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D4, 2008
Vin nn
-La chon t dc
-So snh 3 phng php dp vin
-SDH vin nn
I-la chn t dc
1-c s la chn t dc:
1.1-Mc ch s dng ca vin (yu
cu GPDC):
-GP nhanh:
.Vin r nhanh (Fast Release): t r tnh
bng giy (dng khi cn tc dng nhanh:
h nhit gim au): td siu r: paraceta,
ibu
.Vin t DL: td siu r, tan c: nitrogly
I-la chn t dc
1.1-Mc ch s dng ca vin:
.vin ha tan(vin pha dung dch): td tan/N
.vin si bt: td si bt, tan c,..
-GP ngay (Immediate R.): vin thng thng
-GP chm (Slow R.): vin tan rut, vin ngm
-GP ko di (Extent R.): tc dng 12h, 24h,...
-GP theo nhp (Pulsatile R.): t tim tng 4-6 h
I-la chn t dc
1.1-Mc ch s dng ca vin:
BCHD da vo t dc tc ng
vo GP nhm iu tit ha tan v
hp thu (vai tr ca t dc l iu
tit hp thu: td siu r, td bao tan
rut, td TDKD,...)
1.2-Tnh cht DC:
-D tan: thng l DC t tan
-D n nh ha hc
I-la chn t dc
1.2-Tnh cht DC:
-KTTP (vi DC t tan)
-D trn chy
-Kh nang chu nn (ch s nn)
1.3-Tnh cht t dc:
-D trn chy
-Kh nang chu nn
I-la chn t dc
1.3-Tnh cht t dc:
-Kh nang GP DC
-Tng tc DC-TD: lo ha cp tc (mu
bt, hat, vin: pht hin bang HPLC)
1.4-PP dp vin:
-To ht t: dch to ht
-To ht kh: td kh
-Dp thng: td trn hy
Cng c la chon t dc: TNHT, HPLC,
I-la chn t dc
2-t dc n:
-Vai tr: m bo m vin
(nhm DC tc dng mnh ngy cng nhiu)
-Xu hng nh hng SKD: khi chim > 80%:
.Quyt nh t/c c l ca bt, ht dp
vin: trn chy, chu nn,..: nh hng
n SSm,hl, bn vin.
.Quyt nh c ch GPDC ca vin: ha
tan, khuch tn
I-la chn t dc
-Xu hng nh hng SKD:
.Gy tng tc, tng k:
mI trng kim: calci carbonat, magnesi
carbonat, magnesi oxyd, (B1, B6,...)
hp ph: kao lin, bentonit, magnesi
oxyd,...
to phc: dicalci phosphat, calci
carbonat,...
oxy ha (ion kl): tinh bt, talc,...(VitC,)
I-la chn t dc
Mu
Fe
+++
Tinh bt d.d.
126,6
Talc d.d.
96,6
Talc Nht
1,7
Nc ct
41,0
0,05
Vin Vit C Vn
2,72
Cu
12,0
+++
I-la chn t dc
2-t dc n:
-Ngtac s dng:
.Chn sau cng
.Chn td ng c nhiu vai tr: ndnh-r -ht,...:Avicel, tbt bt,...
.DC t tan nn dng nhm tan c: bc
l nhanh S ha tan
.DC d tan: nu cn, c th dng
nhm k tan
I-la chn t dc
Khng tan trong nc
Tan trong nc
Lactose
Dicalci phosphat
Sucrose
Tricalci phosphat
Dextrose
Calci carbonat
Mannitol
Tinh bt
Sorbitol
I-la chn t dc
3-t dc dnh:
-Vai tr: to hinh vin (lc nn, khun):
ngc vi td r, nh hng trc tip n SKD
-C ch:
.Lin kt ha hc: cu ni H2, gel ha
(sol: dch keo gel:cimen): vai tr ca
nc
.Lin kt vt l: lc Van der Wall: vai tr
ca lc nn
I-la chn t dc
3-t dc dnh:
Xu hng nh hng SKD:
.ko di t r: lm chm GP, ha tan
.a m v nhit vo vin
.to o thn N
-Ngtac s dng:
.Nhm dnh lng: to ht t (phi hp nng)
.Nhm dnh kh: to ht kh, dp thng
.Khng lm dng, chn loi c dnh thch
hp : cn r nhanh: chn h tbt, PVP,... cn
r chm (vin ngm): gm, gelatin,
I-la chn t dc
3-t dc dnh:
.DC d thy phn: dng td dnh khan nc
(PVP, gelatin, EC): aspirin, ampicil,
.DC k bn vi nhit: to ht tng sI, dng
td dnh kh (to ht kh, dp thng):
enzym, protein,...
.DC s nc: to o thn
N:PVP(phenobarbital)
.Lm TN t td c dnh thp, t l nh
I-la chn t dc
TD dnh
Nng
(%)
% trong CT
Tinh bt
5-20
1-5
2-5
1-10
Sucrose
50-75
2-10
Glucose
25-50
2-25
5-10
1-5
10-20
1-5
3-15
2-5
Dn cht cellulose
Gelatin
PVP
I-la chn t dc
4-t dc r:
4.1-Vai tr: m u cho LDA (r = GP):
GP tr li So ca DC
4.2-C ch:
.VMQ: lc mao dn ko N vo lng vin:
tng VMQ v phn b VMQ: tinh bt
.Trng n, ha tan: Avicel, tbt bt,...(siu
r)
.Sinh kh: td si bt (ngoi v trong c
th)
I-la chn t dc
4-t dc r:
I-la chn t dc
4-t dc r:
I-la chn t dc
Kiu cu trc,
tn
Tn thng mi
Explotab(EdwardMendellCo.)
