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Objective::To optimize the matrix prescription of Fufang Huangqi cream and evaluate its rheological properties. Method::With appearance, spreadability and stability as evaluation indexes, the weighting coefficient of each evaluation index was determined by analytic hierarchy process (AHP), criteria importance through intercriteria correlation method (CRITIC) and AHP-CRITIC mixed weighting method. The formulation of Fufang Huangqi cream was optimized by D-optimal mixture design and its rheological properties were evaluated. Result::The weight coefficients of appearance, spreadability and stability according to AHP-CRITIC mixed weighting method were 0.185, 0.282 and 0.532, respectively. According to D-optimal mixture design based on AHP-CRITIC analysis, the optimized formulation of Fufang Huangqi cream was liquid paraffin of 3.70 g, vaseline of 2.00 g, stearic acid of 2.00 g, sodium dodecyl sulfate of 5.90 g, glycerin of 6.00 g and extract of 20.40 g. The rheological parameters of Fufang Huangqi cream was non-newtonian index<1, storage modulus>loss modulus. Conclusion::The preferred matrix formulation is stable and feasible. Fufang Huangqi cream has good appearance and is a shear thinning non-newtonian fluid. Its viscosity and ductility meet the needs of industrial production and clinical application.
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Objective: To prepare osthole foaming microemulsion and study its foaming force. Methods: In this paper, the overall desirability of drug loading rate, half foam life period, and foaming force was taken as index. Based on the result of solubility test and pseudo-ternary phase diagram, the formula for the osthole foaming microemulsion was optimized by D-optimal mixture optimization design test. Results: The optimal ratio of the prescription was as follows: ethyl oleate-Cremophor EL-40-transcutol P-water (8.13: 14.81: 6.58: 71.44); Average particle size was (43.54 ± 3.43) nm (n=3), average polydispersity factor was (0.839 ± 0.092) % (n=3), average potential was (-2.32 ± 0.78) mV (n=3), frothing volume was (8.57 ± 0.28) cm, half foam life period was (6.79 ± 0.32) min. At 37℃, the maximum drug loading of foaming microemulsion was 13.62 mg/g, and the solubility in water was 0.42 mg/mL. Conclusion: Osthole foaming microemulsion was stable, which could greatly increase the solubility of osthole and remarkably enhance the bioavailability of osthole.
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Objective: To develop and optimize a self-microemulsifying drug delivery system (SMEDDS) formula for improving the dissolution of atorvastatin calcium.Methods: Solubility and pseudo-ternary phase diagram were used to select the suitable type and amount range of oil phase, surfactant and co-surfactant.D-optimal mixture design was used to optimize the formula of atorvastatin calcium SMEDDS.The morphology, particle size distribution and zeta potential of the microemulsion were determined by a dilution method.The in vitro drug release profiles of the marketed atorvastatin calcium tablets and the self-made SMEDDS were compared.Results: The formula of atorvastatin calcium SMEDDS was as follows: Capmul MCM as the oil phase, Labrasol as the surfactant and Transcutol P as the co-surfactant with the optimal weight ratio of 13.0∶43.5∶43.5.The self-made SMEDDS was a clear and transparent microemulsion solution with homogeneous small spheres as seen under a transmission electron microscope.The particle size, PdI and zeta potential of the self-made SMEDDS was (34.2±13.6) nm, (0.169±0.04) and (-21.1±1.3) mV, respectively.The in vitro release profile indicated that the accumulated release of the self-made SNEDDS reached up to nearly 100% in 45 min.Conclusion: The optimal formula of atorvastatin calcium SMEDDS optimized by D-optimal mixture design can improve the drug dissolution rate effectively.
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Objective:To optimize the formula of adefovir dipivoxil tablets and investigate the dissolution in vitro. Methods:The formula was optimized by the D-optimal mixture design, the effects of the amount of filler ( X1 ,%) , the amount of disintegrant agent ( X2 ,%) and the amount of binder ( X3 ,%) were selected as the independent variables, and the friability ( Y1 ,%) , disintegration time ( Y2 , min) and dissolution of adefovir dipivoxil ( Y3 ,%) were the dependent variables. The similarity of the self-prepared prepa-ration and the reference preparation was obtained by using f2 similarity factor. The stability of adefovir dipivoxil tablets was evaluated preliminarily by high temperature, high humidity and strong light testing. Results:The optimal formula of adefovir dipivoxil tablets was as follows:the amount of lactose monohydrate was 67. 0%, the weight of croscarmellose sodium was 8. 0% and the amount of pregelati-nized starch was 12. 0%. The prepared tablets had lower friability, shorter disintegration time and higher drug dissolution rate. The dissolution similarity factors of the self-prepared tablets and the reference preparation in four dissolution media were all greater than 50. The results of influencing factor tests showed that the product should be moisture preservation. Conclusion:The formula of adefovir dip-ivoxil tablets optimized by the D-optimal mixture design is similar to that of the reference preparation, and the preparation process is feasible, which can meet the requirements of large production.
