vin nn

ni dung chnh:
T dc
Phng php bo ch
Sinh kh dng
Yu cu cht lng

1.

2.

3.

4.

5.

Mc tiu bi hc Vin nn

Nu c v tr dng thuc, u nhc im

chung v mt SKD v k thut bo ch
ca vin nn.
Trnh by vai tr, cch s dng, cc v d
c th ca 5 nhm t dc: n, r, dnh,
trn, bao dng bo ch vin nn.
So snh 3 phng php bo ch vin nn:
xt ht t, xt ht kh, dp thng.
Trnh by c ch hnh thnh vin nn.
Nu cc yu t thuc phm vi cng thc v
k thut c th nh hng ti SKD vin nn.
Nu c cc tiu chun v phng php

Vin nn
Khi nim
Dng thuc rn, mi vin l mt n v phn liu.
Nn thnh hnh tr, oval, a gic...
Cha 1 hoc nhiu dc cht, c th thm t dc.

La chn t dc v xy dng cng thc

vin nn
Yu cu ca la chn cng thc:

Cng thc ti u v:
- Gii phng dc cht
- bn c hc
- Gi thnh

C s la chn t dc:
1. Tnh cht ca dc cht:
Vt l
Ho hc
Bo ch: chu nn, trn chy..
2. Tnh cht ca t dc c th nh hng n vin
v:
C hc
SKD
3. Yu cu ca vin:
r nhanh?
r chm?
ho tan?
tc dng ko di?
khng dch v?...
4. PP bo ch vin:
xt ht t
xt ht kh

Phn tch mt t dc trong cng thc:

- Nm nhm no
- c dng trong vin cc dng no
- u nhc im
- ng dng:
Dng cho loi vin no
Dc cht no
T l dng (c th)
V d vin (c th) ...

Cc nhm t dc thng dng:

1. n
2. Dnh
3. R
4. Trn
5. Bao
6. Khc: mu, thm, bo qun, tng
n nh

1. Nhm t dc n (diluents/ fillers)

Vai tr:

m bo khi lng vin

Yu cu: - La chn sau cng

- Cng t ht m cng tt
- Tr, khng nh hng n sinh
kh dng v cc tnh cht vt l, ho hc
ca vin.

Phn loi t dc n
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

Cc t dc n in hnh
Lactose
u im:

- Tr
- t ht m
- D phi hp vi cc bt khc

Nhc:
- Chu nn km
- Tng k vi cc cht c nhm chc amin
- C xu hng ko di thi gian r
Cc dng:
Lactose.1H2O: dng kt tinh
Lactose khan: v nh hnh
Lsd:
- Dng phun sy
- C th dp thng vi 20- 50% dc cht
Fast- Flo lactose, Cellactose, tablettose, Ludipress
10

Lactose nghin

V d 1: Vin vitamin B12

Thnh phn 1 vin:
Cyanocobalamin, USP
55g
Lactose khan, bt mn
150 mg
Dung dch gelatin 10%
v
Du thc vt hydrogen ho (Sterotex)
5 mg

V d 1: Vin vitamin B12

Bo ch:
- Ho tan Vitamin B12 trong dung dch gelatin
- Nho dd trn vi lactose to khi m
- Xt ht, sy ht
- Thm Sterotex vo ht kh, dp vin.

Cc t dc n in hnh
Sorbitol

C cc dng: kt tinh , (km bn), ;

v nh hnh.
Sorbitol 834 v Neosorb 80
Vi tnh chu nn v trn chy khc
nhau.

C th b ht m v dnh chy ci nu
m mi trng > 50%

C v ngt mt nn thch hp cho vin nhai,

vin ngm
14

V d 2: Vin ngm bc h
Neosorb
99,3%
Magnesi stearat
0,5 %
Tinh du bc h
0,2%

Cc t dc n in hnh
Tinh bt
u im:

- Tr
- D phi hp
- R tin
Nhc: - Lm vin xp
- m cao (10-14%)
Tinh bt bin tnh:
- L tinh bt c lm bin i v mt vt
l hoc ho hc
- Chu nn, trn chy tt
Vd:
Dn cht carboxy methyl ca tinh bt: Primogel,
Lycatab, Explotab...
Tinh bt thu phn: Emdex, Celutab (cha 9092 % dextrose, 3- 5 % maltose), Starch 1500...

