CN117695236A - Ascorbyl palmitate tablet and its production process - Google Patents
Ascorbyl palmitate tablet and its production process Download PDFInfo
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- CN117695236A CN117695236A CN202311719847.0A CN202311719847A CN117695236A CN 117695236 A CN117695236 A CN 117695236A CN 202311719847 A CN202311719847 A CN 202311719847A CN 117695236 A CN117695236 A CN 117695236A
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- Prior art keywords
- ascorbyl palmitate
- parts
- tablet
- tablets
- ethanol
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- Pending
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- 239000011786 L-ascorbyl-6-palmitate Substances 0.000 title claims abstract description 64
- QAQJMLQRFWZOBN-LAUBAEHRSA-N L-ascorbyl-6-palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](O)[C@H]1OC(=O)C(O)=C1O QAQJMLQRFWZOBN-LAUBAEHRSA-N 0.000 title claims abstract description 64
- 235000010385 ascorbyl palmitate Nutrition 0.000 title claims abstract description 64
- 238000004519 manufacturing process Methods 0.000 title abstract description 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 40
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 38
- 239000004375 Dextrin Substances 0.000 claims abstract description 19
- 229920001353 Dextrin Polymers 0.000 claims abstract description 19
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims abstract description 19
- 235000019425 dextrin Nutrition 0.000 claims abstract description 19
- 235000019359 magnesium stearate Nutrition 0.000 claims abstract description 19
- 235000002906 tartaric acid Nutrition 0.000 claims abstract description 19
- 239000011975 tartaric acid Substances 0.000 claims abstract description 19
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims abstract description 15
- 239000008101 lactose Substances 0.000 claims abstract description 15
- 239000002994 raw material Substances 0.000 claims description 14
- 238000005303 weighing Methods 0.000 claims description 7
- 238000000034 method Methods 0.000 claims description 2
- 230000008569 process Effects 0.000 claims description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 abstract description 42
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 abstract description 15
- 229930003268 Vitamin C Natural products 0.000 abstract description 15
- 239000011718 vitamin C Substances 0.000 abstract description 15
- 235000019154 vitamin C Nutrition 0.000 abstract description 15
- 235000010323 ascorbic acid Nutrition 0.000 abstract description 6
- 239000011668 ascorbic acid Substances 0.000 abstract description 6
- 229960005070 ascorbic acid Drugs 0.000 abstract description 6
- 238000004090 dissolution Methods 0.000 abstract description 3
- 230000000694 effects Effects 0.000 abstract description 3
- 230000003647 oxidation Effects 0.000 abstract description 3
- 238000007254 oxidation reaction Methods 0.000 abstract description 3
- 239000002552 dosage form Substances 0.000 abstract description 2
- 230000001590 oxidative effect Effects 0.000 abstract description 2
- 239000000825 pharmaceutical preparation Substances 0.000 abstract description 2
- 239000011248 coating agent Substances 0.000 abstract 1
- 238000000576 coating method Methods 0.000 abstract 1
- 230000000052 comparative effect Effects 0.000 description 5
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 4
- 229910052791 calcium Inorganic materials 0.000 description 4
- 239000011575 calcium Substances 0.000 description 4
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 4
- 239000000203 mixture Substances 0.000 description 4
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 3
- 239000003963 antioxidant agent Substances 0.000 description 3
- 230000003078 antioxidant effect Effects 0.000 description 3
- 235000006708 antioxidants Nutrition 0.000 description 3
- 210000001519 tissue Anatomy 0.000 description 3
- 230000004888 barrier function Effects 0.000 description 2
- 210000000944 nerve tissue Anatomy 0.000 description 2
- 210000000056 organ Anatomy 0.000 description 2
- 230000035790 physiological processes and functions Effects 0.000 description 2
- 235000021314 Palmitic acid Nutrition 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000032683 aging Effects 0.000 description 1
- 239000010775 animal oil Substances 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 235000015872 dietary supplement Nutrition 0.000 description 1
- 239000003925 fat Substances 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000004519 grease Substances 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 230000036039 immunity Effects 0.000 description 1
