CN117323308A - Vitamin C sodium capsule and preparation method thereof - Google Patents

Vitamin C sodium capsule and preparation method thereof Download PDF

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Publication number
CN117323308A
CN117323308A CN202311519810.3A CN202311519810A CN117323308A CN 117323308 A CN117323308 A CN 117323308A CN 202311519810 A CN202311519810 A CN 202311519810A CN 117323308 A CN117323308 A CN 117323308A
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China
Prior art keywords
sodium
vitamin
solution
preparing
capsule
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CN202311519810.3A
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Chinese (zh)
Inventor
张恒
张戈
张丹
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Zhongjia Biotechnology Hubei Province Co ltd
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Zhongjia Biotechnology Hubei Province Co ltd
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Priority to CN202311519810.3A priority Critical patent/CN117323308A/en
Publication of CN117323308A publication Critical patent/CN117323308A/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
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/24Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005Wall or coating material
    • A61K9/5021Organic macromolecular compounds
    • A61K9/5036Polysaccharides, e.g. gums, alginate; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5089Processes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/02Nutrients, e.g. vitamins, minerals

Abstract

The invention provides a vitamin C sodium capsule and a preparation method thereof, and relates to the technical field of vitamin C sodium capsules. A preparation method of a vitamin C sodium capsule comprises the steps of S1, preparing lecithin solution; s2, putting the sodium ascorbate and tween-80 into lecithin solution, mixing, and carrying out high-speed shearing and stirring to obtain core material solution; s3, preparing chitosan solution; s4, preparing maltodextrin solution; s5, preparing microcapsule emulsion; s6, spray drying the microcapsule emulsion by using a spray dryer to obtain the vitamin C sodium microcapsule. According to the vitamin C sodium capsule and the preparation method thereof, chitosan and maltodextrin are used as composite wall materials of the vitamin C sodium microcapsule, lecithin and tween-80 are selected to prepare a composite emulsifier, spray drying process conditions are optimized, the prepared vitamin C sodium capsule has high embedding rate and retention rate, and meanwhile, the moisture content in the vitamin C sodium microcapsule is low, so that the vitamin C sodium capsule has stable performance, and the shelf life of a product is prolonged.