Cc t dc n in hnh
-

Calci phosphat, dibasic (calci monohydrogen

phosphat)
Khng tan trong nc, tan nh trong dd acid long.
Khng ht m, trung tnh.
Lm cho vin chc
t nh hng n r nu dng t l thp
Tn thng mi: Emcompress (Calci phosphat dib asic,
tinh bt, Mg stearat, Avicel, Primogel)

Dng lm t dc dp thng vi 40-50% trong CT,

To ct cho vin TDKD.
Thay i t l Avicel c th lm thay i SKD ca 1 s
DC t tan,

VD: Vin indomethacin dp thng

T l CaHPO4: Avicel
% indomethacin gii phng sau
30 pht

50: 50

70:30

86:14

66

18

10
17

Cc t dc n in hnh
Calci phosphat
VD 3: Vin phenobarbital 30 mg (dp thng)

Thnh phn 1 vin:

Phenobarbital (bt mn)
30 mg
Calci hydrogen phosphat dihydrat
90 mg
Avicel PH 101
29,5 mg
Tinh bt
4 mg
Talc
1 mg
Magnesi stearat
0,5 mg

VD 3: Vin phenobarbital 30 mg (dp thng)

Bo ch:
- Trn k phenobarbital, calciphosphat cho
ng nht.
- Trn tip ln lt Avicel, tinh bt, talc,
magnesi stearat.
- Dp vin ng knh 7 mm.

2. Nhm t dc dnh (Binders and adhesives)

- Vai tr:
Lm tc nhn lin kt cc tiu phn to thnh
vin, m bo chc cho vin.
- Nguyn tc chn:
Ch dng lng t dc dnh va m bo
chc.
Cc yu t lin quan khi chn t dc dnh:
chc ca ht
Lc dp vin
cng ca vin
Cc t dc trong vin tan/khng tan trong nc
20

Nhm t dc dnh
- Kh nng dnh ca cc t dc:
Nc < cn < h tinh bt < siro n < gelatin<
gm arabic < cc d/c cellulose < PVP.
- Bn cht ca t dc dnh c th nh hng ti:
Tc sy kh
Thi gian nho m
m ca ht...
- Phn loi:
- T dc dnh lng
- T dc dnh kh
- Cch phi hp t dc dnh lng vo hn hp bt:
* Trn td vo hn hp bt, thm dung mi vo
nho

Nhm t dc dnh
Nng cc t dc dnh lng thng dng:
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

22

cc t dc dnh in Hnh
H tinh bt

- L t dc dnh thng dng

- u: + To ra l xp trong vin, lm vin r
nhanh
+ D trn u vi khi bt kp
+ R tin, sn c
- Nhc:
+ Nu sy nhanh ht kh khng u
+ D b nm mc
- C nhiu loi tinh bt vi nhit h ho
khc nhau: sn, m, go, ng, khoai ty...

cc t dc dnh in Hnh
Dn cht cellulose

CH2OR
H

+ Kh nng dnh mnh

C
H

+Trng n v tan chm to dung

dch c nht cao

OR
C
H

O
C

OR

Tn

N
(%)

c im

MC

- CH3

1- 4

Tan trong nc
Khng nh hng n thi gian r

EC

- C2H5

0,5-2

Khng tan trong nc, tan trong cn

Lm vin r chm, thch hp vin
TDKD

HPMC

- CH2- 0,5- 2 Tan trong nc v dung mi hu c

CH(OH)
t nh hng n r
-CH3
24

cc t dc dnh in Hnh
Polyvinyl Pyrrolidon (PVP)

- Dng loi c khi lng phn t 30 000- 50 000

- Dng dung dch 3- 15 %, dch cn d xt ht hn.
- u im: Tan c trong nc v trong cn,
D to ht, sy kh v dp vin
Khng nh hng n r ca vin
- Nhc: d b ht m
- Thng dng:
Cho nhiu loi vin nn
Thch hp cho vin nhai, (vd 4)
25

coPolyvidon (Plasdon S-630)

- Sn phm trng hip ca N- vinyl-2- pyrolidon v
vinyl acetat
- Dng bt phun sy; kch thc TB 0,1 mm
- t ht m
- Dng lm t dc dnh trong vin dp thng, xt ht
t, xt ht kh.

