IL126892A - Pharmaceutical compositions for the sustained release of at least one water-insoluble active principle - Google Patents

Pharmaceutical compositions for the sustained release of at least one water-insoluble active principle

Info

Publication number: IL126892A
Authority: IL; Israel
Prior art keywords: pharmaceutical composition; fact; composition according; active principle; approximately
Prior art date: 1996-05-06

Application number

IL12689297A

Other languages

English (en)

Other versions

IL126892A0 (en

Original Assignee

Debio Rech Pharma Sa

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

1996-05-06

Filing date

1997-04-28

Publication date

2004-07-25

1997-04-28 Application filed by Debio Rech Pharma Sa filed Critical Debio Rech Pharma Sa

1999-09-22 Publication of IL126892A0 publication Critical patent/IL126892A0/xx

2004-07-25 Publication of IL126892A publication Critical patent/IL126892A/en

Links

239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 29
238000013268 sustained release Methods 0.000 title description 4
239000012730 sustained-release form Substances 0.000 title description 4
JVTAAEKCZFNVCJ-REOHCLBHSA-N L-lactic acid Chemical compound C[C@H](O)C(O)=O JVTAAEKCZFNVCJ-REOHCLBHSA-N 0.000 claims abstract description 26
238000013270 controlled release Methods 0.000 claims abstract description 13
229920001519 homopolymer Polymers 0.000 claims abstract description 10
150000003839 salts Chemical class 0.000 claims abstract description 7
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 5
102000004169 proteins and genes Human genes 0.000 claims abstract description 3
108090000623 proteins and genes Proteins 0.000 claims abstract description 3
102000015731 Peptide Hormones Human genes 0.000 claims abstract 2
108010038988 Peptide Hormones Proteins 0.000 claims abstract 2
229920000642 polymer Polymers 0.000 claims description 18
239000007943 implant Substances 0.000 claims description 17
239000004005 microsphere Substances 0.000 claims description 9
NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims description 4
POMLZACZLQPRMY-NCACADTJSA-N (4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-N-[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-propan-2-yl-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide 4-[(3-carboxy-2-hydroxynaphthalen-1-yl)methyl]-3-hydroxynaphthalene-2-carboxylic acid Chemical group C1=CC=C2C(CC=3C4=CC=CC=C4C=C(C=3O)C(=O)O)=C(O)C(C(O)=O)=CC2=C1.C([C@H]1C(=O)N[C@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(N[C@@H](CSSC[C@@H](C(=O)N1)NC(=O)[C@H](N)CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(N)=O)=O)C(C)C)C1=CC=C(O)C=C1 POMLZACZLQPRMY-NCACADTJSA-N 0.000 claims description 3
NHXLMOGPVYXJNR-ATOGVRKGSA-N somatostatin Chemical compound C([C@H]1C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N1)[C@@H](C)O)NC(=O)CNC(=O)[C@H](C)N)C(O)=O)=O)[C@H](O)C)C1=CC=CC=C1 NHXLMOGPVYXJNR-ATOGVRKGSA-N 0.000 claims description 3
101800001288 Atrial natriuretic factor Proteins 0.000 claims description 2
102400001282 Atrial natriuretic peptide Human genes 0.000 claims description 2
101800001890 Atrial natriuretic peptide Proteins 0.000 claims description 2
108060001064 Calcitonin Chemical class 0.000 claims description 2
101000904177 Clupea pallasii Gonadoliberin-1 Chemical class 0.000 claims description 2
101800000414 Corticotropin Chemical class 0.000 claims description 2
239000000055 Corticotropin-Releasing Hormone Chemical class 0.000 claims description 2
102000009025 Endorphins Human genes 0.000 claims description 2
108010049140 Endorphins Proteins 0.000 claims description 2
102400001368 Epidermal growth factor Human genes 0.000 claims description 2
101800003838 Epidermal growth factor Proteins 0.000 claims description 2
102400000321 Glucagon Human genes 0.000 claims description 2
108060003199 Glucagon Proteins 0.000 claims description 2
239000000579 Gonadotropin-Releasing Hormone Chemical class 0.000 claims description 2
