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1. CA2290966 - SELS DE SERTRALINE ET FORMES POSOLOGIQUES DE SERTRALINE, A LIBERATION PROLONGEE

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[ EN ]
CLAIMS:
1. A sustained-release dosage form suitable for oral administration to a mammal in the form of a matrix tablet, an osmotic tablet, a membrane-coated hydrogel tablet, a multiparticulate, or a membrane-coated diffusion-based capsule, tablet or multiparticulate, comprising sertraline, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, which dosage form releases sertraline into a use environment at a rate not exceeding 0.8 mgA/hr/kg, the use environment being either the mammalian gastrointestinal tract or in vitro test medium which is acetate buffer, pH 4.0, and which is 0.075 M in NaCl; provided the dosage form (1) releases not more than 70% of the sertraline contained therein within the first hour following entry into the use environment and (2) releases sertraline at a rate of at least 0.02 mgA/hr/kg.
2. The dosage form as defined in claim 1, wherein the sertraline is present as sertraline free base.
3. The dosage form as defined in claim 1, wherein the sertraline is present as sertraline hydrochloride.
4. The dosage form as defined in claim 1, wherein the sertraline is present as sertraline aspartate.
5. The dosage form as defined in claim l, wherein the sertraline is present as sertraline acetate.
6. The dosage form as defined in claim 1, wherein the sertraline is present as sertraline lactate.
7. The dosage form as defined in any one of claims 1 to 6, wherein the mammal is a human.
8. The dosage form as defined in any one of claims 1 to 6, in the form of a matrix tablet which remains substantially intact during the period of sustained release.
9. The dosage form as defined in any one of claims 1 to 6, in the form of a matrix tablet which is a disintegrating matrix tablet.
10. The dosage form as defined in any one of claims 1 to 6, in the form of a matrix tablet which is partially coated with a polymer which impedes the release of sertraline.
11. The dosage form as defined in any one of claims 1 to 6, in the form of an osmotic tablet.
12. The dosage form as defined in any one of claims 1 to 6, in the form of a membrane-coated hydrogel tablet.
13. The dosage form as defined in any one of claims 1 to 6, which is multiparticulate.
14. The dosage form as defined in any one of claims 1 to 6, in the form of a membrane-coated diffusion-based, capsule, tablet or multiparticulate.
15. A sustained-release dosage form suitable for administration to a mammal in the form of a matrix tablet, an osmotic tablet, a membrane-coated hydrogel tablet, a multiparticulate, or a membrane-coated diffusion-based capsule, tablet or multiparticulate, comprising sertraline, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, which dosage form releases sertraline into a use environment at a rate not exceeding 40 mgA/hr, the use environment being either the mammalian gastrointestinal
tract or in vitro test medium which is acetate buffer, pH 4.0, and which is 0.075 M in NaCl; provided the dosage form (1) releases not more than 70% of the sertraline contained therein within the first hour following entry into the use environment and (2) releases sertraline at a rate of at least 1 mgA/hr.
16. The dosage form as defined in claim 15, wherein the sertraline is present as sertraline free base.
17. The dosage form as defined in claim 15, wherein the sertraline is present as sertraline hydrochloride.
18. The dosage form as defined in claim 15, wherein the sertraline is present as sertraline aspartate.
19. The dosage form as defined in claim 15, wherein the sertraline is present as sertraline acetate.
20. The dosage form as defined in claim 15, wherein the sertraline is present as sertraline lactate.
21. The dosage form as defined in any one of claims 15 to 20, wherein the mammal is a human.
22. The dosage form as defined in any one of claims 15 to 21, in the form of a matrix tablet which remains substantially intact during the period of sustained release.
23. The dosage form as defined in any one of claims 15 to 21, in the form of a matrix tablet which is a disintegrating matrix tablet.
24. The dosage form as defined in any one of claims 15 to 21, in the form of a matrix tablet which is partially coated with a polymer which impedes the release of sertraline.
25. The dosage form as defined in any one of claims 15 to 21, in the form of an osmotic tablet.
26. The dosage form as defined in any one of claims 15 to 21, in the form of a membrane-coated hydrogel tablet.
27. The dosage form as defined in any one of claims 15 to 21, which is multiparticulate.
28. The dosage form as defined in any one of claims 15 to 21, in the form of a membrane-coated diffusion-based tablet or multiparticulate.
