DE4136930A1 - Verfahren zur herstellung einer pharmazeutischen zusammensetzung, die pharmazeutische zusammensetzung sowie deren verwendung - Google Patents
Verfahren zur herstellung einer pharmazeutischen zusammensetzung, die pharmazeutische zusammensetzung sowie deren verwendungInfo
- Publication number
- DE4136930A1 DE4136930A1 DE4136930A DE4136930A DE4136930A1 DE 4136930 A1 DE4136930 A1 DE 4136930A1 DE 4136930 A DE4136930 A DE 4136930A DE 4136930 A DE4136930 A DE 4136930A DE 4136930 A1 DE4136930 A1 DE 4136930A1
- Authority
- DE
- Germany
- Prior art keywords
- poly
- microparticles
- extrusion
- active ingredient
- pharmaceutical composition
- Prior art date
- Legal status (The legal status 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 status listed.)
- Ceased
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 11
- 238000004519 manufacturing process Methods 0.000 title description 7
- 239000000203 mixture Substances 0.000 claims abstract description 22
- 239000011859 microparticle Substances 0.000 claims abstract description 21
- 108090000765 processed proteins & peptides Proteins 0.000 claims abstract description 17
- 238000001125 extrusion Methods 0.000 claims abstract description 16
- 239000007943 implant Substances 0.000 claims abstract description 10
- 229920002988 biodegradable polymer Polymers 0.000 claims abstract description 8
- 239000004621 biodegradable polymer Substances 0.000 claims abstract description 8
- 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 abstract description 7
- 102000005157 Somatostatin Human genes 0.000 claims abstract description 6
- 108010056088 Somatostatin Proteins 0.000 claims abstract description 6
- 229960000553 somatostatin Drugs 0.000 claims abstract description 6
- 229920002253 Tannate Polymers 0.000 claims abstract description 5
- 150000001413 amino acids Chemical class 0.000 claims abstract description 5
- IPCSVZSSVZVIGE-UHFFFAOYSA-M hexadecanoate Chemical compound CCCCCCCCCCCCCCCC([O-])=O IPCSVZSSVZVIGE-UHFFFAOYSA-M 0.000 claims abstract description 4
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims abstract description 4
- 238000002360 preparation method Methods 0.000 claims abstract description 4
- 102000055006 Calcitonin Human genes 0.000 claims abstract description 3
- 108060001064 Calcitonin Proteins 0.000 claims abstract description 3
- BBBFJLBPOGFECG-VJVYQDLKSA-N calcitonin Chemical compound 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 abstract description 3
- 229960004015 calcitonin Drugs 0.000 claims abstract description 3
- -1 poly(1,4-butylene succinate) Polymers 0.000 claims abstract 4
- 101000904177 Clupea pallasii Gonadoliberin-1 Proteins 0.000 claims abstract 3
- 239000000579 Gonadotropin-Releasing Hormone Substances 0.000 claims abstract 3
- 101000857870 Squalus acanthias Gonadoliberin Proteins 0.000 claims abstract 3
- XLXSAKCOAKORKW-AQJXLSMYSA-N gonadorelin Chemical compound 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 abstract 3
- 238000000034 method Methods 0.000 claims description 26
- 239000004480 active ingredient Substances 0.000 claims description 13
- 229950005627 embonate Drugs 0.000 claims description 9
- 102000004196 processed proteins & peptides Human genes 0.000 claims description 6
- 239000003814 drug Substances 0.000 claims description 5
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 5
- 238000010298 pulverizing process Methods 0.000 claims description 4
- 239000000126 substance Substances 0.000 claims description 4
- 241000237858 Gastropoda Species 0.000 claims description 3
- 230000006835 compression Effects 0.000 claims description 3
- 238000007906 compression Methods 0.000 claims description 3
- 235000012438 extruded product Nutrition 0.000 claims description 3
- 239000000843 powder Substances 0.000 claims description 3
- 238000007873 sieving Methods 0.000 claims description 2
- 238000010438 heat treatment Methods 0.000 claims 1
- 229940126601 medicinal product Drugs 0.000 claims 1
- 239000013543 active substance Substances 0.000 abstract description 2
