ABSTRACT
In this paper, nano-sponges of flavonoids from Glycyrrhizae Radix et Rhizoma (LF-NSP) were prepared by agitation-freeze drying method. Box-benhnken design and response surface method based on the single factor experiment was used to optimize the preparation process, with the stirring temperature as well as stirring time and speed as the independent variables, while with drug loading, particle size and the generalized "normalized value" as the response values. In addition, the nano-sponges were characterized by scanning electron microscope (SEM), infraredspectroscopy (FT-IR) and differential scanning calorimetry (DSC), and its release in vitro was also investigated. The results showed that the optimum preparation conditions for glycyrrhizin nano-sponges were as follows：The proportion of main drug and auxiliary drug was 1:2; the proportion of crosslinking agent DPC and β-CD was 4:1; stirring temperature 45 °C for 4.8 h at 245 r·min⁻¹. The comprehensive score of LF-NSP prepared under these conditions was 94.78. FT-IR and DSC results indicated the formation of Glycyrrhiza flavonoids nano-sponges, and SEM showed that they were spherical particles in shape. In release experiment in vitro, the cumulative release of glycyrrhizin flavonoids nano-sponges for 240 min was 81.8%, while that of crude drug was only 31.5%. Nano-sponges can significantly improve the dissolution of flavonoids from Glycyrrhizae Radix et Rhizoma.
Subject(s)
Animals , Drugs, Chinese Herbal , Flavonoids , Glycyrrhiza , Rhizome , Spectroscopy, Fourier Transform InfraredABSTRACT
Objective: To prepare GEN-VES-TPGS nano-micelles and improve the oral bioavailability of genistein (GEN). Methods: GEN-VES-TPGS nano-micelles, made by film hydration, were evaluated with particle size, entrapment efficiency, and drug-loading as indexes. Single factor experiment was used to optimize the formulation and productive technology, including dosages of TPGS, VES, GEN, hydration volume, temperature, and time. Morphology of nano-micelles, release rate in vitro, and pharmacokinetics in rat were investigated. Results: The results showed GEN-VES-TPGS nano-micelles presented with good clarity, appropriate particle diameter (43.50 ± 1.65) nm, negative charge, when the dosages of TPGS, VES, GEN were 200, 30, and 6 mg, respectively. Meanwhile, a condition of 15 mL, 50 ℃ at 3 h to hydrate was necessary to prepare. In this setting, the encapsulation efficiency of the nano-micelles was (98.99 ± 0.69)% and drug-loading rate was (2.57 ± 0.04)%. The pharmacokinetic results in rats showed the oral bioavailability of GEN-VES-TPGS nano-micelles was 162.96% of the GEN APIs. Conclusion: The prepared GEN-VES-TPGS nano-micelles have small particle size and good stability, and increase the oral bioavailability of GEN evidently.
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Objective To optimize the recipe of rhynchophylline sustained release tablet in order to provide a reference for industrial production of the formulation. Method With the release degree as index, the influences of single factors on the release, such as hydroxypropyl methyl cellulose(HPMC)used as an skeleton materials, ethyl cellulose(EC)as blockers and the mass fraction of polyvinylpyrrolidone (PVP)as adhesive, were evaluated to screen the optimal preparation by central composite design and response surface methodology based on the single factor investigation. Result The optimal preparation was as follows: rhynchophylline 9.5%, HPMC: 19%, EC: 7%, PVPP:2.2%, starch:61.5% and talcum powder: 0.8%. The sustained release tablet prepared by the optimized recipe of rhynchophylline had no sudden release effect and the release degree in 12 h was more than 84%. Conclusion The optimized recipe is reasonable and meets the requirements of sustained release formulation, which means it can provide a reference for industrial production of the formulation.
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Objective: To optimiaze the preparation technology of compound Aloe vera L. polysaccharide gel (CAVPG), and evaluate the in vitro release characteristics. Methods: with the appearance of the blank gels, spreadability, viscosity, high temperature stability (place 55℃ water bath for 5 h), low temperature stability (place −20℃ water bath for 24 h) as examining index, screening gel matrix preliminary; With the release degree of aloe polysaccharide, nano-silver, nano-zinc as examining index, investigating the release degree of aloe polysaccharide, nano-silver, nano-zinc in different substrates, determining the gel matrix; the orthogonal test was used to optimize the prescription craft, with the substrate consumption, glycerin dosage, mixing temperature for investigation factors. With the cumulative release degree of AVP, nano-silver and nano-zinc as index, stirring basket method was adopted to determine the cumulative release degree of AVP, nano-silver and nano-zinc. The curve of drug release in vitro was fitted with different release model to estimate the in vitro release characteristics of CAVPG. Results: The optimum prescription process was Aloe vera L. Polysaccharide 2%, nano-silver 1%, nano-zinc 1%, carbomer-980 0.5%, glycerol 5%, a moderate amount of triethanolamine, with PBS buffer up to 100 g, mixing temperature 25℃; Compared with other in vitro release models, zero order equation was the fittest model to nano-silver and nano-zinc, the primary equation was the fittest model to AVP. Conclusion: The gels of CAVPG prescription is reasonable, the prescription craft is simple, the quality is controllable. It has a development prospect.
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Objective To optimize the recipe of rhynchophylline sustained release tablet in order to provide a reference for in?dustrial production of the formulation. Method With the release degree as index,the influences of single factors on the release,such as hydroxypropyl methyl cellulose(HPMC)used as an skeleton materials,ethyl cellulose(EC)as blockers and the mass fraction of polyvinylpyrrolidone(PVP)as adhesive,were evaluated to screen the optimal preparation by central composite design and response surface methodology based on the single factor investigation. Result The optimal preparation was as follows:rhynchophylline 9.5%, HPMC:19%,EC:7%,PVPP:2.2%,starch:61.5%and talcum powder:0.8%. The sustained release tablet prepared by the optimized recipe of rhynchophylline had no sudden release effect and the release degree in 12 h was more than 84%. Conclusion The opti?mized recipe is reasonable and meets the requirements of sustained release formulation,which means it can provide a reference for in?dustrial production of the formulation.
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OBJECTIVE: To prepare indapamide sustained release capsules and investigate its release in vitro. METHODS: Blank pellets, hydrated magnesium silicate, hypromellose cellulose, triethyl citrate, Eudragit RL 100, Eudragit RS 100, Eudragit LS 55, etc, were used as materials to prepare indapamide sustained release capsules The content was determined by HPLC, and the effects of different solid weight gains of sustained release material on release of indapamide from capsules were evaluated by in vitro release test. RESULTS: The release in vitro of the sustained release pills met the requirements when the solid weight gain of the materials was 5.0% to 5.3%. CONCLUSION: The optimum preparation technique of indapamide sustained release capsules is established, which has guiding significance for the practical manufacture.
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Objective: To prepare curcumim thermoresponsive nanogels and study its release characteristics in vitro. Methods: Poly (N-isopropyl acrylamide) (PNIPAm) thermoresponsive nanogels were synthesized by emulsion polymerization method, and then curcumin loaded-PNIPAm nanogels were prepared. The characteristics of PNIPAm nanogels, the drug loading, and the drug release in vitro were investigated. Results: Atomic force micriscopy (AFM) observation showed that PNIPAm nanogels were spherical in shape with homogenous size. Moreover, PNIPAm No. 5 showed a high drug loading (27%). In vitro release study revealed that the 24 h accumulative in vitro release reached 75.2%. Conclusion: The method used to prepare curcumin thermoresponsive nanogels is simple. It is expected to become a novel vehicle potentially nanoparticle drug delivery system of curcumin.