29. A sustained release dosage form suitable for oral administration to a mammal in the form of a matrix tablet, an osmotic tablet, a membrane-coated hydrogel tablet, a multiparticulate, or a membrane-coated diffusion-based capsule, tablet or multiparticulate, comprising sertraline or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier, which dosage form releases sertraline at a rate less than 40 mgA/hr in vitro when dissolution tested in a USP-2 apparatus containing 900 ml of acetate buffer, pH 4.0, which is 0.075 M in NaCl, as follows: (1) if the dosage form is a sustained release tablet or a non-disintegrating sustained release capsule, the USP-2 apparatus is equipped with a paddle stirring at 50 rpm ; (2) if the dosage form is a multiparticulate, the
USP-2 apparatus is equipped with a paddle stirring at 100 rpm ; provided the dosage form (a) releases not more than 70% of the sertraline contained therein within the
first hour following initiation of testing and (b) releases sertraline at a rate of at least 1 mgA/hr.
30. The dosage form as defined in claim 29, wherein the sertraline is present as sertraline free base.
31. The dosage form as defined in claim 29, wherein the sertraline is present as sertraline hydrochloride.
32. The dosage form as defined in claim 29, wherein the sertraline is present as sertraline aspartate.
33. The dosage form as defined in claim 29, wherein the sertraline is present as sertraline acetate.
34. The dosage form as defined in claim 29, wherein the sertraline is present as sertraline lactate.
35. The dosage form as defined in any one of claims 29 to 34, wherein the mammal is a human.
36. The dosage form as defined in any one of claims 29 to 35, in the form of a matrix tablet which remains substantially intact during the period of sustained release.
37. The dosage form as defined in any one of claims 29 to 35, in the form of a matrix tablet which is a disintegrating matrix tablet.
38. The dosage form as defined in any one of claims 29 to 35, in the form of a matrix tablet which is partially coated with a polymer which impedes the release of sertraline.
39. The dosage form as defined in any one of claims 29 to 35, in the form of an osmotic tablet.
40. The dosage form as defined in any one of claims 29 to 35, in the form of a membrane-coated hydrogel tablet.
41. The dosage form as defined in any one of claims 29 to 35, which is multiparticulate.
42. The dosage form as defined in any one of claims 29 to 35, in the form of a membrane-coated diffusion-based tablet or multiparticulate.
43. A temporally delayed plus sustained release dosage form suitable for oral administration to a mammal, comprising sertraline or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier, which dosage form, following ingestion by the mammal, releases sertraline into said mammal's GI tract at a rate less than 1 mgA/hr for an initial delay period of up to 3 hours, and which thereafter releases sertraline at a rate of from 1 mgA/hr to 40 mgA/hr, provided the dosage form releases not more than 70% of the sertraline contained therein within the first hour after the delay period, and wherein the sustained release is achieved by a sustained release dosage form in the form of a tablet, a multiparticulate, or a matrix.
44. The dosage form as defined in claim 43, wherein the delay period is up to two hours.
45. The dosage form as defined in claim 43, wherein the rate of release following the delay period is from 1 mgA/hr to 30 mgA/hr.
46. The dosage form as defined in any one of claims 43 to 45, wherein the sertraline is present as sertraline free base.
47. The dosage form as defined in any one of claims 43 to 45, wherein the sertraline is present as sertraline hydrochloride.
48. The dosage form as defined in any one of claims 43 to 45, wherein the sertraline is present as sertraline aspartate.
49. The dosage form as defined in any one of claims 43 to 45, wherein the sertraline is present as sertraline acetate.
50. The dosage form as defined in any one of claims 43 to 45, wherein the sertraline is present as sertraline lactate.
51. The dosage form as defined in any one of claims 43 to 50, wherein the mammal is a human.
52. A temporally delayed plus sustained release dosage form suitable for administration to a mammal, the dosage form having an initial temporal delay period of up to 3 hours, comprising sertraline or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier, which dosage form, when dissolution tested in vitro in a USP-2 apparatus containing 900 ml of acetate buffer, pH 4.0, which is 0.075 M in NaCl, releases sertraline at a rate less than 1 mgA/hr for a period corresponding to said delay period and, thereafter,
releases sertraline at a rate of from 1 mgA/hr to 40 mgA/hr, provided the dosage form releases not more than 70% of the remaining sertraline contained therein within the first hour following said delay, and wherein the sustained release is achieved by a sustained release dosage form in the form of a tablet, a multiparticulate, or a matrix.
