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1.
Polymeric microparticles containing carvedilol (CRV) were obtained successfully using a simple emulsion/organic evaporating method. Three different formulations were developed using poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) and polycaprolactone (PCL) as polymers; the resulting samples were submitted to physical–chemical characterization and in vivo evaluation. The physical–chemical analysis indicated that the PHBV promoted a porous aspect in the microparticle's surface, while PCL a smooth aspect. The PCL-CRV microparticles showed a higher loading efficiency and a longer drug release time, being selected for in vivo evaluation. The in vivo assays indicated that PCL-CRV polymeric microparticles has a pharmacological antihypertensive effect for a longer period of time, representing a good alternative to improved the life quality of the patient that uses this drug.  相似文献   

2.
The purpose of this work was to develop a modified release system for the herbicide ametryn by encapsulating the active substance in biodegradable polymer microparticles produced using the polymers poly(hydroxybutyrate) (PHB) or poly(hydroxybutyrate-valerate) (PHBV), in order to both improve the herbicidal action and reduce environmental toxicity. PHB or PHBV microparticles containing ametryn were prepared and the efficiencies of herbicide association and loading were evaluated, presenting similar values of approximately 40%. The microparticles were characterized by scanning electron microscopy (SEM), which showed that the average sizes of the PHB and PHBV microparticles were 5.92±0.74 μm and 5.63±0.68 μm, respectively. The ametryn release profile was modified when it was encapsulated in the microparticles, with slower and more sustained release compared to the release profile of pure ametryn. When ametryn was associated with the PHB and PHBV microparticles, the amount of herbicide released in the same period of time was significantly reduced, declining to 75% and 87%, respectively. For both types of microparticle (PHB and PHBV) the release of ametryn was by diffusion processes due to anomalous transport (governed by diffusion and relaxation of the polymer chains), which did not follow Fick's laws of diffusion. The results presented in this paper are promising, in view of the successful encapsulation of ametryn in PHB or PHBV polymer microparticles, and indications that this system may help reduce the impacts caused by the herbicide, making it an environmentally safer alternative.  相似文献   

3.
The aim of this study was to obtain microparticles containing acyclovir (ACV) and chitosan cross-linked with tripolyphosphate using the spray-drying technique. The resultant system was evaluated through loading efficiency, differential scanning calorimetry (DSC), thermogravimetric analysis (TG), X-ray powder diffraction (XRPD), scanning electron microscopy (SEM), in vitro release and stability studies. The results obtained indicated that the polymer/ACV ratio influenced the final properties of the microparticles, with higher ratios giving the best encapsulation efficiency, dissolution profiles and stability. The DSC and XRPD analyses indicated that the ACV was transformed into amorphous form during the spray-drying process.  相似文献   

4.
Morphine-loaded poly(l-lactide)-poly(ethylene glycol)-poly(l-lactide) (PLLA-PEG-PLLA) microparticles were prepared using solution enhanced dispersion by supercritical CO2 (SEDS). The effects of process variables on the morphology, particles size, drug loading (DL), encapsulation efficiency and release properties of the microparticles were investigated. All particles showed spherical or ellipsoidal shape with the mean diameter of 2.04–5.73 μm. The highest DL of 17.92 % was obtained when the dosage ratio of morphine to PLLA-PEG-PLLA reached 1:5, and the encapsulation efficiency can be as high as 87.31 % under appropriate conditions. Morphine-loaded PLLA-PEG-PLLA microparticles displayed short-term release with burst release followed by sustained release within days or long-term release lasted for weeks. The degradation test of the particles showed that the degradation rate of PLLA-PEG-PLLA microparticles was faster than that of PLLA microparticles. The results collectively suggest that PLLA-PEG-PLLA can be a promising candidate polymer for the controlled release system.  相似文献   

