Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Patent
1992-11-30
2000-12-12
Kishore, Gollamudi S.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
424491, 424499, 514 52, 514 21, A61K 914
Patent
active
061595020
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to complexes and compositions for oral delivery of a substances) to the circulation or lymphatic drainage system of a host. The invention also relates to processes for the production of complexes and compositions for oral delivery of a substances) to the circulation or lymphatic drainage system of a host. The invention further relates to a method of delivering a substances) to the circulation or lymphatic drainage system of a host. In addition the invention relates to kits for preparing complexes for oral delivery of a substances) to the circulation or lymphatic drainage system of a host.
BACKGROUND ART
A number of clinical conditions of vertebrates have sufficiently deleterious effects upon the vertebrate to warrant the administration of some pharmaceutically active agent. Such agents may include (i) vaccines, to protect against diseases such as tetanus, diptheria or whoophing cough, (ii) hormones, e.g. insulin, LHRH, vasopressin, oxytocin, or (iii) drugs, e.g. anti-cancer agents, antibiotics. In these cases, a suitable agent is administered to the vertebrate to invoke immunity, to supplement hormone levels, to eliminate the disease causing agent or to provide a therapeutic effect.
Administration of the pharmaceutical to the vertebrate may be via a number of routes including intramuscular (i.m.), subcutaneous (s.c.), or oral (per os, p.o.) administration. I.m. or s.c. administration of the pharmaceutical suffers from the disadvantages that: relatively specialized skills are required to administer the pharmaceutical; large scale administration may be difficult to perform; it is expensive; and a number of side reactions can occur to the agent being administered. For these reasons oral administration of the pharmaceutical is generally preferred. Many antibiotics (tetracycline, penicillin etc), and hormones (progesterone, oestrogen etc) can be successfully administered via the oral route. There are however drugs, hormones and immunogens whose efficacy is almost totally lost upon oral administration (including Calcitonin, Erythropoetin, Granulocyte Colony Stimulating Factor, Stem Cell Factor, Granulocyte Colony Stimulating Factor, LHRH analogues, Somatostatin, Insulin, Interferons, Plasminogen Activator Inhibitors and species of DNA and RNA). This loss of efficacy may be due either to the inability of the intestinal mucosa to absorb these compounds or the breakdown of these substances by various physiological agents in the intestinal milieu. To some extent this effect can be overcome by the administration of extremely large doses of the pharmaceutical agent. This approach, however, is not economically feasible for many pharmaceutical agents.
In an attempt to overcome the problem of degradation a number of encapsulation methods have been employed which enable the encapsulated material to by-pass both the gastric acidity and the pepsin mediated proteolysis encountered within the lumen of the stomach. Typically these methods have involved enteric coated capsules, which only release their contents upon contact with the higher pH of the upper duodenum and jejunum. While this has greatly increased the oral efficacy of a number of compounds, still many substances are pharmaceutically inactive upon oral delivery and must be administered parenterally. Noteable examples of such compounds include Calcitonin, Erythropoietin, Granulocyte Colony Stimulating Factor, Stem Cell factor, Granulocyte Macrophage Colony Stimulating Factor, Somatostatin, Insulin, LHRH and its analogues, Interferons, Plasminogen Activator Factor, species of DNA and RNA, and many vaccines.
In a further extension of the encapsulation process, several new forms of encapsulation have been designed in recent years with the specific purpose of trapping large quantities of pharmaceuticals in subcellular capsules, in the hope that once protected from the intestinal milieu, the capsules would themselves be taken up from the intestine and release their contents systemically. Two basic forms of these capsules ha
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Russell-Jones Gregory John
Westwood Steven William
Biotech Australia Pty LTD
Kishore Gollamudi S.
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