53. The dosage form as defined in claim 52, wherein the delay period is up to two hours.
54. The dosage form as defined in claim 52 or 53, wherein the rate of release following the delay period is from 1 mgA/hr to 30 mgA/hr.
55. The dosage form as defined in any one of claims 52 to 54, wherein the sertraline is present as sertraline free base.
56. ~The dosage form as defined in any one of claims 52 to 54, wherein the sertraline is present as sertraline hydrochloride.
57. ~The dosage form as defined in any one of claims 52 to 54, wherein the sertraline is present as sertraline aspartate.
58. ~The dosage form as defined in any one of claims 52 to 54, wherein the sertraline is present as sertraline acetate.
59. ~The dosage form as defined in any one of claims 52 to 54, wherein the sertraline is present as sertraline lactate.
60. ~The dosage form as defined in any one of claims 52 to 59, wherein said mammal is a human.
61. ~The dosage form as defined in any one of claims 52 to 59, in the form of a tablet.
62. ~The dosage form as defined in any one of claims 52 to 59, which is multiparticulate.
63. ~A spatially delayed plus sustained release dosage form suitable for oral administration to a mammal, comprising sertraline or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier,
which dosage form, following ingestion by the mammal, releses sertraline into said mammal's stomach at a rate less than 1 mgA/hr,
and which, after having passed into the mammal's small intestine, effects sustained release at a rate of from 1 mgA/hr to 40 mgA/hr,
provided the dosage form releases not more than 70% of the sertraline contained therein within the first hour after passing into the mammal's small intestine,
wherein the sustained release is achieved by a sustained release dosage form in the form of a tablet, a multiparticulate, or a matrix,
and wherein the spatial delay is achieved by coating the sustained release dosage form with a pH-triggered or enzyme-triggered coating.
64. ~The dosage form as defined in claim 63, wherein the onset of sustained release is pH-triggered.
65. ~The dosage form as defined in claim 64, wherein the coating is a polymer that prevents release of sertraline at the pH of the stomach, but which is permeable to sertraline at the pH of the small intestine.
66. ~The dosage form as defined in claim 64 or 65, wherein the sustained release dosage form is multiparticulate.
67. ~The dosage form as defined in claim 64 or 65, wherein the sustained release dosage form is a tablet.
68. ~The dosage form as defined in claim 63, which is enzyme-triggered.
69. ~The dosage form as defined in claim 68, wherein the coating is a membrane having a hydrophobic liquid entrained within the pores thereof, the hydrophobic liquid being substantially impermeable to water and sertraline, but capable of changing, through enzymatic degradation, so that the membrane becomes substantially permeable to water and
sertraline when the dosage form moves into the environment of the small intestinal lumen.
70. ~The dosage form as defined in claim 68 or 69, wherein the sustained release dosage form is multiparticulate.
71. ~The dosage form as defined in claim 68 or 69, wherein the sustained release dosage form is a matrix.
72. ~The dosage form as defined in any one of claims 63 to 71, wherein the sertraline is present as sertraline free base.
73. ~The dosage form as defined in any one of claims 63 to 71, wherein the sertraline is present as sertraline hydrochloride.
74. ~The dosage form as defined in any one of claims 63 to 71, wherein the sertraline is present as sertraline aspartate.
75. ~The dosage form as defined in any one of claims 63 to 71, wherein the sertraline is present as sertraline acetate.
76. ~The dosage form as defined in any one of claims 63 to 71, wherein the sertraline is present as sertraline lactate.
77. ~The dosage form as defined in any one of claims 63 to 76, wherein said mammal is a human.
