National Engineering Research Center for Traditional Chinese Medicine

Nanchang, China

National Engineering Research Center for Traditional Chinese Medicine

Nanchang, China
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Hao H.,Shanghai Institute of Pharmaceutical Industry | Hao H.,Fudan University | Jia Y.,Shanghai Institute of Pharmaceutical Industry | Zhang H.,National Engineering Research Center for Traditional Chinese Medicine | And 4 more authors.
Journal of Chinese Pharmaceutical Sciences | Year: 2015

The objective of this study was to prepare monolithic osmotic tablet of quercetin for controlled drug release. Quercetin-PVP solid dispersion was prepared to enhance its solubility and dissolution rate. Solid dispersion, suspending agents, osmotic agents and other conventional excipients were used as tablet core composition and cellulose acetate (CA) with plasticizer as release controlling membrane. Different formulation variables, the amounts of PEO (polyethylene oxide), NaCl, plasticizer, and coating weight gain were optimized to gain the optimum formulation. The mechanism of drug release from monolithic osmotic tablet was also discussed. The optimal monolithic osmotic pump tablet could deliver quercetin at the rate of approximate zero-order up to 12 h, and the cumulative release was 90.74%. The developed monolithic osmotic system for quercetin loaded by solid dispersion was found to be a promising approach for controlled release of poorly-water soluble drug candidates. © 2015 Journal of Chinese Pharmaceutical Sciences, School of Pharmaceutical Sciences, Peking University.


Liu R.,East China University of Science and Technology | Liu R.,National Engineering Research Center for Traditional Chinese Medicine | Wang C.-X.,East China University of Science and Technology | Wang C.-X.,National Engineering Research Center for Traditional Chinese Medicine | And 4 more authors.
Chinese Pharmaceutical Journal | Year: 2012

OBJECTIVE: To study the physical and chemical properties and transdermal delivery characteristics oi capsaicin. METHODS: Equilibrium solubility method, ultraviolet spectrophotometry, bottle-shaking method, differential scanning ealorimetry (DSC) and in vitro diffusion cell method were used to determine the apparent solubility, dissociation constant, apparent oil/water partition coefficient, melting point and percutaneous penetration of capsaicin, respectively. And the permeation characteristics were evaluated by lag time method. RESULTS: Capsaicin was slightly dissolved in water, and the apparent solubility was (22.85 ± 0.06) mg · L-1. It was a weak base with a dissociation constant of (10.25 ± 0.11). The apparent oil/water partition coefficient of capsaicin changed with the pH value, and increased when pH was greater than 8. Its melting point was 60.20°C. The residence time(ttag) was (2.437 ± 0.273) h, the permeability coefficient (P) (7.012 ± 0.341) × 10-2cm · h-1, and the percutaneous penetration rate (Js) (4.647 ± 0.226) μg · cm-2 · h-1. CONCLUSION: Capsaicin possesses appropriate physical and chemical properties for percutaneous penetration and exhibits excellent percutaneous penetration.


Wang C.,East China University of Science and Technology | Wang C.,National Engineering Research Center for Traditional Chinese Medicine | Liu R.,East China University of Science and Technology | Liu R.,National Engineering Research Center for Traditional Chinese Medicine | And 2 more authors.
AAPS PharmSciTech | Year: 2012

A novel drug-in-adhesive matrix was designed and prepared. A thermoplastic elastomer, styrene-isoprene-styrene (SIS) block copolymer, in combination with tackifying resin and plasticizer, was employed to compose the matrix. Capsaicin was selected as the model drug. The drug percutaneous absorption, adhesion properties, and skin irritation were investigated. The results suggested that the diffusion through SIS matrix was the rate-limiting step of capsaicin percutaneous absorption. [SI] content in SIS and SIS proportions put important effects on drug penetration and adhesion properties. The chemical enhancers had strong interactions with the matrix and gave small effect on enhancement of drug skin permeation. The in vivo absorption of samples showed low drug plasma peaks and a steady and constant plasma level for a long period. These results suggested that the possible side effects of drug were attenuated, and the pharmacological effects were enhanced with an extended therapeutic period after application of SIS matrix. The significant differences in pharmacokinetic parameters produced by different formulations demonstrated the influences of SIS copolymer on drug penetrability. Furthermore, the result of skin toxicity test showed that no skin irritation occurred in guinea pig skin after transdermal administration of formulations. © 2012 American Association of Pharmaceutical Scientists.


