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Objective To prepare paeoniflorin gastric floating tablets and to optimize the formulation.Methods Gastric floating tablets were prepared by wet granulation,with floating performance and in vitro cumulative release rate as evaluat indi-cators,single factor tests and orthogonal design test were adopted for the optimal formulation.Results With HPMC K4M 20% as reinforcing materials,NaHCO315% as gas agent,PVPP 7% as the release of accelerator,lactose as a filler,the ob-tained gastric floating tablet can immediately play bleaching,continued to float more than 12 hours,and the cumulative release rate was more than 90%.Conclusion The optimal formulation of paeconiflorin floating tablet has achieved a sustained and slow release request floating,the operability is good.
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CONCLUSION: Uniform design method should be used to optimize the formulation of MH loaded ophthalmic thermosensitive gel. The optimized formulation containing 230 mg·mL-1 P407 and 80 mg·mL-1 PI88 covered the ophthalmic temperature, which can serve as a potential candidate for ophthalmic application.
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OBJECTIVE:To establish a method for determination of the in vitro release rate of gatifloxacin carried by medical biofibrin glue (MBG-Gat).METHODS:The content of Gat was determined by HPLC on ZORBAX300SB-C18 column with column temperate kept at 30 ℃ and detection wavelength was 293 nm;the mobile phase consisted of potassium dihydrogen phosphate buffered solution (pH 3.5)-acetonitrile (76∶24) at a flow rate of 1 mL?min-1.The volume of injection was 20 ?L.MBG-Gat was placed in normal saline for drug release,with the release solution determined in every 12 h for consecutive 9 days.RESULTS:The linear range of Gat was 5～80 ?g?mL-1 (r=0.999 7) with an average recovery rate of 99.77%～103.53%,RSD≤2.77%(n=5).The accumulative release rate of MBG-Gat in normal saline within 9 days reach-ed above 70%.CONCLUSION:The established method for determination of the in vitro drug release of Gat is proved to be sensitive and reproducible,and it is applicable for the determination and analysis of Gat in vitro.The Gat carried by MBG is characterized by sustained release.
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OBJECTIVE:To prepare compound alendronate sodium sustained-release tablet and to investigate its drug release profile in vitro. METHODS: Hydroxy propyl methylcellulose (HPMC), ethylcellulose (EC), and lactis anhydrous were used to prepare sustained-release tablets by wet granule compression technique with release rate in vitro as index. Orthogonal experiment was conducted to optimize the formula. The release rate of the tablets in vitro was investigated. RESULTS: The optimized formula was as follows: HPMC 80 mg, EC 20 mg, and lactis anhydrous 20 mg. 12 h drug release of the preparation was achieved, and the drug release behavior in vitro fitted Higuchi equation. CONCLUSION: The sustained-release tablet is reasonable in formula and satisfactory in slow release efficacy.
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OBJECTIVE: To prepare and establish a release rate method for the determination of ganciclovir lung-targeted microcapsules.METHODS: The microcapsules were prepared by compound emulsion-dispersion solvent evaporation method.The in vitro drug release amount and release rate of the microcapsules were detected by UV spectrophotometry.RESULTS: The microcapsules were regular in shape with an average particle size of 13.87 ?m.The linear range of ganciclovir was 2～20 ?g?mL-1(r=0.999 9) and its average recovery was 99.96%(RSD=1.68%).The entrapment efficiency of the microcapsules was 63.85% and the drug release amount in vitro reached 40% in 24 hours.CONCLUSIONS: The microcapsules show significant sustained release character.
