Ropinirole HCl

Ropinirole a selective dopamine D2 receptors inhibitor with IC50 of 29 nM.

3D printing of tablets using inkjet with UV photoinitiation.[Pubmed:28673860]

Int J Pharm. 2017 Aug 30;529(1-2):523-530.

Additive manufacturing (AM) offers significant potential benefits in the field of drug delivery and pharmaceutical/medical device manufacture. Of AM processes, 3D inkjet printing enables precise deposition of a formulation, whilst offering the potential for significant scale up or scale out as a manufacturing platform. This work hypothesizes that suitable solvent based ink formulations can be developed that allow the production of solid dosage forms that meet the standards required for pharmaceutical tablets, whilst offering a platform for flexible and personalized manufacture. We demonstrate this using piezo-activated inkjetting to 3D print ropinirole hydrochloride. The tablets produced consist of a cross-linked poly(ethylene glycol diacrylate) (PEGDA) hydrogel matrix containing the drug, photoinitiated in a low oxygen environment using an aqueous solution of Irgacure 2959. At a Ropinirole HCl loading of 0.41mg, drug release from the tablet is shown to be Fickian. Raman and IR spectroscopy indicate a high degree of cross-linking and formation of an amorphous solid dispersion. This is the first publication of a UV inkjet 3D printed tablet. Consequently, this work opens the possibility for the translation of scalable, high precision and bespoke ink-jet based additive manufacturing to the pharmaceutical sector.

Nanoencapsulation of a water soluble drug in biocompatible polyesters. Effect of polyesters melting point and glass transition temperature on drug release behavior.[Pubmed:20863892]

Eur J Pharm Sci. 2010 Dec 23;41(5):636-43.

Five polyesters based on 1,3-propanediol or ethylene glycol and an aliphatic dicarboxylic acid were used for the preparation of Ropinirole HCl-loaded nanoparticles. The advantage of the present study is that the used polyesters - as well as poly(lactic acid) (PLA) - have similar degree of crystallinity but different melting points, varying from 46.7 to 166.4 degrees C. Based on polymer toxicity on HUVEC, the biocompatibility of these aliphatic polyesters was found comparable to that of PLA and thus the studied polyesters could be used as drug carriers. Drug encapsulation in polyesters was performed via emulsification/solvent evaporation method. Particle size of drug-loaded nanoparticles was between 140 and 190 nm, as measured by light scattering. Drug loading content for all the polyesters varies between 10 and 16% and their entrapment efficiency is relatively high (32-48%). WAXD patterns of nanoparticles show that Ropinirole HCl lies in amorphous state within polymer matrices. Drug release diagrams reveal that the higher percentage of Ropinirole HCl is released during the first 6h after its insertion in the dissolution medium. Fast release rates of the drug are attributed to high hydrophilicity of Ropinirole HCl. Melting point (T(m)) and glass transition temperature (T(g)) of the host polymer matrices seem to be important parameters, since higher drug release rates are observed in polyesters with low T(m) and T(g).

Pharmacologic profile of ropinirole: a nonergoline dopamine agonist.[Pubmed:9222275]

Neurology. 1997 Jul;49(1 Suppl 1):S58-62.

The use of dopamine agonists as monotherapy or in combination with levodopa in the treatment of Parkinson's disease (PD) allows for reduction or limitation of the levodopa dose, potentially delaying the onset or reducing the severity of late motor complications. Ropinirole is a new nonergoline dopamine agonist that binds specifically to D2-like receptors with a selectivity similar to that of dopamine (D3 > D2 > D4). The chemical structure of ropinirole has the potential to maintain a structure-activity relationship similar to that of dopamine and other effective dopamine agonists without producing ergot-related adverse effects. Ropinirole has demonstrated efficacy in two standard preclinical models of PD and has shown a very low propensity to induce dyskinesia in these studies. This latter property is of potential clinical importance for pharmacotherapy of early PD. This article will present the importance of pharmacologic specificity of dopamine agonists along with the basic pharmacologic characteristics of ropinirole that may contribute to its efficacy in the treatment of PD.

Preclinical pharmacology of ropinirole (SK&F 101468-A) a novel dopamine D2 agonist.[Pubmed:1673248]

Pharmacol Biochem Behav. 1991 Jan;38(1):147-54.

These studies characterise the pharmacology of ropinirole, a selective D-2 agonist. High-affinity human caudate binding revealed a Ki for D2 receptors of 2.9 x 10(-8) M with no affinity for D1 at 10(-4) M in the rat. Ropinirole was weakly active at alpha 2-adrenoceptors and 5-HT2 receptors but inactive at 5-HT1, benzodiazepine and gamma-aminobutyric acid receptors or alpha 1 and beta-adrenoceptors. In rodents, ropinirole, like apomorphine, caused biphasic spontaneous locomotor activity and contralateral circling in 6-OHDA-lesioned mice with no tolerance to the latter after 14 days treatment. Amphetamine caused ipsilateral responses in the lesioned mice. Ropinirole did not cause marked stereotypies. In marmosets ropinirole (0.05-1.0 mg/kg SC or 0.1 mg/kg PO) reversed all motor and behavioural deficits induced by MPTP. This response started 10-20 minutes after dosing, and exceeded 2 hours. No tolerance was seen following chronic b.i.d. treatment. Similar results were obtained with 1-dopa plus benserazide; however, 1-dopa always caused emesis, whereas beneficial effects were shown with ropinirole in the absence of this side effect. These results support the continued clinical assessment of ropinirole for the treatment of Parkinson's disease.

Ropinirole hydrochloride is a potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease.

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