Description

Vitamin C sodium capsule and preparation method thereof
Technical Field
The invention relates to the technical field of sodium vitamin C capsules, in particular to a sodium vitamin C capsule and a preparation method thereof.
Background
Sodium ascorbate (L-AscorbicAcidSodiumSalt) is a vitamin C enhancer widely used at home and abroad. Vitamin C has been replaced gradually, but besides the United states, italy and Switzerland, no sodium ascorbate preparation is available in China for people to use as a medicine. Vitamin C is a clinical basic common medicine and is widely applied to the prevention and treatment of various diseases. Because vitamin C has larger acidity (the pH value of 4% solution is 2.4), clinical symptoms such as gastric acid secretion increase are not suitable for long-term use, and the vitamin C is used with some medicines for treating ulcers at present; in addition, many drugs cannot be used together with acidic vitamin C. The existing clinical application of vitamin C has the disadvantages of increased indication, increased dosage and long service life, ensures safe administration for expanding the application range of the vitamin C, and is urgently needed to develop a vitamin C sodium capsule with a pH value close to neutral so as to replace the oral preparation of the vitamin C to be applied clinically.
Aiming at the problems, the inventor discloses an invention patent with application number 200310111592.6 and the invention name of vitamin C sodium capsule, and discloses a vitamin C sodium capsule which has stable product performance, good moisture retention, nearly neutral PH value and wide application range and can replace an oral preparation of vitamin C in clinical application. However, in the subsequent production process, the vitamin C sodium capsule and the preparation process thereof cannot ensure the stability of the performance for a long time, and the shelf life of the product cannot reach the expectancy. In order to solve the problem, the present inventors provide a sodium vitamin C capsule and a preparation method thereof.
Disclosure of Invention
Aiming at the technical problems that the existing vitamin C sodium capsule cannot guarantee the stability of the performance for a long time and the shelf life of the product cannot reach the expected, the invention provides the vitamin C sodium capsule and the preparation method thereof, wherein chitosan and maltodextrin are used as the composite wall material of the vitamin C sodium microcapsule, lecithin and tween-80 are selected to prepare a composite emulsifier, the spray drying process condition is optimized, the prepared vitamin C sodium capsule has higher embedding rate and retention rate, and meanwhile, the moisture content in the vitamin C sodium microcapsule is low, so that the vitamin C sodium capsule is favorable for preserving the product, the performance of the vitamin C sodium capsule is stable, and the shelf life of the product is prolonged.
Therefore, the technical scheme of the invention is that the preparation method of the vitamin C sodium capsule comprises the following specific steps:
s1, preparing a lecithin solution, and adding lecithin into a buffer solution to prepare the lecithin solution;
s2, preparing a core material solution, putting sodium ascorbate and tween-80 into a lecithin solution, mixing, and carrying out high-speed shearing and stirring by a high-speed emulsifying and dispersing machine to obtain the core material solution;
s3, preparing a chitosan solution, and preparing the chitosan solution in a chitosan buffer solution;
s4, preparing a maltodextrin solution, and adding maltodextrin into the buffer solution to prepare the maltodextrin solution;
s5, preparing microcapsule emulsion, namely adding chitosan solution into core material solution while stirring, adding maltodextrin solution while stirring, performing high-speed shearing and stirring by using a high-speed emulsifying and dispersing machine, and performing high-pressure homogenization by using a homogenizer to obtain microcapsule emulsion;
s6, spray drying the microcapsule emulsion by using a spray dryer to obtain the vitamin C sodium microcapsule.
Preferably, the buffer is a solution of sodium acetate-acetic acid at a concentration of 0.1mo/L and a pH of 3.0.
Preferably, the mass ratio of lecithin to tween-80 is 2:1.
Preferably, when preparing the core material solution, the high-speed emulsifying and dispersing machine is set to 10000-15000r/min, and the working time is 3-5min.
Preferably, in preparing the microcapsule emulsion, a high-speed emulsifying disperser is arranged as follows
10000-15000r/min, and the working time is 3-5min.
Preferably, when preparing microcapsule emulsion, the homogenizer is set to 35-40Mpa, and the homogenization times are 2-3 times.
Preferably, the air inlet temperature of the spray dryer is 185-190 ℃ and the air outlet temperature is 80-85 ℃.
The vitamin C sodium capsule is prepared by adopting the method and comprises the following raw materials in parts by weight: 6 parts of chitosan, 100 parts of maltodextrin, 65 parts of sodium ascorbate, 12 parts of lecithin and 6 parts of tween-80.
The vitamin C sodium capsule and the preparation method thereof have the beneficial effects that the chitosan and the maltodextrin are used as the composite wall material of the vitamin C sodium microcapsule, so that the vitamin C sodium capsule has good film forming property, good mechanical stability, good biocompatibility and increased strength and compactness of the microcapsule film, and the raw materials are easy to obtain and low in price; the lecithin and the Tween-80 are selected to prepare the composite emulsifier, spray drying process conditions are optimized, the air inlet temperature is 185-190 ℃, and the spray drying method with the air outlet temperature of 80-85 ℃ is adopted, so that the prepared vitamin C sodium capsule has higher embedding rate and retention rate, and meanwhile, the moisture content in the vitamin C sodium microcapsule is low, thereby being beneficial to the preservation of products, ensuring the stability of the performance of the vitamin C sodium capsule and prolonging the shelf life of the products.