102000002746 Inhibins Human genes 0.000 claims description 2
108010004250 Inhibins Proteins 0.000 claims description 2
102000004877 Insulin Human genes 0.000 claims description 2
108090001061 Insulin Proteins 0.000 claims description 2
102000014150 Interferons Human genes 0.000 claims description 2
108010050904 Interferons Proteins 0.000 claims description 2
102400000050 Oxytocin Human genes 0.000 claims description 2
101800000989 Oxytocin Proteins 0.000 claims description 2
XNOPRXBHLZRZKH-UHFFFAOYSA-N Oxytocin Natural products N1C(=O)C(N)CSSCC(C(=O)N2C(CCC2)C(=O)NC(CC(C)C)C(=O)NCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(CCC(N)=O)NC(=O)C(C(C)CC)NC(=O)C1CC1=CC=C(O)C=C1 XNOPRXBHLZRZKH-UHFFFAOYSA-N 0.000 claims description 2
102100027467 Pro-opiomelanocortin Human genes 0.000 claims description 2
108010057464 Prolactin Proteins 0.000 claims description 2
102100024819 Prolactin Human genes 0.000 claims description 2
108010056088 Somatostatin Proteins 0.000 claims description 2
102000005157 Somatostatin Human genes 0.000 claims description 2
101000857870 Squalus acanthias Gonadoliberin Chemical class 0.000 claims description 2
229920002253 Tannate Polymers 0.000 claims description 2
GXBMIBRIOWHPDT-UHFFFAOYSA-N Vasopressin Chemical class N1C(=O)C(CC=2C=C(O)C=CC=2)NC(=O)C(N)CSSCC(C(=O)N2C(CCC2)C(=O)NC(CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(CCC(N)=O)NC(=O)C1CC1=CC=CC=C1 GXBMIBRIOWHPDT-UHFFFAOYSA-N 0.000 claims description 2
108010004977 Vasopressins Chemical class 0.000 claims description 2
102000002852 Vasopressins Human genes 0.000 claims description 2
KBZOIRJILGZLEJ-LGYYRGKSSA-N argipressin Chemical class C([C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CSSC[C@@H](C(N[C@@H](CC=2C=CC(O)=CC=2)C(=O)N1)=O)N)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C1=CC=CC=C1 KBZOIRJILGZLEJ-LGYYRGKSSA-N 0.000 claims description 2
229960004015 calcitonin Drugs 0.000 claims description 2
BBBFJLBPOGFECG-VJVYQDLKSA-N calcitonin Chemical class N([C@H](C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(N)=O)C(C)C)C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 BBBFJLBPOGFECG-VJVYQDLKSA-N 0.000 claims description 2
NSQLIUXCMFBZME-MPVJKSABSA-N carperitide Chemical compound C([C@H]1C(=O)NCC(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@H](C(NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CSSC[C@@H](C(=O)N1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(O)=O)=O)[C@@H](C)CC)C1=CC=CC=C1 NSQLIUXCMFBZME-MPVJKSABSA-N 0.000 claims description 2
IDLFZVILOHSSID-OVLDLUHVSA-N corticotropin Chemical class C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)NC(=O)[C@@H](N)CO)C1=CC=C(O)C=C1 IDLFZVILOHSSID-OVLDLUHVSA-N 0.000 claims description 2
229960000258 corticotropin Drugs 0.000 claims description 2
229940116977 epidermal growth factor Drugs 0.000 claims description 2
MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 claims description 2
229960004666 glucagon Drugs 0.000 claims description 2
XLXSAKCOAKORKW-AQJXLSMYSA-N gonadorelin Chemical class C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)NCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 XLXSAKCOAKORKW-AQJXLSMYSA-N 0.000 claims description 2
IPCSVZSSVZVIGE-UHFFFAOYSA-M hexadecanoate Chemical compound CCCCCCCCCCCCCCCC([O-])=O IPCSVZSSVZVIGE-UHFFFAOYSA-M 0.000 claims description 2
239000000893 inhibin Substances 0.000 claims description 2
239000003112 inhibitor Substances 0.000 claims description 2
