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TPGS/Natrural VE Cas 9002-96-4

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  • Last update:

    2018-07-20 13:40

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    289

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Shanghai LianLu Industrial Co.,Ltd
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lulian(Mr.)  

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Shanghai

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Room 702, Building 46, No.900, Haili Rd, Jinshan, Shanghai 201508, China

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http://www.sh-lianlu.com/ http://www.link-bridge.com/com/lulian/

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Product Details


1.APPLICATIONS of VITAMIN E TPGS

Emulsifier - TPGS has amphiphilc properties and is therefore used as emulsifier for nutraceuticals and pharmaceuticals (Lehr 2005). Emulsifier for injectable formulations


DRUG DELIVERY SYSTEM

· Drug solubilizer – It directly increases the bioavailability and delivery of poorly soluble drugs

· Protects drugs from crystallization Provide Vitamin E or poorly soluble nutraceuticals in liquid dosage form Reduces drug sensitivity on skin and tissues

· Acts as a vehicle in semi-dosage form and also for pulmonary (inhalation) dosage form

· Carrier for wound care and treatment

· A thermal binder in melt granulations / extrusion process


ABSORPTION ENHANCER

ANTIOXIDANT

Vehicle for lipid - based drug delivery - Vitamin E TPGS is an important extension to a range of drug delivery products

Source of natural Vitamin E - used in pharmaceutical formulations as well as dietary supplements Extensively used in solid, topical and ophthalmic dosage forms

AMPHIPHILIC (SURFACE-ACTIVE) PROPERTIES

Vitamin E TPGS is amphiphile, that is it has a dual nature. Part of the molecule exhibits hydrophilicity and the other lipophilicity. General accepted view is that the polyethylene glycol portion serves as the hydrophilic polar head (water soluble), while the tocopherol succinate portion serves as the lipophilic alkyl tail (water insoluble).

STABILITY

Vitamin E TPGS is stable when exposed to oxygen, heat, light, or oxidizing agents. It is unstable to alkali. Vitamin E TPGS is known to be stable excipient with a shelf-life of 4 years when stored in the original unopened container at room temperature. Vitamin E TPGS is stable under the conditions of heat sterilization. Stability data will be available soon.


SAFETY AND TOXICOLOGY

Regarding the safety of Vitamin E TPGS, various studies have been conducted in the last decades. EFSA (European Food Safety Authority) has conducted studies to assess the safety and bioavailability of Vitamin E TPGS for use in food particularly for nutritional / medical purposes. From toxicology studies, an overall no-observed-adverse-effect level (NOAEL) of 1000 mg / kg body weight per day can be derived. Vitamin E TPGS is not genotoxic. Also approved by US-FDA (United States - Food and Drug Administration).

 

Vitamin E TPGS is a non-toxic multi-role excipient used in pharmaceutical and nutraceutical applications. Vitamin E TPGS has been shown to improve the bioavailability of poorly absorbed drugs by acting as an absorption and permeability enhancer. As a water soluble compound, Vitamin E TPGS can be used to dissolve lipophilic and other insoluble ingredients and can also used as an efficient source of natural Vitamin E, both for therapeutic and nutritional purposes.


Vitamin E TPGS is a multi role excipient used in nutraceutical and pharmaceutical applications.

Vitamin E TPGS has shown proven and recognized properties to improve bioavailability of poorly absorbed drugs vitamins micro-nutrients acting as an absorption and permeability enhancer and to developp Self Emulsifying Drug Delivery System (SEEDS) for poorly soluble drugs as an emulsifier. As a water soluble compound, Vitamin E TPGS is also used as an efficient source of natural Vitamin E, both for therapeutic purposes and nutrition. In Addition Vitamin E TPGS has physical properties that make it a relevant plasticizer for innovative technologies in the pharmaceutical industry such as hot melt extrusion.

A lot of pharmaceutical companies have incorporated Vitamin E TPGS mainly in oral dosage forms for years but new delivery applications are being investigated:

• parenteral delivery

• topical delivery

- dermal

- nasal

- pulmonary


Vitamin E TPGS, a water soluble derivative of natural Vitamin E, is a multirole excipient for pharmaceutical drug delivery innovation. Vitamin E TPGS is a non-ionic surfactant used as:

· solubilizer of poorly soluble drugs

· absorption enhancer

· emulsifier

· vehicle for lipid-based drug formulation

· antioxidant

Vitamin E TPGS is also used as an efficient source of natural Vitamin E both for therapeutic and nutrition purposes.


