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The study assessed the phytochemical, nutritional and antioxidant properties of a functional tea made from mixture of Utazi leaf Gongronema latifolium), Nchanwu leaf (Ocimum gratissimum) and Turmeric rhizome (Curcuma longa). The three spices were individually processed by drying and mincing before combining them at different ratios that resulted to 16 samples. The samples were generated through D-optimal mixture design using statistical software (Design Expert version 12). The samples were evaluated for phytochemical, nutritional and antioxidant properties. The fresh raw materials were destalked (for the leaves), sorted, washed, withered, oxidized for 24 h, oven dried at 60oC for 30 min, cooled and milled, and packaged. Fresh turmeric rhizome were sorted, washed blanched at 90oC for 2 min, cooled, peeled, sliced, oven dried at 60oC for 30 min, cooled, milled and packaged in teabags and high density polyethylene. The alkaloids, saponin, phenol, cardiac glycoside, flavonoid, tannin, steroid and anthocyanin content ranged from 12.00-22.00, 0.42-1.15, 11.67-15.63, 0.06-0.67, 12.67-22.00, 0.56-0.89, 1.00-1.67, 46.00-54.00 mg/100g respectively. The vitamin C and E content ranged from 3.03-4.13, 0.31-0.64 mg/100g respectively. The minerals iron and zinc content of the tea samples ranged from 3.53-4.70, 0.06-0.78 ppm respectively. The sensory evaluation score of the tea infusion of the sample AB and DA were ‘liked very much’ with the rating of 8.60 and 8.20 respectively, these samples were more acceptable to the panelist. The antioxidant scavenging activity ranged from 42.00-47.00% with sample EC exhibiting the highest level of activity, and the proportion was 70g, 24.62g, 5.38g of Utazi leave, Nchanwu leave, and Turmeric rhizome.
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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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SUMMARY Blepharitis is a common chronic eye condition that causes eyelid inflammation, leading to inflamed, irritated, sticky and itchy eyelids and flaking of the skin. For its treatment, patients often need indefinite use of an eyelid cleaning solution which usually cost more than 20 USD per 80 ml bottle and lasts, on average, one month. For those patients unable to afford the treatment, physicians recommend the use of a do it yourself (DIY) solution. However, the efficacy of DIY eyelid solutions might fluctuate according to the type of blepharitis present in the patient and inadequate pH stabilization of the solution might promote additional itchiness, irritation, and dryness of the skin and eyes. Thus, we propose an optimized DIY solution prototype for symptom management in patients with chronic blepharitis. The formulation contains a significant ratio of tea tree oil and resulted in suitable pH and foam expansion values. The low cost and ease of preparation of the designed formulation make it an affordable, effective alternative in the treatment of chronic blepharitis.
RESUMEN La blefaritis crónica es una condición ocular que causa inflamación en los párpados, dando como resultado párpados irritados, pegadizos y descamación de la piel. Pacientes con esta condición necesitan usualmente de la aplicación de una solución de limpieza de párpados que cuesta en promedio 20 USD por cada 80 ml de solución y tiene un rendimiento de un mes. Para aquellos pacientes incapaces de costear el tratamiento, los médicos recomiendan el uso de soluciones hazlo tú mismo (DIY en inglés). Sin embargo, la eficacia de estas en el tratamiento de la condición puede fluctuar de acuerdo con el tipo de blefaritis presente. Adicionalmente, una inadecuada estabilización del pH de la solución puede promover una mayor irritación, resequedad y picazón en la piel y en los ojos. Por lo tanto, en este trabajo proponemos un prototipo experimental de solución DIY para el manejo sintomático de pacientes con blefaritis crónica. La formulación contiene una proporción significativa de aceite de árbol de té y posee un pH adecuado y alta producción de espuma para su correcta aplicación en la piel. El bajo costo y facilidad de preparación hacen de ella una alternativa efectiva y asequible en el tratamiento de la blefaritis crónica.
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Objective To prepare water-in-oil gardenoside emulsion, optimize its formulation process, and evaluate the quality. Methods The formulation was optimized based on emulsification time, oil floating time and phase separation time, and investigated the optimal gardenoside emulsion by the single factor investigation and mixture design. The properties, stability, content, and in vitro release of the emulsion were also studied. Results The mean particle size of gardenoside emulsion was (5.48 ± 0.02) μm and the value of PDI was 0.125 ± 0.096; Centrifugation accelerated test was performed at 4 000 r/min for 15 min without delamination; The average mass fraction of gardenoside emulsion was 92.14% and RSD was 1.86% (n = 3); The in vitro release of gardenoside emulsions at pH 4.5, 6.8, and 7.4 was up to 105.32%, 98.41%, and 98.70%, respectively, while the in vitro release at pH 1.2 was up to 63.45%; Finally, the law of drug release was explained by fitting equation. Conclusion The high speed shear mechanical method can be used to prepare gardenoside emulsion, and the quality evaluation of the optimized prescription meets the requirements.
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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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AIM To prepare the moisture-proof granules of polysaccharides from Astragali Radix.METHODS Mixture design was adopted in the optimization of excipient proportion after moisture absorption determination of mixed powder of polysaccharides and seven excipients.With the influencing factors of ethanol concentration,ethanol amount,drying temperature and drying time,together with the evaluation indices of moisture absorption rate and non-forming rate,the preparation was optimized by orthogonal test based on single factor test.The critical relative humidities were then compared after drawing moisture absorption curves of polysaccharides,mixed powder and granules.RESULTS The mixed powder with an optimal ratio (1 ∶ 2) of polysaccharides to mixed excipients (46.3％ lactose,14.5％ mannitol and 39.2％ microcrystalline cellulose) was found to remain the moisture absorption rate of 11.6％ within 168 h.The optimal conditions were determined to be 70％ for ethanol concentration,0.125 times for ethanol amount,55 ℃ for drying temperature,and 60 min for drying time,the moisture absorption rate was 8.1％ within 168 h,and the non-forming rate was 11.46％.Compared with polysaccharides and mixed powder,the granules showed relatively lower initial velocity and acceleration (absolute value) of moisture absorption,and relatively higher critical relative humidity.CONCLUSION The granules of polysaccharides from Astragali Radix prepared by this method show a good moisture-proof effect.