- 125000003473 lipid group Chemical group 0.000 description 1
- 238000002844 melting Methods 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- 230000035764 nutrition Effects 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 235000019198 oils Nutrition 0.000 description 1
- 235000014593 oils and fats Nutrition 0.000 description 1
- 125000001312 palmitoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 230000002000 scavenging effect Effects 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- A61K31/375—Ascorbic acid, i.e. vitamin C; Salts thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/06—Free radical scavengers or antioxidants
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Toxicology (AREA)
- Biochemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses an ascorbyl palmitate tablet and a production process thereof, belonging to the technical field of pharmaceutical preparations. The technical proposal is as follows: the coating comprises the following components in parts by weight: 12-16 parts of ascorbyl palmitate, 1-3 parts of dextrin, 1-3 parts of lactose, 0.5-2 parts of 50% ethanol, 0.02-0.04 part of tartaric acid and 0.03-0.08 part of magnesium stearate. The dissolution rate and bioavailability of the ascorbyl palmitate tablets prepared by the invention are much better than those of other dosage forms prepared by vitamin C; since ascorbyl palmitate itself has a good oxidation resistance, the quality of the ascorbyl palmitate tablets is very stable, and the effect of light, air, moisture and the like on the ascorbyl palmitate tablets in production or in transportation is small. Ascorbyl palmitate tablets are capable of providing lipid-soluble protection against oxidative free radicals to areas of tissue not reached by ascorbic acid.
Description
Technical Field
The invention relates to the technical field of pharmaceutical preparations, in particular to an ascorbyl palmitate tablet and a production process thereof.
Background
Ascorbyl Palmitate (AP) is white or yellowish powdery crystal esterified by ascorbic acid (vitamin C) and palmitic acid (C16:0), has slight orange smell, has a melting point of 107-117 ℃, is extremely insoluble in water and is easily dissolved in ethanol, diethyl ether and animal and vegetable oil, and has extremely stable properties in a concentrated or crystalline state, and is commonly used as an oil antioxidant.
Vitamin C, also known as ascorbic acid, is used in foods as an antioxidant and a nutritional supplement, but ascorbic acid is water-soluble and is poorly effective as an antioxidant in oils and fats. The ascorbyl palmitate which is a derivative produced by esterifying water-soluble ascorbic acid and palmitoyl is soluble in grease, and has not only all physiological functions of vitamin C, but also many characteristics which are not possessed by vitamin C. Such as ascorbyl palmitate, can penetrate biological barriers to reach tissues and organs not accessible to vitamin C, and are good carriers for delivery of vitamin C to nerve tissues. The ascorbyl palmitate can protect lipid parts such as cell membranes from being oxidized, has the nutrition and health care functions of scavenging free radicals, resisting oxidation, resisting aging and the like, and is far superior to vitamin C. Ascorbyl palmitate has the following structural formula:
therefore, there is a need to develop an ascorbyl palmitate tablet to solve the problem that the existing vitamin C tablet is not fat soluble.
Disclosure of Invention
The invention aims to solve the technical problems that: overcomes the defects of the prior art, and provides an ascorbyl palmitate tablet and a production process thereof, wherein the dissolution and bioavailability of the prepared ascorbyl palmitate tablet are much better than those of other dosage forms prepared from vitamin C.
The technical scheme of the invention is as follows:
in one aspect, the invention provides an ascorbyl palmitate tablet, which comprises the following components in parts by weight: 12-16 parts of ascorbyl palmitate, 1-3 parts of dextrin, 1-3 parts of lactose, 0.5-2 parts of 50% ethanol, 0.02-0.04 part of tartaric acid and 0.03-0.08 part of magnesium stearate.
Preferably, the composition comprises the following components in parts by weight: 12 parts of ascorbyl palmitate, 1.5 parts of dextrin, 1 part of lactose, 1 part of 50% ethanol, 0.025 part of tartaric acid and 0.06 part of magnesium stearate.
Preferably, the composition comprises the following components in parts by weight: 13 parts of ascorbyl palmitate, 2 parts of dextrin, 1 part of lactose, 1 part of 50% ethanol, 0.025 part of tartaric acid and 0.06 part of magnesium stearate.