Drawings
Fig. 1 is a flow chart of a method for preparing a sodium vitamin C capsule according to the present invention.
Detailed Description
The following description of the embodiments of the present invention will be made clearly and completely with reference to the accompanying drawings, in which it is apparent that the embodiments described are only some embodiments of the present invention, but not all embodiments. All other embodiments, which can be made by those skilled in the art based on the embodiments of the invention without making any inventive effort, are intended to be within the scope of the invention.
As shown in fig. 1, the invention provides a preparation method of a vitamin C sodium capsule, which comprises the following specific steps:
s1, preparing a lecithin solution, and adding lecithin into 0.1mo/L acetic acid-sodium acetate solution with pH of 3.0 to prepare the lecithin solution.
S2, preparing a core material solution, putting the sodium ascorbate and the tween-80 into the lecithin solution, mixing, and carrying out high-speed shearing and stirring by a high-speed emulsifying and dispersing machine to obtain the core material solution. The high-speed emulsifying and dispersing machine is set to 10000-15000r/min, and the working time is 3-5min.
S3, preparing a chitosan solution, and adding chitosan into an acetic acid-sodium acetate solution with the concentration of 0.1mo/L and the pH of 3.0 to prepare the chitosan solution.
S4, preparing a maltodextrin solution, and adding maltodextrin into a 0.1mo/L acetic acid-sodium acetate solution with the pH of 3.0 to prepare the maltodextrin solution.
The invention creatively takes chitosan and maltodextrin as composite wall materials of vitamin C sodium microcapsules, wherein the chitosan is a linear polymer with a similar cellulose structure, is an alkaline polysaccharide existing in nature, is a product of chitosan after deacetylation by a chemical method, has the structural formula of (1, 4) -2-amino-2-deoxidization-beta-glucan, has the characteristics of no toxicity, no smell and easy biodegradation, has good film forming property, good mechanical stability, good biocompatibility, certain excellent performances of antibiosis, tumor resistance and the like, is easy to obtain raw materials, is low in price, and is an ideal microcapsule wall material, and has great application potential in the field of controlled release medicines. Maltodextrin is a product of incomplete hydrolysis of starch, is a polysaccharide which is not sweet and has nutritional value, is not easy to absorb water, has low viscosity and good water solubility, has no surface activity and no emulsifying property, can be used as a filler to increase the strength and the compactness of a microcapsule membrane, and is a microcapsule wall material with higher cost performance.
S5, preparing microcapsule emulsion, adding the chitosan solution into the core material solution while stirring, adding the maltodextrin solution while stirring, performing high-speed shearing and stirring by using a high-speed emulsifying and dispersing machine, and performing high-pressure homogenization by using a homogenizer to obtain the microcapsule emulsion. The high-speed emulsifying and dispersing machine is set to 10000-15000r/min, and the working time is 3-5min. The homogenizer is set at 35-40Mpa, and the homogenizing times are 2-3 times.
When preparing microcapsule emulsion, it is often necessary to add an emulsifier to obtain emulsion with higher stability and better dispersion of core material; the emulsion has poor stability, and is unfavorable for the emulsion to be sprayed into small liquid drops and formed into a film by an atomizer, so that the core material cannot be fully embedded. The vitamin C sodium microcapsule emulsion belongs to oil-in-water solution, and oil-in-water type emulsifier should be selected to obtain emulsion with good stability, and the emulsifier has hydrophilic-lipophilic balance (HLB) of 7-18, and is suitable for use as oil-in-water (O/W) emulsifier.
The lecithin is a natural surfactant, has surface activity, and physiological activities of deferring senility, preventing cardiovascular and cerebrovascular diseases, strengthening brain and developing intelligence, preventing senile dementia, protecting liver and the like, and is widely used in various fields; tween is a commonly used food emulsifier, and because polysorbate molecules have more hydrophilic groups-polyoxyethylene groups, the polysorbate molecules have strong hydrophilicity, and the tween-80 is often used as an oil-in-water (O/W) type emulsifier, so that the tween-80 has stronger emulsifying property in the tween series.
According to the invention, lecithin and tween-80 are selected to prepare the composite emulsifier, and the inventor researches that when the mass ratio of the lecithin to the tween-80 is 2:1, namely the HLB value is 9.7, the emulsion with chitosan and maltodextrin as wall materials has the best emulsion stability, so that a stable emulsion can be obtained, and therefore, the mass ratio of the lecithin to the tween-80 in the composite emulsifier is 2:1.
In order to ensure that the vitamin C sodium microcapsule product has higher embedding rate and retention rate, and simultaneously considers the problems of the carrying capacity, the production cost and the like of the vitamin C sodium, the invention adopts the chitosan with the content of 0.6 percent, the maltodextrin with the content of 10 percent, the adding amount of the vitamin C sodium with the content of 6.5 percent and the using amount of the composite emulsifier with the content of 1.8 percent.
