Safety of psuedoephedrine drug products
First Claim
Patent Images
1. A pharmaceutical drug product comprising at least one drug substance selected from the group consisting of:
- amorphous sibutramine pamoate characterized by at least one method selected from;
a PXRD diffractogram of FIG. 1;
a DSC thermogram of FIG. 5; and
an FTIR spectrum of FIG. 3;
polymorphic sibutramine pamoate characterized by at least one method selected from;
a PXRD diffractogram of FIG. 2;
a DSC thermogram of FIG. 6; and
an FTIR spectrum of FIG. 4;
amorphous nortriptyline pamoate characterized by at least one method selected from;
a DSC thermogram of FIG. 9; and
an FTIR spectrum of FIG. 11;
polymorphic nortriptyline pamoate characterized by at least one method selected from;
a DSC thermogram of FIG. 10; and
an FTIR spectrum of FIG. 12;
amorphous clomipramine pamoate characterized by at least one method selected from;
a PXRD diffractogram of FIG. 16;
a DSC thermogram of FIG. 20; and
an FTIR spectrum of FIG. 18;
polymorphic clomipramine pamoate characterized by at least one method selected from;
a PXRD diffractogram of FIG. 17;
a DSC thermogram of FIG. 21; and
an FTIR of FIG. 19;
amorphous promethazine pamoate characterized by at least one method selected from;
a PXRD diffractogram of FIG. 26;
a DSC thermogram of FIG. 32;
an FTIR spectrum of FIG. 29;
a PXRD diffractogram of FIG. 27;
a DSC thermogram of FIG. 33; and
an FTIR spectrum of FIG. 30;
andpolymorphic promethazine pamoate characterized by at least one method selected from;
a PXRD diffractogram of FIG. 28;
a DSC thermogram of FIG. 34; and
an FTIR spectrum of FIG. 31.
1 Assignment
0 Petitions
Accused Products
Abstract
A pharmaceutical drug product with at least one drug substance capable of providing immediate release or modified release profiles. The drug substance is selected from an amorphous form with an active pharmaceutical ingredient and a first organic counterion wherein the amorphous form has a phase transition temperature of at least 100° C.; and a morphological form with the active pharmaceutical ingredient and a second organic counterion wherein the morphological form of the drug substance has a phase transition temperature of at least 100° C.
-
Citations
149 Claims
-
1. A pharmaceutical drug product comprising at least one drug substance selected from the group consisting of:
-
amorphous sibutramine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 1 ;a DSC thermogram of FIG. 5 ; andan FTIR spectrum of FIG. 3 ;polymorphic sibutramine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 2 ;a DSC thermogram of FIG. 6 ; andan FTIR spectrum of FIG. 4 ;amorphous nortriptyline pamoate characterized by at least one method selected from; a DSC thermogram of FIG. 9 ; andan FTIR spectrum of FIG. 11 ;polymorphic nortriptyline pamoate characterized by at least one method selected from; a DSC thermogram of FIG. 10 ; andan FTIR spectrum of FIG. 12 ;amorphous clomipramine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 16 ;a DSC thermogram of FIG. 20 ; andan FTIR spectrum of FIG. 18 ;polymorphic clomipramine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 17 ;a DSC thermogram of FIG. 21 ; andan FTIR of FIG. 19 ;amorphous promethazine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 26 ;a DSC thermogram of FIG. 32 ;an FTIR spectrum of FIG. 29 ;a PXRD diffractogram of FIG. 27 ;a DSC thermogram of FIG. 33 ; andan FTIR spectrum of FIG. 30 ;and polymorphic promethazine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 28 ;a DSC thermogram of FIG. 34 ; andan FTIR spectrum of FIG. 31 . - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 84, 85, 86)
-
-
27. A method of administering drug product to a patient comprising:
-
providing said drug product to said patient as an oral dose wherein said drug product comprises at least one drug substance selected from the group consisting of; amorphous sibutramine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 1 ;a DSC thermogram of FIG. 5 ; andan FTIR spectrum of FIG. 3 ;polymorphic sibutramine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 2 ;a DSC thermogram of FIG. 6 ; andan FTIR spectrum of FIG. 4 ;amorphous nortriptyline pamoate characterized by at least one method selected from; a DSC thermogram of FIG. 9 ; andan FTIR spectrum of FIG. 11 ;polymorphic nortriptyline pamoate characterized by at least one method selected from; a DSC thermogram of FIG. 10 ; andan FTIR spectrum of FIG. 12 ;amorphous clomipramine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 16 ;a DSC thermogram of FIG. 20 ; andan FTIR spectrum of FIG. 18 ;polymorphic clomipramine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 17 ;a DSC thermogram of FIG. 21 ; andan FTIR of FIG. 19 ;amorphous promethazine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 26 ;a DSC thermogram of FIG. 32 ;an FTIR spectrum of FIG. 29 ;a PXRD diffractogram of FIG. 27 ;a DSC thermogram of FIG. 33 ; andan FTIR spectrum of FIG. 30 ;and polymorphic promethazine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 28 ;a DSC thermogram of FIG. 34 ; andan FTIR spectrum of FIG. 3 ;administering said oral dose to a patient wherein no more than 50%, by weight, of active pharmaceutical ingredient of said drug substance releases in a stomach and at least 50%, by weight, of said active pharmaceutical ingredient releases in an intestine. - View Dependent Claims (28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57)