5.
The purpose of this study was the development and characterization of wheat gluten microspheres for use as controlled release devices, and the evaluation of the effect of the addition of poly (ethylene glycol) (PEG). Diltiazem hydrochloride was used as the model drug in the in vitro release essay. The physical–chemical and morphological properties of the microspheres were evaluated, as well as their encapsulation efficiency. Porosity varied with the presence or absence of PEG. The diltiazem encapsulation efficiency was 72.8% and 96.7% for wheat gluten and gluten/PEG 95/05 microspheres, respectively. The DSC and FTIR results indicated interactions between the microparticles and additives used. In the in vitro release tests it was observed that, for all the studied systems, the burst effect occurred in the first 2 h of release and the microspheres prepared with PEG had a faster release rate. In the attempt to elucidate the release mechanism, the systems were treated based on two well known mathematical models: the Higuchi and the power law. It was found that the microsphere release mechanism is not exclusively diffusion-controlled and, probably, the release occurs through a combination of partial diffusion through the swelling matrix and hydrophilic pores.  相似文献   

6.
Purpose: To develop and characterize microparticles containing fluoride sources (FS) from sodium fluoride, sodium monofluorophosphate (MFP) or aminofluoride and evaluate their characteristics as fluoride delivery systems.

Methods: Ethylcellulose microparticles containing fluoride (EM) were prepared by emulsification of ethyl acetate dispersion containing polymer and FS (ethylcellulose:FS ratio of 1:0.25 wt/wt) with aqueous external phase containing polysorbate 80 (0.8% vol/vol) using the volume ratio (organic:aqueous) of 1:5. The organic solvent was evaporated; microparticles were collected by centrifuging, washed with deionized water and freeze-dried. Gelatin microparticles containing FS (GM) was obtained by dispersion of the natural polymer in water, adding FS (6:1 wt/wt) and 20% (wt/wt) of mannitol. The final dispersions were spray-dried. Particle morphology and size were investigated using optical microscopy. The content of fluoride ions in the microparticles was quantified using a potentiometric method. The encapsulation efficiency and in vitro release profile of fluoride was also determined.

Results: Microparticles exhibited polydispersity and mean diameters <145.35 and <124.22 µm for EM and GM, respectively. Considering the entrapment efficiency, the spray-drying technique exhibited greater values than microencapsulation by emulsification and solvent evaporation. The release profile of fluoride ions from microparticles was shown to be modified, fitted first order and guided by Fickian diffusion.

Conclusions: Microparticles prepared with ethylcellulose or gelatin can be used as platform for oral delivery of fluoride, providing a means to increase the local supply of this ion in a controlled manner, providing an increased protection against caries. Moreover, further investigations are needed to demonstrate this property in vivo.  相似文献   

7.
In the present study, antileukemic enzyme L-asparaginase (ASNase) was encapsulated into poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) nanocapsules in order to decrease the immunogenicity and toxicity of the enzyme and to increase its in vivo half life in mice. Nanocapsules were prepared by water-in-oil-in-water approach and each phase was changed systematically. By changing the pH of the w2 phase to the isolelectric point of L-ASNase, the encapsulation efficiency was increased from 23.7% to 28.0%. Also, modification of ASNase with PEG2 increased the encapsulation efficiency from 23.7% to 27.9% and protected the enzyme against denaturation. Combination of the various optima enabled a substantial increase in the activity (0.074–0.429 U/mg nanocapsule). The enzyme activity in the blood due to unmodified PHBV nanocapsules dropped to 38% of its initial value 4 h after injection. When the same sample was tested for the enzyme content in the circulation by using the radio-labeled enzyme a much lower enzyme (30% of initial) could be detected after a shorter time (3 h). The PHBV nanocapsules with heparin conjugated on their surface had a longer presence in the circulation than unmodified PHBV nanocapsules. After 6 h, around 50% of the enzyme was still present in the blood. Radioactivity measurements using the same sample showed a sharp decrease in enzyme amount in the circulation in the early stages. However, radioactivity was still detectable at the eighth hour. No adverse effects and symptoms of anaphylaxis were observed upon injection of encapsulated ASNase-PHBV nanocapsules to mice i.v. through the tail vein.  相似文献   

8.
The aim of this study was to produce cinnarizine loaded Eudragit® L100-55 microparticles by coacervation technique in order to achieve pH responsive drug release using hydroxypropyl methycellulose (HPMC) as stabilizer. The effect of enteric polymer: HPMC ratio on properties of microparticles was investigated with regard to particle size distribution, morphology, yield, encapsulation efficiency, in vitro drug release profiles and interaction between cinnarizine and Eudragit® L100-55. High drug encapsulation efficiency was seen in all microparticles. Particle diameter increased when the enteric polymer content was higher relative to HPMC. In vitro dissolution studies demonstrated that the drug release from the microparticles was dependent upon enteric polymer: HPMC ratio and particle size distribution. At the ratio of at least 3.75:1 of enteric polymer: HPMC, drug release was suppressed most significantly in low pH (hydrochloric acid as medium) while rapid drug release was observed in pH 7.4.  相似文献   

