http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-104974058-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0d3728f8fe672b5af7a83a0b676baaa7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_764c37797762f79bedf08832dbf3a65a |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C229-42 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-196 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C227-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-06 |
| filingDate | 2006-07-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8d1da7fb492c150595d55490288c11f3 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_427000f491db4a62421dd8049978ac9c |
| publicationDate | 2015-10-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-104974058-A |
| titleOfInvention | Positively-charged water-soluble diclofenac prodrugs with high skin penetration velocity |
| abstract | The invention provides positively-charged water-soluble diclofenac prodrugs with high skin penetration velocity. In a ''structural formula 1'' of a general formula (1), novel positively-charged water-soluble diclofenac prodrugs are designed and synthesized. The compounds as shown in the above-mentioned ''structural formula 1'' of the general formula (1) can be synthesized by reaction of functionalized derivatives (like acid halides or mixed anhydrides) of diclofenac with proper alcohol, thioalcohol or amine. Positively-charged amino groups on prodrug molecules greatly improve the solubility of a drug, and promote the drug to enter cytoplasm by combination with negative charges on biological membrane phosphate terminal groups. Experimental results show that the prodrug, i.e., 2-[(2,6-dichlorophenyl)amino]phenylacetate diethylaminoethyl acetate, has a human skin penetration velocity which is nearly 250 times as fast as the human skin penetration velocity of the prodrugs, i.e., 2-[(2,6-dichlorophenyl)amino]phenylacetate (diclofenac) and 2-[(2,6-dichlorophenyl)amino]phenylacetate ethyl. In plasma, more than 90% of the prodrugs can return to a parent drug in a few minutes. The prodrugs can be applied in medicine to treat human or animal states that any diclofenac can treat; in treatment, oral administration and transdermal administration are available, so that most of side effects of diclofenac are avoided, wherein the most significant side effects comprise gastrointestinal discomforts like indigestion, bleeding in stomach and duodenal, gastric ulcer and gastritis. Through a controlled release transdermal administration system of the prodrugs, the plasma drug concentration is stabilized in an optimal therapeutic level, so the treatment effects are improved, and the side effects of diclofenac are decreased. |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-109620821-A |
| priorityDate | 2006-07-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 76.