Solubilization of pharmaceutical substances in an organic solven

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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514 21, 530412, 530418, 530419, 530427, 424450, 424489, A61K 3800, A23J 100

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active

057705593

ABSTRACT:
Provided is a method for preparing a true, homogeneous solution of a pharmaceutical substance dissolved in an organic solvent in which the pharmaceutical substance is not normally soluble. Solubilization is obtained by forming a hydrophobic ion pair complex involving the pharmaceutical substance and an amphiphilic material. The resulting organic solution may be further processed to prepare pharmaceutical powders. A biodegradable polymer may be co-dissolved with the pharmaceutical substance and the amphiphilic material and may be incorporated into a pharmaceutical powder. A preferred method for preparing pharmaceutical powders is to subject the organic solution to gas antisolvent precipitation using a supercritical gas antisolvent such as carbon dioxide. Also provided is a method for making hollow particles having a fiber-like shape which would provide enhanced retention time in the stomach if ingested by a human or animal host.

REFERENCES:
patent: 4851211 (1989-07-01), Adjei et al.
patent: 4897256 (1990-01-01), Adjei et al.
patent: 5043280 (1991-08-01), Fischer et al.
Helenius et al., "Solubilization of Membranes by Detergents," Biochimica Biophysica Acta, 415 (1975) pp. 29-79, Elsevier Scientific Publishing Company, Amsterdam.
Dorin et al., "Recovering Refractile Bodies Containing Heterologous Proteins from Microbial Hosts and Their Use," Chemical Abstracts, 107:38079y (1987).
Zaks et al., "Enzymatic Catalysis in Nonaqueous Solvents," Journal of Biological Chemistry, vol. 263, No. 7 (Mar. 5, 1988) pp. 3194-3201, American Society for Biochemistry and Molecular Biology, Inc.
Abu-Hamidyyah et al., "General Anesthetic Agents and the Conformation of Proteins. 2. Strengthening of Hydrophobic Interaction in B-lactoglobulin by l-alkanols and the cutoff effect in anesthetic potency," Chemical Abstracts, 110:205059n (1989).
Mazzenga et al., "The Transdermal Delivery of Zwitterionic Drugs I: the solubility of Zwitterionic Salts," Journal of Controlled Release, 16 (1991) pp. 77-88, Elsevier Science Publishers, Amsterdam.
Wells, et al., "Effect of Surfactants on Release of Highly Water-Soluble Medicinal Compound From an Inert, Heterogeneous Matrix," Journal of Pharmaceutical Sciences, vol. 81, No. 5 (May 1992) pp. 453-457, American Pharmaceutical Association.
Yeo, et al., "Formation of Microparticulate Protein Powder Using a Supercritical Fluid Antisolvent," Biotechnology and Engineering, vol. 41 (1993) pp. 341-346, John Wiley & Sons, Inc.
Randolph et al., "Sub-Micrometer-Sized Biodegradable Particles of Poly(L-Lactic Acid) via The Gas Antisolvent Spray Precipitation Process," Preprint, Biotechnology Progress 9 (Jul./Aug. 1993) pp. 429-435, American Chemical Society and American Institute of Chemical Engineers.
Powers et al., "Enhanced Solubility of Proteins and Peptides in Nonpolar Solvents Through Hydrophobic Ion Pairing," Biopolymers, vol. 33 (1993) pp. 927-932, John Wiley & Sons, Inc.
Matsuura et al., "Structure and Stability of Insulin Dissolved in 1-octanol," Journal of the American Chemical Society, vol. 115, No. 4, (1993) pp. 1261-1264, American Chemical Society.
Adjei et al., "Effect of ion-pairing on 1-octanol-water partitioning of peptide drugs. I: The nonapeptide leuprolide acetate," International Journal of Pharmaceutics, 90 (1993) pp. 141-149, Elsevier Science Publishers, Amsterdam.
Bromberg et al., "Detergent-Enabled Transport of Proteins and Nucleic Acids Through Hydrophobic Solvents," Proc. Nat'l. Acad. Sci. USA, vol. 91 (Jan. 1994) pp. 143-147.
Meyer et al., "Selective Precipitation of Interleukin-4 Using Hydrophobic Ion Paring: A Method for Improved Analysis of Proteins Formulated with Large Excesses of Human Serum Albumin," Pharmaceutical Research, vol. 11, No. 10 (1994) pp. 1492-1495, Plenum Publishing Corporation.
Meyer et al., "Solution Behaviour of .alpha.-Chymotrypsin Dissolved in Nonpolar Organic Solvents Via Hydrophobic Ion Pairing," Biopolymers, vol. 35 (1995) pp. 451-456, John Wiley & Sons, Inc.
Bromberg et al., "Transport of Proteins Dissolved in Organic Solvents Across Biomimetic Membranes," Proc. Nat'l. Acad. Sci. USA, vol. 92 (Feb. 1995) pp. 1262-1266.
Wells et al, Journal of Pharmaceutical Science, vol. 81, No. 5, pp. 453-457, 1992.
Zaks et al., Journal of Biological Chemistry, vol. 263, No. 7, pp. 3194-3201, 1988.
Abu Hamidiyyah et al, Chemical Abstracts, vol. 110, Ref. #205054n, 1989.

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