78. ~A sustained release pH-triggered dosage form suitable for oral administration to a mammal, the dosage form having an initial delay period prior to the onset of sustained release, comprising sertraline or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier, which dosage form, when tested in vitro in a USP-2 apparatus,
releases sertraline into 0.1. N HCl. at a rate less than 1 mgA/hr for 1 hour and, thereafter,
releases sertraline into phosphate buffer, pH 6.8 containing 1% polysorbate 80 at a rate of from 1 mgA/hr to 40 mgA/hr, provided the dosage form releases not more than
70% of the remaining sertraline contained therein within the first hour following said delay.
79. ~The dosage form as defined in claim 78, comprising a sustained release dosage form coated with a coating comprising a polymer that prevents release of sertraline in the HCl at a rate exceeding 1 mgA/hr, but which is permeable to and allows sustained release of sertraline in said phosphate buffer.
80. ~The dosage form as defined in claim 78, wherein the sustained release dosage form is multiparticulate.
81. ~The dosage form as defined in claim 78, wherein the sustained release dosage form is a tablet.
82. ~The dosage form as defined in any one of claims 78 to 81, wherein the sertraline is present as sertraline free base.
83. ~The dosage form as defined in any one of claims 78 to 81, wherein the sertraline is present as sertraline hydrochloride.
84. ~The dosage form as defined in any one of claims 78 to 81, wherein the sertraline is present as sertraline aspartate.
85. ~The dosage form as defined in any one of claims 78 to 81, wherein the sertraline is present as sertraline acetate.
86. ~The dosage form as defined in any one of claims 78 to 81, wherein the sertraline is present as sertraline lactate.
87. ~The dosage form as defined in any one of claims 78 to 86, wherein the mammal is a human.
88. ~A sustained release enzyme-triggered dosage form suitable for oral administration to a mammal, the dosage form having an initial delay period prior to the onset of sustained release, comprising sertraline or a pharmaceutically acceptable salt thereof and a~ pharmaceutically acceptable carrier, which dosage form, when tested in vitro in a USP apparatus,
releases sertraline into 0.1 N HCl at a rate less than 1 mgA/hr for a period of 1 hour and, thereafter,
releases sertraline at a rate of 1 mgA/hr to 40 mgA/hr into phosphate buffer, pH 6.8, containing 1% polysorbate 80 and in the presence of an enzyme suitable for triggering the onset of the sustained release, provided the dosage form releases not more than 70% of the remaining sertraline contained therein within the first hour following the delay.
89. ~The dosage form as defined in claim 88, comprising a sustained release dosage form coated with a membrane having a hydrophobic liquid entrained within the pores thereof, the hydrophobic liquid being substantially impermeable to water and sertraline in the acid, but capable of changing in the buffer, through enzymatic degradation in the presence of the enzyme, so that the membrane becomes substantially permeable to water and sertraline.
90. ~The dosage form as defined in claim 88 or 89, wherein the sustained release dosage form is multiparticulate.
91. ~The dosage form as defined in claim 88 or 89, wherein the sustained release dosage form is a tablet.
92. ~The dosage form as defined in any one of claims 88 to 91, wherein the sertraline is present as sertraline free base.
93. ~The dosage form as defined in any one of claims 88 to 91, wherein the sertraline is present as sertraline hydrochloride.
94. ~The dosage form as defined in any one of claims 88 to 91, wherein the sertraline is present as sertraline aspartate.
95. ~The dosage form as defined in any one of claims 88 to 91, wherein the sertraline is present as sertraline acetate.
96. ~The dosage form as defined in any one of claims 88 to 91, wherein the sertraline is present as sertraline lactate.
97. ~The dosage form as defined in any one of claims 88 to 96, wherein the mammal is a human.
98. ~A sustained release dosage form suitable for oral administration to a mammal, comprising sertraline, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, which dosage form, when orally dosed to the mammal, results in a maximum sertraline plasma concentration, C max. which is less than 80% of the C max determined when an equal dose of sertraline is orally administered in the form of an immediate release bolus provided the sustained release dosage form (1) releases not more than 70% of the sertraline contained therein within the first hour following ingestion and (2) releases sertraline at a rate of at least 1 mgA/hr, wherein the sustained
release dosage form is in the form of a tablet, a multiparticulate, or a matrix.