ZPNFWUPYTFPOJU-LPYSRVMUSA-N iniprol Chemical compound C([C@H]1C(=O)NCC(=O)NCC(=O)N[C@H]2CSSC[C@H]3C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@H](C(N[C@H](C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=4C=CC(O)=CC=4)C(=O)N[C@@H](CC=4C=CC=CC=4)C(=O)N[C@@H](CC=4C=CC(O)=CC=4)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC=4C=CC=CC=4)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC2=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](CC=2C=CC=CC=2)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H]2N(CCC2)C(=O)[C@@H](N)CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N2[C@@H](CCC2)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC(O)=CC=2)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N2[C@@H](CCC2)C(=O)N3)C(=O)NCC(=O)NCC(=O)N[C@@H](C)C(O)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@H](C(=O)N1)C(C)C)[C@@H](C)O)[C@@H](C)CC)=O)[C@@H](C)CC)C1=CC=C(O)C=C1 ZPNFWUPYTFPOJU-LPYSRVMUSA-N 0.000 claims description 2
229940125396 insulin Drugs 0.000 claims description 2
229940079322 interferon Drugs 0.000 claims description 2
QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 2
229960001723 oxytocin Drugs 0.000 claims description 2
XNOPRXBHLZRZKH-DSZYJQQASA-N oxytocin Chemical class C([C@H]1C(=O)N[C@H](C(N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CSSC[C@H](N)C(=O)N1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)=O)[C@@H](C)CC)C1=CC=C(O)C=C1 XNOPRXBHLZRZKH-DSZYJQQASA-N 0.000 claims description 2
230000001175 peptic effect Effects 0.000 claims description 2
229940097325 prolactin Drugs 0.000 claims description 2
229960000553 somatostatin Drugs 0.000 claims description 2
VBEQCZHXXJYVRD-GACYYNSASA-N uroanthelone Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)C(C)C)[C@@H](C)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CCSC)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CS)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CS)NC(=O)CNC(=O)[C@H]1N(CCC1)C(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC(N)=O)C(C)C)[C@@H](C)CC)C1=CC=C(O)C=C1 VBEQCZHXXJYVRD-GACYYNSASA-N 0.000 claims description 2
229960003726 vasopressin Drugs 0.000 claims description 2
SWXOGPJRIDTIRL-DOUNNPEJSA-N (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-n-[(2s)-1-amino-3-(1h-indol-3-yl)-1-oxopropan-2-yl]-19-[[(2r)-2-amino-3-phenylpropanoyl]amino]-16-[(4-hydroxyphenyl)methyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-propan-2-yl-1,2-dithia-5,8,11,14,17-pent Chemical compound C([C@H]1C(=O)N[C@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(N[C@@H](CSSC[C@@H](C(=O)N1)NC(=O)[C@H](N)CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(N)=O)=O)C(C)C)C1=CC=C(O)C=C1 SWXOGPJRIDTIRL-DOUNNPEJSA-N 0.000 claims 1
102000055006 Calcitonin Human genes 0.000 claims 1
108010051696 Growth Hormone Proteins 0.000 claims 1
108010071384 Peptide T Proteins 0.000 claims 1
102100038803 Somatotropin Human genes 0.000 claims 1
239000000122 growth hormone Substances 0.000 claims 1
108700029852 vapreotide Proteins 0.000 claims 1
229960002730 vapreotide Drugs 0.000 claims 1
239000000203 mixture Substances 0.000 description 22
238000009472 formulation Methods 0.000 description 17
238000000034 method Methods 0.000 description 7
229940079593 drug Drugs 0.000 description 5
239000003814 drug Substances 0.000 description 5
238000001125 extrusion Methods 0.000 description 4
229920002988 biodegradable polymer Polymers 0.000 description 3
239000004621 biodegradable polymer Substances 0.000 description 3
229940088597 hormone Drugs 0.000 description 3
239000005556 hormone Substances 0.000 description 3
229920000747 poly(lactic acid) Polymers 0.000 description 3
230000000750 progressive effect Effects 0.000 description 3
230000002459 sustained effect Effects 0.000 description 3
238000002560 therapeutic procedure Methods 0.000 description 3
238000011282 treatment Methods 0.000 description 3
CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 2
241001465754 Metazoa Species 0.000 description 2
241000700159 Rattus Species 0.000 description 2
239000013543 active substance Substances 0.000 description 2
229920001577 copolymer Polymers 0.000 description 2
238000001035 drying Methods 0.000 description 2
JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
238000002360 preparation method Methods 0.000 description 2
108090000765 processed proteins & peptides Proteins 0.000 description 2
