Chidzidzo Chitsva Pamusoro peNon-Opioid Kurapa kwePost-Operative Pain

Cali Biosciences Co., Ltd. yakazivisa mhedzisiro yakabudirira muChikamu IIb chekudzidza kwayo kweperioperative refu-inobata analgesic chigadzirwa CPL-01, yakawedzera-kuburitswa injectable version yeNaropin® (ropivacaine hydrochloride), yakagadzirwa neCali Biosciences kurapa mushure mekushanda. kurwadziwa kwekuvhiya uye kuderedza kudiwa kwemaopioid.

Iyi Phase IIb yekiriniki yekuyedza yakarongedzerwa kuenderera mberi nekuongorora mabhenefiti ekiriniki eCPL-01 uye kuenzanisa neaya aripo ekurapa marwadzo emishonga pamusika. Muedzo wakaratidza yakanakisa dose-mhinduro yekubudirira. Muyero yakarongwa parizvino seyekuzotengeswa dhesi, gumi nemana vanhu vakagamuchira CPL-14 vakaratidza yaireva AUC kuburikidza nemaawa makumi manomwe nemaviri wWOCF yakagadziridzwa NRS-A (iyo yekutanga magumo) ye01, ichiratidza maitiro ekukosha kune gumi nematanhatu zvidzidzo. avo vakagamuchira placebo (p=72) uye zvakanyanya nani pane zvidzidzo zve286.8 zvakagamuchira Naropin®. Kurevesa kwekiriniki kwakaratidzwa nekuratidza musiyano weanopfuura imwe AUC point paawa. 

Uyezve, kushandiswa kweopioid kuburikidza nemaawa 72 eCPL-01 zvidzidzo zvakagamuchira iyo-inotengeswa dose yakagurwa nepakati kana ichienzaniswa neboka re placebo kana boka reNaropin® (zvinoreva 7.9 mg, kusiyana ne15 mg ye placebo uye 16 mg yeNaropin®). Kutaura zvazviri, inenge 2/3 yezvidzidzo zveCPL-01 (9/14) yaida maopioid zvachose mushure memaawa 72 ekutanga mushure mekuvhiyiwa, zvichienzaniswa nehafu yezvidzidzo zveNaropin® uye 30% yeavo placebo.

Pakanga pasina kuwana zvine musoro kwekuchengetedza; kurapwa chete kwakabuda zviitiko zvakashata zvakaitika mune zvinopfuura imwechete CPL-01 nyaya kune ese cohorts mukati meyedzo (n = 40) yaive kusvotwa, kurutsa, kuvimbiswa, kurwara kwemusoro parasthesia, uye dzungu - zvese zviitiko zvinowanzoitika mushure mekuvhiyiwa uye zvinogona kuitika. mushure mekushandisa opioid; hapana chimwe cheizvi chaifungidzirwa kuti chine chekuita neCPL-01. 

Iyo pharmacokinetics yemushonga yakawedzera kutsigira kuchengetedzeka kwayo - chikonzero chikuru chekuti ropivacaine inogara kwenguva refu iri kugadzirwa, ine zvakanakira pane iripo parizvino inobata kwenguva refu bupivacaine. Izvo zvinoreva Cmax ye ropivacaine muzvidzidzo zvakagamuchira 600 mg dose yaiva 978 ng/mL, yakaderera zvikuru kudarika chikumbaridzo apo chepfu yemwoyo inogona kuonekwa (4000 ng/mL). CPL-01 yakasvika pakukwirira kwayo kwemaawa anenge gumi nemasere mushure mekutonga, kusiyana neNaropin® (iyo inosvika mairi mukati meawa yekutanga mushure mekutonga).