Wang C.,East China University of Science and Technology | Wang C.,National Engineering Research Center for Traditional Chinese Medicine | Han W.,East China University of Science and Technology | Tang X.,National Engineering Research Center for Traditional Chinese Medicine | And 2 more authors.
AAPS PharmSciTech | Year: 2012

We prepared pressure-sensitive adhesive (PSA) patches based on styrene-isoprene-styrene (SIS) thermoplastic elastomer using hot-melt coating method. The liquid paraffine is added in the PSA matrices as a plasticizer to moderate the PSA properties. Three drugs, methyl salicylate, capsaicin, and diphenhydramine hydrochloride are selected as model drugs. The Fourier transform infrared spectroscopy, differential scanning calorimetry test, and wide-angle X-ray diffraction test indicate a good compatibility between drugs and matrices. Peppas equation is used to describe drug release profile. Different drug-matrix absorption, as indicative of drug-matrix interaction, accounts for the variation in release profiles of different drugs. Furthermore, atomic force microscopy and rheological studies of the PSA samples are performed to investigate the effect of SIS structure and plasticizer of PSA on drug release behaviors. For methyl salicylate and capsaicin, drug diffusion in the PSA matrices is the main factor controlled by the release kinetic constant k. The high [SI] diblock content and high plasticizer amount in matrix provide the PSA with a homogeneous and soften microstructure, resulting in a high diffusion rate. But for water-soluble drugs such as diphenhydramine hydrochloride, the release rate is governed by water penetration with the competition from diffusion mechanisms. © 2012 American Association of Pharmaceutical Scientists.


Wang C.-X.,Kunming University of Science and Technology | Wang C.-X.,East China University of Science and Technology | Han W.,East China University of Science and Technology | Liu R.,East China University of Science and Technology | Tang X.-Z.,National Engineering Research Center for Traditional Chinese Medicine
Gao Xiao Hua Xue Gong Cheng Xue Bao/Journal of Chemical Engineering of Chinese Universities | Year: 2014

In order to investigate the effect of matrix structure on drug release profiles, hot-melt pressure sensitive adhesives were made with different styrene-isoprene-styrene block copolymers. Methyl salicylate, capsaicin, and diphenhydramine hydrochloride were selected as model drugs to perform the release experiment. The result shows that the drugs exist in a dispersed or dissolved state in the matrix and no crystallization occurs with the drug concentration up to 2%. The drug release profile is controlled by the diffusion mechanism in the matrix. The drug with high solubility in the matrix gives a high diffusion coefficient, and leads to have a fast release behaviors. On the other hand, the block copolymer with homogeneous and mesh-like microstructures possesses more free volume of intermolecular, which causes the reduction of the energy storage modulus and viscosity of the matrix and results in a higher diffusion rate of the drugs.


Wang C.,East China University of Science and Technology | Wang C.,National Engineering Research Center for Traditional Chinese Medicine | Ma J.,National Pharmaceutical Engineering and Research Center | Liu R.,East China University of Science and Technology | And 3 more authors.
Drug Development and Industrial Pharmacy | Year: 2014

Objective: To design and evaluate a novel pressure sensitive adhesive (PSA) patch containing traditional Chinese medicine (TCM) using styrene-isoprene- styrene (SIS) copolymer. Method: A mixture D-optimal design with ternary response surface diagram was employed in the optimization process. The proportions of SIS copolymer, tackifying resin and plasticizer were selected as the independent variables while tack force, peel strength of the patch and skin penetrability of methyl salicylate were selected as the dependent variables. The optimized patch was then evaluated including in vivo absorption, pharmacological activities and skin irritation, by comparing with a commercial patch based on natural rubber. Results: The optimized patch, which comprised 30.0% SIS copolymer, 26.6% tackifying resin and 43.4% plasticizer, was superior to commercial patch in skin permeation, pharmacological activities and skin biocompatibility. Conclusion: SIS copolymer was a suitable substitute to natural rubber in producing patches containing TCM formula. © 2014 Informa Healthcare USA, Inc. All rights reserved.


Cheng L.,Jiangxi University of Traditional Chinese Medicine | Luo X.-J.,Jiangxi University of Traditional Chinese Medicine | Luo X.-J.,National Engineering Research Center for Traditional Chinese Medicine | Han X.-L.,Jiangxi University of Traditional Chinese Medicine | And 4 more authors.
Zhongguo Zhongyao Zazhi | Year: 2016

Based on the basic theory of thermodynamics, the thermodynamic parameters and related equations in the process of water adsorption and desorption of Chinese herbal decoction pieces were established, and their water absorption and desorption characteristics were analyzed. The physical significance of the thermodynamic parameters, such as differential adsorption enthalpy, differential adsorption entropy, integral adsorption enthalpy, integral adsorption entropy and the free energy of adsorption, were discussed in this paper to provide theoretical basis for the research on the water adsorption and desorption mechanism, optimum drying process parameters, storage conditions and packaging methods of Chinese herbal decoction pieces.