Preferably, the composition comprises the following components in parts by weight: 16 parts of ascorbyl palmitate, 3 parts of dextrin, 2 parts of lactose, 1 part of 50% ethanol, 0.04 part of tartaric acid and 0.08 part of magnesium stearate.
In another aspect, the invention provides a process for producing the ascorbyl palmitate tablets, which comprises the following steps:
s1, weighing all the components;
s2, uniformly mixing the components to obtain a mixed raw material;
and S3, tabletting the mixed raw materials by a tablet press to obtain the ascorbyl palmitate tablets.
Compared with the prior art, the invention has the following beneficial effects:
1. the dissolution rate and bioavailability of the ascorbyl palmitate tablet prepared by the invention are much better than those of other formulations prepared by vitamin C. Since ascorbyl palmitate itself has a good oxidation resistance, the quality of the ascorbyl palmitate tablets is very stable, and the effect of light, air, moisture and the like on the ascorbyl palmitate tablets in production or in transportation is small. Ascorbyl palmitate tablets are capable of providing lipid-soluble protection against oxidative free radicals to areas of tissue not reached by ascorbic acid.
2. The ascorbyl palmitate tablet prepared by the invention not only has all physiological functions of vitamin C, but also has the characteristics that many vitamin C does not have, such as that the ascorbyl palmitate can penetrate biological barriers, so that tissues and organs which cannot be reached by the vitamin C are reached, the ascorbyl palmitate tablet is a good carrier for conveying the vitamin C to nerve tissues, the absorption of components is promoted, and the immunity of a human body is enhanced.
Detailed Description
In order to make the technical solution of the present invention better understood by those skilled in the art, the technical solution of the present invention will be clearly and completely described in the following in conjunction with the embodiments of the present invention.
Example 1
The production process of the ascorbyl palmitate tablet of the embodiment comprises the following steps:
s1, respectively weighing 12 parts of ascorbyl palmitate, 1.5 parts of dextrin, 1 part of lactose, 1 part of 50% ethanol, 0.025 part of tartaric acid and 0.06 part of magnesium stearate according to parts by weight for subsequent use;
s2, uniformly mixing 12 parts of ascorbyl palmitate, 1.5 parts of dextrin, 1 part of lactose, 1 part of 50% ethanol, 0.025 part of tartaric acid and 0.06 part of magnesium stearate to obtain a mixed raw material;
and S3, tabletting the mixed raw materials by a tablet press to obtain the ascorbyl palmitate tablets.
Example 2
The production process of the ascorbyl palmitate tablet of the embodiment comprises the following steps:
s1, respectively weighing 13 parts of ascorbyl palmitate, 2 parts of dextrin, 1 part of lactose, 1 part of 50% ethanol, 0.025 part of tartaric acid and 0.06 part of magnesium stearate according to parts by weight for subsequent use;
s2, uniformly mixing 13 parts of ascorbyl palmitate, 2 parts of dextrin, 1 part of lactose, 1 part of 50% ethanol, 0.025 part of tartaric acid and 0.06 part of magnesium stearate to obtain a mixed raw material;
and S3, tabletting the mixed raw materials by a tablet press to obtain the ascorbyl palmitate tablets.
Example 3
The production process of the ascorbyl palmitate tablet of the embodiment comprises the following steps:
s1, respectively weighing 16 parts of ascorbyl palmitate, 3 parts of dextrin, 2 parts of lactose, 1 part of 50% ethanol, 0.04 part of tartaric acid and 0.08 part of magnesium stearate according to parts by weight for subsequent use;
s2, uniformly mixing 16 parts of ascorbyl palmitate, 3 parts of dextrin, 2 parts of lactose, 1 part of 50% ethanol, 0.04 part of tartaric acid and 0.08 part of magnesium stearate to obtain a mixed raw material;
and S3, tabletting the mixed raw materials by a tablet press to obtain the ascorbyl palmitate tablets.
