The Study Of Glaucoma Ophthalmic Puerarin Flexible Liposomes Temperature Sensitive Gel

Statistics show that glaucoma can seriously affect the health of the elderly. In blinding diseases,it has been ranking second in the world.Pharmacological studies have shown that PUE has blood pressure and β receptor blockade,PUE is one of the effective therapeutic agent for glaucoma.However, due to the PUE has poor solubility and Ordinary Drops are easy loss at Corneal,ointments has poor patient compliance and deficiencies in terms of the formulation. It is difficult to achieve effective prevention and therapeutic purposes.Thus, this experiment was prepared PUE-FL-TSG,In order to take advantage of the flexible liposomes having a hydrophilic lipophilic as the carrier would facilitate its drug through the cornea after wrapping and use temperature-sensitive gel can occur phase transition to improve the liquid preparation easy to drain the anterior corneal after ocular administration,thereby enhancing the bioavailability of the drug in the eye. The experiment as follows in this paper.1、PUE content was determined by HPLC,dynamic determined its equilibrium solubility in different organic solvents and various PBS.Determined the oil/water partition coefficient and obtained 1gP = 0.7.Therefore, the choice was prepared PUE-FL,in order to promote PUE through the cornea about use hydrophilic lipophilic carrier.2、Encapsulation efficiency and drug loading as comprehensive survey indicators,used orthogonal experimental design to optimize the preparation of optimal formulation of PUE-FL.Encapsulation efficiency as the indexes.used central composite design-response surface methodology to optimize the best preparation PUE-FL.The results show that under optimal conditions obtained PUE-FL encapsulation efficiency was 70.22%,state grain round, small and uniform particle size distribution, Zeta potential absolute value is small, the deformation is good, and the need to save less sediment temperature, PUE-FL-TSG preparation for the foundation.3、Used poloxamer (P407 and P188) as study of factors, the gelation temperature of STF before and after dilution as evaluation, used design-response surface methodology to optimize the optimal prescription, and the PUE-FL-TSG the optimal prescription composition is 23.0% P407 and 3.5% P188. The results show that, Under the optimal conditions prescriptions, PUE-FL-TSG was liquid at room temperature,besides,under the physiological conditions of the eye it can immediately phase to gel, can achieve the goal of convenient dosing.4、Adopted no membrane stripping voltammetry to study the dissolution amount and vitro release of PUE-FL-TSG and PUE-TSG,Used dialysis bag method to investigated the vitro release of different formulations.The results showed that the dissolution amount of two gels in the same time does not exist significant difference, but at the releases initial, PUE-FL-TSG has certain inhibitory effect to the burst of PUE-TSG, but also has good sustained release, it described PUE-FL-TSG is a ophthalmic preparations of stable release and higher bioavailability.5、Preliminary studied the rheological properties, stability, ocular residence time and irritating.The results show that PUE-FL-TSG should be stored in the dark, eye retention time was significantly better than its liquid formulation,It is non-irritating and has a certain IOP-lowering effect on rabbits.Description PUE-FL-TSG is safe and reliable, can be used to treat glaucoma preparations.In summary,PUE-FL-TSG can improve the burst phenomenon of ordinary temperature-sensitive gel at early delivery.It is a liquid before administration,easy to use and patient compliance is strong.After administration phase becomes gel state,eye stranded for a long time, non-irritating and has a high bioavailability.It is laid the foundation for the study of new drug delivery about ophthalmic preparations,is expected to become the new direction of development of ophthalmic preparations,it has some practical value.