TPGS-VE
Tocofersolan
CAS: 9002-96-4
Molecular Formula: (C2H4O)nC33H54O5
TPGS-VE - Names and Identifiers
| Name | Tocofersolan |
| Synonyms | TPGS-VE tocofersolan Tocofersolan Tocophersolan tocopherosolan DL-A-TOCOPHEROL POLYETHYLENE GLYCOL SUCCINATE d-alpha-tocopheryl polyethylene glycol succinate DL-ALPHA-TOCOPHEROL POLYETHYLENE GLYCOL SUCCINATE poly(oxy-1,2-ethanediyl),alpha-(4-((3,4-dihydro-2,5,7,8-tetramethyl-2-(4,8,12 2-hydroxyethyl 2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-3,4-dihydro-2H-chromen-6-yl butanedioate 2-ethanediyl),.alpha.-[4-[[3,4-dihydro-2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-2H-1-benzoPoly(oxy-1 alpha-(4-((3,4-dihydro-2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-2h-1-benzopyran-6-yl)oxy)-1,4-dioxobutanol poly(ethylene glycol) succinate |
| CAS | 9002-96-4 |
| InChI | InChI=1/C35H58O6/c1-24(2)12-9-13-25(3)14-10-15-26(4)16-11-20-35(8)21-19-30-29(7)33(27(5)28(6)34(30)41-35)40-32(38)18-17-31(37)39-23-22-36/h24-26,36H,9-23H2,1-8H3 |
TPGS-VE - Physico-chemical Properties
| Molecular Formula | (C2H4O)nC33H54O5 |
| Density | 1.01g/cm3 |
| Melting Point | 34-38°C |
| Boling Point | 662.7°C at 760 mmHg |
| Flash Point | 195.4°C |
| Solubility | H2O: soluble1g/10 mL, clear to faintly turbid, colorless to faintly yellow |
| Vapor Presure | 1.83E-18mmHg at 25°C |
| Appearance | Solid |
| Color | White to Pale Yellow Waxy |
| Storage Condition | 2-8°C |
| Sensitive | Easily absorbing moisture |
| Refractive Index | 1.496 |
| MDL | MFCD00146616 |
TPGS-VE - Risk and Safety
| WGK Germany | 2 |
| RTECS | TR1581200 |
TPGS-VE - Reference
| Reference Show more | 1. Xue Feng, Yuting Chen, Luya Li, Yuqian Zhang, Lantong Zhang & Zhiqing Zhang (2020) Preparation, evaluation and metabolites study in rats of novel amentoflavone-loaded TPGS/soluplus mixed nanomicelles, Drug Delivery, 27:1, 137-150, DOI: 10.1080/10717544.201 2. [IF=6.419] Xue Feng et al."Preparation, evaluation and metabolites study in rats of novel amentoflavone-loaded TPGS/soluplus mixed nanomicelles."Drug Deliv. 2020;27(1):137-150 3. [IF=6.419] Yuting Chen et al."Preparation and antitumor evaluation of hinokiflavone hybrid micelles with mitochondria targeted for lung adenocarcinoma treatment."Drug Deliv. 2020;27(1):565-574 4. [IF=4.213] Zhonghui Xie et al."Rapamycin loaded TPGS-Lecithins-Zein nanoparticles based on core-shell structure for oral drug administration."Int J Pharmaceut. 2019 Sep;568:118529 |
TPGS-VE - Standard
Authoritative Data Verified Data
This product is a mixture of vitamin E succinate and polyethylene glycol, which is mainly composed of monoesterified polyethylene glycol and a small amount of diesterified polyethylene glycol. Containing not less than 25.0% of a-tocopherol (C29H5Q0 2).
Last Update：2024-01-02 23:10:35
TPGS-VE - Trait
Authoritative Data Verified Data
- This product is a white to light yellow waxy solid; Odorless.