Primojel(GenerichemCorp.)
Tablo(Blanver,Brazil)
AcDiSol(FMCCorp.)
NymcelZSX(Nyma,Netherlands)
Primellose(Avebe,Netherlands)
Solutab(Blanver,Brazil)
3. Cross-linked polyvinylpyrrolidone
(Crospovidone)
CrospovidoneM(BASF
Corp.)
KollidonCL(BASFCorp.)
PolyplasdoneXL(ISPCorp.)
I-la chn t dc
5-t dc trn:
-Vai tr: lm thun li cho qu trinh dp vin
.Diu ha s chy: m bo SSm,hlg (NLS, Ae)
.Chng dnh: vin khng dnh chy, ci (talc)
.Lm trn: gip y vin khi ci (acid bo,..)
.Dn truyn, phn b lc nn (talc,Aerosil)
-C ch:
.Bm dnh to mng lm nhn b mt: mn,
nh
.Chng tch in b mt: cch in
I-la chn t dc
5-t dc trn:
-Xu hng nh hng SKD:
.Ko di thi gian r, hn ch GP, ha tan
-Ngtac s dng:
.Khng lm dng, chn ng loi, lng
.Kt hp nhiu loi c c ch tc dng khc
nhau iu ha tc dng: tal-magnesi
stearat
.Vin pha dd dng td trn ha tan: NLS,
PEG,
I-la chn t dc
(t dc trn)
T dc
T l dng
0,25- 2
Acid stearic
0,25-4
0,25-2
Sp
1- 5
1-5
I-la chn t dc
(t dc chng dnh, tang chy))
T dc
Talc
Tinh bt
Cab-O-Sil (SiO2)
T l (%)
chng dnh
T l (%)
tang chy
1-5
3-10
5-10
0,1- 0,5
0,1-0,5
Aerosil (SiO2)
DL-leucin
Natri lauryl sulfat
1- 3
3-10
<1
I-la chn t dc
6-t dc Bao:
6.1-Vai tr:
.Che du mi v: paracetamol, ti,...
.Bo v DC (bao bo v): 3B, alphachymo.
.Hn ch tng k: polyvit
.Kim sot GP: bao tan rut, bao TDKD
.Tang thm m
6.2-C ch: to mng mng ngoi vin
(film)
I-la chn t dc
6-t dc bao:
6.3-Yu t nh hng SKD: thnh phn v
dy mng bao
-Thphn mng bao:
.Polyme to mng: a dng ty yu cu bao
.Cht ha do (to knh): thn D, thn N
.Cht n-chng dnh: talc, titan dioxyd,
Aerosil,...
.Cht mu.
I-la chn t dc
Polyme to mng:
-Bo v: khng cn tr GPDC(d tan): DC
cellulose(CMC, HPC, HPMC,..), Shellack,
PVP, Eud. E,...
-Tan rut: khng dch v (1-2h), r trong
dch rut (30ph) theo 2 c ch:
.do men: cu trc este: CAP, HPMCP,...
.do phn li theo bc thang pH:
Eudragit,...
-KSGP: EC; Eudragit R, L, RL,RS,...
D dy mng bao: ty theo yu cu GP
I-la chn t dc
Loi mng bao
1. Bao bo v
(Conventional
film coating)
-
Bo v DC
Tang v p
Khng nh h
ng n
GPDC
Polyme
DC cellulose:
HPMC(Pharmacoat, Methocel)
HPC
HEC
MHEC
Cc vinyl:
PVA (Opadry AMB)
Nha acrylic:
-Polydimethylaminoethyl
methacrylat- methylacrylat acid
este
-Polyethylacrylatmethylmethacrylat
I-la chn t dc
Loi mng bao
Bao hn dch
Aquateric
Aquacoat
DC cellulose: EC
Nha acrylic:
- Poly ethylmethacrylat
- Poly(ethylacrrylat,
methylmethacrylat)triethylammonioethylmethacrylat
clorid (Eudragit RL12,5;
RL100; RS12,5; RS100 )
Aquoat
Eudragit
L30D
Eudragit
NE 30D
Eudragit
RL30D;
RS30D
Ht kh
-trnh m,
to
-d r
-tit kim
S
Dp thng
-trnh m,
to
-d r
-tit kim
S, t
-m, to
-kh r
-tn S, t
- bn
thp
-k u m,
hl
-DC chy
tt
-Cn t dc
dp thng
S skd vin
Indomethacin
Furocemid
Ampicilin
Izoniazid
Pirocicam
Ciprofloxacin
Metronidazol
Griseofulvin
Cloroquin
Papaverin
Quinin
Diazepam
Paracetamol
Tetracyclin
Erythromycin
Penecilin V
Theophylin