CN1249178A - Puerrarin injection for perfusion and its preparing process - Google Patents

Abstract

A puerarin injection for perfusion by intravenous drip is prepared from puerarin through dissolving puerarin in fresh injection water in the ratio of 0.05-0.45% (g/ml), treating by activated carbon used for injection, regulating pH value, regulating osmotic pressure with sodium chloride, ultrafiltering, introducing chlorine gas into it and aseptic sealing. Said injection features no content of propandiol, low viscosity, easy filtering, and high utilization rate of raw material, and can be used to cure coronary heart disease, angina pectoris, myocardial infarction, cerebral infarction, and retina arterial and venous embolism.

Description

Puerrarin injection for perfusion and preparation method thereof

The present invention relates to a kind of is intravenous transfusion preparation of Main Ingredients and Appearance and preparation method thereof with puerarin (Purerarin), is a kind of Puerrarin injection for perfusion and preparation method thereof specifically.

Puerarin has pharmacological action widely; experimental results show that puerarin has coronary artery dilating, improves coronary circulation, improves the Ischemic Heart contractile function, reduces myocardial oxygen consumption, increases function such as local cerebral microvascular flow; acute cerebral ischemia there is significant protective effect, B-adrenergic receptor is had blocking effect.Be mainly used in the treatment of diseases such as angina pectoris, myocardial infarction, high blood viscosity, arrhythmia, cerebral infarction and retina artery and vein thromboembolism clinically.

The 2ml puerarin injection of using clinically includes 50mg or 100mg puerarin at present.Because the dissolubility of puerarin in water is little, only be 4.5g/l, therefore in the preparation technology of said preparation, need to add a large amount of cosolvents, as in the 2ml injection, adding 50% propylene glycol,, make that the liquid viscosity of preparation is very big in addition because solution will add heavy dose of propylene glycol, in preparation process, increase filtering difficulty, influenced the utilization rate of material.In clinical use, treating consumption every day is the 600-800mg puerarin, and promptly daily requirement props up with the injection 6-8 of 2ml:100mg, and reuse 5% glucose infusion liquid or isotonic sodium chloride transfusion dilution posterior vein instil, and therefore use also pretty troublesome clinically.

The purpose of this invention is to provide Puerrarin injection for perfusion of a kind of be directly used in intravenous drip that does not contain propylene glycol and preparation method thereof.

Realize that purpose technical scheme of the present invention is:

The present invention is a kind of intravenous transfusion preparation, and the primary structure formula is formula I:

Its Main Ingredients and Appearance is a puerarin, and content is 0.05%-0.45% (g/ml), and wherein preferred content proportioning is 0.16%-0.3% (g/ml), dissolves with fresh water for injection.

This infusion preparation is to form by following prepared:

A) dissolve puerarin with fresh water for injection;

B) add pin activated carbon mixing, boil 15-20 minute after-filtration and remove activated carbon;

C) use alkaline solution oxygen sodium oxide or sodium carbonate or sodium bicarbonate to adjust the pH value of puerarin solution to 4.0-7.0;

D) ooze to waiting according to the osmotic pressure of drop data method under the freezing point with sodium hydride adjusting puerarin solution;

E) feed nitrogen after the ultrafiltration, be encapsulated in infusion bottle or the bag, in 115 ℃ of following 30 minutes pressure sterilizings.

The present invention has the following advantages: 1, liquid achromatism and clarity can be directly used in intravenous drip clinically; 2, easy to use, reduced the link of microbiological contamination; 3, this preparation does not contain organic cosolvents such as propylene glycol, avoided because of adding the side effect that propylene glycol causes, and viscosity is little, easily filter, the utilization ratio of raw materials height, the injection raw material availability that contains propylene glycol is 80%, and this infusion preparation raw material availability is more than 95%.

Embodiment 1:

Be the Puerrarin injection for perfusion 100 of 0.45% (g/ml) and be example in order to content.

The medicinal puerarin powder of 45 grams is joined in the 9.5l fresh water for injection after the heating for dissolving, add the needle-use activated carbon of 15 grams through the salt acid treatment, 20 minutes after-filtration of heated and boiled, filtrate is cooled to below 40 ℃, transferring PH with the 1mol/l sodium carbonate liquor is 4.7, adds 86.66 gram medicinal sodium chlorides, stirring and dissolving, with the drug level of fresh water for injection regulator solution, make it to become contain in the 1l solution 4.5 the gram puerarins.Charge into nitrogen, sterile filling in 115 ℃ of following pressure sterilizings 30 minutes, promptly gets the infusion preparation that every bottle of (bag) 200ml solution contains the 900mg puerarin in 200ml infusion bottle (bag).