- 239000004615 ingredient Substances 0.000 abstract description 2
- 229920000621 Poly(1,4-butylene succinate) Polymers 0.000 abstract 1
- 238000007580 dry-mixing Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 description 8
- 229920000642 polymer Polymers 0.000 description 6
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 description 4
- 229920001577 copolymer Polymers 0.000 description 4
- 239000006185 dispersion Substances 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 238000002156 mixing Methods 0.000 description 4
- 239000002245 particle Substances 0.000 description 4
- WQGWDDDVZFFDIG-UHFFFAOYSA-N pyrogallol Chemical compound OC1=CC=CC(O)=C1O WQGWDDDVZFFDIG-UHFFFAOYSA-N 0.000 description 4
- 239000002904 solvent Substances 0.000 description 4
- 229920000229 biodegradable polyester Polymers 0.000 description 3
- 239000004622 biodegradable polyester Substances 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 2
- 238000013270 controlled release Methods 0.000 description 2
- 229940088597 hormone Drugs 0.000 description 2
- 239000005556 hormone Substances 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 230000033001 locomotion Effects 0.000 description 2
- 229920000728 polyester Polymers 0.000 description 2
- 102000004169 proteins and genes Human genes 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- 230000001105 regulatory effect Effects 0.000 description 2
- 230000001954 sterilising effect Effects 0.000 description 2
- 238000004659 sterilization and disinfection Methods 0.000 description 2
- 229960003604 testosterone Drugs 0.000 description 2
- RKDVKSZUMVYZHH-UHFFFAOYSA-N 1,4-dioxane-2,5-dione Chemical compound O=C1COC(=O)CO1 RKDVKSZUMVYZHH-UHFFFAOYSA-N 0.000 description 1
- 108091003079 Bovine Serum Albumin Proteins 0.000 description 1
- 102000018997 Growth Hormone Human genes 0.000 description 1
- 108010051696 Growth Hormone Proteins 0.000 description 1
- 102000009151 Luteinizing Hormone Human genes 0.000 description 1
- 108010073521 Luteinizing Hormone Proteins 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- 108010050144 Triptorelin Pamoate Proteins 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
- 238000010420 art technique Methods 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 229940098773 bovine serum albumin Drugs 0.000 description 1
- 239000012876 carrier material Substances 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 238000005056 compaction Methods 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 230000001934 delay Effects 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 239000000122 growth hormone Substances 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 229940040129 luteinizing hormone Drugs 0.000 description 1
- 238000002844 melting Methods 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 150000002942 palmitic acid derivatives Chemical class 0.000 description 1
- 229920000747 poly(lactic acid) Polymers 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 238000009827 uniform distribution Methods 0.000 description 1
- 238000010792 warming Methods 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical class [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH3616/90A CH681425A5 (el) | 1990-11-14 | 1990-11-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DE4136930A1 true DE4136930A1 (de) | 1992-08-20 |
Family
ID=4259807
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE4136930A Ceased DE4136930A1 (de) | 1990-11-14 | 1991-11-11 | Verfahren zur herstellung einer pharmazeutischen zusammensetzung, die pharmazeutische zusammensetzung sowie deren verwendung |
Country Status (12)
| Country | Link |
|---|---|
| JP (1) | JPH04288021A (el) |
| AT (1) | AT397198B (el) |
| BE (1) | BE1004923A5 (el) |
| CA (1) | CA2055115A1 (el) |
| CH (1) | CH681425A5 (el) |
| DE (1) | DE4136930A1 (el) |
| ES (1) | ES2049617B1 (el) |
| FR (1) | FR2668707B1 (el) |
| GB (1) | GB2249725B (el) |
| IT (1) | IT1252870B (el) |
| NL (1) | NL9101877A (el) |
