ABSTRACT
In this study a new soluble solid curcumin nanoemulsion powder was prepared using spray-drying technology to improve the solubility and bioavailability of curcumin. The liquid nanoemulsion consisted of curcumin, Capryol 90, Transcutol P, and Cremophor RH40. The solid nanoemulsion was prepared by spray-drying the liquid nanoemulsion in laboratory spray dryer, using lactose as solid carrier. The in vitro release from powder formulation was 97.6% within 15 min while the release from the curcumin crystalline was about 10%. An oral pharmacokinetic study was conducted in rats and the relative bioavailability of spray-dried curcumin powder significantly increased compared with that of curcumin crystalline. The Cmax value of solid curcumin nanoemulsion powder was 5.5-fold greater than the value of the curcumin crystalline in aqueous suspension. The absorption mechanism of the spray-dried curcumin powders was discussed. The results indicate that spray-drying in combination with nanoemulsion was a powerful methodology for improving the dissolution rate and oral bioavailability of curcumin
ABSTRACT
Solid dispersion technique has been developed many years for improving solubility of water-insoluble drugs, aiming to achieve a better oral bioavailability. However, this technique exhibits many inconveniences when used for large-scale tableting procedures. The objective of current research work was to develop cilnidipine solid dispersions [SDs] to improve the dissolution behaviors of this water-insoluble drug. Moreover, an innovative granulation method was designed to simplify the traditional tableting technology used in solid dispersion technique. Three different kinds of polymers, polyethylene glycol [PEG], polyvinylpyrrolidone [PVP] and poloxamer, were used as carriers to prepare solid dispersions. The interactions in the solid state were characterized by differential scanning calorimetry [DSC], powder Xray diffraction [PXRD] and FT-IR spectroscopy. The designed granulation method was employed to prepare solid dispersion tablets and the formulation was optimized through investigating the dissolution behaviors. The results indicated PEG solid dispersion showed the best effect both on physical characterizations and dissolution studies. Furthermore, all type of solid dispersions significantly improved the dissolution rates when compared to pure drug and its corresponding physical mixture [PM]. The solid dispersion tablets prepared in simplified tableting method exhibited better operability, stability and dissolution behavior than the tablets prepared in traditional ways, which brought more opportunities to solid dispersion technique for industrial production
Subject(s)
Tablets/chemistry , Technology, Pharmaceutical/methods , Water/chemistry , X-Ray Diffraction/methods , Spectroscopy, Fourier Transform Infrared/methods , Poloxamer/chemistry , Polyethylene Glycols/chemistry , Polymers/chemistry , Povidone/chemistry , Powders , Solubility , Dihydropyridines/chemistry , Drug Carriers/chemistryABSTRACT
OBJECTIVE:To optimize the formulation of dextromethorphan hydrobromide sustained-release tablets. METHODS: The dextromethorphan hydrobromide sustained-release tablets were prepared with HPMC as sustained release matrix. Orthogonal test was performed to optimize the formulation with in vitro accumulative drug release rate as index and the amount of HPMC and lactose as well as ethylcellulose (EC) concentration as factors. Then verification test on the in vitro drug release characteristics of the optimized tablets were performed and the influencing factors (high temperature,high light,and high moisture) were investigated as well. RESULTS: The optimized formulation of dextromethorphan hydrobromide sustained-release tablets was as follows: 30 mg HPMC,50 mg lactose,and 8% EC. The accumulative drug release rate at 8 h was above 70%. In the influencing factor test,the tablets were stable under all conditions except at high moisture condition. CONCLUSION: The optimized formulation of dextromethorphan hydrobromide sustained-release tablets is feasible.
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OBJECTIVE:To prepare epirubicin hydrochloride solid lipid nanoparticle(EPI-SLN) and investigate its physicochemical property. METHODS: EPI-SLN was prepared by ultrasonic dispersion technique with glyceryl behenate as matrix,and the appearance,particle size,? electric potential,and entrapment efficiency of the SLN were evaluated and its stability at 3 month storing at 4 ℃ was investigated. RESULTS: EPI-SLN assumed spherical shape with a particle diameter of (212.8?6.2) nm,? electric potential of (-24.7?0.3) mV and entrapment efficiency of 82 %. The EPI-SLN at 4 ℃ was stable after storing for 3 months,showing no marked change in mean diameter,? electric potential or entrapment efficiency. CONCLUSION: The prepared EPI-SLN is up to the standard.
