Abstract:
:The treatment of patients suffering from advanced Parkinson's disease is highly challenging, because the efficacy of the "gold standard" levodopa declines with time. Co-administration of the dopamine receptor agonist apomorphine is beneficial, but difficult due to the poor oral bioavailability and short half-life of this drug. In order to overcome these restrictions, PLGA-based microparticles allowing for controlled parenteral delivery of this morphine derivative were prepared using (solid-in-)oil-in-water extraction/evaporation techniques. Particular attention was paid to minimize spontaneous oxidation of the labile drug and to optimize the key features of the microparticles, including encapsulation efficiency, initial burst release and particle size. Various formulation and processing parameters were adjusted in this respect. The systems were thoroughly characterized using SEM, EDX, DSC, laser diffraction, headspace-GC as well as in vitro drug release measurements in agitated flasks and flow-through cells. Importantly, apomorphine could effectively be protected against degradation during microparticle preparation and within the delivery systems upon exposure to phosphate buffer pH 7.4 (containing 0.2% ascorbic acid) at 37 °C: 90% intact drug was released at a constant rate during about 10d.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Regnier-Delplace C,Thillaye du Boullay O,Siepmann F,Martin-Vaca B,Degrave N,Demonchaux P,Jentzer O,Bourissou D,Siepmann Jdoi
10.1016/j.ijpharm.2013.01.008subject
Has Abstractpub_date
2013-02-25 00:00:00pages
68-79issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(13)00021-5journal_volume
443pub_type
杂志文章abstract::Biocompatible microemulsions composed of Peceol(®), lecithin, ethanol and water developed for encapsulation of hydrophilic drugs were investigated. The binary mixture Peceol(®)/ethanol was studied first. It was shown that the addition of ethanol to pure Peceol(®) has a significant fluidifying and disordering effect on...
journal_title:International journal of pharmaceutics
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abstract::It has been demonstrated that orally administered cholestyramine is distributed throughout the stomach and provides prolonged gastric residence via mucoadhesion. Gamma scintigraphy was used to compare the gastric emptying and residence of this resin with two formulations known to exhibit retentive or bioadhesive prope...
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pub_type: 临床试验,杂志文章,随机对照试验
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