Zhu D.,China Pharmaceutical University | Lin Z.,China Pharmaceutical University | Yan Y.,China Pharmaceutical University | Yu B.,China Pharmaceutical University | And 3 more authors.
Evidence-based Complementary and Alternative Medicine | Year: 2011

Oxidative stress is involved in the pathogenesis of ischemic neuronal injury. A Chinese herbal formula composed of Poria cocos (Chinese name: Fu Ling), Atractylodes macrocephala (Chinese name: Bai Zhu) and Angelica sinensis (Chinese names: Danggui, Dong quai, Donggui; Korean name: Danggwi) (FBD), has been proved to be beneficial in the treatment of cerebral ischemia/reperfusion (I/R).This study was carried out to evaluate the protective effect of FBD against neuronal oxidative stress in vivo and in vitro. Rat I/R were established by middle cerebral artery occlusion (MCAO) for 1h, followed by 24h reperfusion. MCAO led to significant depletion in superoxide dismutase and glutathione and rise in lipid peroxidation (LPO) and nitric oxide in brain. The neurological deficit and brain infarction were also significantly elevated by MCAO as compared with sham-operated group. All the brain oxidative stress and damage were significantly attenuated by 7 days pretreatment with the aqueous extract of FBD (250mgkg-1, p.o.). Moreover, cerebrospinal fluid sampled from FBD-pretreated rats protected PC12 cells against oxidative insult induced by 0.2mM hydrogen peroxide, in a concentration and time-dependent manner (IC 50 10.6, ET50 1.2h). However, aqueous extract of FBD just slightly scavenged superoxide anion radical generated in xanthinexanthine oxidase system (IC50 2.4mgml-1) and hydroxyl radical generated in Fenton reaction system (IC50 3.6mgml-1). In conclusion, FBD was a distinct antioxidant phytotherapy to rescue neuronal oxidative stress, through blocking LPO, restoring endogenous antioxidant system, but not scavenging free radicals. Copyright © 2011 Zhihong Lin et al.


Liu Y.-X.,Henan University | Wu X.-C.,Henan University | Hao H.-J.,Shanghai Institute of Pharmaceutical Industry | Song X.-Y.,Henan University | And 3 more authors.
Academic Journal of Second Military Medical University | Year: 2016

Objective To prepare lappaconitine hydrobromide push-pull osmotic pump controlled release tablets and screen for the optimal formulation. Methods The percent of cumulative release was used as the evaluation index for the drug release profile in vitro. The effects of PEO N750, PEO WSR303, and plasticizer amounts and coating weight gain on the releasing behavior were investigated through single-factor method. Based on single-factor study on the compositions, the optimal formulation for lappaconitine hydrobromide push-pull osmotic pump controlled release tablet was selected via orthogonal design. The in vitro release of the optimized formulation was also fitted to different models. Results The results of orthogonal design indicated that coating weight gain had a significant effect on the drug release in vitro —<0. 05). The optimal formula was as follows; lappaconitine hydrobromide 20 mg, PEO N750 160 mg, NaCl 30 mg in drug layer; PEO WSR303 75 mg, NaCl 20 mg in the push layer; and plasticizer PEG 4000 was 10% and weight gain was 5% in the coating composition The release rate of the tablets with optimized formulation was constant within 12 h, and the cumulative release could reach 95. 02 %. Conclusion The current method to prepare lappaconitine hydrobromide push-pull osmotic pump controlled release tablets is stable, and the in vitro drug release has an excellent zero-release profile within 12 h (r=0. 992 1), which meets the standard for controlled release. © 2016, Academic Journal of Second Military Medical University. All Rights Reserved.


Hao H.-J.,Shanghai Institute of Pharmaceutical Industry | Jia Y.-Z.,Shanghai Institute of Pharmaceutical Industry | Han R.,Shanghai Institute of Pharmaceutical Industry | Zhang H.-Q.,National Engineering Research Center for Traditional Chinese Medicine | And 2 more authors.
Chinese Journal of New Drugs | Year: 2015

Objective: To prepare candesartan cilexetil, an indissolvable drug, into monolithic osmotic pump tablets. Methods: Solid dispersion technology was adopted to enhance its solubility, and the optimal formulation of candesartan cilexetil solid dispersion osmotic pump tablets was selected via the single-factor method and orthogonal design. The release in vitro of the optimized formulation was also fitted to different models. Results: The tablets with optimized formulation achieved the desired zero-order release profile in 14 hours (r=0.993 3), and the cumulative release was 88.36%. Conclusion: Candesartan cilexetil can be prepared into monolithic osmotic pump tablets based on the intermediate of solid dispersion technology, which has an obvious characteristic of zero release. ©, 2015, Chinese Journal of New Drugs Co. Ltd. All right reserved.

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