model MP-01), and dissolve HPC-L with water (specific amount? 447.5g) , PEG6000, sodium saccharin, essence and tartrazine, prepared into 5% HPC solution as a binder, set the spray volume to 10g/min, spray pressure to 0.5MPa, air intake volume to 1m ³ /min, air intake temperature to 80°C, Spray the liquid in the way of top spray, dry it with hot air at 40-50°C after spraying, discharge the material, and pass through a 20-mesh sieve to obtain flavored granules;

5) Packing: 4) the flavoring granules are packed in an aluminum-plastic composite bag at 1g/bag.

Example 2

Preparation:

According to the preparation process described in Example 1, the packaging specification is 2g/bag in an aluminum-plastic composite bag.

Example 3

Preparation:

According to the preparation process described in Example 1, the packaging specification is 3g/bag in an aluminum-plastic composite bag.

Example 4

Preparation:

According to the preparation process described in Example 1, the packaging specification is 1g/bag in an aluminum-plastic composite bag.

Example 5

Preparation:

According to the preparation process described in Example 1, the packaging specification is 1g/bag in an aluminum-plastic composite bag.

Example 6

Preparation:

According to the preparation process described in Example 1, the packaging specification is 1g/bag in an aluminum-plastic composite bag.

Example 7

Preparation:

According to the preparation process described in Example 1, the packaging specification is 1g/bag in an aluminum-plastic composite bag.

Example 8

Preparation:

According to the preparation process described in Example 1, the packaging specification is 1g/bag in an aluminum-plastic composite bag.

Example 9

Preparation:

According to the preparation process described in Example 1, the packaging specification is 1g/bag in an aluminum-plastic composite bag.

Example 10 Stability investigation

The vitamin C composition granules prepared according to Examples 1-9 were placed at 60° C./10 days to investigate indicators such as taste, appearance, vitamin C content, and the results showed that the quality was stable (see Table 1 below), and Obviously better than vitamin C sugar-coated tablets (produced by Changzhou Fourth Pharmaceutical Factory Co., Ltd., batch numbers are 20100701, 20100702, 20110301) (see Table 2 below):

Table I

Table II

Table 1 and Table 2 clearly show that the vitamin C composition of the present invention is superior to vitamin C sugar-coated tablets in terms of appearance and content. The stability of the vitamin C composition of the present invention is greatly improved.

Claims (1)

1. a vitamin C composition, is characterized in that, described compositions is grouped into by the one-tenth of following weight:

Preparation method:

1) vitamin C, sodium ascorbate, calcium pantothenate, calcium stearate are fully mixed evenly, and are crushed to particle diameter 25-50 μ m, obtain core granule;

2) by 1) core granule be placed in fluidized-bed coating machine, unit type SFP-01, is formulated as 8% alcoholic solution as serosity using acrylic resin L100 and dehydrated alcohol 316.25g, continuously spray coating; Set discharge rate 10g/min, atomisation pressure 0.5MPa, intake 1m ³/ min, 80 ℃ of inlet temperature; 50 ℃ of dry 15min after coating;

3) by 2) granule is crossed 80 mesh sieves and is obtained taste masked particle after coating;

4) by 3) granule mixes and is placed on fluid bed with microcrystalline Cellulose, microcrystalline Cellulose-sodium carboxymethyl cellulose, unit type MP-01, water 447.5g dissolves HPC-L, PEG6000, saccharin sodium, essence and lemon yellow, be mixed with 5%HPC solution as binding agent, setting spouting liquid is 10g/min, atomisation pressure 0.5MPa, intake 1m ³/ min, 80 ℃ of inlet temperature, by the mode hydrojet of top spray, after having sprayed, in 40-50 ℃ of hot air drying, discharging, crosses 20 mesh sieves, obtains taste masking granule;

5) packing: taste masking granule 4) is packaged as 1g/ bag with Aluminum-plastic composite bag.