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Objective: To prepare the total ginkgo flavonoid (TGF) self- microemulsifying oral fast dissolving films (SMEOFDF) and evaluate its in vitro properties. Methods: The formulation of TGF self-microemulsifying drug delivery system (SMEDDS) was optimized based on the solubility method and the pseudo-ternary phase diagram, and then the influence of formulation on disintegration time and film forming property were observed by single factor test. Microemulsified performance, disintegration time, content uniformity, and release profiles in vitro were investigated. The surface feature of TGF SMEOFDF was detected by scanning electron microscope and the crystal form of drug was characterized by differential scanning calorimetry. Results: The average particle size was (48.1 ± 5.45) nm with non-difference from SMEDDS. The average time to disintegrating was (9.94 ± 0.26) s and the releasing drug at 5 min of TGF SMEOFDF was (70.98 ± 0.31)% in vitro. Conclusion: SMEOFDF which has both advantages of SMEDDS and fast dissolving oral films is a new dosage form with profound application prospect.
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Objective: To study the formulation of puerarin (PUE) self-microemulsifying drug delivery system (SMEDDS). Methods: The optimum formulation of PUE SMEDDS was screened by test of solubility, compatibility of oil and surfactant, and pseudo-ternary phase diagram, and the prescription of PUE SMEDDS was optimized by particle size, self-microemulsifying time, and drug loading; The physicochemical characteristics and stability were also determined. Results: The optimum SMEDDS composed of Miglyol 812N (19.0%), oleic acid (19.0%), polysorbate 80 (19.0%), EL-35 (19.0%), 1, 2-propanediol (19.0%), and puerarin (5.0%). The particle size was (17.28 ± 0.24) nm, and self- microemulsifying time was less than 120 s; The appearance, content of PUE, particle size, and self-microemulsifying time had no obvious changes under room temperature storage for six months. Conclusion: The acquired PUE SMEDDS is stable with small particle size, which meets the needs of good SMEDDS formulation.
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Objective To optimize the formulation of self-microemulsifying drug delivery systems containing tanshinone ⅡA(tanshinone ⅡA-SMEDDS) and assess the quality of tanshinone ⅡA-SMEDDS. Methods Pseudoternary phase diagrams were used to choose the oil,emulsifier,co-emulsifier,and their proportion in the formulation on the basis of the ability to form emulsions and regions. Then the self-emulsifying time,droplet and morphology,size distribution,?-potential,stability,and other aspects of the quality were evaluated. Results The formulation of tanshinone ⅡA-SMEDDS was as follows:ethyl oleate-Labrasol-PEG 400=10%:45%:45%,drug loading ratio was 2.25 mg/g. The self-microemulsifying time of tanshinone ⅡA-SMEDDS in 0.1 mol/L hydrochloric acid solution was less than 1 min,the emulsion drops were spherical shape with average particle size of (84.9?2.1) nm and the average ?-potential (-24.0?1.15) mV (n=3). So tanshinone ⅡA-SMEDDS was stable. Conclusion In this paper,the tanshinone ⅡA-SMEDDS has a good self-emulsifying performance. It is expected to further stabilize the preparation of tanshinone ⅡA self-microemulsifying agents.
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Objective To study formulation and characteristics of self-microemulsifying drug delivery system for breviscapine(BRV-SMEDDS).Methods The optimum formulations of BRV-SMEDDS were screened by solubility tests,formula compatibility,and pseudo-ternary phase diagrams.And the physicochemical characters,dissolution in vitro and in situ rat's intestine absorption of BRV-SMEDDS were also observed.Results The optimum formulation of SMEDDS was composed of Maisine 35-1-Cremophor RH40-PEG400-TEA=25∶40∶35∶7.The particle diameter was 88.6 nm.The percent of accumulated dissolution of BRV in SMEDDS in vitro was up to 97.8% at 1h,which was 8.0 times as much as that of BRV powder,and 5.1 times as BRV tablets.In the tests of in situ rat's intestine absorption,the permeability coefficient of BRV-SMEDDS was increased by 3.4 times as much as BRV powder,and 3.3 times as BRV tablets.Conclusion The dissolution and absorption of BRV is improved by formulation of SMEDDS.It could provide reference for the new dosage form of BRV.
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Objective To develop the formulation of self-microemulsifying drug delivery system for hawthorn leaves flavonoids (HAW-SMEDDS). Methods The optimum formulations of oil phase, surfactant, and assistant surfactant for HAW-SMEDDS were screened by solubility test, compatibility test, and pseudo-ternary phase diagrams, with the time of formulating microemulsion, the consequence of visual examination, and particle size as indexes. The dissolution of HAW-SMEDDS was measured, taking the commercial tablet Yixintong Tablet as reference. Results The optimum self-microemulsifying drug delivery system was composed of Labrasol (35%), Transcutol P (10%). The particle diameter was (39.5?5.4) nm, the time of self-microemulsifying was less than 1 min. The percent of accumulated dissolution of hawthorn leaves flavonoids in SMEDDS in distilled water was up to 70% at 10 min, while that in the Yixintong Tablet was less than 50% at 60 min. Conclusion The formulation of HAW-SMEDDS preparation could meet the request of the design. It could provide the reference for the new dosage form.
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Objective The self-microemulsifying drug delivery system(SMEDDS) with tanshinone ⅡA was prepared in order to develop its new dosage forms.Methods Pseudo ternary phase diagrams were used to evaluate the self-microemulsification existence area under emulsifier,coemulsifer,and oil phase.The HPLC analysis in vitro was set up.Solubility in various vehicles was determined.The self-microemulsification efficiency was assessed,such as stability,particle size,and Zeta potential.Results The solubi-lity of tanshinone ⅡA in SMEDDS was about 2.5 mg/g,droplet size was within 20 nm,and the absolute value of Zeta potential was over 60 mV.The stability of SMEDDS with tanshinone ⅡA was better in centrifugal condition with high temperature but not good enough to the light.Conclusion The SMEDDS can make tanshinone ⅡA solublized in water,and is an optimum vehicle in new dosage forms of tanshinone ⅡA.
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Objective To develop self-microemulsifying drug delivery system(SMEDDS) of Acanthopanax senticosus total saponins(ASTS) and the determination method.Methods The equilibrium solubility of ASTS in different compositions of oils,emulsifier and assistant emulsifier was investigated.The self-microemulsion formula was optimized by constructing the pseudo-ternary phase diagrams of blank SMEDDS and the studying the self-microemulsifying efficiency and the stability of drug-loaded SMEDDS.Taking isofraxidin,an effective component of A.senticosus,as the content determination index,the content was determined by HPLC.Results The optimal self-microemulsion formula was composed of Caf,propanediol,and ethyl linolenate.The ratio of them was 16∶4∶5.The average particle size was 40 nm.The average content of isofraxidin was 92.6 ?g/mL.Conclusion The acquired microemulsion with small particle size is stable.The content determination method of taking isofraxidin as the quality control index is accurate and reliable.