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OBJECTIVE: To prepare enramycin self-microemulsifying drug delivery system (SMEDDS) and evaluate its quality. METHODS: The formulations of enramycin SMEDDS were screened by solubility experiment and self-emulsifying grading test. The formulation was optimized using Design Expert Software, taking particle size as dependent variable and the usage amoumts of oil, surfactant, and cosurfactant as independent variables. RESULTS: The optimized formulation of enramycin SMEDDS consisted of 20% ethyl oleate, 40% RH40, and 40% 1,2-propylene glycol. 1.0 g mixture contained 20 mg enramycin, which dispersed rapidly into water and the particle size of the formed emulsion was (27.81±0.79)nm. The enramycin SMEDDS dissolved by more than 90% within 10 min, much faster than that of enramycin API. The particle size and concentration of SMEDDS were stable at alternative temperature cycles (4 and 40℃) for 48 h, and the SMEDDS formulation had no effect on the bacteriostasis of enramycin. CONCLUSION: The quality of enramycin SMEDDS is stable. The system increases the dissolution of enramycin significantly and could be advantageous to improve the oral bioavailability of enramycin.
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To optimize the matrix formulation of Chaizhi cataplasma (CC) and investigate its release and transdermal absorption properties in vitro. The optimized matrix formulation of cataplasma containing liquid herbal extract is determined by using D-optimal mixture design, with initial bonding strength, endurance bonding strength and gel strength as the evaluating indicators. Modified Franz diffusion cells were used to study the in vitro release and transdermal absorption of geniposide in CC. The optimized matrix formulation of CC contained NP700, aluminum glycinate, tartaric acid, glycerin, PVPK90 and water (9∶0.7∶0.8∶30∶5∶30.5). Cumulative release rate of geniposide in CC was (77.02±3.73)% in 24 h. The percutaneous penetration rate of geniposide was 7.25 μg•cm⁻²•h⁻¹ and the 24 h permeated amount was (156.22±4.90) μg•cm⁻². The optimized CC prepared by the D-optimal mixture design showed a good adhesion and formability. The in vitro release of the geniposide in CC was in accordance with the first order equation, while its in vitro transdermal absorption was close to the zero order equation.
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Objective: To optimize the matrix formulation of Hanbishu Cataplasma (HC) and to investigate its realease and transdermal absorption properties in vitro. Methods: To optimize the cataplasma with liquid extract by D-optimal mixture design, using initial bonding strength, endurance bonding strength, and gel strength as evaluating indicators, and to validate the optimal formulation. Modified Franz diffusion cells were used to study the in vitro release and transdermal absorption of osthole in the HC. Results: The matrix formulation of HC was as follows: NP700 6.97 g, aluminum glycinate 0.30 g, tartaric acid 0.25 g, glycerin 35.00 g, PVP K90 3.87 g, water 43.61 g, and Hanbishu liquid extract 10 g. Cumulative release rate of osthole in HC was (63.30 ± 0.05)% in 24 h. The percutaneous penetration rate of osthole was 0.16 μg/(cm2∙h) and the 24 h permeated amount was (3.61 ± 0.32) μg/cm2. Conclusion: The optimal prescription of HC optimized by D-optimal mixture design has good adhesion and formability. In vitro release characteriistics of osthole in HC conform to the first dynamical equation, and the transdermal absorption behavior is a zero-order kinetics.
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Objective: To explore the feasibility of self-emulsifying drug delivery system (SEDDS) for multicomponents simuitaneous solubilization. Methods: The curcumin (Cur) components were used as model drug, D-optimal mixture design was used to optimize SEDDS prescription, and the contents of bisdemethoxycurcumin (BDMC), demethoxycurcumin (DMC), and Cur, SEDDS particle size, and emulsifying time were made as indicators to select and evaluate SEDDS, so as to explore the feasibility of SEDDS for the multicomponents simuitaneous solubilization. Results: The optimal SEDDS prescription was Obleique CC497-Tween 20-Transcutol P (0.21:0.50:0.29), SEDDS particle size was (248.8 ± 3.4) nm, and emulsifying time was (70 ± 1) s. At 37°C, the maximum loading capacities of SEDDS for BDMC, DMC, and Cur were 2.998, 12.220, and 52.561 mg/g, respectively, and the solubilities in water were 0.107, 0.661, and 1.648 mg/mL. Conclusion: SEDDS can realize the solubilization of multicomponent simultaneously.
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Objective: To optimize the matrix formulation of Periplaneta americana Cream. Methods: To optimize the blank matrix formulation by D-optimal mixture design, using presentation, spread property, centrifugal stability, cold stability, and thermostability as evaluating indicators, and to investigate the dosage of P. americana extract. Results: The matrix formulation of P. americana Cream was as follows: glycerol 11.00 g, stearic acid 14.00 g, triethanolamine 3.50 g, atolein 18.00 g, petrolin 10.00 g, water 43.50 g, and the amount of P. Americana extract 1.0 g. Conclusion: D-optimal mixture design is an effective and systematic method which could optimize the matrix formulation to reach the optimum presentation and physical property.