Vin nn

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

Vin Vit C Php

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

Calci sulfat dihydrat

Lactose

Dicalci phosphat

Sucrose

Tricalci phosphat

Dextrose

Calci carbonat

Mannitol

Tinh bt

Sorbitol

Tinh bt bin tnh

Cellulose vi tinh th

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

Tinh bt bin tnh

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:

4.3-Xu hng nh hng SKD:

t v mc r quyt nh SKD
-t r : ty yu cu tng loi vin
-mc r: quyt nh Sbmtx:
.r ht to: S hn ch, Vhtan hn ch
.r ht nh: S ln, Vhtan tt
.R mn: S ti a, Vhtan ti a

I-la chn t dc
4-t dc r:

4.3-Xu hng nh hng SKD:

BCQU thng quan tm n t r. Nu th
ha tan thi khng cn th r
4.4-S dng:
-R trong:phi hp trc khi to ht, lm ht
r thnh TP, h VMQ phn b u trong
vin
-R ngoi: phi hp vi ht (td trn), lm
vin r thnh ht

I-la chn t dc
Kiu cu trc,
tn

Tn thng mi

1. Tinh bt bin tnh;

sodium starch
glycolate; Sodium
carboxymethyl starch

Explotab(EdwardMendellCo.)
Primojel(GenerichemCorp.)
Tablo(Blanver,Brazil)

2. Cellulose bin tnh;

croscarmellose; Crosslinked sodium
carboxymethyl
cellulose

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

Mui stearat (Mg, Ca, Na)

0,25- 2

Acid stearic

0,25-4

Sterotex (Du ht bng hydrogen

ho)

0,25-2

Sp

1- 5

Sterowet (Ca stearat-NLS)

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 dung dch

Bao hn dch

2. Bao tan rut DC cellulose:

(Enteric film
CAP
coating)
PVAP
HPMCP
HPMCAS
Nha acrylic:
Polymethacrylat (Eudragit
L12,5; L100; S12,5; S100;
L100-55)

Aquateric

3. Bao kim sot

gii phng thuc
( Sustainedrelease, or
Controlledrelease)

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

Ii-so snh 3 pp dp vin

Ht t
- bn cao
-ng u
m, hl
-d thao tc

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

Vin tNHT DDVN iii

Aspirin

Indomethacin

Furocemid

Ampicilin

Izoniazid

Pirocicam

Ciprofloxacin

Metronidazol

Griseofulvin

Cloroquin

Papaverin

Quinin

Diazepam

Paracetamol

Tetracyclin

Erythromycin

Penecilin V

Theophylin