Benefits:

- Enhancement of Bioavailability by increasing solubility of poorly water-soluble APIs and by formulation of Self Emulsifying Drug Delivery System (SEEDS)

- Thermal stability for hot melt extrusion as a versatile plasticizer with solubilizer properties and as Antioxidant for sensitive excipients

 

Track records:

Formulation using TPGS has been developed for commercial drugs :

Two anti HIV drugs, AGENERASE® (Amprenavir) soft gel capsules and oral solution and APTIVUS® (Tripanavir) oral solution

One anti HCV drug, VIEKERA Pack™ (combination of 3 APIs) tablets

 

Vitamin E TPGS

Alpha Tocopheryl Polyethylene Glycol Succinate (TPGS) is widely used as a water-soluble vitamin E formulation. TPGS is synthesized from the lipid-soluble antioxidant, α-tocopherol (vitamin E) by grafting to a polyethylene glycol (PEG) oligomer through a succinate diester linker. Vitamin-E TPGS is amphiphile that is it has a dual nature. Vitamin-E TPGS is prepared from two different sources - Natural and synthetic vitamin E.

 

Applications

· Emulsifier

· Drug delivery system

· Dietary supplements

· Food and beverages

· Personal care

· Cosmetics

· Animal nutrition

 

D-α-Tocopheryl polyethylene glycol 1000 succinate (simply TPGS or Vitamin E TPGS) is formed by the esterification of Vitamin E succinate with polyethylene glycol 1000. As novel nonionic surfactant, it exhibits amphipathic properties and can form stable micelles in aqueous vehicles at concentration as low as 0.02 wt%. It has been widely investigated for its emulsifying, dispersing, gelling, and solubilizing effects on poorly water-soluble drugs. It can also act as a P-glycoprotein (P-gp) inhibitor and has been served as an excipient for overcoming multidrug resistance (MDR) and for increasing the oral bioavailability of many anticancer drugs. Since TPGS has been approved by FDA as a safe pharmaceutic adjuvant, many TPGS-based drug delivery systems (DDS) have been developed. In this review, we discuss TPGS properties as a P-gp inhibitor, solubilizer/absorption and permeation enhancer in drug delivery and TPGS-related formulations such as nanocrystals, nanosuspensions, tablets/solid dispersions, adjuvant in vaccine systems, nutrition supplement, plasticizer of film, anticancer reagent and so on. This review will greatly impact and bring out new insights in the use of TPGS in DDS.


Uses:

· Pharmaceutical – it greatly enhances the absorption, bioavailability and effectiveness of pharmaceutical ingredients (APIs).

· Dietary Supplements – it is used to formulate supplements, especially those created to improve absorption of vitamin E and other lipophilic nutrients and nutraceuticals.

· Food and Beverage – it can be employed to fortify foods and beverages, sports drinks, water and juices.

· Personal Care – it serves as an ethanol free, hypoallergenic, non-irritating emulsifier/excipient in personal care and cosmetic applications.

· Animal Nutrition Products – it supplies a highly absorbable and bioavailable vitamin E for animals that do not efficiently absorb traditional forms of vitamin E.


· Emulsifier/ Solubilizer of poorly soluble drugs

· Vehicle for lipid-based drug formulation

· Dietary supplements/ Animal nutrition

· Food and beverages

· Personal care/ Antioxidant

· Cosmetics

· Absorption enhancer


2.TPGS / Vitamin E Polyethylene Glycol Succinate【USP39】

CAS#:  9002-96-4   

Molecular formula:   C33H54O5.(C2H4O)n

Structural formula:

 

Description

D -α-tocopheryl polyethylene glycol 1000 succinate is a water-soluble derivative of natural-source vitamin E. Off-white or yellowish waxy solid, almost tasteless, soluble in water and most of the polar organic solvents such as ethanol. It is amphipathic, miscible with water, and forms a variety of liquid crystalline phases in water. The excipient melts at 37–41℃ and is heat stable at temperatures ≤200℃.