Vin
dp
thng

2.Nhm t dc dnh
Phi hp t dc dnh:

- Phi hp 2 hoc 3 loi t dc

- Thm cht ho do lm tng sc cng
ca dch, gim mi mn cho vin:
VD: PG, PEG 400, glycerin, hexylen glycol...

27

V d 4: Vin nhai khng acid

Thnh phn:
Nhm hydroxyd, gel kh
mg
Magnesi hydroxyd, bt mn
mg
ng
Manitol, bt mn
mg
Dung dch PVP 10% trong ethanol
Magnesi
stearat
mg
Cab-O-Sil
Glycerin

200
200
20 mg
180
50% v
12
4 mg
8 mg

Bo ch:
- Trn 4 thnh phn u.
- Thm glycerin vo dd PVP nho m
- Xt ht qua ry 0,8 mm.
- Trn tinh du vi t dc trn, trn vo ht
kh.
- Dp vin
C th trn bt PVP (10 mg) vo khi bt
kp, dng cn 50% xt ht.

3. Nhm t dc r ( Disintergrants)
Cch r ca vin:
- R ht to: R nhanh nhng ho tan chm
- R ht nh: R thnh ht , ho tan nhanh
- R keo/ r tiu phn: R thnh cc tiu phn
mn
C ch r:
Vi mao qun: Trong vin c cc l xp to thnh h
thng vi mao qun, mao qun
Trng n
Ho tan
Sinh hi

30

Cch phi hp t dc r vo cng thc vin:

- Trc khi to ht (trn vo khi bt kp)

- Trn vi ht trc khi dp vin
- Kt hp c 2 cch trn.

Cc t dc r in hnh
Tinh bt
- R theo c ch vi mao qun do tinh bt c cu trc xp
- Tc r v cch r ph thuc vo xp v s phn
b vi mao qun trong lng vin
- Thi gian r khng ph thuc vo lc nn.
- T l dng:

T dc
Tinh bt (ng, khoai...)

T l trong CT(%)
1-20

Tinh bt Na glycolat (DST, Primojel,

Explotab)

1- 20 ( ti u 4%)

Tinh bt bin tnh (National 1551,

Amijel)

5-10

Tinh bt ng bin tnh( Starch

3-8

32

DST

Upon Exposure to 100% RH Air

Cc t dc r in hnh
MC,

Cellulose v dn
cht

CMC,
NaCMC

(Ac-Di-Sol) (siu r)
Cellulose vi tinh th ( MCC- Micro crystalline
cellulose)
-Tn thng mi:
Avicel: PH101, 102;
Emcocel
Microcel...
- Cu trc si, c kh nng ht nc v trng n mnh
- Kt dnh, chu nn v trn chy tt
- T l dng t 10%

KTTP ca mt s MCC
Tn t dc

KTTP m)

Tn t dc

KTTP (m)

Avicel PH -101

50

Emcocel 50M

51

Avicel PH -102

90

Emcocel 90M

91

Avicel PH -105

20

Vivacel 101

50

Avicel PH -112

100

Vivacel 102

100

Avicel PH -200

180

Vivacel 12

180

Vivacel 20

20

VD: Mt s tnh cht ca Emcocel 90M:

- Gc ngh: 34,4o
- Khi lng ring biu kin: 0,35 g/cm3
- chy: 1,41 g/s
35

V d 5:
Acetaminophen

325
mg

30 mg

Dung dch
gelatin 10% v
PEG 5%

Pseudoephedrin HCL

Chlorpheniramin
maleat

2 mg

Starch 1500

15 mg

ng

20 mg

Sterowet C

15 mg

Cellulose vi tinh th

30 mg

Cab- O- Sil

0,2
mg

36

V d 5:

Bo ch:
Trn DC vi ng.
Thm td dnh nho thnh khi m.
Xt ht qua ry 1,2 mm, sy.
Sa li ht qua ry 1 mm.
Trn ht vi Cab-O-Sil, Avicel, tinh bt,
trong 15 pht
Thm Sterowet C, dp vin

Cc t dc siu r

Kiu cu trc, tn

Tn thng mi

1. Tinh bt bin
tnh; sodium
starch glycolate;
Sodium
carboxymethyl
starch

Explotab(EdwardMendellC
o.)
Primojel(GenerichemCorp.)
Tablo(Blanver,Brazil)

2. Cellulose bin
tnh;
croscarmellose;
Cross-linked
sodium
carboxymethyl
cellulose

AcDiSol(FMCCorp.)
NymcelZSX(Nyma,Netherl
ands)
Primellose(Avebe,Netherlan
ds)
Solutab(Blanver,Brazil)

3. Nhm t dc r
T dc r sinh kh (CO2)

Thnh phn t dc sinh kh:

- Acid: acid tartric, citric, malic, fumaric...
- Kim: Natri hydrocarbonat, natri carbonat,

kali hydrocarbonat...