Embodiment 2:

To produce 100 bottles of content is that the puerarin transfusion of 0.05% (g/ml) is an example.

The medicinal puerarin powder of 5.0 grams is joined in the 9.5l fresh water for injection after the heating for dissolving, add the needle-use activated carbon of 20 grams through the salt acid treatment, 15 minutes after-filtration of heated and boiled, filtrate is cooled to below 40 ℃, transferring PH with the 1mol/l sodium hydroxide solution is 5.7, adds 89.7 gram medicinal sodium chlorides, stirring and dissolving, with the drug level of fresh water for injection regulator solution, make it to become contain in the 1l solution 0.5 the gram puerarin.Charge into nitrogen, sterile filling in 115 ℃ of following pressure sterilizings 30 minutes, promptly gets every bottle (bag) and contains the infusion preparation that 100ml solution contains the 50mg puerarin in the 100ml solution bottle (bag).

Embodiment 3:

With the puerarin transfusion that to prepare 100 bottles of (or bag) content be 0.24% (g/ml) is example.

The medicinal puerarin powder of 60 grams is joined in the 20l fresh water for injection after the heating for dissolving, add the needle-use activated carbon of 40 grams through the salt acid treatment, 15 minutes after-filtration of heated and boiled, filtrate is cooled to below 40 ℃, transferring PH with the 1mol/l sodium hydroxide solution is 5.5, adds 220 gram medicinal sodium chlorides, stirring and dissolving, with the drug level of fresh water for injection regulator solution, make it to become contain in the 1l solution 2.4 the gram puerarins.Charge into nitrogen, sterile filling in 115 ℃ of following hot pressing minute, promptly gets every bottle (bag) and contains the infusion preparation that 250ml solution contains the 600mg puerarin in the 250ml solution bottle (bag).

Embodiment 4:

With the puerarin transfusion that to prepare 100 bottles of (or bag) content be 0.16% (g/ml) 500ml is example.

The medicinal puerarin powder of 80 grams is joined in the 45l fresh water for injection after the heating for dissolving, add the needle-use activated carbon of 45 grams through the salt acid treatment, 15 minutes after-filtration of heated and boiled, after the filtrate cooling, transferring PH with the 1mol/l sodium hydroxide solution is 4.5, adds 444.4 gram medicinal sodium chlorides, stirring and dissolving, with the drug level of fresh water for injection regulator solution, make it to become contain in the 1l solution 1.6 the gram puerarins.Feed nitrogen, sterile filling in 115 ℃ of following pressure sterilizings 30 minutes, promptly gets every bottle (bag) and contains the infusion preparation that 500ml solution contains the 800mg puerarin in the 500ml solution bottle (bag).

Embodiment 5:

With the puerarin transfusion that to prepare 100 bottles of (or bag) content be 0.4% (g/ml) 100ml is example.

The medicinal puerarin powder of 40 grams is joined in the 9.5l fresh water for injection after the heating for dissolving, add 20 gram needle-use activated carbons, 15 minutes after-filtration of heated and boiled, filtrate is cooled to below 40 ℃, with 1mol/l sodium bicarbonate (NaHCO ₃) changing sodium solution, to transfer PH be 6.5, adds 80 gram medicinal sodium chlorides, stirring and dissolving with the drug level of fresh water for injection regulator solution, makes it to become and contains 4 gram puerarins in the 1l solution.Feed nitrogen, sterile filling in 115 ℃ of following pressure sterilizings 30 minutes, promptly gets every bottle (bag) and contains the infusion preparation that 100ml solution contains the 400mg puerarin in the 100ml solution bottle (bag).

Claims (3)

1, a kind of puerarin (Purerarin) infusion preparation, its primary structure formula are formula I:

It is characterized in that it is a kind of intravenous transfusion preparation, Main Ingredients and Appearance is a puerarin, and with the fresh water for injection dissolving, its content is 0.05%-0.45% (g/ml).

2, a kind of Puerrarin injection for perfusion according to claim 1 is characterized in that its content is 0.16%-0.24% (g/ml).

3, a kind of preparation method of Puerrarin injection for perfusion according to claim 1 is characterized in that it is to be prepared from by following technical process:

A) diffusing fresh water for injection dissolving puerarin;

B) add pin activated carbon mixing, boil 15-20 minute after-filtration and remove activated carbon;

C) use alkaline solution sodium hydroxide or sodium carbonate or sodium bicarbonate to regulate the pH value of puerarin solution to 4.0-7.0;

D) ooze to waiting according to the osmotic pressure of drop data method under the freezing point with sodium chloride adjusting puerarin solution;

E) feed nitrogen after the ultrafiltration, be encapsulated in infusion bottle or the bag, in 115 ℃ of following 30 minutes pressure sterilizings.