 

Function

1) As a solubilizer:

TPGS increases the permeability of amprenavir by inhibiting efflux. Amprenavir is a new HIV protease inhibitor. At present, Amprenavir products  which use TPGS as an excipient are currently available in the United States, such as Agenerase ™ oral liquid and capsules. It has also been reported that micellar solubilization of TPGS increases estradiol solubility and permeation. After combined with cyclosporine A, TPGS increased the solubility of cyclosporine A, thereby enhancing the cyclosporine A bioavailability.

2) Apply to solid dispersion technology:

Water-soluble excipient such as lactose, mannitol, hydroxypropyl methyl cellulose and the like are added into the TPGS drug mixture to accelerate drug release. Adding hydrophobic materials, such as wax, can slow down dissolution. In addition, an expansiveness excipient can be added at the bottom of the capsule, and then expanded after exposure to water thus pushing the liquid crystal matrix into the intestinal tract.

3) As a plasticizer:

TPGS as a plasticizer reduce the interaction among the polymer molecules, so that the polymer chains are more likely to move. It provides polymer molecules with greater freedom mobile space, allowing more stretching and elastic membrane.

4) As an emulgator:

TPGS is amphiphilic. Experiments show that both in water and oil phase, TPGS has such high entrapment efficiency.

5) As a sorbefacient:

TPGS can improve gastrointestinal absorption of animals and people.

6) Others:

TPGS is waxy solid at room temperature. As an ophthalmic preparation, the viscosity is high which can extend the residence time on the surface of the cornea, reduce the stimulus and significantly increase the solubility of indissolvable drug in the eye. As a surfactant, it can make sprays from Glucocorticoid Beclometasone Dipropionate and treat respiratory illness through nasal drug delivery.


Process Flow sheet

 


3.TPGS / Vitamin E Polyethylene Glycol Succinate

TPGS / Vitamin E Polyethylene Glycol SuccinateUSP39

CAS#:  9002-96-4   

Molecular formula:   C33H54O5.(C2H4O)n

Structural formula:

 

Description

D -α-tocopheryl polyethylene glycol 1000 succinate is a water-soluble derivative of natural-source vitamin E. Off-white or yellowish waxy solid, almost tasteless, soluble in water and most of the polar organic solvents such as ethanol. It is amphipathic, miscible with water, and forms a variety of liquid crystalline phases in water. The excipient melts at 37–41℃ and is heat stable at temperatures ≤200℃.

 

Function

1) As a solubilizer:

TPGS increases the permeability of amprenavir by inhibiting efflux. Amprenavir is a new HIV protease inhibitor. At present, Amprenavir products  which use TPGS as an excipient are currently available in the United States, such as Agenerase ™ oral liquid and capsules. It has also been reported that micellar solubilization of TPGS increases estradiol solubility and transdermal  permeation. After combined with cyclosporine A, TPGS increased the solubility of cyclosporine A, thereby enhancing the cyclosporine A bioavailability.

2) Apply to solid dispersion technology:

Water-soluble excipient such as lactose, mannitol, hydroxypropyl methyl cellulose and the like are added into the TPGS drug mixture to accelerate drug release. Adding hydrophobic materials, such as wax, can slow down dissolution. In addition, an expansiveness excipient can be added at the bottom of the capsule, and then expanded after exposure to water thus pushing the liquid crystal matrix into the intestinal tract.

3) As a plasticizer:

TPGS as a plasticizer reduce the interaction among the polymer molecules, so that the polymer chains are more likely to move. It provides polymer molecules with greater freedom mobile space, allowing more stretching and elastic membrane.

4) As an emulgator:

TPGS is amphiphilic. Experiments show that both in water and oil phase, TPGS has such high entrapment efficiency.

5) As a sorbefacient:

TPGS can improve gastrointestinal absorption of animals and people.

6) Others:

TPGS is waxy solid at room temperature. As an ophthalmic preparation, the viscosity is high which can extend the residence time on the surface of the cornea, reduce the stimulus and significantly increase the solubility of indissolvable drug in the eye. As a surfactant, it can make sprays from Glucocorticoid Beclometasone Dipropionate and treat respiratory illness through nasal drug delivery.

 

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