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The aim of this study was to investigate the combined influence of 3 independent variables in the preparation of sustained release Nateglinide (NTG) microspheres by O/W solvent emulsification method. A 3-factor, 3-level Box–Behnken design was used to derive second order polynomial equation and construct contour plots to predict responses. The independent variables selected were polymer concentration (A), surfactant concentration (B) and speed of the stirrer (C). Percentage drugloading (Y1) and Percentage drug release (Y2) were considered dependent variables. The prepared microspheres were evaluated for percentage of yield, drug loading, drug release study in 6.8 phosphate buffer, Fourier transform infrared (FT-IR), X-ray diffraction (XRD), scanning electron microscopy analysis. Contour plots were constructed to show the effects of of A, B, C on Y1 and Y2. The yield of microspheres was found to be in the range of 42.29–97.22 %. The drug loading was found to be in the range of 12.18 % (F9) to 24.55 % (F14). FT-IR analysis revealed no drug excipient interference. The morphology of evaluated microspheres were found to be spherical and smooth in nature. In XRD analysis crystalline pattern of pure NTG was changed to amorphous pattern when converted to microspheres. Out of 17 batches, formulation batches F1, F4, F12, F14, F17 had percentage drug loading 52.75, 50.78, 43.88, 47.45, 44.78 % at 10 h respectively which indicated excellent sustained drug release pattern. From this study it was concluded that NTG loaded ethyl cellulose sustained release microspheres were developed using 3-factor, 3-level Box–Behnken design.

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기사명 저자명 페이지 원문 목차
Preparation and characterization of alginate gel core-lipid nanocapsules for co-delivery of hydrophilic and hydrophobic anti-cancer drugs Bijay Kumar Poudel, Roshan Pradhan, Biki Gupta, Ju Yeon Choi, Chul Soon Yong, Jong Oh Kim pp.485-491
A microemulsion-based hydrogel formulation containing voriconazole for topical skin delivery Yo-Han Kim, Chung Kil Song, Eunjae Jung, Dong-Hwan Kim, Dae-Duk Kim pp.517-524
Sustained delivery of cefdinir to upper gastrointestinal tract using calcium alginate beads : a formulation by design Radhakrishnan Praveen, Sandeep Kumar Singh, Priya Ranjan Prasad Verma, Jerome Karippamattom George pp.455-463
Advances in investigations on the mechanism of cancer multidrug resistance and the liposomes-based treatment strategy Fan Zeng, Rui-Jun Ju, Xue-Tao Li, Wan-Liang Lu pp.493-504
In vitro characterization and pharmacodynamic evaluation of furosemide loaded self nano emulsifying drug delivery systems(SNEDDS) Pankajkumar Yadav, Ekta Yadav, Amita Verma, Saima Amin pp.443-453
Evaluation of drug–drug interaction potential between DA-9801 and metformin Hyun-Uk Jeong, Hee Eun Kang, Sang-Zin Choi, Miwon Son, Im-Sook Song, Hye Suk Lee pp.401-409
Formulation and evaluation of taste-masked paracetamol-lipid sachets and chewable tablets Wessam M. El-Refaie, Magda A. El-Massik, Ossama Y. Abdallah, Nawal M. Khalafallah pp.431-442
A rapid and selective LC–MS/MS method for the quantification of aripiprazole in beagle dog plasma and its application to a pharmacokinetic study Sook-Jin Kim, Sang-Hyuk Lee, Yong-Soo Kim, Hyo-Rin Jung, Hea-Young Cho pp.465-472
Angiopep-2-conjugated liposomes encapsulating γ-secretase inhibitor for targeting glioblastoma stem cells Shuhua Xuan, Dae Hwan Shin, Jin-Seok Kim pp.473-483
Targeted siRNA therapy using cytoplasm-responsive nanocarriers and cell-penetrating peptides Hiroaki Okada pp.505-516
Formulation and development of nateglinide loaded sustained release ethyl cellulose microspheres by O/W solvent emulsification technique Gokul Khairnar, Vinod Mokale, Jitendra Naik pp.411-422
Evaluation of chaperone ability of S. rosmarinus against protein aggregation Abbas Heidari, Arezou Ghahghaei, Jafar Valizadeh pp.423-430

참고문헌 (17건) : 자료제공( 네이버학술정보 )

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번호 참고문헌 국회도서관 소장유무
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8 Keilson L, Mather S, Walter YH, Subramanian S, Mcleod JF (2000) Determination of nateglinide in human plasma by highperformance liquid chromatography with pre-column derivatization using a coumarin-type fluorescent reagent. J Clin Endocrinol Metab 85:1081 미소장
9 Li S, Lin S, Chien YW, Daggy BP, Mirchandani HL (2001) Statistical optimization of gastric floating system for oral controlled delivery of calcium. AAPS Pharm Sci Tech 2: article 1 미소장
10 Naik JB, Deshmukh RK, Kamle VV (2013) Development of sustained released microparticles of Diclofenac sodium using polymer complex by spray drier. AJPTR 3:892–904 미소장
11 Nateglinide tablets. US FDA label. http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/021204s014lbl.pdf 미소장
12 Nazzal S, Khan MA (2002) Response surface methodology for the optimization of ubiquinone self-nanoemulsified drug delivery system. AAPS Pharm Sci Tech 3: article 3 미소장
13 Shinkai H, Toi H, Kumashiro I, Seto Y, Fukuma M, Dan K, Toyoshima SN (1988) Acylphenylalanines and related compounds. A new class of oral hypoglycemic agents. J Med Chem 31:2092–2097 미소장
14 Subhedar P, Naik JB, Muley DN (2010) Effect of polymer concentration on sustained release microparticles of metformin hydrochloride prepared by using spray dryer. Polym Plast Eng Technol 49:267–271 미소장
15 Takesada H, Matsuda K, Ohtake R (1996) Structure determination of metabolites isolated from urine and bile after administration of AY4166, a novel D-phenylalanine derivative hypoglycemic agent. Bioorg Med Chem 4:1771–1781 미소장
16 Weaver ML, Orwig BA, Rodriguez LC (2001) Pharmacokinetics and metabolism of nateglinide in humans. Drug Metab Dispos 29:415–421 미소장
17 AAPS PharmSciTech volume 7, issue 4—Editorial 네이버 미소장

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