Cc t dc khc: n, dnh phi tan c

T dc trn ch dng t l nh khng tan

Thm cc t dc iu hng v ph hp

39

V d 6: Vin paracetamol- codein

Thnh phn:
Paracetamol
Codein phosphat
Dioctyl natri sulphosuccinat
Aspartam
Natri saccharin
Natri bicarbonat
Acid citric khan
PVP
PEG 6000
Aerosil
Nc tinh khit

500 mg
8 mg
2mg
17 mg
3 mg
1533 mg
1133 mg
20 mg
67 mg
20 mg
v

V d 6: Vin paracetamolcodein
Bo ch:
- Ho tan PVP, DONS, saccarin trong nc
ct.
- Trn cc DC vi aspartam, nabica. To ht
bng dd trn, sy ht ti m di 0,5%.
- Trn ht vi cc t dc cn li.
- Dp vin vi chy c ng knh 23 mm,
F>7 kg/cm2.

4. Nhm t dc trn
Phn loi

Vai tr

1. Lm trn
(lubricants)

Gim

lc ma st gia
vin v thnh ci
Gip y vin ra khi
ci.
Vin bng, p

2. Chng dnh
(antiadherents)

Chng dnh chy , ci

3. iu
cng chy

r v ho
ho s
tanchy
ca vin c Tng
th b
(glidents)
nh
hng bi:
- Loi t dc trn
- Din tch b mt ht
- Thi gian trn
- Lc trn

Ht

T dc
trn
42

Cc cht lm trn (lubricants):

T dc trn khng tan trong nc:

+ Hiu qu lm trn cao, dng vi t l thp.
+ Nn phi hp vi cc t dc trn nhm khc.
+ Trn t dc trn v t dc r ngoi (tinh bt)
lm gim tnh s nc ca vin (VD5).

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

Talc

1-5

1-5 sulfat
*Sterowet
Sterowet: Hn hp calci stearat v natri lauryl

Laminar Structure of
Magnesium Stearate

Cc cht lm trn (lubricants):

T dc trn tan trong nc:

Hiu qu lm trn khng cao

Dng cho cc vin ho tan (vin si bt) (VD 6)

T dc
Acid boric
Natri benzoat+acetat
NaCL

T l dng (%)
1
1-5
5

DL- Leucin

1-5

Carbowax (PEG) 4000, 6000

1-5

Natri oleat

Natri benzoat

Natri acetat

Natri lauryl sulfat

1-5

45

- T dc chng dnh v iu ho s chy :

T dc
Talc
Tinh bt
Cab-O-Sil (SiO2)

T l (%)
chng dnh

T l (%)
tng 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

#Mt t dc c nhiu vai tr, nhng mc khc

nhau
46

Vic la chn t dc trn ph thuc vo:

ng dng
Loi vin
Yu cu v r v ho tan
Tng k ca DC
Gi

Lng t dc trn chy ph thuc:

- Kch thc ht: vin dp thng c kch thc ht (bt)

nh hn nn cn nhiu t dc trn hn
- Kch thc t dc: VD Aerosil c kch thc 2-20nm th
kh nng bao ph din tch 200-300 m2/g

Tnh cht trn chy ca ht:

Tc d ch y ca ht khi c t dc ch y
F= Tc d ch y ca ht khng c t dc ch y
47

PTMHue- 2008

48

V d 7: Vin nn dp thng
Thnh phn:
Chlorpheniramin maleat 4,0 mg
Pseudoephedrin hydroclorid
60,0 mg
Avicel PH101 37,5 mg
Fast-Flo lactose
113,0 mg
Ac-Di-Sol
2,2 mg
Cab-O-Sil
1,1 mg
Acid stearic 1,3 mg
Magnesi stearat
1,1 mg

Yu cu:
1. Nu vai tr cc thnh phn trong cng thc?
2. Gii thch s phi hp t dc trn trong cng
thc?