102400000113 Calcitonin Human genes 0.000 description 1
206010013654 Drug abuse Diseases 0.000 description 1
AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Polymers OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 1
239000000095 Growth Hormone-Releasing Hormone Substances 0.000 description 1
229920000954 Polyglycolide Polymers 0.000 description 1
102100028255 Renin Human genes 0.000 description 1
108090000783 Renin Proteins 0.000 description 1
VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
102100022831 Somatoliberin Human genes 0.000 description 1
101710142969 Somatoliberin Proteins 0.000 description 1
238000013019 agitation Methods 0.000 description 1
239000007864 aqueous solution Substances 0.000 description 1
239000008280 blood Substances 0.000 description 1
210000004369 blood Anatomy 0.000 description 1
239000002775 capsule Substances 0.000 description 1
239000001569 carbon dioxide Substances 0.000 description 1
229910002092 carbon dioxide Inorganic materials 0.000 description 1
230000015556 catabolic process Effects 0.000 description 1
238000005354 coacervation Methods 0.000 description 1
238000007906 compression Methods 0.000 description 1
230000006835 compression Effects 0.000 description 1
229940124558 contraceptive agent Drugs 0.000 description 1
239000003433 contraceptive agent Substances 0.000 description 1
238000006731 degradation reaction Methods 0.000 description 1
239000006185 dispersion Substances 0.000 description 1
238000004090 dissolution Methods 0.000 description 1
230000000694 effects Effects 0.000 description 1
238000005516 engineering process Methods 0.000 description 1
230000035558 fertility Effects 0.000 description 1
238000001914 filtration Methods 0.000 description 1
238000010438 heat treatment Methods 0.000 description 1
238000001794 hormone therapy Methods 0.000 description 1
238000002513 implantation Methods 0.000 description 1
238000002347 injection Methods 0.000 description 1
239000007924 injection Substances 0.000 description 1
239000004310 lactic acid Substances 0.000 description 1
235000014655 lactic acid Nutrition 0.000 description 1
238000011866 long-term treatment Methods 0.000 description 1
239000011159 matrix material Substances 0.000 description 1
229940127554 medical product Drugs 0.000 description 1
VUZPPFZMUPKLLV-UHFFFAOYSA-N methane;hydrate Chemical compound C.O VUZPPFZMUPKLLV-UHFFFAOYSA-N 0.000 description 1
239000003094 microcapsule Substances 0.000 description 1
239000004570 mortar (masonry) Substances 0.000 description 1
238000011328 necessary treatment Methods 0.000 description 1
238000011275 oncology therapy Methods 0.000 description 1
239000003960 organic solvent Substances 0.000 description 1
206010033675 panniculitis Diseases 0.000 description 1
238000007911 parenteral administration Methods 0.000 description 1
239000000825 pharmaceutical preparation Substances 0.000 description 1
229940127557 pharmaceutical product Drugs 0.000 description 1
239000004626 polylactic acid Substances 0.000 description 1
229920001184 polypeptide Polymers 0.000 description 1
238000001556 precipitation Methods 0.000 description 1
102000004196 processed proteins & peptides Human genes 0.000 description 1
230000002035 prolonged effect Effects 0.000 description 1
230000005855 radiation Effects 0.000 description 1
230000001105 regulatory effect Effects 0.000 description 1
239000013557 residual solvent Substances 0.000 description 1
238000007873 sieving Methods 0.000 description 1
239000000243 solution Substances 0.000 description 1
239000002904 solvent Substances 0.000 description 1
210000004304 subcutaneous tissue Anatomy 0.000 description 1
239000000126 substance Substances 0.000 description 1
208000011117 substance-related disease Diseases 0.000 description 1
238000006467 substitution reaction Methods 0.000 description 1
239000003826 tablet Substances 0.000 description 1
230000001225 therapeutic effect Effects 0.000 description 1

