Puerarin derivatives powder injection and its production method

1. Study on the preparation process of tetraacetylpuerarin freeze-dried powder injection

1.1 Preparation process screening

1.1.1 Research route, see Figure 3.

1.1.2 Screening of the types of solubilizing excipients

1.1.2.1 Single factor screening of solubilizing excipients

Take 0.05g of tetraacetylpuerarin, accurately weigh, and mix with 0.2g of polysorbate 80, PVP, HP-β-CD, glycerin, PEG400 (polyethylene glycol 400) and F68 (poloxamer 188) respectively , Add 5ml deionized water to grind to make it into a supersaturated solution. Pour into a stoppered centrifuge tube, shake well, centrifuge at 3000r / min for 10min, aspirate the supernatant, and immediately inject 1μL after passing through a 0.22μm filter membrane for HPLC determination. Calculate its solubility in different solubilizing excipients and repeat it twice. The results are shown in Table 2-8.

Table 2-8 Single factor investigation results of tetraacetylpuerarin solubilizing excipients (n=2)

The results show that the

Example 1:

Prescription (calculated by 1000)

Tetraacetylpuerarin 50g

Poloxamer 500g

Polysorbate 80500g

Add water for injection to 5000ml

Made into 1000

Among them, poloxamer is the carrier and scaffold of the dispersion, and polysorbate 80 is the solubilizer.

2. Preparation process

(1) Liquid preparation: weigh 50 g of tetraacetylpuerarin and 500 g of poloxamer in a sterile operating room, mix them, add 5000 ml of absolute ethanol and grind for 5 minutes to fully dissolve them. Then weigh 500 g of polysorbate 80 and add 5000 ml of sterile water for injection to dissolve it with slight heat. Mix the two evenly, recover the ethanol at low temperature, and add sterile water for injection to 5000ml.

(2) Filtration, intermediate inspection and packaging: use 1‰ activated carbon to remove pyrogens, and then use sterilized φ0.22μm (Sartobran-p produced by SARTORIUS, Germany) filter for suction; take a sample to measure the pH value And content. Divide, 5ml per bottle.

(3) Pre-free

Example 2:

Prescription (calculated by 1000)

Tetraacetylpuerarin 1g

Poloxamer 5g

Polysorbate 806g

Add water for injection to 5000ml

Made into 1000

Preparation process: the same as in Example 1.