99. ~The dosage form as defined in claim 98, which provides a total blood drug exposure that is not proportionately decreased as much as C max.
100. ~The dosage form as defined in claim 98 or 99, wherein the sertraline is present as sertraline free base.
101. ~The dosage form as defined in claim 98 or 99, wherein the sertraline is present as sertraline hydrochloride.
102. ~The dosage form as defined in claim 98 or 99, wherein the sertraline is present as sertraline aspartate.
103. ~The dosage form as defined in claim 98 or 99, wherein the sertraline is present as sertraline acetate.
104. ~The dosage form as defined in claim 98 or 99, wherein the sertraline is present as sertraline lactate.
105. ~The dosage form as defined in any one of claims 98 to 104, wherein the mammal is a human.
106. ~The dosage form as defined in any one of claims 98 to 105, in the form of a tablet.
107. ~The dosage form as defined in any one of claims 98 to 105, which is multiparticulate.
108. ~The dosage form as defined in any one of claims 98 to 105, which is a delayed plus sustained release form exhibiting a delay period of up to three hours prior to the onset of sustained release, said dosage form releasing sertraline at a rate of not more than 1 mgA/hr during said delay period.
109. ~The dosage form as defined in claim 108, wherein the delay is temporal.
110. ~The dosage form as defined in claim 108, wherein the delay is spatial.
111. ~A use of the sustained-release dosage form according to any one of claims 1 to 14 for treating a~ psychiatric illness, premature ejaculation, chemical dependency, premenstrual dysphoric disorder, or obesity in a patient in need of such treatment.
112. ~A use of the sustained-release dosage form according to any one of claims 15 to 28 for treating a psychiatric illness, premature ejaculation, chemical dependency, premenstrual dysphoric disorder, or obesity in a patient in need of such treatment.
113. ~A use of the sustained-release dosage form according to any one of claims 29 to 42 for treating a psychiatric illness, premature ejaculation, chemical dependency, premenstrual dysphoric disorder, or obesity in a patient in need of such treatment.
114. ~A use of the sustained-release dosage form according to any one of claims 43 to 51 for treating a psychiatric illness, premature ejaculation, chemical dependency, premenstrual dysphoric disorder, or obesity in a~ patient in need of such treatment.
115. ~A use of the sustained-release dosage form according to any one of claims 52 to 62 for treating a psychiatric illness, premature ejaculation, chemical dependency, premenstrual dysphoric disorder, or obesity
in a patient in need of such treatment.
116. ~A use of the sustained-release dosage form according to any one of claims 63 to 77 for treating a psychiatric illness, premature ejaculation, chemical dependency, premenstrual dysphoric disorder, or obesity in a patient in need of such treatment.
117. ~A use of the sustained-release dosage form according to any one of claims 78 to 87 for treating a psychiatric illness, premature ejaculation, chemical dependency, premenstrual dysphoric disorder, or obesity in a patient in need of such treatment.
118. ~A use of the sustained-release dosage form according to any one of claims 88 to 97 for treating a psychiatric illness, premature ejaculation, chemical dependency, premenstrual dysphoric disorder, or obesity in a patient in need of such treatment.
119. ~A use of the sustained-release dosage form according to any one of claims 98 to 110 for treating a psychiatric illness, premature ejaculation, chemical dependency, premenstrual dysphoric disorder, or obesity in a patient in need of such treatment.
120. ~Sertraline acetate.
121. ~Sertraline acetate of claim 120 having the X-ray crystal structure of Figure 1.
122. ~Sertraline acetate ~ 1/4 hydrate.
123. ~A pharmaceutical composition comprising sertraline acetate of claim 120 and a pharmaceutically acceptable carrier or diluent.
124. ~A pharmaceutical composition comprising sertraline acetate of claim 121 and a pharmaceutically acceptable carrier or diluent.
125. ~A pharmaceutical composition comprising sertraline acetate ∙ 1/4 hydrate of claim 122 and a pharmaceutically acceptable carrier or diluent.
