Sustained release formulations using non-aqueous emulsions
A non-aqueous, emulsion technology, applied in non-active ingredients medical preparations, medical preparations containing active ingredients, drug delivery, etc., can solve problems such as low viscosity of fluorocarbons
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example 1
[0096] Example 1: Synthesis of blank microspheres by H / F based bulk emulsion.
[0097] Materials and methods
[0098] Oil and water based emulsion systems are often used for polymer microparticle or nanoparticle synthesis, where hydrophobic polymer materials are dissolved in an organic phase and dispersed in an aqueous continuous phase. However, for water-soluble polymers such as PEG, carboxymethyl cellulose (CMC), and polymers that are readily hydrolyzed in the presence of water, including polyanhydrides, aliphatic polyesters with short midblocks (eg, polylactic acid) As with certain poly(amino acids), such as poly(glutamic acid), conventional water-based emulsion systems are not ideal. The following examples demonstrate the utility of the disclosed H / F emulsion systems for producing the water-soluble or water-degradable polymer microparticles described above. In some embodiments, those polymers are first dissolved in a hydrocarbon solvent comprising polar solvents such a...
example 2
[0105] Example 2: Effect of homogenization speed.
[0106] Materials and methods
[0107] One (1) mL of DCM with 30% w / v or 40% w / v POE was added to 9 mL of FC-40 with 0.5% (w / w) FS FC-40 and mixed with VWR 7mm x The VWR Handheld Homogenizer 200 for the 95mm sawtooth generator probe operates at three homogenization speeds, namely, low (approximately 50% of full power), medium (approximately 60% of full power) and high (approximately 70% of full power) ) for emulsification. The resulting emulsion was stirred under vacuum. The formed microspheres were washed and dried under vacuum.
[0108] result
[0109] as in image 3 shows that for a POE of 30%, low homogenization speed yields larger microsphere sizes, while high homogenization speed yields smaller sizes (Table 2). 40% of POEs showed the same trend. These results show that adjusting the homogenization speed can control the microsphere size.
[0110] Table 2: Microsphere sizes of POE spheres produced at different ...
example 3
[0112] Example 3: General procedure for encapsulation of protein SDPs in POE microspheres by S / H / F based bulk emulsion method.
[0113] Materials and methods
[0114] as in Figure 4 As shown in , the bulk emulsion synthesis can be divided into three steps: formulation, emulsification, and hardening. Due to the different parameters used in these three steps, the properties of the products will vary. The general procedure is described as follows:
[0115] For formulation, 10%-30% w / w total solids weight of VEGF Trap SDP (or fluorescently labeled SDP (F-SDP) for fluorescence imaging) was dispersed in 500 μL by vortexing followed by sonication for 5 minutes 10-35% w / v POE in ethyl acetate. These suspensions were then added to 9.5 mL of FC-40 with 0.1-0.5% w / w FS. Emulsification can be accomplished by stirring, vortexing, or homogenizing using a benchtop homogenizer. The structure of the emulsion is Figure 5 displayed in. Immediately after emulsification, in-process ali...
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