, (551) K562/ADR. 2 (Abcc2/Mrp2) ( ) Aeroto-Niu-O16. CCl 4 ,,,, (685) (663)

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2 , (551),, (558),, (565) RNA,, (573),, (580),,, (588) K562/ADR,,,,,,, (594) A PC12,,,,,, (600),,,,, (604) UVB HaCaT DNA,,,, (609) ,,,,, (614) C27,,,, (619) 2 (Abcc2/Mrp2) ( ),,,,,,, (624),,,, (630),,,,, (634) LubriTose AN,,,, (640) RGD,,,, (646),,, (652),,,,,, (657) Aeroto-Niu-O16,,,, (664),,,,,, (670) ph,, (677) CCl 4,,,,,,, (680) β-,,,, (685) (599) 2012 (623) (639) 2012 (645) 2012 (663)

3 640 Acta Pharmaceutica Sinica 2012, 47 (5): LubriTose AN 1, 1, 1, 1*, 2 ( 1., 2., ) : LubriTose AN,, LubriTose AN, LubriTose AN, LubriTose AN LubriTose AN, LubriTose AN LubriTose AN LubriTose AN, LubriTose AN, : LubriTose AN; ; ; ; : R943 :A : (2012) Micromeritic evaluation of the direct compression excipient LubriTose AN ZHANG Yi-lan 1,TIANChao 1, HU Dan-rong 1,KEXue 1*, TIAN Ji-lai 2 (1. Department of Pharmaceutics, 2. Pharmacy Experimental Center, China Pharmaceutical University, Nanjing , China) Abstract: This study is to report the evaluation of the micromeritic properties of LubriTose AN, which is expected to provide preliminary theoretical basis for the direct compression technology. From the aspects of flowability, compressibility and dilution potential, the angle of repose, flow velocity, the Carr index, tensile strength, elastic recovery, yield pressure and the lubricating ability of LubriTose AN were determined. Also, model drugs were selected to investigate the dilute potential under the desirable compressing performance. Compared to the physical mixtures, the flowability of LubriTose AN was better, and the deformation mechanism was the same with anhydrous lactose, both brittle deformation. The compressibility and compaction of LubriTose AN was slightly better than that of physical mixtures under low and moderate pressure. The dilution potential of LubriTose AN were high for most of hydrophobic drugs. The lubricate ability was desirable under different rotational speeds. LubriTose AN is an excellent co-processed excipient, which is helpful for the promotion and improvement of the tablet manufacturing level. Key words: LubriTose AN; co-processed excipient; micromeritics; direct compression; lactose anhydrous Shangraw [1], : ; : :. * Tel: , kexue1973@vip.sina.com, ;,,, [2],, [3]

4 : LubriTose AN 641,, ( ), [4, 5], [6], [7],, Ludipress, Avicel, StarLac, Microlac, Cellactose [8] LubriTose AN, (GMS) 96 4,, LubriTose AN,,, LubriTose AN ( Kerry, : 200 LB DR), ( Kerry, Anhydrous lactose DT, : ), (, : ), (, : C M), C (, : ), (, > 95%), (, : ), (, : ), (, : , > 99%), (, >90%, : ), (, 96.07%, : ), ( ) (78X-2B, ); (FT-2000, ); (ZBS-6B, ); (Philips XL-30, Eindhoven, Holland); (series 2600c, Malvern Instruments, Worcestershire, UK); BT-1000 ( ); Rimek (Rimek Minipress, Karnawati Engineering Ltd.); Fette (Fette 2901 rotary tablet machine, ) LubriTose AN LubriTose AN BT-1000, LubriTose AN (, w/w =99 1, ), 1%,, LubriTose AN 96 4,, (99 1) BT-1000, LubriTose AN, : (1 / ) 100%,, 5 cm ( ),,, 100 ml, ml 1cm, (n) (V n ) n 1 n V 0 V inf V 0 Vn = + ; a = ; C = C ab a V 0 V 0 C ; n, ; a ( ), a, ; b, b, n/c n, 1/a, 1/ab, a b Fette 2901, LubriTose AN : 24 h, (f c, kg) ( d h, cm), (σ T,MPa) σ T = 2 fc π hd (yield pressure, P y ) 300 mg, 9mm, Fette h,

