Process of preparing immunoglobulin for intravenous...

Drug – bio-affecting and body treating compositions – Immunoglobulin – antiserum – antibody – or antibody fragment,... – Free from infectious agents

Reexamination Certificate

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C530S390100, C530S415000, C530S417000

Reexamination Certificate

active

06338849

ABSTRACT:

This application is a 371 of PCT/CN99/00081.
FIELD OF THE INVENTION
The present invention relates to a process for preparing a biological product, particularly for preparing immunoglobulin for intravenous injection (IVIG) by using a double-sterilized method without including any protectant.
BACKGROUND OF THE INVENTION
The production of immunoglobulin started in 1949. Since the invention of IVIG in the 1960s, more than thirty (30) kinds of IVIG products, produced by 29 manufacturers in 12 countries, have appeared in the international marketplace.
Human placental blood IVIG first appeared in China in 1985, and the regulations of its manufacture and assay are recorded in “The China National Regulations of Biological Products”. In 1992, pilot-plant production of lyophilized low pH IVIG was approved by the Ministry of Health of the Peoples Republic of China.
There have been many instances of epidemic type-C hepatitis caused by the repeated injection of large doses of IVIG Evidence has shown that it is difficult to ensure the safety of such injections without procedures for virus sterilization in the course of IVIG production. Since the 1990s, virus sterilization, as an essential procedure in the production of IVIG, has been regulated by many countries throughout the world.
Pasteurization was the earliest method used for virus sterilization. For example, virus sterilization may be accomplished in IVIG products by heating for 10 hours at 60° C. Methods such as low pH incubation, dry heat, irradiation, and filtration have also been developed to accomplish virus sterilization. In addition, as a result of the rapid spread of AIDS, a method using detergent to destroy the lipid-containing envelope of a virus was developed for HIV. Presently, most IVIG products are prepared using lyophilization, in which saccharose serves as a protectant and excipient.
Although the above-mentioned virus sterilization techniques are useful against the HIV, HBV, HCV, and other viruses with common pathogenic factors, differences in effectiveness among the various known methods of virus sterilization remain. Furthermore, it has been noted that a virus existing in the presence of a protectant may be better able to survive the sterilization process. According to recent literature (Ref. Murphy P. et al., J-Med-Virol, 41(1):61-64, 1993), although the presence of a protectant has some effect for keeping the natural activity of a protein, it can yield a certain protection for a virus. As a result, trace amounts of viruses may remain in the product.
In addition, organic solvents used in detergent sterilization are not completely recovered, which affects not only the purity of the product, but also can produce undesirable effects when the product is administered intravenously. For example, it has been reported in several cases that the use of saccharose as a protectant can lead to acute failure of kidney function. (Ref. Winward D B et al., Pharmacotherapy, 15(6):765-722, 1995; Hifenhaus L.& Nowak T., Vox Sang 67 (Suppl.) 1:62-66, 1994; Horowitz B.et al., Blood, 86(11): 4331-4336, 1995).
Also, the clinical side effects of lyophilized IVIG outweigh the benefits of the liquid products because the lyophilization process causes polymerization of the IVIG molecule. Thus, the preparation of IVIG using a lyophilization process is not favorable for large-scale production.
SUMMARY OF THE INVENTION
The object of this invention is to overcome the deficiencies in the techniques for producing IVIG that use existing methods for virus sterilization. The present invention is a process for preparing a biological product, particularly for preparing immunoglobulin for intravenous injection (IVIG), by using a double-sterilized method without including any protectant. Specifically, the process incorporates a virus-sterilizing method with two different mechanisms, which serve to approach complete virus-sterilization. As a result, IVIG may be used more effectively and safely in the clinical environment.
DETAILED DESCRIPTION OF THE INVENTION
The first step for preparing immunoglobulin for intravenous injection (IVIG) according to the present invention is Pasteurization. As a raw material, Cohn's component II (F II) is dissolved in between and including 2-fold and 10-fold distilled ice water. The pH is adjusted to between and including 3.5 and 5.0 with an acetic acid solution having a concentration between and including 0.2 and 2.0 mmol/L. The solution is passed through an ultra-filter membrane having a molecular weight cut-off between and including 10 and 100 kDa, in order to remove alcohol and salt and achieve a sodium ion concentration of between and including 1 and 10 mmol/L. The IVIG concentration is adjusted to between and including 0.5% and 2% and then bottled. The bottles are filled with gaseous CO
2
until the internal pressure is between and including 0.7 and 200 kPa. Next, the bottles are sealed in the absence of any protectant and sterilized at 60° C.±1° C. for 10 hours.
The second step for preparing immunoglobulin for intravenous injection (IVIG) according to the present invention is incubation treatment at low pH. After Pasteurization is complete, the F II solution is cleaved and purified with an ultra-filter membrane having a molecular weight cut-off between and including 10 and 100 kDa. In the event that the IVIG solution has a purity less than 97%, the purity of the solution is increased to 97% or above using gel adsorption techniques. The IVIG solution is then concentrated to between and including 5% and 10%. The pH is adjusted to 4.1±0.3. The solution is then filtered to remove and stored at room temperature for 21 days. The osmotic is adjusted by adding between and including 5% and 10% Once quality is assured, the product may be bottled using 25 or 50 ml bottles.
In order to demonstrate the effectiveness of the present invention, virus sterilization using Pasteurization, incubation at low pH, and a combination of Pasteurization and incubation at low pH (double sterilization method) as described in the present invention is shown using the indicator viruses VSV, Polio-I, and Sindbis.
TABLE 1
Pasteurization - sterilizing effect on three kinds of viruses at 60° C.
VSV
Polio-I
Sinbis
Log TCID
50
/0.1 ml
Log TCID
50
/0.1 ml
Log PFU/ml
Sterilizing
control
Treated
control
treated
control
treated
time (h)
sample
sample
sample
sample
sample
sample
0
6
6.5
4 × 10
6
1
6
4
6.5
2
4 × 10
6
  10
4
4
6
3
6.3

