Preparation and pharmacokinetic evaluation of long-acting injectable oily suspensions for ophiopogonis radix polysaccharide MDG-1 / 中国中药杂志

ABSTRACT

<p><b>OBJECTIVE</b>To evaluate in vivo pharmacokinetics of Ophiopogonis Radix polysaccharide MDG-1 oily suspension injection prepared with different prescriptions in rats, and explore the feasibility of the long-acting drug delivery of MDG-1 Injection by using the oily suspension drug release system.</p><p><b>METHOD</b>MDG-1 microparticles were prepared by the anti-solvent precipitation method. Their size and size distribution were characterized. Castor oil with a high viscosity or aluminum stearate were added into soybean oil with a low viscosity, in order to prepare oily media with different viscosities, detect their rheological properties and screen out superior prescriptions for in vivo evaluation.</p><p><b>RESULT</b>The average size of microparticles was 21.81 microm, and the span between them was 2.63. The in vivo evaluation was conducted for prescriptions of mixed oil (soybean oil/castor oil, 2: 3) and soybean oils gelled by 2% and 4% aluminium stearate. Among them, the prescription of soybean gelled by 4% aluminium stearate could significantly reduce C(max) and prolong the apparent t1/2, with the MDG-1 release time of several days.</p><p><b>CONCLUSION</b>It is feasible to achieve the long-acting MDG-1 drug delivery by using oily media with a high viscosity.</p>