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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.


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.


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.


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.


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.

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