-
-
58. A method of administering an active pharmaceutical to a patient comprising:
-
providing a drug product comprising at least one drug substance to said patient wherein said drug substance is selected from the group consisting of; amorphous sibutramine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 1 ;a DSC thermogram of FIG. 5 ; andan FTIR spectrum of FIG. 3 ;polymorphic sibutramine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 2 ;a DSC thermogram of FIG. 6 ; andan FTIR spectrum of FIG. 4 ;amorphous nortriptyline pamoate characterized by at least one method selected from; a DSC thermogram of FIG. 9 ; andan FTIR spectrum of FIG. 11 ;polymorphic nortriptyline pamoate characterized by at least one method selected from; a DSC thermogram of FIG. 10 ; andan FTIR spectrum of FIG. 12 ;amorphous clomipramine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 16 ;a DSC thermogram of FIG. 20 ; andan FTIR spectrum of FIG. 18 ;polymorphic clomipramine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 17 ;a DSC thermogram of FIG. 21 ; andan FTIR of FIG. 19 ;amorphous promethazine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 26 ;a DSC thermogram of FIG. 32 ;an FTIR spectrum of FIG. 29 ;a PXRD diffractogram of FIG. 27 ;a DSC thermogram of FIG. 33 ; andan FTIR spectrum of FIG. 30 ;and polymorphic promethazine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 28 ;a DSC thermogram of FIG. 34 ; andan FTIR spectrum of FIG. 31 ;introducing said drug substance to a first drug absorption location of said patient wherein a portion of said active pharmaceutical in said drug substance is released from said drug substance yielding a released active pharmaceutical and a modified drug substance comprising a second ratio of said active pharmaceutical to said organic counterion of less than 2;
1;introducing said modified drug substance to a second drug absorption location of said patient wherein a remainder of said active pharmaceutical is released yielding an active ingredient and a free organic counterion. - View Dependent Claims (59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105)
-
-
106. A pharmaceutical drug product comprising:
-
an amorphous drug substance selected from the group consisting of; amorphous sibutramine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 1 ;a DSC thermogram of FIG. 5 ; andan FTIR spectrum of FIG. 3 ;amorphous nortriptyline pamoate characterized by at least one method selected from; a DSC thermogram of FIG. 9 ; andan FTIR spectrum of FIG. 11 ;amorphous clomipramine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 16 ;a DSC thermogram of FIG. 20 ; andan FTIR spectrum of FIG. 18 ; andamorphous promethazine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 26 ;a DSC thermogram of FIG. 32 ;an FTIR spectrum of FIG. 29 ;a PXRD diffractogram of FIG. 27 ;a DSC thermogram of FIG. 33 ; andan FTIR spectrum of FIG. 30 ;and a morphological drug substance comprising an active pharmaceutical ingredient and an organic counterion; wherein said organic counterion is defined by; - View Dependent Claims (107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128)
-
-
129. A pharmaceutical drug product comprising:
-
an amorphous drug substance comprising an active pharmaceutical ingredient and a organic counterion; and a morphological drug substance selected from the group consisting of; polymorphic sibutramine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 2 ;a DSC thermogram of FIG. 6 ; andan FTIR spectrum of FIG. 4 ;polymorphic nortriptyline pamoate characterized by at least one method selected from; a DSC thermogram of FIG. 10 ; andan FTIR spectrum of FIG. 12 ;polymorphic clomipramine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 17 ;a DSC thermogram of FIG. 21 ; andan FTIR of FIG. 19 ;and polymorphic promethazine pamoate characterized by at least one method selected from; a PXRD diffractogram of FIG. 28 ;a DSC thermogram of FIG. 34 ; andan FTIR spectrum of FIG. 3 ;wherein said organic counterion is defined by Structure A - View Dependent Claims (130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149)
-
Specification