Classifications

- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
- A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)

Landscapes

Health & Medical Sciences (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Epidemiology (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Chemical & Material Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Medicinal Preparation (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

IL12689297A 1996-05-06 1997-04-28 Pharmaceutical compositions for the sustained release of at least one water-insoluble active principle IL126892A (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
FR9605630A FR2748205A1 (fr)	1996-05-06	1996-05-06	Compositions pharmaceutiques pour la liberation controlee de principes actifs insolubles
PCT/EP1997/002187 WO1997041836A1 (fr)	1996-05-06	1997-04-28	Compositions pharmaceutiques pour la liberation prolongee de principes actifs insolubles

Publications (2)

Publication Number	Publication Date
IL126892A0 IL126892A0 (en)	1999-09-22
IL126892A true IL126892A (en)	2004-07-25

Family

ID=9491862

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
IL12689297A IL126892A (en)	1996-05-06	1997-04-28	Pharmaceutical compositions for the sustained release of at least one water-insoluble active principle

Country Status (9)

Country	Link
US (1)	US6245346B1 (fr)
EP (1)	EP0896527A1 (fr)
JP (1)	JP2000509403A (fr)
AU (1)	AU710539B2 (fr)
CA (1)	CA2253377A1 (fr)
FR (1)	FR2748205A1 (fr)
IL (1)	IL126892A (fr)
NO (1)	NO985145D0 (fr)
WO (1)	WO1997041836A1 (fr)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
DE10024451A1 (de) *	2000-05-18	2001-11-29	Asta Medica Ag	Pharmazeutische Darreichungsform für Peptide, Verfahren zu deren Herstellung und Verwendung
WO2002058671A1 (fr) *	2001-01-26	2002-08-01	Debio Recherche Pharmaceutique S.A.	Microparticules pharmaceutiques exemptes d"eclatement
WO2003000156A1 (fr)	2001-06-22	2003-01-03	Southern Biosystems, Inc.	Implants coaxiaux a liberation prolongee d'ordre 0
GB0122113D0 (en) *	2001-09-11	2001-10-31	Astrazeneca Ab	Composition
US6987111B2 (en) *	2003-08-06	2006-01-17	Alkermes Controlled Therapeutics, Ii	Aripiprazole, olanzapine and haloperidol pamoate salts
WO2006078320A2 (fr)	2004-08-04	2006-07-27	Brookwood Pharmaceuticals, Inc.	Procede de production de systemes d'administration, et systemes d'administration
PT1941798E (pt)	2004-12-17	2012-08-22	Devgen Nv	Composições nematodicidas
US20070106271A1 (en) *	2005-11-09	2007-05-10	Searete Llc, A Limited Liability Corporation	Remote control of substance delivery system
WO2009085952A1 (fr)	2007-12-20	2009-07-09	Brookwood Pharmaceuticals, Inc.	Procédé pour préparer des microparticules ayant un faible volume de solvant résiduel
US8604101B2 (en) *	2010-03-24	2013-12-10	Basf Se	Process for producing aqueous dispersions of thermoplastic polyesters
KR20130039729A (ko)	2010-03-24	2013-04-22	바스프 에스이	열가소성 폴리에스테르의 수성 분산액의 제조 방법
EP2598553B1 (fr) *	2010-07-26	2016-04-27	Université de Genève	Compositions comprenant des polymères préparés à partir d'acides 2-hydroxyalkyliques
CA2849663A1 (fr)	2011-09-23	2013-03-28	Basf Se	Utilisation d'une dispersion aqueuse de polyesters biodegradables
US9956164B2 (en)	2014-04-16	2018-05-01	Veyx-Pharma Gmbh	Veterinary pharmaceutical composition and use thereof

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US3773919A (en)	1969-10-23	1973-11-20	Du Pont	Polylactide-drug mixtures
US4622244A (en) *	1979-09-04	1986-11-11	The Washington University	Process for preparation of microcapsules
GB2209937B (en) *	1987-09-21	1991-07-03	Depiopharm S A	Water insoluble polypeptides
CH679207A5 (fr)	1989-07-28	1992-01-15	Debiopharm Sa
GB2246514B (en) *	1990-08-01	1993-12-15	Scras	Sustained release pharmaceutical compositions and the preparation of particles for use therein
DE69101291T2 (de) *	1990-08-30	1994-07-07	Senju Pharma Co	Zusammensetzung zur kontrollierten Abgabe von Medikamenten.
DE69327542T2 (de) *	1992-11-17	2000-07-06	Yoshitomi Pharmaceutical Industries, Ltd.	Ein antipsychotikum enthaltende mikrokugel zur verzögerten freisetzung und verfahren für ihre herstellung
DE69519685T2 (de) *	1994-09-30	2001-08-02	Takeda Chemical Industries, Ltd.	Oral anzuwendende arzneizubereitung mit verzögerter wirkstoffabgabe
US5869079A (en) *	1995-06-02	1999-02-09	Oculex Pharmaceuticals, Inc.	Formulation for controlled release of drugs by combining hydrophilic and hydrophobic agents