S6, spray drying the microcapsule emulsion by using a spray dryer to obtain the vitamin C sodium microcapsule.
In order to obtain a microcapsule product of good quality, it is also important to control the process conditions of spray drying. The temperature of the air inlet of the spray drying directly relates to the drying rate and the final moisture content of the microcapsule, and simultaneously influences the particle structure, hygroscopicity and the stability of thermosensitive components of the microcapsule, and the temperature of the air outlet of the spray drying influences the speed-down drying time, the microstructure of the surface, the flowability of the microcapsule and the like. The invention optimizes the spray drying process parameters.
The microcapsule spray drying process comprises two stages of constant-speed drying and deceleration drying, wherein the temperature of an air inlet of a spray drying tower influences the constant-speed drying process, and the temperature of an air outlet influences the deceleration drying process. After the spray drying process is optimized by the inventor, the process conditions of spray drying adopt an air inlet temperature of 185-190 ℃ and an air outlet temperature of 80-85 ℃. The embedding rate of the sodium ascorbate microcapsule prepared by the spray drying method can reach 91.15%, and the retention rate of sodium ascorbate can reach 94.05%.
The water content of the vitamin C sodium microcapsule prepared by the spray drying method is lower than 2.30%, and the water content of the vitamin C sodium microcapsule is low, so that the vitamin C sodium microcapsule is favorable for preserving products.
The scanning electron microscope image of the internal structure of the vitamin C sodium microcapsule prepared by the spray drying method shows that the particle size and the morphology of the vitamin C sodium microcapsule are uniform, the surface structure is complete, no crack, hole and fracture phenomenon is seen, the internal structure of the microcapsule is good, and the microcapsule has good embedding effect.
The invention provides a vitamin C sodium capsule which is prepared by adopting the preparation method of the vitamin C sodium capsule, and comprises the following raw materials in parts by weight: 6 parts of chitosan, 100 parts of maltodextrin, 65 parts of sodium ascorbate, 12 parts of lecithin and 6 parts of tween-80.
According to the vitamin C sodium capsule and the preparation method thereof, chitosan and maltodextrin are used as composite wall materials of the vitamin C sodium microcapsule, so that the vitamin C sodium capsule has good film forming property, good mechanical stability, good biocompatibility and increased strength and compactness of the microcapsule film, and raw materials are easy to obtain and low in price; the lecithin and the Tween-80 are selected to prepare the composite emulsifier, spray drying process conditions are optimized, the air inlet temperature is 185-190 ℃, and the spray drying method with the air outlet temperature of 80-85 ℃ is adopted, so that the prepared vitamin C sodium capsule has higher embedding rate and retention rate, and meanwhile, the moisture content in the vitamin C sodium microcapsule is low, thereby being beneficial to the preservation of products, ensuring the stability of the performance of the vitamin C sodium capsule and prolonging the shelf life of the products.
Compared with the vitamin C oral preparation, the vitamin C sodium capsule provided by the invention has the advantages of quicker and more sufficient absorption and higher bioavailability. In addition, vitamin C is absorbed from the intestine into the blood circulation by diffusion or sodium ion channels. Vitamin C cannot directly pass through the sodium ion channel and can pass through the sodium ion channel only in the form of a vitamin C sodium compound after being combined with sodium ions, and vitamin C sodium can directly pass through the sodium ion channel, so that the absorption speed of the vitamin C sodium is nearly hundreds of times faster than that of the vitamin C, and the bioavailability is greatly improved.
Under radiation exposure, radiation can trigger oxidative stress reaction to generate active oxygen with strong oxidation effect, and the active oxygen can damage cell membranes and genes and also damage organs such as marrow, intestinal tracts and the like. The vitamin C sodium capsule is a high-efficiency antioxidant, can block free radical reaction, can eliminate active oxygen generated by radiation by reducing the generation of oxidation free radicals, and can reduce the damage of lipid peroxide to skin, organs and the like.
The vitamin C sodium capsule can accelerate the healing of wounds of patients after surgical operations. The treatment group was orally administered 1g of vitamin C sodium capsule per day by double-blind experiment, and the control group was not treated. After one month, the wound healing rate of the treatment group reached 84% and the control group was only 43%. In addition, the wound dehiscence rate is closely related to low plasma ascorbic acid levels. Of 875 post-surgical patients, the plasma ascorbate level was 13.9% for low patient wound dehiscence, whereas the plasma ascorbate level was only 1.7% for normal patient wound dehiscence. The mechanism is as follows: the vitamin C sodium capsule improves secretion and synthesis of collagen, and promotes wound healing.
However, the foregoing description is only illustrative of the present invention and is not intended to limit the scope of the invention, so that the substitution of equivalent elements or equivalent variations and modifications within the scope of the invention are intended to fall within the scope of the claims.

