http://rdf.ncbi.nlm.nih.gov/pubchem/patent/PL-175946-B1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_1782fde68e8711188a1881f5284fe0b0 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-57 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K9-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K9-16 |
| filingDate | 1993-02-25^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9a6577357c69adb040ddbe9c97b15f5c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3141358635e9a9a1e4d966d2117f143a |
| publicationDate | 1999-03-31^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | PL-175946-B1 |
| titleOfInvention | Pharmaceutical agent, sustained release particle and method for producing a sustained release particle |
| abstract | A pharmaceutical composition comprising an acceptable carrier or diluent and an androgenic steroid, characterized byn57) in that it contains sustained release particles, preferably in an amount of from 10-70% by weight, containing the substancenan active androgenic agent selected from the group consisting of megestrol acetate and medroxyprogesterone acetate,ndispersed in a sustained release polymer or copolymer binder, preferablynselected from the group consisting of polyglycolic acid (PGA) and polylactic acid (PLA), poly (DL-lactic-co-glycolic acid)n(DL PLGA), poly (D-lactic-co-glycolic acid) (D PLGA) and poly (L-lactic-co-glycolic acid)n(L PLGA), poly (ε-caprolactone), poly (ε-caprolactone-co-lactic acid), poly (ε-caprolactone-co-acidnglycolic acid), poly (β-hydroxybutyric acid), poly (alkyl 2-cyartoacrylate), poly (hydroxyethyl methacrylate), polyamide,npoly (amino acid) (preferably L-leucine, glutamic acid, L-aspartic acid), poly (esterurea),npoly (2-hydroxyethyl-Dl-aspartamide), polyacetals, polyorthoester, polycarbonate, polymaleamide, polysaccharidenand their copolymers, biocompatible with human tissues and biodegradable in the body to biocompatiblenmetabolic products, the weight ratio of steroid to binder being from 1: 4 to 7: 3, andnthe androgenic steroid has a Ki value for the androgen receptor below about 2'10'8M and has an inhibitory effect on growthnZR-75-1 human breast cancer cells mediated by the androgen receptor, reaching half the maximumnvalues at a concentration below 3.0 nanomoles per liter, and has no visible masculinizing activity.n5. A method for producing a sustained release particle characterized by producing sustained release microspheresna release with an average size of between 5 µm and 40 µm by dissolution in an organic solvent conat least one androgenic compound selected from the group consisting of medroxyprogesterone acetate and acetatenmegestrol and a controlled release polymer having hydrolyzable ester linkages to formnthe mixture and adds said mixture to water under sufficient agitation to form microspheres,nhaving an average size between 5 µm and 40 µm, and then separating said microspheres from the solution and subjected tonmicrospheres exposed to vacuum at a pressure not lower than 6.65 χ 103 Pa and at a temperature not higher than 30 ° C fornfor a period of at least 24 hours, and subject the microspheres to a second vacuum at a pressure belown1.33 χ 101 2 * * 5 Pa and a temperature 7 to 12 ° C lower than the glass transition temperature of the said microspheres for a period of timensufficient to reduce the content of residual r |
| priorityDate | 1992-06-24^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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