Comparative example 1
The production process of the ascorbyl palmitate tablet of the comparative example comprises the following steps:
s1, respectively weighing 20 parts of ascorbyl palmitate, 1.5 parts of dextrin, 1 part of calcium hydrophosphate, 1 part of 50% ethanol, 0.025 part of tartaric acid and 0.06 part of magnesium stearate according to parts by weight for subsequent use;
s2, uniformly mixing 20 parts of ascorbyl palmitate, 1.5 parts of dextrin, 1 part of calcium hydrophosphate, 1 part of 50% ethanol, 0.025 part of tartaric acid and 0.06 part of magnesium stearate to obtain a mixed raw material;
s3, tabletting the mixed raw materials by a tablet press, wherein the tablet is not easy to form.
Comparative example 2
The production process of the ascorbyl palmitate tablet of the comparative example comprises the following steps:
s1, respectively weighing 1 part of ascorbyl palmitate, 1.5 parts of dextrin, 1 part of calcium hydrophosphate, 1 part of 50% ethanol, 0.025 part of tartaric acid and 0.06 part of magnesium stearate according to parts by weight for later use;
s2, uniformly mixing 1 part of ascorbyl palmitate, 1.5 parts of dextrin, 1 part of calcium hydrophosphate, 1 part of 50% ethanol, 0.025 part of tartaric acid and 0.06 part of magnesium stearate to obtain a mixed raw material;
and S3, tabletting the mixed raw materials by a tablet press to obtain the ascorbyl palmitate tablets.
However, the tablet of comparative example 2 had too little ascorbyl palmitate to achieve the effect.
Claims (5)
1. The ascorbyl palmitate tablet is characterized by comprising the following components in parts by weight: 12-16 parts of ascorbyl palmitate, 1-3 parts of dextrin, 1-3 parts of lactose, 0.5-2 parts of 50% ethanol, 0.02-0.04 part of tartaric acid and 0.03-0.08 part of magnesium stearate.
2. The ascorbyl palmitate tablet according to claim 1, comprising the following components in parts by weight: 12 parts of ascorbyl palmitate, 1.5 parts of dextrin, 1 part of lactose, 1 part of 50% ethanol, 0.025 part of tartaric acid and 0.06 part of magnesium stearate.
3. The ascorbyl palmitate tablet according to claim 1, comprising the following components in parts by weight: 13 parts of ascorbyl palmitate, 2 parts of dextrin, 1 part of lactose, 1 part of 50% ethanol, 0.025 part of tartaric acid and 0.06 part of magnesium stearate.
4. The ascorbyl palmitate tablet according to claim 1, comprising the following components in parts by weight: 16 parts of ascorbyl palmitate, 3 parts of dextrin, 2 parts of lactose, 1 part of 50% ethanol, 0.04 part of tartaric acid and 0.08 part of magnesium stearate.
5. The process for producing ascorbyl palmitate tablets according to any of claims 1-4, comprising the steps of:
s1, weighing all the components;
s2, uniformly mixing the components to obtain a mixed raw material;
and S3, tabletting the mixed raw materials by a tablet press to obtain the ascorbyl palmitate tablets.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202311719847.0A CN117695236A (en) | 2023-12-14 | 2023-12-14 | Ascorbyl palmitate tablet and its production process |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202311719847.0A CN117695236A (en) | 2023-12-14 | 2023-12-14 | Ascorbyl palmitate tablet and its production process |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN117695236A true CN117695236A (en) | 2024-03-15 |
Family
ID=90156489
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202311719847.0A Pending CN117695236A (en) | 2023-12-14 | 2023-12-14 | Ascorbyl palmitate tablet and its production process |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN117695236A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN120514678A (en) * | 2025-07-23 | 2025-08-22 | 烟台泰燊生物技术有限公司 | A selenized carrageenan vitamin complex and its preparation method and application |
-
2023
- 2023-12-14 CN CN202311719847.0A patent/CN117695236A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN120514678A (en) * | 2025-07-23 | 2025-08-22 | 烟台泰燊生物技术有限公司 | A selenized carrageenan vitamin complex and its preparation method and application |
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