Claims (8)

1. The preparation method of the vitamin C sodium capsule is characterized by comprising the following specific steps:
s1, preparing a lecithin solution, and adding lecithin into a buffer solution to prepare the lecithin solution;
s2, preparing a core material solution, putting sodium ascorbate and tween-80 into a lecithin solution, mixing, and carrying out high-speed shearing and stirring by a high-speed emulsifying and dispersing machine to obtain the core material solution;
s3, preparing a chitosan solution, and preparing the chitosan solution in a chitosan buffer solution;
s4, preparing a maltodextrin solution, and adding maltodextrin into the buffer solution to prepare the maltodextrin solution;
s5, preparing microcapsule emulsion, namely adding chitosan solution into core material solution while stirring, adding maltodextrin solution while stirring, performing high-speed shearing and stirring by using a high-speed emulsifying and dispersing machine, and performing high-pressure homogenization by using a homogenizer to obtain microcapsule emulsion;
s6, spray drying the microcapsule emulsion by using a spray dryer to obtain the vitamin C sodium microcapsule.
2. The method for preparing a sodium ascorbate capsule according to claim 1, wherein the buffer is a solution of sodium acetate-acetate at a concentration of 0.1mo/L and a pH of 3.0.
3. The method for preparing a vitamin C sodium capsule according to claim 2, wherein the mass ratio of lecithin to tween-80 is 2:1.
4. The method for preparing a sodium ascorbate capsule according to claim 3, wherein the high-speed emulsifying and dispersing machine is set to 10000-15000r/min and the working time is 3-5min when preparing the core material solution.
5. The method for preparing a sodium ascorbate capsule according to claim 4, wherein the high-speed emulsifying and dispersing machine is 10000-15000r/min and the working time is 3-5min when preparing microcapsule emulsion.
6. The method of claim 5, wherein the homogenizer is set to 35-40Mpa and the number of homogenization is 2-3.
7. The method for preparing a sodium ascorbate capsule of claim 6, wherein the spray dryer has an inlet air temperature of 185-190 ℃ and an outlet air temperature of 80-85 ℃.
8. A sodium vitamin C capsule prepared by the preparation method of the sodium vitamin C capsule according to claim 7, which is characterized by comprising the following raw materials in parts by weight: 6 parts of chitosan, 100 parts of maltodextrin, 65 parts of sodium ascorbate, 12 parts of lecithin and 6 parts of tween-80.
CN202311519810.3A 2023-11-14 2023-11-14 Vitamin C sodium capsule and preparation method thereof Pending CN117323308A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202311519810.3A CN117323308A (en) 2023-11-14 2023-11-14 Vitamin C sodium capsule and preparation method thereof

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Application Number Priority Date Filing Date Title
CN202311519810.3A CN117323308A (en) 2023-11-14 2023-11-14 Vitamin C sodium capsule and preparation method thereof

Publications (1)

Publication Number Publication Date
CN117323308A true CN117323308A (en) 2024-01-02

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Country Status (1)

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