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OBJECTIVE:To study the preparation method of ranolazine sustained release tablets and to optimize the preparation technology conditions for these preparations. METHODS: The preparation technology conditions were optimized by orthogonal design with the amounts of HPMCP, MC, PH101 and the hardness of ranolazine sustained release tablets as indexes. The optimized results were verified and the in vitro release of ranolazine sustained release tablets was determined. RESULTS: The optimum preparation technology conditions of ranolazine sustained release tablets were as follows: the amounts of HPMCP, MC, PH101 and the hardness were 150mg, 75mg, 30mg, and 10kg, respectively; and the in vitro release rates at 2, 6, and 12h were (29.33?1.05)%, (59.9?1.53)% and (95.60?1.31)%, respectively. CONCLUSION: The delayed release effect of ranolazine sustained release tablets coincided with the predictive value on the whole, and the preparation technology was reproducible. The in vitro accumulated drug release was in conformity with the requirements.
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OBJECTIVE:To optimize the formulation of alprazolam sustained-release tablet and investigate its in vitro release profile.METHODS:Orthogonal experiment was carried out to optimize the formulation of alprazolam sustained-release tablet with the matching percentages of hydroxypropyl methyl cellulose(HPMC),ethyl cellulose and lactose and the specification of the HPMC as factors and with the in vitro release rate as index.The in vitro release rate of the optimized preparation was investigated as well.RESULTS:The optimal formulation of alprazolam sustained-release tablet as follows:the matching percentages of HPMC,ethyl cellulose and lactose were 30%,4% and 15%,respectively,and the specification of the HPMC was K4M.The alprazolam sustained-release tablet prepared in this optimized formulation achieved a sustained release of 24 h with its release profile in line with the Higuchi equation.CONCLUSION:The optimized alprazolam sustained-release tablet is reasonable in formulation and characterized by sustained release.
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OBJECTIVE: To prepare clomipramine hydrochloride sustained release tablet and study its in vitro release rate.METHODS: Orthogonal experiment was carried out to optimize the formulation and the preparation was prepared taking by the formula dosage of HPMC,lactose and amylum pregelatinisatum as factors and the in vitro release rate as index.The in vitro drug release rate was investigated as well.RESULTS: The optimal formulation was as follows: HPMC 45 mg,lactose 35 mg,and amylum pregelatinisatum 40 mg.The preparation prepared in the optimal formulation had a sustained release of 24 h and the release behavior of the tablets followed the zero order equation.CONCLUSION: The formula of the sustained release tablets is reasonable and which had satisfactory sustained release efficacy.
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OBJECTIVE: To prepare double-layer sustained release ornidazole films and investigate its release rate in vitro.METHODS: The double-layer sustained release ornidazole films film were prepared by the method of homogenate.The formula of the films were optimized by orthogonal experiment with the mass ratio of polyviol to CMC-Na(factor A),the total amount of polyviol and CMC-Na(B) and the amount of glycerol(C) as factors.The concentration of ornidazole was determined by ultraviolet spectrophotometry and its release rate was also computed.RESULTS: The double-layer sustained release film was well-shaped.The optimized formula of the film was as follows: factor A=1∶1,B=4.5 g,C=4.0 g.The standard curve of ornidazole was linear within a range of 1～20 ?g?mL-1(r=0.999 5,n=6),with an average recovery of 100.3%(RSD=1.3%,n=5).A continuous releasing of 11.0 hours was achieved for the prepared films and its cumulative release amount in vitro within 8 hours reached 81.50%.CONCLUSIONS: The preparative method of the films was simple,and the film had a slow-release property.
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OBJECTIVE: To optimize the formulation of metformin hydrochloride sustained-release pellets prepared using film coating technology. METHODS: Taking release rate in vitro as index, the formulation of the film-coat was prelimilarily selected using one facotr sreening method and optimzed using orthogonal test. The release rate of the prepared metformin hydrochloride sustained-release pellets was determined and compared with that metformin hydrochloride pellets. RESULTS: The optimized formulation was as follows: the film material of Eudragit NE 30D and Eudragit L 30D55 at a ratio of 10∶1 were added with 40% talcum powder and 0.25% sodium dodecyl sulfate. The release rate of the metformin hydrochloride sustained-release pellets was higher than that of metformin hydrochloride pellets. CONCLUSION: The metformin hydrochloride sustained-release pellets were up to the requirements of sustained release and characterized by 24h continuous drug release.