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OBJECTIVE:To prepare Yinxingye extract pellets and study its in vitro drug release rate.METHODS:The Yinxingye extract were coated with 3 coating materials(opadryⅡ,Eudragit L30D-55 and Eudragit S 100,respectively)to be prepared into pallets by centrifugalized palletizing method;and the 3 different coated pallets were prepared into mixed pallets in an pre-designed ratio.The in vitro release of the 3 coated pallets and the mixed-coated pallets were determined by changing the pH-gradient of media(0.1 mol?L-1 hydrochloric acid,pH 5.8 PBS,pH 7.2 PBS).RESULTS:The pallets coated with 3 different coating materials released quickly in 0.1 mol?L-1 hydrochloric acid,pH 5.8 PBS and pH 7.2 PBS,and the pellets with mixed coating materials had a sustained release until a complete release within about 8 h in pH gradient-changed media.CONCLUSION:The preparation process is feasible and provides theoretic basis for industrial production.
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OBJECTIVE:To optimize the preparation technology of roxithromycin microspheres.METHODS:The microspheres of roxithromycin were prepared by the emulsion-solvent diffusion method with ethylcellulose used as capsule wall material.The preparation technology of microspheres was optimized by orthogonal experiment taking encapsulation efficiency as index with the ratio of roxithromycin to ethylcellulose(A),the concentration of ethylcellulose(B)and the ratio of water phase to oil phase(C)as factors.The appearance,particle diameter,drug-loading amount,encapsulation efficiency,in vitro release and bitter smell were studied.RESULTS:The optimal preparation conditions were as follows:A was 1∶1,B was 30 ?g?mL-1 and C was 4∶1.The microspheres obtained were round and well-distributed with mean diameter of 75.0～90.0 ?m,drug-loading amount of 45%～46%,encapsulation efficiency of over 90% and sustained release for over 13 hours.No bitter taste of the roxithromycin-ethylcellulose microspheres was felt by the majority of subjects.CONCLUSION:The roxithromycin microspheres made by optimization technology was bitter-masked and sustained release.
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OBJECTIVE:To observe the anti-inflammatory,diuretic,and antipyretic action of Miniaoning granules after improvement of its preparation technology.METHODS:The rats' feet swelling degree and the mice's ear swelling degree,the urine volume,and the body temperature action of Miniaoning granules in vitro were observed through rats' feet swelling method,dimethyl benzene-induced mice ear swelling method,diuretic experiment,yeast-induced rats' febrile,respectively.RESULTS:After medication,the degree of rats' feet swelling and mice's ear swelling were significantly attenuated,and the urine volume increased markedly and body temperature lowered.CONCLUSION:As compared with the original formulations,Miniaoning granules prepared in improved technology have similar antipyretic effect but more potent anti-inflammatory and.diuretic action.
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OBJECTIVE: To prepare and evaluate the quality of clarithromycin microcapsules.METHODS: Clarithromycin microcapsules were prepared by emulsion-solvent volatilixation method using ethylcellulose as capsule wall material.The particle size,entrapment efficiency,the loading amount and the drug release property in vitro were investigated.RESULTS: The prepared microcapsules were well-distributed in particle size with average particle size at 33.0～38.0 ?m,encapsulation efficiency at above 87%,loading amount above 45%,and accumulative drug release rate of 75% at 6 h.CONCLUSION: The method is simple and feasible and the quality of prepared microcapsules is up to the standard.
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Objective To investigate the in vivo pharmacokinetics of ligustilide in Ligusticum chuan-xiong essential oil after ig administration in rats. Methods The concentration of ligustilide in plasma of rats after ig administration of ?-cyclodextrin compound in L. chuanxiong enssential oil was determined by RP-HPLC method with the osthole as the internal standard. The plasma concentration-time curve was plotted. The main pharmacokinetic parameters of ligustilide were obtained by 3P97 software. Results Ligustilide in rats fits the two compartments model and the main pharmcokinetic parameters were as follows: tl/2(?), (1.429?1.161) h; tl/2(?), (6.877?2.275) h; t(peak), (3.401?1.951) h; and AUC were (70.87?25.92) ?g/mL?h, respectively. Conclusion RP-HPLC Method with osthole as the internal standard is accrurate, sensitive, and rapid for the study on pharmacokinetics of ligustiliden in rats in vivo.