9.
In the present study, biogenic silica nanoparticles (bSNPs) were synthesized from groundnut shells, and thoroughly characterized to understand its phase, and microstructure properties. The biopolymer was synthesized from yeast Wickerhamomyces anomalus and identified as Poly (3‐hydroxybutyrate‐co ‐3‐hydroxyvalerate) (PHBV) by GC‐MS and NMR analysis. The bSNPs were reinforced to fabricate PHBV/SiO2 nanocomposites via solution casting technique. The fabricated PHBV/SiO2 nanocomposites revealed intercalated hybrid interaction between the bSNPs and PHBV matrix through XRD analysis. PHBV/SiO2 nanocomposites showed significant improvement in physical, chemical, thermo‐mechanical and biodegradation properties as compared to the bare PHBV. The cell viability study revealed excellent biocompatibility against L929 mouse fibroblast cells. The antibacterial activity of PHBV/SiO2 nanocomposites was found to be progressively improved upon increasing bSNPs concentration against E. coli and S. aureus.Inspec keywords: X‐ray diffraction, microorganisms, antibacterial activity, nanoparticles, cellular biophysics, nanofabrication, silicon compounds, nanocomposites, filled polymers, nanomedicine, biomedical materials, casting, biodegradable materials, food packaging, food safety, biological NMROther keywords: antibacterial applications, poly(3‐hydroxybutyrate‐co‐3‐hydroxyvalerate), PHBV matrix, biodegradable PHBV‐SiO2 nanocomposite, thermomechanical biodegradation properties, biogenic silica nanoparticles, groundnut shells, microstructure properties, biopolymer, yeast Wickerhamomyces anomalus, GC‐MS, NMR analysis, food packaging, intercalated hybrid interaction, XRD analysis, cell viability study, solution casting, SiO2   相似文献   

10.
Objective: To mask the bitterness of Chlorpheniramine Maleate via encapsulating drug into Eudragit EPO microparticles, and then incorporate these microparticles into orally disintegrating films (ODF) and orally disintegrating tablets (ODT) for pediatric uses.

Methods: Spray drying of water-in-oil emulsion was utilized to encapsulate Chlorpheniramine Maleate into Eudragit EPO microparticles. Based on an orthogonal experimental design L9 (33), polynomial regression models were developed to evaluate correlation between microparticle properties (encapsulation efficiency and drug release) and variables (X1: weight ratio of polymer to drug, X2: volume ratio of oil to water and X3: Q-flow of spray dryer). ODF and ODT formulations were evaluated including weight variation, content uniformity, tensile strength, disintegration time, friability and dissolution profiles. The bitterness taste test was evaluated in 10 adult volunteers.

Results and discussion: From polynomial regression analysis, the best values of variables leading to the optimized microparticles were X1?=?10, X2?=?3 and X3?=?45. The optimized microparticles were incorporated into ODF and ODT with satisfactory weight and drug content uniformity, and acceptable physical strength. Both dosage forms disintegrated immediately (less than 40?s) in simulated saliva solutions. The outcome of taste-masking test indicated that microparticles alleviated drug bitterness significantly; bitterness was not discernible with microparticles incorporated in ODT, whereas only slight bitterness was detected from microparticles incorporated into ODF.

