drug carrier

Guide Line

1. Intrinsic viscosity vs. average molecular weight

PLA-00series

PLA-75series

PLA-50series

2. Solubility

PLA PLGA
0005 0010 0015 0020 7505 7510 7515 7520 5005 5010 5015 5020
Methylene chloride ○ ○ ○ ○ ○ ○ ○ ○ ○ ○ ○ ○
Chloroform ○ ○ ○ ○ ○ ○ ○ ○ ○ ○ ○ ○
Acetone ○ ○ ○ ○ ○ ○ ○ ○ ○ ○ ○ ○
Ethyl Acetate ○ ○ ○ ○ ○ ○ ○ ○ ○ ○ ○ ○
THF ○ ○ ○ ○ ○ ○ ○ ○ ○ ○ ○ ○
Toluene ○ ○ ○ ○ ○ ○ ○ ○ △ △ △ △
Ethanol △ △ △ △ △ △ △ △ △ △ × ×
Methanol △ △ △ △ △ △ △ △ △ △ × ×
n-Haxane × × × × × × × × × × × ×
Water × × × × × × × × × × × ×

Test Method : solution was prepared by dissolving the polymer in
    its 25 times by volume of solvent, and solubility
    was expressed by the following criterion

Criterion : ○ ; homogeneously soluble
    △ ; soluble, but partly remains undissolved
    × ; very slightly soluble

3. Hydrolysis of PLA and PLGA

3.Hydrolysis of PLA and PLGA

4. Half-life of copolymers with various ratios of Lactic acid and Glycolic acid in implanted rat tissue 1)

Component ratio

5.Correlation of drug release between in vitro and in vivo 2)

Correlation of drug release between in vitro and in vivo

6. Release profile of TRH form PLGA microspheres 2)

Effects of molecular weight of PLGA (75/25) on release profile of TRH from microspheres.

Release profile of TRH from microspheres with different copolymer ratios of PLGA

7. Example of preparations

1. Preparation of microsphere 2) 4) 5)

     　　In-water drying method is shown		   2. Preparation of implant 3)
Correlation of drug release between in vitro and in vivo

References

1) R. Miller, J.M. Brady and D. Cutright, J. Biome. Materd. Res., 11, 711-19 (1977)
2) T. Heye, H. Okada, Y. Ogawa and H. Toguchi, Int. J. Pharm., 72, 199-205 (1991)
3) M. Asano, H. Fukazaki, M. Yoshda, M. Kumakura, T. Mashino, H. Yuasa, K. Imai and H. Yamada, Drug design and delivery,

5, 301-20 (1990)

4) Y. Ogawa, Clinical Pharmacy, 4 (13), 40-43 (1988)
5) Y. Ogawa, M. Yamamoto, H. Okada, T. Yashiki and T. Shimamoto, Chem. Pharm. Bull., 36 (3), 1095-1103 (1988)

Notes

  • U. Siemann, Eur. Polym. J., 28 (3), 293-7 (1992)
  • J.M. Ruiz and J.P. Benoit, J. Controlled Release, 16, 177-86 (1991)
  • J.M. Ruiz, J.P. Busnel and J.P. Benoit, Pharm. Res., 7 (9), 928-34 (1990)
  • T. Shimamoto, J. Andrology, 8 (1), S-14-16 (1987)
  • H. Okada, T. Heya, Y. Ogawa and T. Shimamoto, J. Pharmacol. Exp. Ther., 244 (2), 744-50 (1988)
  • Y. Ogawa, M. Yamamoto, S. Takada, H. Okada and T. Shimamoto, Chem. Pharm. Bull., 36 (4), 1502-7 (1988)
  • Y. Ogawa, H. Okada, T. Shimamoto and T. Shimamoto, Chem. Pharm. Bull., 36 (7), 2576-81 (1988)
  • Y. Ogawa, Pharm tech Japan, 5 (10), 1121-7 (1989)
  • K. Suda, K. Shiota, T. Masaki and T. Fujita, Endocrinol. Japan, 38 (1), 37-45 (1991)
  • H. Okada, T. Heya, Y. Ogawa, H. Taguchi and T. Shimamoto, Pharm. Res., 8 (5), 584-7 (1991)
  • H. Okada, Y. Inoue, T. Heya, H. Ueno, Y. Ogawa and H. Toguchi, Pharm. Res., 8 (6), 787-91 (1991)

    • Further detail Technical information will be provided upon your request.