http://rdf.ncbi.nlm.nih.gov/pubchem/patent/KR-20060118450-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_382ccfc2ebebcaee15aa7cda4cee86bc |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-26 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-0019 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-496 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-497 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-19 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-38 |
| classificationIPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K47-26 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K9-19 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-496 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K47-38 |
| filingDate | 2004-10-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fc08ae61cdacf12d166a3e1d40df1ed3 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3dfde226634f0059136189d447e2d532 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1bab6b76ccd643666362380626742cc8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dc8c29f5ce50b3cbf4f43d2fcfd72faf |
| publicationDate | 2006-11-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | KR-20060118450-A |
| titleOfInvention | Controlled Release Sterile Aripiprazole Injections, Methods for Manufacturing the Same, and Methods for Using the Same |
| abstract | In the present invention there is provided a lyophilized sterile aripiprazole formulation which releases aripiprazole for at least 1 week, preferably 2, 3 or 4 weeks and 6 weeks or longer at a therapeutic dose in a composition comprising water for injection. do.n n n Lyophilized Aripiprazole formulations of the inventionn n n (a) aripiprazole, andn n n (b) comprises a container containing aripiprazole,n n n Weeks that release a therapeutic dose of aripiprazole at least one week, preferably two, three or four weeks and six to six weeks or more upon injection, preferably at intramuscular injection, as a composition comprising water Form a suspension for use.n n n The lyophilized aripiprazole formulation of the invention is preferablyn n n (a) aripiprazole,n n n (b) one or more suspending agents,n n n (c) optionally one or more solidifying agents,n n n (d) optionally one or more buffers, andn n n (e) Optionally, one or more pH adjusters will be included.n n n Microparticle sizes within the 1-30 μm range of the lyophilized aripiprazole formulation are essential for injectable formulations that release the aripiprazole from at least one week and six weeks to longer, for example, up to eight weeks.n n n It has been found that the smaller the microparticle size of the lyophilized aripiprazole, the shorter the time for sustained release. Thus, when the microparticle size according to the invention is about 1 μm, the aripiprazole will be released over a period of less than three weeks, preferably two weeks. When the microparticle size is at least about 1 μm, aripiprazole will be released over at least 2 weeks, preferably from about 3 to 4 weeks, up to 6 weeks or more. Thus, according to the present invention, aripiprazole release persistence can be modified by changing the aripiprazole microparticle size in lyophilized formulations.n n n "Microparticle size" means volume microdiameter as measured by laser-light dispersion (LLS) technology. Particle size distribution is measured by LLS technology and microparticle size is calculated from particle size distribution.n n n In addition, the present invention provides controlled release sterile aripiprazole injections in the form of sterile suspensions, ie, lyophilized preparations suspended in water for injection, wherein a therapeutic dose of aripiprazole is injected upon injection, preferably intramuscularly. Release over at least a week,n n n (a) aripiprazole,n n n (b) its container, andn n n (c) contains water for injection.n n n The controlled release sterile aripiprazole injection in the form of a sterile suspension of the present invention allows for high drug loading per unit volume of the formulation to allow relatively high doses of aripiprazole delivery even at low dosages (0.1-600 mg per mL of suspension). drug).n n n According to the present invention there is also provided a process for preparing the lyophilized sterile aripiprazole formulation described above according to the following steps:n n n (a) preparing a sterile solid aripiprazole, preferably having a particle size distribution and a fine particle size within the range of about 5 to 100 μm,n n n (b) preparing a sterile container for sterile solid aripiprazole,n n n (c) combining the sterile solid aripiprazole with a sterile container to form a primary sterile suspension,n n n (d) reducing the microparticle size of aripiprazole in the primary sterile suspension to within the range of about 1 to 30 μm to form a final sterile suspension, andn n n (e) freeze drying the final sterile suspension to form a lyophilized sterile aripiprazole suspension of the desired polymorph (anhydride, monohydrate, or a mixture of both).n n n In carrying out the method, reducing the microparticle size in the primary sterile suspension to the desired microparticle size is carried out using a sterile wet grinding process, preferably sterile wet ball grinding.n n n Sterile wet grinding is essential for forming homogeneous sterile aripiprazole formulations with the desired microparticle size distribution.n n n Additionally according to the present invention there is provided a method of lyophilization of the final sterile aripiprazole suspension, producing a lyophilized sterile aripiprazole in the preferred polymorph, ie anhydride, monohydrate, or a mixture of both.n n n Also provided by the present invention are methods of treating schizophrenia and related diseases, comprising administering to the patient in need thereof a therapeutic dose of said controlled release injectable aripiprazole formulation.n n n Unexpected findings have shown that aripiprazole suspension suspended in an aqueous solvent system will maintain a fairly constant aripiprazole drug plasma concentration when administered by injection, preferably intramuscular injection. No large “burst phenomenon” is observed and it is surprising that by using the aripiprazole suspension of the present invention, a constant aripiprazole drug plasma concentration can be maintained from one to eight weeks. The daily starting dose for the aripiprazole formulation administered orally is 15 mg. In order to perform a drug administration corresponding to an oral dosage of 1 to 8 weeks or more, it is necessary to administer a very large amount of drug at one time. The water soluble aripiprazole injection of the present invention can be administered to deliver large amounts of drug without causing patient compatibility issues.n n n Aripiprazole injectables of the present invention include aripiprazole in anhydride or monohydrate crystal form or a mixture of both. If monohydrate is used, it is possible to maintain an extended drug plasma concentration.n n n Aripiprazole injectables of the invention may be administered as ready-to-use aqueous suspensions; However, the suspension can be lyophilized to provide more useful drugs.n n n n Aripiprazole, Injections, Sterile Lyophilisation, Antipsychotics, Schizophrenia |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/KR-20150003336-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/KR-20180085049-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/KR-20200064173-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/KR-101125210-B1 |
| priorityDate | 2003-10-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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