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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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The enzyme α-L-rhamnosidase specifically cleaves terminal rhamnose residues from a wide variety of natural products. This property endows this enzyme with important biotechnological potential as L-rhamnosidase could be employed in a variety of applications, including removing bitterness from citrus fruit juices, improving the aroma of wines and converting clinically important steroids. This work optimized α-L-rhamnosidase solid-state fermentation production from Aspergillus niger 426 using statistical methods. Firstly, a statistical mixture-design with three components to determine the best ratio of nutrients for enzyme production was carried out. The optimal conditions consisted of growing the fungi in media containing 0.14 g of cane sugar bagasse, 1.25 g of soybean hulls and 3.05 g of rice straw; these conditions achieved a maximum α-L-rhamnosidase activity of 1.92 U / mL. Next, a 3² Box-Behnken design to optimize culture moisture levels and nutrient solution pH values for enzyme production was carried out. α-L-rhamnosidase activity increased to 3.02 U / mL when medium moisture was 75.5% and pH value of 4.0.
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The flowers of Tagetes patula L., Asteraceae, commonly known as French marigold, are used in folk medicine as an antiseptic, diuretic, blood purifier and insect repellent. This study was conducted to optimize the extraction process through the biomonitoring of flavonoids, using a statistical mixture simplex-centroid design, to evaluate the effect of the solvents water, ethanol and acetone, as well as mixtures of these solvents, assessed by the total flavonoid content. The extracts were tested for dry residue, radical scavenging activity, chromatographic profile, and larvicidal activity. The acetone extract had the highest total flavonoid content, 25.13 ± 1.02% (4.07%); and the best radical scavenging activity, with IC50 of 15.74 μg/ml ± 1.09 (6.92%), but with lower dry residue, 6.62 ± 1.33% (20.10%). The water extracts showed higher levels of dry residue, but lower total flavonoid content and radical scavenging activity than the acetone extract. The positive correlation between the total flavonoid content and radical scavenging activity of the extracts showed that flavonoids contribute significantly to the antioxidant capacity. The statistical mixture design allowed us to optimize the extraction of flavonoids from flowers of T. patula, with acetone as the best extraction solvent. Preliminary studies on the biological activity of the optimized extracts demonstrated a larvicidal effect of the acetone extract on Aedes aegypti mosquitoes.
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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.
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The present study describes the design and development of buoyant matrices of dipyridamole. The matrices were prepared by direct compression method using simplex lattice design as an optimization technique. Amount of HPMC K4M (X1), sodium bicarbonate (X2) and ethyl cellulose (X3) were used as the independent variables where floating lag time (Y1) and percentage drug release at 6h (Y2) were considered as the response variables. As per the simplex lattice design total 7 formulations were formulated. Matrices were evaluated for physical parameters, in-vitro buoyancy, in-vitro drug release, water uptake studies. Drug release data was fitted into different kinetic models. The results of response variables were statistically evaluated using design expert 8.0 software. Polynomial models were generated for all the response variables using multiple linear regression analysis (MLRA) approach. A statistical model incorporating 7 interactive terms was used to evaluate the responses. The results of response variables are expressed for model analysis by Scheffe’s special cubic model. Graphical representation was done by response surface plots and contour plots. The resulted model equation showed that factor X1 responsible for prolongation of drug release. On the basis of acceptance criteria the formulation coded by DP3 was selected as a promising formulation from the simplex lattice batches which fitted best to zero order release kinetic model.
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Se desarrolló por primera vez en Cuba, una formulación de jalea de piroxicam al 0,5 %. Se tomó como referencia la composición de la formulación líder del mercado FELDENE GELâ, a la cual se le efectuaron algunas modificaciones. Se realizaron 4 experimentos en las evaluaciones preliminares que sirvieron de base para la etapa posterior de diseño y optimización de la formulación. Se aplicó un diseño de experimentos con mezcla, para lo cual se emplearon como variables independientes la concentración de Carbopol 940, trietanolamina y hidroxipropilmetilcelulosa. Se evaluó la influencia de estos componentes en el pH, el área de extensibilidad y en algunas propiedades organolépticas. A partir de estos resultados, se seleccionó una formulación óptima.
For the first time in Cuba a 0.5 % Piroxican jelly formula was developed. The point of reference was the leader formula from FELEDENE GELâ; market which underwent some modifications. During first assessments four experiments were carried out as basis for the later stage of formula design and optimization. An experimental design with mixture was applied using as independent variables the concentration of Carbopol 940, Trietanolamine, and Hidroxypropyl methylcellulose. Influence of these components on pH, the extensibility area, and on some organoleptic properties. From these results, an optimal formula was selected.
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OBJECTIVE:To evaluate the application of mixture design in the design of formulation.METHODS:Isosorbide mononitrate (ISMN) was used as model drug,and the formulation of ISMN sustained-release tablet was optimized by the mixture design.The optimized ISMN sustained-release tablets were compared with the ISMN sustained-release tablets in market in respect of the release rate in vitro.RESULTS:The comparison between the validating value and the target value of the optimized sample showed a similarity factor(f2) of 86.56,and there were no differences between the optimized sample and that in market in respect of the drug release in vitro.CONCLUSION:The mixture design is applicable for the optimization of formulation and it can be used to predict the drug release in vitro.