What is the advantage of alprostadil with PG phospholipid egg yolk phospholipidyl glycerol EPG?

Egg yolk phosphatidylglycerol EPG, as PG phospholipid for alprostatil, is an auxiliary emulsifier. In this article, AVT Xiaobian will take you to understand why the yolk phosphatidylglycerol is widely loved!

Before introducing egg yolk phosphatidylglycerol EPG, let's take a look at PG phospholipids.

Phosphatidylglycerol (PG) is a kind of phospholipid existing in pulmonary surfactants. Its basic structure is L-glycerol-3-phosphate skeleton. It is linked to saturated or unsaturated fatty acids by ester bonds at positions 1 and 2, and glycerol forms a single ester with phosphate. It is a precursor of surfactants, and its presence in neonatal amniotic fluid (>0.3) is an indicator of fetal lung maturity.

About 98% of type I cells and 2% of type II cells are present in the alveolar surface region, which secretes pulmonary surfactant. As soon as the surfactant is secreted, it must be immediately distributed on the surface of type I cells, and phosphatidylglycerol is considered to be an important substance in this process. Most of the surfactant deficiency in preterm infants is associated with a deficiency of phosphatidylglycerol, although Jin accounts for less than 5% of the surfactant phospholipids in the lung.

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In the field of pharmaceutical excipients, although phosphatidylglycerol PG is not as widely used as phosphatidylcholine (PC), due to its unique structure and physicochemical properties, it plays an extremely important role in the development of some key preparations. Among them, the 2-year shelf life of alprostil injection was marketed by Fuji Pharmaceuticals in January 2014. It was because of the replacement of oleic acid with egg yolk phosphatidylglycerol (EPG) in the original CHU formula that the shelf life of alprostol injection was successfully increased from 1 year to 2 years, triggering a revolution in the industry!

Egg yolk phosphatidylglycerol EPG is a kind of phospholipid product? The detailed information is as follows:

| Chinese name: egg yolk phosphatidyl glycerol

| trade name: egg yolk phosphatidyl glycerol

| chemical name: 1, 2-2 acyl - sn - glycerol - 3 - phosphate - [1 - rac - glycerine]

| English chemical name: 1, 2 - Diacyl - sn - Glycero - 3 - Phospho - [1 - rac - glycerol]

| molecular formula: C40H76NaO10P

| manufacturers: YiWeiTa (Shanghai) pharmaceutical technology co., LTD

| the CAS no. : 383907-64-0

| DMF number: 8997

| and registration number: F20170000042

| levels: medicinal injection level

| executive standard: enterprise standard

| purpose: liposome membrane material, emulsifier

| solubility: soluble in chloroform, slightly soluble in ethanol, insoluble in water

| molecular weight: 782.284

| preservation conditions: - below 20 ℃, shading, sealing, refrigeration, transport and preservation

| note: avoid together with strong acid, strong alkali, strong oxidizing substances

In addition to its application in alprostadil, EPG also has some applications in liposome drug development, which is still mainly in scientific research. Due to the characteristics of low phase transition temperature, low rigidity and electronegativity, it is different from saturated PG phospholipids such as DPPG in application, and is often used in the development of insoluble drugs or liposomes with special requirements.