126. ~A pharmaceutical composition for treating a disease or condition selected from anorexia, impulse disorders, onychophagia, premenstrual syndrome, psychotic disorders of the schizophrenictype, inflammatory disorders, hyperactive immune system disorders, and chemical dependency in a subject suffering from one or more of the diseases or conditions comprising an effective amount of sertraline acetate and a pharmaceutically acceptable carrier or diluent.
127. ~A pharmaceutical composition for treating a disease or condition selected from anorexia, impulse disorders, onychophagia, premenstrual syndrome, psychotic disorders of the schizophrenictype, inflammatory disorders, hyperactive immune system disorders, and chemical dependency in a subject suffering from one or more of the diseases or conditions comprising an effective amount of sertraline acetate of claim 121 and a pharmaceutically acceptable carrier or diluent.
128. ~A pharmaceutical composition for treating a disease or condition selected from anorexia, impulse disorders, onychophagia, premenstrual syndrome, psychotic disorders of the schizophrenictype, inflammatory disorders,
hyperactive immune system disorders, and chemical dependency in a subject suffering from one or more of the diseases or conditions comprising an effective amount of sertraline acetate ~ 1/4 hydrate and a pharmaceutically acceptable carrier or diluent.
129. ~A pharmaceutical composition for treating mental depression in a mentally-depressed subject comprising an effective amount of sertraline acetate and a~ pharmaceutically acceptable carrier or diluent.
130. ~A pharmaceutical composition for treating mental depression in a mentally-depressed subject comprising an effective amount of sertraline acetate of claim 121 and a pharmaceutically acceptable carrier or diluent.
131. ~A pharmaceutical composition for treating mental depression in a mentally-depressed subject comprising an effective amount of sertraline acetate ~ 1/4 hydrate and a pharmaceutically acceptable carrier or diluent.
132. ~A pharmaceutical composition for treating an anxiety-related disorder in a subject suffering therefrom comprising an effective amount of sertraline acetate and a pharmaceutically acceptable carrier or diluent.
133. ~A pharmaceutical composition for treating an anxiety-related disorder in a subject suffering therefrom comprising an effective amount of sertraline acetate of claim 121 and a pharmaceutically acceptable carrier or diluent.
134. ~A pharmaceutical composition for treating an anxiety-related disorder in a subject suffering therefrom comprising an effective amount of sertraline acetate ~ 1/4
hydrate and a pharmaceutically acceptable carrier or diluent.
135. ~Sertraline L-lactate.
136. ~Sertraline L-lactate of claim 135 having the X-ray crystal structure of Figure 3.
137. ~A pharmaceutical composition comprising sertraline
L-lactate of claim 135 and a pharmaceutically acceptable carrier or diluent.
138. ~A pharmaceutical composition comprising sertraline
L-lactate of claim 136 and a pharmaceutically acceptable carrier or diluent.
139. ~A pharmaceutical composition for treating a disease or condition selected from anorexia, impulse disorders, onychophagia, premenstrual syndrome, psychotic disorders of the schizophrenictype, inflammatory disorders, hyperactive immune system disorders, and chemical dependency in a subject suffering from one or more of the diseases or conditions comprising an effective amount of sertraline
L-lactate and a pharmaceutically acceptable carrier or diluent.
140. ~A pharmaceutical composition for treating a disease or condition selected from anorexia, impulse disorders, onychophagia, premenstrual syndrome, psychotic disorders of the schizophrenictype, inflammatory disorders, hyperactive immune system disorders, and chemical dependency in a subject suffering from one or more of the diseases or conditions comprising an effective amount of sertraline
L-lactate of claim 136 and a pharmaceutically acceptable carrier or diluent.
141. ~A pharmaceutical composition for treating mental depression in a mentally-depressed subject comprising an effective amount of sertraline L-lactate and a pharmaceutically acceptable carrier or diluent.
142. ~A pharmaceutical composition for treating mental depression in a mentally-depressed subject comprising an effective amount of sertraline L-lactate of claim 136 and a pharmaceutically acceptable carrier or diluent.
143. ~A pharmaceutical composition for treating an anxiety-related disorder in a subject suffering therefrom comprising an effective amount of sertraline L-lactate and a pharmaceutically acceptable carrier or diluent.
144. ~A pharmaceutical composition for treating an anxiety-related disorder in a subject suffering therefrom comprising an effective amount of sertraline L-lactate of claim 136 and a pharmaceutically acceptable carrier or diluent.