Conclusion: Both ODF and ODT are shown to be suitable vehicles for taste masked Chlorpheniramine Maleate microparticles with potential for pediatric uses.  相似文献   

11.
Biocomposites of a biopolymer and the coproduct of corn bioethanol industry, dried distillers’ grains with solubles (DDGS), were produced by reactive melt extrusion and injection molding. The biopolymer matrix was a blend of polyhydroxy(butyrate-co-valrerate), PHBV, and poly(butylene adipate-co-terphthalate), PBAT. The effect of compatibilizer, polymeric methylene diphenyl diisocyanate (PMDI), and corn oil lubricant was studied. The change in melt processing force suggested the occurrence of chemical reactions during the processing. This hypothesis was further investigated by infrared spectroscopy by which the formation of urethane and urea bonds between DDGS and polymeric matrix was approved. Dynamic mechanical analysis confirmed the occurrence of crosslinks at PBAT–PHBV interface showing that the tan δ curves for PBAT and PHBV of the matrix shifted slightly towards each other. Moreover, the calculated parameter of interaction, A, from tan δ curves admitted the stronger bond at the DDGS–matrix interface as a result of addition of PMDI compatibilizer. Also, scanning electron microscopy images revealed improved interfacial adhesion at the DDGS–matrix interface as well as PBAT–PHBV interface within the matrix itself. The obtained crosslinked interfaces resulted in improvement in the strength, modulus, and elongation-at-break of biocomposites. Moreover, a synergism of PMDI and corn oil effects led to a dramatic improvement in impact strength of this biocomposite system so that the respective value for the prepared DDGS biocomposite increased from 75 to 212 J/m with addition of 1 % of PMDI and 3 % of corn oil.  相似文献   

12.
Solid and microcellular components made of poly (3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV)/poly (butylene adipate-co-terephthalate) (PBAT) blend (weight ratio of PHBV:PBAT = 30:70), recycled wood fiber (RWF), and nanoclay (NC) were prepared via a conventional and microcellular-injection molding process, respectively. Morphology, thermal properties, and mechanical properties were investigated. The addition of 10% RWF (both untreated and silane-treated) reduced the cell size and increased the cell density of the microcellular components. Also, the addition of 10% RWF (both untreated and silane-treated) generally increased the specific Young’s modulus and tensile strength, but decreased the specific toughness and strain-at-break in both solid and microcellular components. Moreover, unlike the neat PHBV/PBAT blend, microcellular PHBV/PBAT/RWF (both untreated and silane-treated) composites showed higher specific toughness and strain-at-break compared to their solid counterparts. In addition, higher specific toughness and strain-at-break was observed in the PHBV/PBAT/untreated-RWF composite compared with the PHBV/PBAT/silane-treated RWF composite, particularly in the microcellular components. The degree of PHBV crystallinity increased significantly in both solid and microcellular PHBV/PBAT/RWF composites although the degree of PHBV crystallinity in the solid components was slightly higher than that of their microcellular counterparts. The effects of adding 2% nanoclay on the properties of the PHBV/PBAT/silane-treated-RWF composite were also investigated. The nanoclays exhibited an intercalated structure in the composites based on XRD analysis and did not induce significant changes in the cell morphology and mechanical properties of the PHBV/PBAT/silane-treated-RWF composite. However, it did improve its thermal stability.  相似文献   

13.
ABSTRACT

Beta-estradiol has been recommended for the long-term therapy of osteoporosis and its oral formulations are subjected to intensive first pass metabolism. The present investigation was aimed at preparing and characterizing biodegradable microparticles of beta-estradiol with polymers such as PLA, PLGA 85/15, PLGA 75/25, and their mixtures. The microparticles were prepared by solvent evaporation method using methylene chloride as a solvent and polyvinyl alcohol as a surfactant. The drug-polymer ratios were 1:3, 1:5, and 1:7. The prepared microparticles (twelve formulations) were tested for encapsulation efficiency and in vitro drug release in 50% methyl alcohol/phosphate buffer pH 7.4. The results showed that the encapsulation efficiency varied from 81 to 100% and the formulation fabricated from PLGA 85/15 (1:3) showed less burst and consistent long time release. This formulation when further characterized displayed irregular spherical shape with an average particle size of 72 µm. The crystallinity of the drug was reduced when investigated using X-ray diffractometry. No chemical interaction between the drug and the polymer was observed as evidenced by FT-IR analysis. The results indicated that beta-estradiol biodegradable microparticles with PLGA 85/15 (1:3) could be a suitable approach for long term therapy of osteoporosis.  相似文献   

