CN-121987563-A - New vitamin C injection composition and preparation method thereof

Abstract

The invention discloses a composition and a preparation method of vitamin C injection, wherein the prescription consists of vitamin C, sodium bicarbonate, hydrochloric acid, thioglycerol and water for injection, wherein the dosage of the thioglycerol is 20mg/ml. The vitamin C injection disclosed by the invention has the advantages of simple composition, stable quality, simple and efficient preparation process, low impurity level of a finished product and good safety.

Inventors

• JI XIJING
• LIU JIANHAO
• CHEN YUANDONG
• YANG YIQUN
• DING XUELEI

Assignees

• 江苏润恒制药有限公司

Dates

Publication Date

20260508

Application Date

20241106

Claims (8)

1. 1. The vitamin C injection consists of vitamin C, sodium bicarbonate, hydrochloric acid, thioglycerol and water for injection.
2. 2. The vitamin C injection as claimed in claim 1, wherein the formulation comprises an antioxidant.
3. 3. The vitamin C injection as claimed in claim 2, wherein the antioxidant in the formulation is one of sodium sulfite, sodium bisulfite, sodium metabisulfite, sodium thiosulfate, dibutylphenol, and thioglycerol.
4. 4. A vitamin C injection as claimed in claim 3, wherein the antioxidant in the formulation is thioglycerol.
5. 5. The vitamin C injection according to claim 4, wherein the dosage of the antioxidant in the prescription is 1-50 mg/ml.
6. 6. The vitamin C injection according to claim 5, wherein the dosage of the antioxidant in the prescription is optimized to be 10-30 mg/ml.
7. 7. The vitamin C injection as claimed in claim 6, wherein the amount of antioxidant in the formulation is further optimized to 20mg/ml.
8. 8. The vitamin C injection as claimed in claim 1, wherein the preparation method comprises the steps of adding 80% of water for injection (cooled to below 25 ℃) into a movable tank, adding sodium bicarbonate, stirring to dissolve, introducing nitrogen gas under the liquid surface for 10min, adding vitamin C, stirring to dissolve, continuously introducing nitrogen gas under the liquid surface, measuring pH, adjusting pH to 6.5 (range: 6.4-6.6) by using sodium bicarbonate solution/hydrochloric acid solution, performing nitrogen gas on the liquid surface, adding thioglycerol, stirring for 5min, continuously introducing nitrogen gas on the liquid surface, and supplementing the nitrogen-filled water for injection to the full amount.

Description

New vitamin C injection composition and preparation method thereof Technical Field The invention relates to the field of pharmaceutical preparations, in particular to a composition of a novel vitamin C injection and a preparation method thereof. Background Vitamin C is a water-soluble vitamin, and is chemically named as L- (+) -threose type 2,3,4,5, 6-pentahydroxy-2-hexenoic acid-4-lactone, and also named as L-ascorbic acid, and has a molecular formula of C6H8O6 and a molecular weight of 176.12. The structural formula is shown in figure 1. Vitamin C is a monoclinic crystal, usually in the form of a tablet or sometimes in the form of a needle, odorless, tasteless, acid-soluble in water and strongly reducing. Is involved in complex metabolic processes of organism, can promote growth and enhance resistance to diseases, and can be used as nutritional supplement. The vitamin C injection has the main indications of (1) enhancing organism resistance, being used for preventing and treating various acute and chronic infectious diseases or other diseases, (2) being used for the auxiliary treatment of the post-illness recovery period, the wound healing period and the allergic diseases, and (3) being used for preventing and treating scurvy. Vitamin C is a water-soluble vitamin essential to the human body and plays an important role in various physiological processes as an antioxidant and a cofactor for various enzymes. Most vertebrates can synthesize vitamin C by themselves, but human beings can only acquire vitamin C from diet due to the inactivation mutation of the synthetase gene, and vitamin C is mainly absorbed in the upper section of small intestine and enters the blood circulation through active transportation so as to be utilized by organisms. Since then, it has been found that it is widely used as an adjuvant for the treatment of vitamin C deficiency and other diseases. The existing vitamin C preparations mainly comprise chewable tablets, effervescent tablets, injection, suppositories and the like. According to patent CN 102247317A, vitamin C injection is prepared from vitamin C, sodium bicarbonate, sodium bisulphite, cysteine hydrochloride and edetate disodium. The vitamin C injection is produced through the process of adding CO 2 into water for injection in the weight and volume ratio of 70% to saturate, adding cysteine hydrochloride, sodium bisulphite and edetate disodium dissolved in warm water, stirring to dissolve, adding vitamin C, stirring to add sodium bicarbonate slowly to full amount, dissolving, filtering, packing and sterilizing at 121 deg.c for 8 min. For example, the vitamin C injection is prepared from vitamin C, sodium bicarbonate, sodium metabisulfite, L-cysteine, disodium ethylenediamine tetraacetate and sodium diethyldithiocarbamate according to the prescription of the patent CN 102885771A. The production process of the vitamin C injection comprises the steps of sequentially adding disodium ethylenediamine tetraacetate, sodium metabisulfite and L-cysteine into injection water saturated by nitrogen, adding vitamin C after complete dissolution, stirring to enable the vitamin C to be completely dissolved, then adding sodium bicarbonate, adding sodium diethyl dithiocarbamic acid, finally adding injection water to fix volume to obtain a mixed solution, adding active carbon for injection, stirring for 5-20 min, filtering for decarburization, finely filtering the filtered filtrate by an ultrafiltration membrane with the pore diameter of 0.22nm, continuously introducing nitrogen gas into the finely filtered filtrate, and sterilizing after filling under ventilation conditions to obtain the high-concentration vitamin C injection. In the existing prescription, in order to stabilize the product quality, an antioxidant is added into the prescription, and oxygen control is performed in the processes of liquid preparation and encapsulation. The antioxidants in the two prescriptions are sodium bisulphite and sodium metabisulfite respectively, and disodium edentate is used as an antioxidant synergist, so that the sodium bisulphite has the risk of stimulating skin mucosa, the sodium metabisulfite has the possibility of sensitization, and the application of disodium edentate can reduce the blood calcium concentration of a human body. Based on safety consideration, the inventor provides an antioxidant with high safety, and the safety is considered while the effectiveness of the preparation is ensured. Disclosure of Invention The invention aims at providing a safe and effective antioxidant auxiliary material. The invention also provides a prescription of the injection and a specific process preparation method, and the process is simple and efficient and is easy for large-scale production. The invention aims at realizing the technical scheme that the vitamin C injection comprises vitamin C, sodium bicarbonate, hydrochloric acid, thioglycerol and water for injection. The vitamin C injection is characterized in th