- This product is soluble in ethanol and insoluble in n-hexane.
specific rotation
take about 0.9g of this product, weigh it accurately, place it in a test tube with a plug, heat it in a water bath at 60 ° C to melt it, and add 10ml of ethanol to dissolve it, place heating jacket in 1 0~1 0 5 ° C and reflux until completely dissolved, add 2g of sodium hydroxide, reflux for 30 minutes, add 2 drops of phenolphthalein indicator solution while hot, it was titrated with hydrochloric acid solution (1 - 2) until the pink color disappeared, and it was packed. Then it was allowed to cool, heptane (25ml) was added, packed, mixed well, and allowed to stand. Take the upper layer of liquid to the stopper test tube, add water 10ml, plug, shake, static stratification. Add 10ml of potassium ferricyanide solution (2g of potassium ferricyanide is dissolved in 10ml of 0.2mol/l sodium hydroxide solution) to the test tube, shake, and let stand to separate layers, take the heptane layer, dry it with anhydrous sodium sulfate, and determine it according to law (General rule 0621 ) , and shall not be less than 24.0 °.
acid value
take this product about l.O g, precision weighing, add ethanol-ether (1 : 1) mixture. [Add phenolphthalein indicator solution 1.0 before use, with sodium hydroxide titration solution (O. 1 mol/L) titrated to slightly pink] 25ml, and fully dissolved by shaking. With sodium hydroxide titration solution (O .lmol/L) titration, acid value (General 0713) shall not exceed 1.5.
Last Update：2022-01-01 11:26:01
TPGS-VE - Differential diagnosis
Authoritative Data Verified Data
In the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
Last Update：2022-01-01 11:26:01
TPGS-VE - Exam
Authoritative Data Verified Data
water-soluble
take about 20g of this product, heat to melt, add boiling water 80ml, continue to stir, cool to room temperature, and the solution should be clear within 3 hours.
Last Update：2022-01-01 11:26:02
TPGS-VE - Content determination
Authoritative Data Verified Data
measured by gas chromatography (General 0521).
- The chromatographic conditions and system suitability test uses a capillary column with 5% phenyl-95% methyl polysiloxane (or similar polarity) as the stationary liquid; The initial temperature is 250°C, the temperature was raised to 290°C at a rate of 10°C per minute for 6 minutes; The inlet temperature was 280°C; And the detection temperature was 300°C. The number of theoretical plates shall not be less than 5000 calculated by tocopherol, the tailing factor of tocopherol peak shall not exceed 2.0, and the separation degree between a-tocopherol and the peak of internal standard substance shall meet the requirements. Determination of correction factor an appropriate amount of arachidonic acid ethyl ester was taken, dissolved and diluted with isooctane to prepare a solution containing 12mg per 1 ml as an internal standard solution. Another α-tocopherol reference product about 30mg, precision weighing, set to a test tube, add pyridine 2ml and N ,0 bis (trimethylsilyl) containing 1% trimethylsilane 0.5ml of trifluoroacetamide solution was heated in a water bath at 100 ° C. For 10 minutes, and allowed to cool to room temperature. 5ml of internal standard solution was added precisely, and 20ml of isooctane was added thereto. 1W was injected into the gas chromatograph, and the correction factor was calculated.
- determination method: take about 0.15g of this product, weigh it accurately, place it in a test tube with a plug, heat it in a water bath at 60°C to melt it, add vitamin C45mg, and add an appropriate amount of zeolite, add ethanol solution (add phenolphthalein solution per 1L of ethanol solution 0.25ml)20ml, placed in a heating mantle, heated to reflux at 100°C until the sample was completely dissolved, potassium hydroxide 0.25g was added, reflux was continued for 30 minutes, and dilute hydrochloric acid was added dropwise while hot until the pink color disappeared. Cool to room temperature, add water 20ml to wash the inner wall of the test tube, add 5ml of internal standard solution precisely, plug, mix well, and let stand for stratification. Take 3ml of the upper layer solution, put it in a stopper test tube, add 2ml of pyridine and 2.5ml of JV, 0-bis (trimethylsilyl) trifluoroacetamide solution containing 1% of trimethylchlorosilane, and heat it in a water bath at 100°C for 10 min, cool to room temperature, add 12ml isooctane, plug, shake; Take 1u1 injection gas chromatograph, measurement, calculation, obtained.