14.
A matrix based on chitosan lactate and poloxamer 407 was evaluated as a delivery system for the vaginal administration of the antifungal drug econazole. The matrix was investigated both containing the pure drug and after introducing microparticles of Eudragit RS 100 containing econazole. Eudragit RS 100 microparticles were prepared using an emulsion-extraction method and dispersed in a solution containing chitosan lactate (2% w/w) and poloxamer 407 (1.7% w/w). The microparticles, obtained with a yield of 64% w/w and an encapsulation efficiency of 42% w/w, had a diameter of less than 2 μm and a drug loading of 13% w/w. The compressed matrices, characterized by DSC, swelling, erosion, release and mucoadhesion studies, had behaviours dependent on the relative amounts of the contained microparticles. The matrix without microparticles (MECN) showed zero-order release kinetics, with a maximum drug-release of 60% w/w, while those containing 50 or 75% w/w microparticles showed a diffusion controlled release up to 8 and 16 h, respectively, and a linear trend after those time intervals, caused by the erosion process, which allowed reaching a drug-release of approximately 100% w/w at 22 h. In in vitro experiments, the matrices were mucoadhesive and active in inhibiting the growth of Candida albicans 796.  相似文献   

15.
16.
In this work, chemically bonded poly(D, L-lactide)-polyethylene glycol-poly(D, L-lactide) (PLA-PEG-PLA) triblock copolymers with various PEG contents and PLA homopolymer were synthesized via melt polymerization, and were confirmed by FTIR and 1H-NMR results. The molecular weight and polydispersity of the synthesized PLA and PLA-PEG-PLA copolymers were investigated by gel permeation chromatography. Hydrophilicity of the copolymers was identified by contact angle measurement. PLA-PEG-PLA and PLA microparticles loaded with and without PTX were then produced via solution enhanced dispersion by supercritical CO2 (SEDS) process. The effect of the PEG content on the particle size distribution, morphology, drug load, and encapsulation efficiency of the fabricated microparticles was also studied. Results indicate that PLA and PLA-PEG-PLA microparticles all exhibit sphere-like shape with smooth surface, when PEG content is relatively low. The produced microparticles have narrow particle size distributions and small particle sizes. The drug load and encapsulation efficiency of the produced microparticles decreases with higher PEG content in the copolymer matrix. Moreover, high hydrophilicity is found when PEG is chemically attached to originally hydrophobic PLA, providing the produced drug-loaded microparticles with high hydrophilicity, biocompatibility, and prolonged circulation time, which are considered of vital importance for vessel-circulating drug delivery system.  相似文献   

17.
Encapsulation of albendazole, a class II compound, into polymeric microparticles based on chitosan-sodium lauryl sulfate was investigated as a strategy to improve drug dissolution and oral bioavailability. The microparticles were prepared by spray drying technique and further characterized by means of X-ray powder diffractometry, infrared spectroscopy and scanning electron microscopy. The formation of a novel polymeric structure between chitosan and sodium lauryl sulfate, after the internal or external gelation process, was observed by infrared spectroscopy. The efficiency of encapsulation was found to be between 60 and 85% depending on the internal or external gelation process. Almost spherically spray dried microparticles were observed using scanning electron microscopy. In vitro dissolution results indicated that the microparticles prepared by internal gelation released 8% of the drug within 30?min, while the microparticles prepared by external gelation released 67% within 30?min. It was observed that the AUC and Cmax values of ABZ from microparticles were greatly improved, in comparison with the non-encapsulated drug. In conclusion, the release properties and oral bioavailability of albendazole were greatly improved by using spraydried chitosan-sodium lauryl sulphate microparticles.  相似文献   