| SE (1) | SE506448C2 (el) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4223282A1 (de) * | 1991-07-22 | 1993-01-28 | Debio Rech Pharma Sa | Zubereitung zur stetigen und kontrollierten abgabe von medikamentoesen substanzen und verfahren zu deren herstellung |
| WO2004096178A1 (en) * | 2003-05-02 | 2004-11-11 | The University Of Nottingham | Nano and microparticle drug delivery systems comprising polyesters containing aliphatic dicarboxylate residues and residues of aliphatic polyols |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5456917A (en) * | 1993-04-12 | 1995-10-10 | Cambridge Scientific, Inc. | Method for making a bioerodible material for the sustained release of a medicament and the material made from the method |
| US5945128A (en) * | 1996-09-04 | 1999-08-31 | Romano Deghenghi | Process to manufacture implants containing bioactive peptides |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3978203A (en) * | 1974-07-12 | 1976-08-31 | Dynatech Corporation | Sustained release of pharmaceuticals from polyester matrices |
| US4481353A (en) * | 1983-10-07 | 1984-11-06 | The Children's Medical Center Corporation | Bioresorbable polyesters and polyester composites |
| US4962091A (en) * | 1986-05-23 | 1990-10-09 | Syntex (U.S.A.) Inc. | Controlled release of macromolecular polypeptides |
| GB2209937B (en) * | 1987-09-21 | 1991-07-03 | Depiopharm S A | Water insoluble polypeptides |
| CH672887A5 (el) * | 1987-10-14 | 1990-01-15 | Debiopharm Sa | |
| CH679207A5 (el) * | 1989-07-28 | 1992-01-15 | Debiopharm Sa | |
| IT1243390B (it) * | 1990-11-22 | 1994-06-10 | Vectorpharma Int | Composizioni farmaceutiche in forma di particelle atte al rilascio controllato di sostanze farmacologicamente attive e procedimento per la loro preparazione. |
-
1990
- 1990-11-14 CH CH3616/90A patent/CH681425A5/fr not_active IP Right Cessation
-
1991
- 1991-10-31 BE BE9101009A patent/BE1004923A5/fr not_active IP Right Cessation
- 1991-11-01 GB GB9123241A patent/GB2249725B/en not_active Expired - Fee Related
- 1991-11-04 FR FR9113563A patent/FR2668707B1/fr not_active Expired - Fee Related
- 1991-11-07 CA CA002055115A patent/CA2055115A1/en not_active Abandoned
- 1991-11-08 IT ITBS910119A patent/IT1252870B/it active IP Right Grant
- 1991-11-11 DE DE4136930A patent/DE4136930A1/de not_active Ceased
- 1991-11-11 NL NL9101877A patent/NL9101877A/nl active Search and Examination
- 1991-11-12 AT AT0223591A patent/AT397198B/de not_active IP Right Cessation
- 1991-11-13 JP JP91297358A patent/JPH04288021A/ja active Pending
- 1991-11-13 SE SE9103348A patent/SE506448C2/sv not_active IP Right Cessation
- 1991-11-13 ES ES09102518A patent/ES2049617B1/es not_active Expired - Lifetime
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4223282A1 (de) * | 1991-07-22 | 1993-01-28 | Debio Rech Pharma Sa | Zubereitung zur stetigen und kontrollierten abgabe von medikamentoesen substanzen und verfahren zu deren herstellung |
| WO2004096178A1 (en) * | 2003-05-02 | 2004-11-11 | The University Of Nottingham | Nano and microparticle drug delivery systems comprising polyesters containing aliphatic dicarboxylate residues and residues of aliphatic polyols |
Also Published As
| Publication number | Publication date |
|---|---|
| ES2049617B1 (es) | 1997-03-16 |
| NL9101877A (nl) | 1992-06-01 |
| BE1004923A5 (fr) | 1993-02-23 |
| FR2668707B1 (fr) | 1995-05-24 |
| GB9123241D0 (en) | 1991-12-18 |
| CA2055115A1 (en) | 1992-05-15 |
| AT397198B (de) | 1994-02-25 |
| ATA223591A (de) | 1993-07-15 |
| SE506448C2 (sv) | 1997-12-15 |
| SE9103348D0 (sv) | 1991-11-13 |
| ITBS910119A0 (it) | 1991-11-08 |
| SE9103348L (sv) | 1992-05-15 |
| ITBS910119A1 (it) | 1993-05-08 |
| FR2668707A1 (fr) | 1992-05-07 |
| GB2249725B (en) | 1994-08-10 |
| CH681425A5 (el) | 1993-03-31 |
| JPH04288021A (ja) | 1992-10-13 |
| IT1252870B (it) | 1995-06-28 |
| GB2249725A (en) | 1992-05-20 |
| ES2049617A1 (es) | 1994-04-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8110 | Request for examination paragraph 44 | ||
| 8131 | Rejection |