Injectable drug combination and preparation method thereof

A composition and injection technology, which can be used in drug combinations, antipyretics, antitumor drugs, etc., can solve problems such as affecting cardiovascular function, long-term safety inspection of stabilizers and excipients, and reduce potential safety hazards. , good safety, the effect of preventing side effects

Inactive Publication Date: 2012-02-01

SHANGHAI INST OF PHARMA IND

5 Cites 4 Cited by

AI-Extracted Technical Summary

Problems solved by technology

However, the active drug used in this patent is magnesium salvianolic acid B, and magnesium ions will affect cardiovascular function to a certa...

Abstract

The invention provides an injectable drug combination and a preparation method thereof. The injection preparation which is a freeze-dried powder injection comprises salvianolic acid B and a pharmacologically allowable pH regulator, without other excipients. The addition of the pH regulator is pH being 4-5 in the pre-freeze drying system. The salvianolic acid B injection preparation provided by the invention selects a proper pH range without the addition of a supporting agent to ensure the stabilization of the injection as well as the pharmacological acceptability of the injection. The invention has advantages of safe clinical use, no bad effect of inducing hemolysis, good safety and stable quality for long-term storage with the stability and safety completely meeting the requirement of the injection preparation and the requirement of clinical application. The injection prepared by the technology needs no addition of auxiliary materials such as a stabilizer, a freeze-drying excipient and so on and the hidden danger of the injection is decreased. The invention avoids the use of magnesium salt and the side effect of magnesium ion to cardiovascular system can be prevented.

Application Domain

Organic active ingredientsPowder delivery +12

Technology Topic

Pharmaceutical preservativesSide effect +10

Image

Examples

Experimental program(3)
Comparison scheme(2)
Effect test(2)

Example Embodiment

[0030] Example 1

[0031] Preparation of freeze-dried powder injection:

[0032] 29.5g Na 3 PO 4 Dissolve in 1800ml water for injection and make 0.1mol/L Na 3 PO 4 Solution; prepare an appropriate amount of 1mol/L NaOH solution for later use; weigh 200g of salvianolic acid B and add the above 0.2mol/L Na 3 PO 4 The solution is 1800ml, after stirring evenly, the above 1mol/L NaOH solution is added dropwise to pH 4.0, 0.5% injection activated carbon is added to remove heat source, and water for injection is added to 2000ml. Filter with 0.22um microporous membrane, dispense into 10ml freeze-drying bottles, and freeze-dry.

[0033] Freeze-drying curve:

[0034] -40℃, 5h (the lowest eutectic point -12.3℃)

[0035] -25℃, 14h

[0036] 0℃, 3h

[0037] 20℃, 2h

[0038] Stability: The freeze-dried powder injection of salvianolic acid B was placed for three months under accelerated conditions at a temperature of 40°C and a relative humidity of 75%. Taking the crude drug as the standard, the content of salvianolic acid B in the sample was determined by HPLC external standard method, and the content decreased by about 0.4%.

Example Embodiment

[0039] Example 2

[0040] Dissolve 14.4g of NaOH in 1800ml of water for injection to form a 0.2mol/L NaOH solution; prepare an appropriate amount of 1mol/L NaOH solution for use; weigh 200g of salvianolic acid B and add the above 0.2mol/L NaOH solution 1800ml, after stirring evenly, add dropwise the above 1mol/L NaOH solution to pH 5.0, add 0.5% injection activated carbon to remove heat source, add water for injection to 2000ml. Filter with 0.22um microporous membrane, dispense into 10ml freeze-drying bottles, and freeze-dry.

[0041] Freeze-drying curve:

[0042] -40℃, 5h (the lowest eutectic point -8.3℃)

[0043] -20℃, 14h

[0044] 0℃, 3h

[0045] 20℃, 2h

[0046] Stability: The freeze-dried powder injection of salvianolic acid B was placed for three months under accelerated conditions at a temperature of 40°C and a relative humidity of 75%. Taking the crude drug as the standard, the content of salvianolic acid B in the sample was determined by HPLC external standard method, and the content decreased by about 0.6%.

Example Embodiment

[0047] Example 3

[0048] Dissolve 14.4g of NaOH in 1800ml of water for injection to form a 0.2mol/L NaOH solution; prepare an appropriate amount of 1mol/L NaOH solution for use; weigh 200g of salvianolic acid B and add the above 0.2mol/L NaOH solution 1800ml, after stirring evenly, add dropwise the above 1mol/L NaOH solution to pH 7.0, add 0.5% injection activated carbon to remove heat source, add water for injection to 2000ml. Filter with 0.22um microporous membrane, dispense into 10ml freeze-drying bottles, and freeze-dry.

[0049] Freeze-drying curve:

[0050] -40℃, 5h (the lowest eutectic point -8.3℃)

[0051] -20℃, 14h

[0052] 0℃, 3h

[0053] 20℃, 2h

[0054] Stability: The freeze-dried powder injection of salvianolic acid B was placed for three months under accelerated conditions at a temperature of 40°C and a relative humidity of 75%. Taking the raw material drug as the standard, the content of salvianolic acid B in the sample was determined by HPLC external standard method, and the content decreased by about 7.2%.

PUM

Description & Claims & Application Information

We can also present the details of the Description, Claims and Application information to help users get a comprehensive understanding of the technical details of the patent, such as background art, summary of invention, brief description of drawings, description of embodiments, and other original content. On the other hand, users can also determine the specific scope of protection of the technology through the list of claims; as well as understand the changes in the life cycle of the technology with the presentation of the patent timeline. Login to view more.