18.
Despite the unique properties, application of garlic essential oil (GEO) is too limited in food and drugs, due to its low water solubility, very high volatility and unpleasant odour. In this work, a nanoemulsion containing GEO was formulated to cover and protect the volatile compounds of GEO. The encapsulation efficiency of formulated nanoemulsions was measured by gas chromatography and obtained encapsulation efficiency ranged from 91 to 77% for nanoemulsions containing 5–25% GEO, respectively. The 2,2‐diphenyl‐1‐picrylhydrazyl method for antioxidant activity measurement showed that free radical scavenging capacity of nanoemulsions intensified during storage time. The electrical conductivity of the samples was constant over storage time while linearly increased by raising the temperature. Thermogravimetric analysis was used to determine the thermal resistance of nanoemulsions and their ingredients. Interestingly, microbial tests cleared that the control nanoemulsion with a particle size below 100 nm (nanoemulsion without GEO) also showed antimicrobial activity. Disk diffusion method showed that pure GEO and also formulated nanoemulsions had a stronger effect against Gram‐positive bacterium (Staphylococcus aureus) than Gram‐negative bacterium (Escherichia coli).Inspec keywords: emulsions, nanostructured materials, antibacterial activity, microorganisms, electrical conductivity, thermal analysis, thermal resistance, oils, nanobiotechnology, food safety, cellular biophysicsOther keywords: garlic oil‐in‐water nanoemulsion, antimicrobial aspects, physicochemical aspects, garlic essential oil, GEO, volatile compounds, encapsulation efficiency, gas chromatography, 2,2‐diphenyl‐1‐picrylhydrazyl method, antioxidant activity measurement, free radical scavenging capacity, storage time, electrical conductivity, thermogravimetric analysis, thermal resistance, antimicrobial activity, disk diffusion method, Gram‐positive bacterium, Staphylococcus aureus, Gram‐negative bacterium, Escherichia coli  相似文献   

19.
The aim was to design sterile biodegradable microparticulate drug delivery systems based on poly(dl-lactide) (PLA) and poly(?-caprolactone) (PCL) and containing ivermectin (IVM), an antiparasitic drug, for subcutaneous administration in dogs. The drug delivery system should: (i) ensure a full 12-month protection upon single dose administration; (ii) be safe with particular attention regarding IVM dosage and its release, in order to prevent over dosage side effects. This preliminary work involves: polymer selection, evaluation of the effects of γ-irradiation on the polymers and IVM, investigation and set up of suitable microparticle preparation process and parameters, IVM-loaded microparticles in vitro release evaluation.

Results of gel permeation chromatography analysis on the irradiated polymers and IVM mixtures showed that combination of IVM with the antioxidant α-tocopherol (TCP) reduces the damage extent induced by irradiation treatment, independently on the polymer type.

Solvent evaporation process was successfully used for the preparation of PLA microparticles and appropriately modified; it was recognized as suitable for the preparation of PCL microparticles. Good process yields were achieved ranging from 76.08% to 94.72%; encapsulation efficiency was between 85.76% and 91.25%, independently from the polymer used. The type of polymer and the consequent preparation process parameters affected microparticle size that was bigger for PCL microparticles (480–800?µm) and solvent residual that was >500?ppm for PLA microparticles. In vitro release test showed significantly faster IVM release rates from PCL microparticles, with respect to PLA microparticles, suggesting that a combination of the polymers could be used to obtain the suitable drug release rate.  相似文献   

20.
Biodegradable, biocompatible, renewable and non-toxic polyhydroxyalkanoates (PHAs) based nanoparticles are the novel nanotherapeutic tool which are used for the encapsulation of antineoplastic drugs for cancer therapy. In this study, poly-3-hydroxybutyrate-co-5 mol% 3-hydroxyvalerate (PHBV-S), poly-3-hydroxybutyrate-co-11 mol% 3-hydroxyvalerate (PHBV-11) and poly-3-hydroxybutyrate-co-15 mol% 3-hydroxyvalerate (PHBV-15) were used as a nanocarrier for encapsulation of Ellipticine (EPT). EPT is a model anticancer drug. Physicochemical characteristics such as particle size, its morphology and zeta potential of blank and EPT loaded PHBV-S, PHBV-11 and PHBV-15 nanoparticles were studied. In vitro cytotoxicity tests confirmed that the blank PHBV-S, PHBV-11 and PHBV-15 nanoparticles were demonstrating significant biocompatibility without affecting the survival of cancer cell line A549. The loading efficiency of EPT in PHBV nanoparticles was observed in the range of 39.32 to 45.65%. The % inhibition of cancer cell line A549 ranged from 64.28 to 67.77% in comparison to EPT alone in which % inhibition found to be ≤ 45.11%. The IC50 value for each of three different formulations of EPT loaded PHBV nanoparticles ranged from 1.00 to 1.31 μg/mL. The order of % inhibition of cancer cell line A549 for drug loaded nanoparticles was EPT-PHBV-15 > EPT-PHBV-S > EPT-PHBV-11. This system had demonstrated a great potential to increase the cytotoxic effect of EPT by increasing its bioavailability.  相似文献   

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