5. nhm t dc bao
Nguyn liu dng trong bao film:
Polyme
Cht ho do
Cht n v chng dnh
Cht mu
Dung mi

- Polyme c vai tr chnh, quyt nh mc ch

bao:

Bao bo v

Bao tan rut

Bao gii phng ko di

- Cc thnh phn khc c th nh hng n tnh

5. nhm t dc bao
Polyme
Loi mng bao
Bao bo v
(Conventional
film coating)
1.

Bo v DC
Tng 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
-Polyethylacrylat-methylmethacrylat
(Eudragit E12,5; E100)

5. nhm t dc bao:
Loi mng bao

Polyme
Bao dung dch

Bao hn
dch

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

2.

DC cellulose: EC
Nha acrylic:
- Poly ethylmethacrylat
- Poly(ethylacrrylat,
methylmethacrylat)triethyl
-

Aquoat
Eudragit
L30D

Eudragit
NE 30D
Eudragit
RL30D;

5. nhm t dc bao

Cht ho do (plasticizers):
polyols, such as polyethylene glycol 400
organic esters, such as diethyl phthalate
oils/glycerides, such as fractionated
coconut oil.

Pha ch dch bao

Theo nguyn tc pha ch hn dch
Polyme thng c thi gian trng n v ho tan
lu
Thi gian khuy trc khi bao:1-2 gi
Lm nng v tip tc khuy trong khi bao

Pha ch hn dch bao

Cng thc bao:
HPMC
PEG 6000
Titandioxyd
Magnesi stearat
Mu erythrosin
Ethanol
Nc

BAO TIU PHN CHE V

Paracetamol Special Granular

Mallinkrodt Inc.
Particle size: 99.5% 150 - 420m
Surface area (Blaine): 259.4 cm/g
EUDRAGIT E PO

Taste masking (n=9)

15 % polymer:
27 sec
30 % polymer:
59 sec
Smooth and mild

PHNG PHP CHE V CHO VIN NHAI

EUDRAGIT L 100-55 + VerapamilHCl
Dosing

Milling

Kneading
Cooling

Feeding

Melting

Homogenizing
and discharge

Granulating

Mixing
Dextrose
Kollidone 90 F
PEG 6000

Tableting

Chewable tablets with neutral taste!

Polymers for Targeted Release

Mouth

Stomach

EUDRAGIT
L 30 D-55
L 100-55
Thin layers < 50 m

Duodenum
EUDRAGIT
L 30 D-55
L 100-55

Jejunum
EUDRAGIT
L 100
L 12.5

Ileum

Colon

EUDRAGIT
FS 30 D
S 100
S 12.5

v d 9
Natri diclofenac
25 mg
Aerosil 200
MCC
Lactose
Magnesi stearat
Tinh bt m
PVP
Acetyl phtalat cellulose
HPMC 4cp
Diethyl phtalat
Oxyd st
Titan dioxyd
Phn tch vai tr ca tng t dc trong cng thc bao.

phng php bo ch vin nn

Vin nn
- Xt ht t
- Xt ht kh
- Dp thng

Mc ch to ht
Tng cng lin kt gia cc tiu phn bt ,
m bo chc cho vin
Trnh hin tng phn lp ca khi bt, m
bo s phn tn dc cht ng nht trong
vin
Gim hin tng dnh chy ci khi dp vin
do gim din tch tip xc gia nguyn liu
v thnh ci (gim lc ma st)
Tng kch thc tiu phn ci thin
chy ca bt

Yu cu ca ht
Trn chy
Chu nn
Nn:
- Hnh dng thch hp: hnh cu c t
trng cao nn d lin kt thnh vin.
- Kch thc thch hp : nh hng n
chy v ch s nn
Kch thc thng thng t 0,5- 1,5 mm
Vin cng nh kch thc ht cng nh
v ngc li

C ch hnh thnh vin nn

Khi cha nn cc tiu phn xp xa nhau, gia cc ti

phn c khong trng- cha khng kh.

