Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Patent
1996-07-22
1997-09-30
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
424468, 424480, 424494, 424497, A61K 916, A61K 950
Patent
active
056723601
DESCRIPTION:
BRIEF SUMMARY
The present invention is a U.S. National Phase application of PCT/US94/13606, claiming priority of U.S. Ser. No. 08/156,468, filed Nov. 23, 1993. Priority is also claimed from U.S. Ser. No. 08/086,248, filed Jul. 1, 1993 now abandoned.
BACKGROUND OF THE INVENTION
The present invention relates to bioavailable sustained-release pharmaceutical formulations of analgesia drugs, in particular opioid analgesics, which provide an extended duration of effect when orally administered.
It is the intent of all sustained-release preparations to provide a longer period of pharmacologic response after the administration of the drug than is ordinarily experienced after the administration of the rapid release dosage forms. Such longer periods of response provide for many inherent therapeutic benefits that are not achieved with corresponding short acting, immediate release preparations. This is especially true in the treatment of cancer patients or other patients in need of treatment for the alleviation of moderate to severe pain, where blood levels of an opioid analgesic medicament must be maintained at a therapeutically effective level to provide pain relief. Unless conventional rapid acting drug therapy is carefully administered at frequent intervals to maintain effective steady state blood levels of the drug, peaks and valleys in the blood level of the active drug occur because of the rapid absorption, systemic excretion of the compound and through metabolic inactivation, thereby producing special problems in maintenance of analgesic efficacy.
The prior art teaching of the preparation and use of compositions providing the sustained-release of an active compound from a carrier is basically concerned with the release of the active substance into time psychologic fluid of the alimentary tract. However, it is generally recognized that the mere presence of an active substance in the gastrointestinal fluids does not, by itself, insure bioavailability.
In order to be absorbed, the active drug substance must be in solution. The dissolution time required for a given proportion of an active substance from a unit dosage form is determined as the proportion of the amount of active drug substance released from a unit dosage form over a specified time base by a test method conducted under standardized conditions. The physiologic fluids of the gastrointestinal tract are the media for determining dissolution time. The present state of the art recognizes many satisfactory test procedures to measure dissolution time for pharmaceutical compositions, and these test procedures are described in official compendia world wide.
The primary principle guiding the use of opioid analgesics in the management of chronic pain is the individualization of dosages to meet the different and changing opioid requirements among and within each individual patient. Pain management authorities stress the importance of titration. Titration to the appropriate dose for a particular patient is necessitated by the wide inter-individual differences in the response of different patients to given doses of opioids. While a multitude of factors are responsible for wide inter-individual differences in the response to opioid analgesics, one important factor is rooted in the wide inter-individual variation in metabolism and pharmacokinetics.
Those opioids which are most efficiently titrated are those with relatively short elimination half-lives in the range of 3 to 5 hours (e.g., morphine, hydromorphone, oxycodone) as compared to long (12 to 72 hours) and more variable half-life analgesics(e.g., methadone, levorphanol). The shorter half life drugs approach steady-state concentrations in approximately a day rather than in several days to a week or more. Only at steady-state can one expect that the balance between efficacy and side effects will persist at a given dosing schedule. Having confidence that the patient is at approximate steady-state a day or so following initiation of dosing allows for much quicker assessment of whether the dosage is appropriate for that indivi
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Geoff
Goldenheim Paul
Kaiko Robert F.
Sackler Richard S.
Benston, Jr. William E.
Page Thurman K.
Purdue Pharma L.P.
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