4 × 10
6
<10
4
5
5.8
2
6.3

4 × 10
6
<10
3
7
5.8
1
6.3

4 × 10
6
<10
2
10 
5.8

6

4 × 10
6

As shown in Table 1, the sterilizing effect of Pasteurization on the Polio-I virus is remarkable, but less so for the VSV and Sindbis viruses.
TABLE 2
Low pH incubation - sterilizing effect on two kinds of
viruses at pH 4.0, 23° C.
Sindbis (Log PFU/ml)
Time
VSV (Log TCID
50
/0.1 ml)
control
treated
(day)
control sample
treated sample
sample
sample
0
6.5
  4 × 10
6
3
6.5
1
  4 × 10
5
<10
4
7
8

3.5 × 10
6
<10
3
14 
6

3.5 × 10
6
<10
0
21 
5.5

3.5 × 10
4

As shown in Table 2, the sterilizing effect of low pH incubation demonstrates that VSV is sensitive to an acidic environment of pH 4.0 because it was rendered inactive on the seventh day after treatment. The sterilizing effect of low pH incubation demonstrates that Sindbis is less sensitive to the same acidic environment because it was rendered inactive on the twenty-first day after treatment.
TABLE 3
Double sterilization - sterilizing effect on three kinds of viruses
VSV
Polio-I
Sindbis
Log TCID
50
/0.1 ml
Log TCID
50
/ml
Log PFU/ml
Sterilizing
control
treated
control
treated
control
treated
time (h)
sample
sample
sample
sample
sample
sample
60° C.
0
6
6.5
  4*10
6
heating
5
6
2
6.5
  4*10
6
10
3
Stored at
10 
6

6.3

  4*10
6

pH 4.0
 7 days
5.5

6

3.5*10
6

23° C.
14 days
5.5

6

3.5*10
6

21 days
5

5.5

3.5*10
6

As shown in Table 3, the effect of double sterilization

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