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Ganciclovir (Ganciclovir, GCV) is a new potent anti-herpes virus drugs, ocular drug delivery for the treatment of herpes simplex virus keratitis (herpes simplex keratitis). The purpose of the research and development of this article gels in order to extend the time of drug action in order to increase efficacy. Ultraviolet analytical method of GCV in the 3.988-15.95μg/ml range, good linear relationship of the concentration and absorption degree. Effects of GCV in distilled water, different pH values, the aqueous gel is commonly used in the solubility of the non-aqueous solvent, GCV smaller solubility in distilled water and a variety of non-aqueous solvent, the solubility of 2.14 mg / ml in distilled water, while in the presence of a base SOLUTION, GCV into a salt thereof, at pH = 10, the solubility increased to 13.62 mg / ml. Basic prescription according to the gelling agent, stability, viscosity, etc., as an index, the effects of pH value, the amount of carbomer, polymeric substance, hydroxypropyl-β-cyclodextrin (HP-beta-CD) The amount of such factors to determine the prescription of the gelling agent of the present GCV: GCV was 1%, the carbomer to 2%, 12% HP-β-CD, 1,2 - propylene glycol was 10%, glycerol 10% ; according to the general preparation method of the gelling agent and the gelling agent characteristics, optimization of the preparation process. Transparent the GCV gels obtained, even delicate, in line with the relevant provisions of the Pharmacopoeia of the People's Republic of China on the gels. HPLC analysis method of preparation used in drug content determination, stability study. In 4.016-16.06μg/ml range, the concentration and the peak area showed good linearity, precision test results, the average recovery was 97.2%, an average dose of 95.2% of the labeled amount. The effects of the preparation on the stability of the high temperature, low temperature and centrifugation. Were 40,60,80,100 ℃ accelerated test, made a preliminary study of its thermal degradation kinetics, fitting a kinetic equation: 1nk = -6162.6 / T 13.187 6-month test results show that the stability of gels. According to the in vivo characteristics of eye medication, no film dissolution model, also investigated the gel dissolution and drug release behavior. Prescription form to determine the case, the different nature of the drug has a constant release rate. The experimental factors (such as: the release area, the oscillation frequency) and formulation factors (such as: carbomer with HP-beta-CD amount) can affect the gel dissolution and drug release rate. Free diffusion model of the diffusion behavior of the drug in the gel. Internal water-based channel transport of the drug through the gel process in line with the the Fick mechanism. 24h in just less than 10% of drug release by diffusion. To increase the polymer concentration, the resulting aqueous channel tortuous and the viscosity of the gel increases, is the main reason for the decrease of the drug diffusion coefficient. Establishment of the rabbit eye herpes simplex virus keratitis model, the results showed that the gels formulations were significantly better than the commercially available drug aqueous solution group. The gel stability was good, no vivo acute irritant reaction, found ocular application requirements.
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