145. ~Sertraline L-aspartate.
146. ~A pharmaceutical composition comprising sertraline
L-aspartate of claim 145 and a pharmaceutically acceptable carrier or diluent.
147. ~A pharmaceutical composition for treating a~ disease or condition selected from anorexia, impulse disorders, onychophagia, premenstrual syndrome, psychotic disorders of the schizophrenictype, inflammatory disorders, hyperactive immune system disorders, and chemical dependency in a subject suffering from one or more of the diseases or conditions comprising an effective amount of sertraline Laspartate and a pharmaceutically acceptable carrier or diluent.
148. ~A pharmaceutical composition for treating mental depression in a mentally-depressed subject comprising an effective amount of sertraline L-aspartate and a pharmaceutically acceptable carrier or diluent.
149. ~A pharmaceutical composition for treating an anxiety-related disorder in a subject suffering therefrom comprising an effective amount of sertraline L-aspartate and a pharmaceutically acceptable carrier or diluent.
150. ~The pharmaceutical composition according to any one of claims 132 to 134, wherein the anxiety-related disorder is obsessive-compulsive disorder.
151. ~The pharmaceutical composition according to claim 143 or 144, wherein the anxiety-related disorder is obsessive-compulsive disorder.
152. ~The pharmaceutical composition according to claim 149, wherein the anxiety-related disorder is obsessive-compulsive disorder.
153. ~A use of sertraline acetate in the manufacture of a medicament for the treatment of a psychiatric illness, premature ejaculation, chemical dependency, premenstrual dysphoric disorder, or obesity.
154. ~A use of sertraline acetate according to claim 121 in the manufacture of a medicament for the treatment of a psychiatric illness, premature ejaculation, chemical dependency, premenstrual dysphoric disorder, or obesity.
155. ~A use of sertraline acetate ~ 1/4 hydrate in the manufacture of a medicament for the treatment of a psychiatric illness, premature ejaculation, chemical dependency, premenstrual dysphoric disorder, or obesity.
156. ~A use of sertraline acetate in the manufacture of a medicament for the treatment of a disease or condition selected from anorexia, impulse disorders, onychophagia, premenstrual syndrome, psychotic disorders of the schizophrenictype, inflammatory disorders, hyperactive immune system disorders, and chemical dependency.
157. ~A use of sertraline acetate according to claim 121 in the manufacture of a medicament for the treatment of a disease or condition selected from anorexia, impulse disorders, onychophagia, premenstrual syndrome, psychotic disorders of the schizophrenictype, inflammatory disorders, hyperactive immune system disorders, and chemical dependency.
158. ~A use of sertraline acetate ~ 1/4 hydrate in the manufacture of a medicament for the treatment of a disease or condition selected from anorexia, impulse disorders, onychophagia, premenstrual syndrome, psychotic disorders of the schizophrenictype, inflammatory disorders, hyperactive immune system disorders, and chemical dependency.
159. ~A use of sertraline acetate in the manufacture of a medicament for the treatment of mental depression.
160. ~A use of sertraline acetate according to claim 121 in the manufacture of medicament for the treatment of mental depression.
161. ~A use of sertraline acetate ~ 1/4 hydrate in the manufacture of a medicament for the treatment of mental depression.
162. ~A use of sertraline acetate in the manufacture of a medicament for the treatment of anxiety-related disorder.
163. ~A use of sertraline acetate according to claim 121 in the manufacture of a medicament for the treatment of anxiety-related disorder.
164. ~A use of sertraline acetate ~ 1/4 hydrate in the manufacture of a medicament for the treatment of anxietyrelated disorder.
165. ~The use according to any one of claims 162 to 164, wherein the anxiety-related disorder is obsessive-compulsive disorder.
166. ~A use of sertraline L-lactate for the manufacture of a medicament for the treatment of a psychiatric illness, premature ejaculation, chemical dependency, premenstrual dysphoric disorder, or obesity.
167. ~A use of sertraline L-lactate according to claim 136 for the manufacture of a medicament for the treatment of a psychiatric illness, premature ejaculation, chemical dependency, premenstrual dysphoric disorder, or obesity.