1996
- 1996-05-06 FR FR9605630A patent/FR2748205A1/fr active Pending
1997
- 1997-04-28 US US09/180,451 patent/US6245346B1/en not_active Expired - Fee Related
- 1997-04-28 JP JP9539493A patent/JP2000509403A/ja active Pending
- 1997-04-28 AU AU27735/97A patent/AU710539B2/en not_active Ceased
- 1997-04-28 IL IL12689297A patent/IL126892A/en not_active IP Right Cessation
- 1997-04-28 EP EP97921812A patent/EP0896527A1/fr not_active Withdrawn
- 1997-04-28 WO PCT/EP1997/002187 patent/WO1997041836A1/fr not_active Ceased
- 1997-04-28 CA CA002253377A patent/CA2253377A1/fr not_active Abandoned
1998
- 1998-11-04 NO NO985145A patent/NO985145D0/no not_active Application Discontinuation

Also Published As

Publication number	Publication date
US6245346B1 (en)	2001-06-12
FR2748205A1 (fr)	1997-11-07
JP2000509403A (ja)	2000-07-25
WO1997041836A1 (fr)	1997-11-13
NO985145L (no)	1998-11-04
CA2253377A1 (fr)	1997-11-13
IL126892A0 (en)	1999-09-22
AU710539B2 (en)	1999-09-23
AU2773597A (en)	1997-11-26
EP0896527A1 (fr)	1999-02-17
NO985145D0 (no)	1998-11-04

Legal Events

Date	Code	Title	Description
2004-12-15	FF	Patent granted
2006-01-15	MM9K	Patent not in force due to non-payment of renewal fees

Publication	Publication Date	Title
DE69728371T2 (de)	2005-01-13	Verfahren zur herstellung von implantaten, die leuprolid enthalten
DE69332210T2 (de)	2003-04-24	Biologisch abbaubares, schmelzgesponnenes abgabesystem zur kontrollierten freisetzung
CA2125148C (fr)	1999-05-11	Matrice de verre a base de carbohydrates pour la liberation prolongee d'agents therapeutiques
DE3853853T2 (de)	1995-12-07	Verabreichungsformen für Pharmaka.
AU779938B2 (en)	2005-02-17	Compressed microparticles for dry injection
EP1484033B1 (fr)	2011-02-23	Compositions polymeres liquides pour la liberation controlee de substances bioactives
US5192741A (en)	1993-03-09	Sustained and controlled release of water insoluble polypeptides
US4650665A (en)	1987-03-17	Controlled release of pharmacologically active agents from an absorbable biologically compatible putty-like composition
US5288496A (en)	1994-02-22	Growth promoters for animals
US4568536A (en)	1986-02-04	Controlled release of pharmacologically active agents from an absorbable biologically compatible putty-like composition
CN101801415B (zh)	2015-09-23	利培酮化合物的持续递送制剂
AU710539B2 (en)	1999-09-23	Pharmaceutical compositions for the sustained release of insoluble active principles
US20210212934A1 (en)	2021-07-15	Methods for providing long-lasting anesthetic effect using microparticles
CZ20031124A3 (cs)	2003-12-17	Polymerní formulace leuprolidu pro podání se zlepšenou účinností
EP0158277A2 (fr)	1985-10-16	Préparations implantables à libération contrôlée de peptides régulateurs et procédé pour leur fabrication
AU2008259411B2 (en)	2013-10-17	Slow release pharmaceutical composition made of microparticles
JP2003517014A (ja)	2003-05-20	即放性および徐放性成分を含有する医薬インプラントおよび投与方法
CH683749A5 (de)	1994-05-13	Pharmazeutische Nasalzusammensetzung.
US5643595A (en)	1997-07-01	Growth promoters for animals
TWI399224B (zh)	2013-06-21	含有曲普瑞林醋酸鹽之固體持續釋放調配物
GB1573459A (en)	1980-08-20	Absorbable polymer drug compositions
EP0275961B1 (fr)	1994-06-08	Préparation médicale orale à libération prolongée
WO1999051201A1 (fr)	1999-10-14	Preparation a liberation prolongee
AU777393B2 (en)	2004-10-14	Improved growth stimulant compositions
Faraja et al.	2020	Preparation, In Vitro and In Vivo Studies of Vitamin B12 Loaded Implants