5 642 Acta Pharmaceutica Sinica 2012, 47 (5): (P) (h) (h 0 ) Heckel, P y 1 1 ln = P + A h0 P 1 y h (elastic recovery, E R ),,,, (H 0 ) 24 h (H t ), E R, E R, E H H H t 0 R = 0 100%, LubriTose AN ( 80%), Fette 2901,, LubriTose AN C LubriTose AN, Rimek, ( ), LubriTose AN 1 LubriTose AN 1, LubriToseAN LubriTose AN 125 μm BT-1000, LubriTose AN 40.7 ±0.2 ( x ± s, n =3), 44.7 ±0.4 ( x ± s, n =3), LubriTose AN 2.2 Figure 1 Scanning electron microscope of LubriTose AN, ;,, 15% 25%, 1, LubriToseAN, Table 1 Carr index of LubriTose AN and physical mixture. n = 3, x ± s Parameter LubriTose AN Physical mixture Bulk density/g cm ± ± Tapped density/g cm ± ± Carr index /% , LubriToseAN, LubriTose AN 2.3,,, LubriTose AN 2, LubriToseAN Table 2 (n = 3) Group Flow rate of LubriTose AN and its physical mixture Weight /g Time /s Flow velocity /g s 1 LubriTose AN Physical mixture , LubriTose AN (a) (b), 3,

6 : LubriTose AN 643 LubriTose AN Table 3 Parameter in Kawakita equation Group a (flowability index) b (packing index) LubriTose AN Physical mixture LubriTose AN ( -β- ) Heckel, MPa, -β-,, LubriTose AN -β-, ( ),, LubriToseAN, 3 3.1,, LubriTose AN, 2,, LubriTose AN,, LubriTose AN Figure 3 Heckel curve of LubriTose AN and anhydrous lactose 3.3 LubriTose, 4, LubriTose AN, Figure 4 Relationship of elastic recovery and pressure of LubriTose AN and physical mixture Figure 2 Relationship of pressure and tensile strength of LubriTose AN and its physical mixture 3.2, [9], 3 :, ( ),,,,, LubriToseAN,, :,,, ;, LubriTose AN, ;, r min 1, LubriTose AN, 5,, LubriToseAN,, 200 N,

7 644 Acta Pharmaceutica Sinica 2012, 47 (5): Figure 5 Ejection force of ibuprofen tablet under different compression force and different speed. A: 15 r min 1 ;B:25 r min 1 ;C:35 r min 1, 400 N LubriTose AN GMS 0.8%, 1%, LubriTose AN, LubriTose AN, 6, 80%, (5 12 kn), (15 75 r min 1 ), 200 N 75 r min 1, LubriTose AN,, LubriToseAN, (100 r min 1 ) 75%,, 30%; 20%, C 10%, LubriToseAN, LubriTose AN, LubriTose AN,,,,, LubriTose AN,, [10],, LubriTose AN, LubriTose AN, LubriTose AN, ; ; ; ; References Figure 6 Ejection force of ibuprofen compression under different press speed 5 LubriTose AN,, : 80%, 60%, 50%, [1] Shangraw RF, Demarest DA. Survey of current practices in the formulation and manufacture of tablets and capsules [J]. Pharm Technol, 1993, 17: [2] Gohel MC, Jogani PD. A review of co-processed directly compressible excipients [J]. J Pharm Pharm Sci, 2005, 8: [3] Olowosulu AK, Oyi A, Isah AB, et al. Formulation and evaluation of novel coprocessed excipients of Maize Starch and Acacia Gum (StarAc) for direct compression tabletting [J].

8 : LubriTose AN 645 Int J Pharm Res Innov, 2011, 2: [4] Gao CS, Wang W, Huang J, et al. Study on compressibility paracetamol tablets [J] Braz J Pharm Sci, 2010, 46: 205 and tablet-forming ability of cellactose 80 [J]. ( ), 2007, 42: Chin Pharm J [8] Yao J. Application Directory of Pharmaceutical Excipients ( ) [M]. Beijing: China Medical Science [5] Mirani AG, Patankar SP, Borole VS, et al. Direct compression high functionality excipient using coprocessing technique: a Press, 2011: [9] Cui FD. Pharmaceutical Powder Compaction Technology ( brief review [J]. Curr Drug Deliv, 2011, 8: [6] Block LH, Moreton RC, Apte SP, et al. Co-processed ) [M]. 2008: Beijing: Chemical Industry Press, excipients [J]. Pharm Forum, 2009, 35: [7] Ogunjimi AT, Alebiowu G. A quantitative study of the influence of coprocessing of binders on the mechanical properties of [10] Uzunovic A, Vranic E. Effect of magnesium stearate concentration on dissolution properties of ranitidine hydrochloride coated tablets [J]. Bosn J Basic Med Sci, 2007, 7: ,,,,,,,, 15, (

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