Last Update：2022-01-01 11:26:03
TPGS-VE - Category
Authoritative Data Verified Data
pharmaceutical excipients, solubilizers and emulsifiers.
Last Update：2022-01-01 11:26:03
TPGS-VE - Storage
Authoritative Data Verified Data
sealed, protected from light.
Last Update：2022-01-01 11:26:03
TPGS-VE - Reference Information
| Introduction | vitamin E polyethylene glycol succinate (TPGS) is a water-soluble derivative of vitamin E, it is formed by reacting the carboxyl group of vitamin E succinate with the hydroxyl group of polyethylene glycol. Because it contains both vitamin E lipophilic group and polyethylene glycol hydrophilic long chain, it has good surfactant properties and water solubility, which can significantly increase the absorption of insoluble drugs in the gastrointestinal tract, increased bioavailability. |
| properties | Since vitamin E polyethylene glycol succinate contains both vitamin E lipophilic group and long hydrophilic chain of polyethylene glycol, therefore, it has good surfactant properties and water solubility, which can significantly increase the absorption of insoluble drugs in the gastrointestinal tract and improve the bioavailability. |
| characteristics | in recent years, many studies have found that TPGS not only can be used as pharmaceutical excipients, but also has many unique characteristics, as absorption enhancers and multidrug resistance reversal agents, TPGS can also be applied to prodrugs, micelles, liposomes, TPGS-copolymer carriers to improve the solubility, permeability and stability of the preparation, so as to achieve slow, controlled release and targeting effect, promote the absorption of drugs. |
| Application | vitamin E polyethylene glycol succinate has been widely used in the study of preparations, as a solubilizer, absorption promoter, emulsifier, plasticizers and carriers for poorly water-soluble or fat-soluble drug delivery systems, such as solid dispersions, carriers for ocular administration, carriers for intranasal administration, and the like. in foreign countries, vitamin E polyethylene glycol succinate has been widely used in the study of preparations, as solubilizers, absorption enhancers, emulsifiers, plasticizers and carriers of water-insoluble or fat-soluble drug delivery systems, examples include solid dispersions, carriers for ocular administration, carriers for intranasal administration, and the like. In recent years, many studies have found that TPGS can be used as pharmaceutical excipients, but also has many unique characteristics, such as absorption enhancers and multidrug resistance reversal agents, TPGS can also be applied to prodrugs, micelles, liposomes, TPGS-copolymer carrier to improve the solubility, permeability and stability of the preparation, so as to achieve slow, controlled release and targeting effect, promote the absorption of drugs. |
| preparation | vitamin E polyethylene glycol succinate (TPGS) is a water-soluble derivative of vitamin E, it is formed by reacting the carboxyl group of vitamin E succinate with the hydroxyl group of polyethylene glycol. weigh 5.6 grams of natural vitamin E succinate with a purity of 90%, 20 grams of polyethylene glycol 600 with a molecular weight of 600, and 0.8 grams of concentrated sulfuric acid with a mass percentage of 98%, put it into a three-necked bottle, the reaction was stirred at 100 ° C. For 2 hours and cooled to room temperature after completion of the reaction. The reaction product was transferred to a round-bottom flask, and 150ml of ethyl acetate was added to the round-bottom flask to obtain a mixture. The mixture was transferred to a separatory funnel, extracted three times with saturated brine, and the organic phase was collected. The organic phase was distilled off to obtain 8.3g of TPGS. The product was 90.1% pure by HPLC, the conversion of vitamin E succinate was 89.2%, and the yield of TPGS was 79.2%. |
| biological activity | Tocofersolan is a synthetic polyethylene glycol derivative of α-tocopherol. |
Last Update：2024-04-09 19:05:15
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