168. ~A use of sertraline L-lactate for the manufacture of a medicament for the treatment of a disease or condition selected from anorexia, impulse disorders, onychophagia, premenstrual syndrome, psychotic disorders of the schizophrenictype, inflammatory disorders, hyperactive immune system disorders, and chemical dependency.
169. ~A use of sertraline L-lactate according to claim 136 for the treatment of a disease or condition selected from anorexia, impulse disorders, onychophagia, premenstrual syndrome, psychotic disorders of the schizophrenictype, inflammatory disorders, hyperactive immune system disorders, and chemical dependency.
170. ~A use of sertraline L-lactate for the manufacture of a medicament for the treatment of mental depression.
171. ~A use of sertraline L-lactate according to claim 136 for the manufacture of a medicament for the treatment of mental depression.
172. ~A use of sertraline L-lactate for the manufacture of a medicament for the treatment of anxiety-related disorder.
173. ~A use of sertraline L-lactate according to claim 136 for the manufacture of a medicament for the treatment of anxiety-related disorder.
174. ~The use according to claim 172 or 173, wherein the anxiety-related disorder is obsessive-compulsive disorder.
175. ~A use of sertraline L-aspartate for the manufacture of a medicament for the treatment of a~ psychiatric illness, premature ejaculation, chemical dependency, premenstrual dysphoric disorder, or obesity.
176. ~A use of sertraline L-aspartate for the manufacture of a medicament for the treatment of a disease or condition selected from anorexia, impulse disorders, onychophagia, premenstrual syndrome, psychotic disorders of the schizophrenictype, inflammatory disorders, hyperactive immune system disorders, and chemical dependency.
177. ~A use of sertraline L-aspartate for the manufacture of a medicament for the treatment of mental depression.
178. ~A use of sertraline L-aspartate for the manufacture of a medicament for the treatment of anxietyrelated disorder.
179. ~The use according to claim 178, wherein the anxiety-related disorder is obsessive-compulsive disorder.
180. ~A process for preparing sertraline acetate comprising reacting a salt of sertraline with a base in the presence of a suitable organic solvent to form sertraline free base, partitioning said sertraline free base into an organic solvent: and reacting said sertraline free base with acetic acid in the presence of a suitable organic solvent.
181. ~The process of claim 180, wherein the salt of sertraline is sertraline hydrochloride and said solvent is hexane.
182. ~A process for preparing sertraline acetate comprising reacting sertraline free base with acetic acid in the presence of a suitable organic solvent.
183. ~A process for preparing sertraline L-lactate comprising reacting a salt of sertraline with a base in the presence of a suitable organic solvent to form sertraline free base, partitioning said sertraline free base into an organic solvent and reacting said sertraline free base with
L-lactic acid in the presence of a suitable organic solvent.
184. ~The process of claim 183, wherein the salt of sertraline is sertraline hydrochloride and said solvent is ethyl acetate.
185. ~The process of claim 183, wherein the salt of sertraline is sertraline mandelate and the solvent is ethyl acetate.
186. ~A process for preparing sertraline L-lactate comprising reacting sertraline free base with L-lactic acid in the presence of a suitable organic solvent.
187. ~A process for preparing sertraline L-aspartate comprising reacting a salt of sertraline with a base in the presence of a suitable organic solvent to form sertraline free base, partitioning the sertraline free base into an organic solvent and reacting the sertraline free base with aspartic acid in the presence of a suitable organic solvent.
188. ~The process of claim 187, wherein the salt of sertraline is sertraline hydrochloride and the solvent is ethyl acetate saturated with water.
189. ~A process for preparing sertraline L-aspartate comprising reacting sertraline free base with L-aspartic acid in the presence of a suitable organic solvent.
190. ~A commercial package comprising:
a) the dosage form of any one of claims 1 to 110, and
b) instructions for the use thereof for treating a psychiatric illness, premature ejaculation, chemical dependency, premenstrual dysphoric disorder, or obesity in a~ patient in need of such treatment.
191. ~A commercial package comprising:
a) the pharmaceutical composition of any one of claims 126 to 134, 139 to 144 and 147 to 152, and
b) instructions for the use thereof.