Khi nn cc tiu phn xp st li, khong trng bin

thnh cc mao qun, vi mao qun
- Cc tiu phn xp st li sinh ra lc lin kt tiu
phn , gip hnh thnh vin
- Nu nn nhanh, m khng kh s chng li lc nn
- Tng lc nn n mc no th lc lin kt
khng tng- lc nn ti hn.

Gii nn
- Vi cc tiu phn n hi, vin d bong mt.
- Cc tiu phn bin dng do, khi nn lc phn hi
nh, lc lin kt hnh thnh t thay i sau khi gii
nn.

Cc tnh cht ca vin nh hng bi lc nn

T trng v xp:
- T trng biu kin ca vin tng khi tng lc nn ti
nn gii hn.
- xp ca vin t l nghch vi lc nn,
cng ca vin:
- Lc nn tng, cng tng ti nn ti hn
- Din tch b mt ring (SS)= din tch b mt ca 1g
nguyn liu

SS ln nht khi xp
khong 1%,

SS

F thay i
nguyn liu
F

tu

loi

Cc tnh cht ca vin nh hng bi lc nn

r:
Tng lc nn, gim xp, tng thi gian thm nc,
tng thi gian r
T r

1%

5%
10%

Vin sulfadiazin xt ht vi
h tinh bt ng
15%

Lc
nn

Cc tnh cht ca vin nh hng bi lc nn

ho tan
Vin khng r: Tc ho tan khng ph thuc vo lc
nn.
Vin r: Kh d on trc c nh hng
Vin qui c: tc ng ca yu t cng thc hn l lc nn

VD: Vin sulfadimid c xt ht vi cc t dc dnh khc nhau

Lc nn
(MN/m2)

T50% (pht)
H tinh bt

Dd MC

Dd gelatin

200

54,0

0,5

10,0

400

42,0

0,8

4,5

600

35,0

1,1

3,0

800

10,0

1,2

4,6

1000

7,0

1,4

4,9

Vai tr ca nc
trong qu trnh hnh thnh vin
-

Nc lm gim tnh n hi ca tiu phn,

tng tnh do, tnh chu nn.

- Lm hnh thnh cu ni hydro gia cc tiu

phn, lm tng lc lin kt tiu phn.
Do vy nu ht kh qu vin khng chc.
Hm m ca ht t1- 7%.
- Nu ht hay bt t qu, lm trt cc tiu
phn, khng kt dnh c v vin cng
khng chc.

5. nhm t dc bao
C 4 phng php bao chnh:

1.
2.
3.
4.

Bao ng
Bao mng mng/ film
Vi nang
Bao bng phng php dp vin

Qui trnh bao mng mng

Tnh lng dch bao
Pha ch dch bao
Bao vin:
- Sy
- Phun dch
- o vin

Tnh lng dch bao

- vin hinh tr dt: A= . (d. h + 1/2d2)
- Thuc nang, vin hnh thun: A= . d. h
- Dng gn hnh cu (ht, pellet): A= . d2

A: Din tch b mt (mm2)

D: ng knh (mm)
H: Chiu cao ca vin (mm)

Sinh kh dng vin nn

PTMHue- 2008

75

PTMHue- 2008

76

Sinh kh dng vin nn

Mi lin quan gia r v SKD

VD: Vin nn Aspirin
Bit d
c

Thi gian
r (giy)

Lng DC ho
tan sau 10
pht

Nng
trong nc
tiu sau 1h

256

242

24,3

35

206

16,5

10

165

18,1

13

156

13,6

10

127

12,1

cc yu t nh hng ti SKD ca vin nn

ng dng

VD: nh hng ca cc loi thc n ti nng ca

griseofulvin trong huyt tng khi ung liu 1 g
Bo cao

2,5Nng
(mg.ml-1)

Margarin
60g
Margarin
30g
Protein cao
i

Thi gian (h)

nh hng ca t dc n n skd ca vin nn

VD: nh hng ca lng tinh bt n tc ho
tan ca vin nn acid salicylic

nh hng ca t dc r n skd ca vin nn

Batch

Ibuprofen (mg)

200

200

200

200

Croscarmellose
sodium (mg)

50

Crospovidone (mg)

50

Coprocessed
superdisintegrant
(mg)

50

Cab-O-Sil (%)

0.5

0.5

0.5

0.5

HPC (%)

ibuprofen tablets

AAPS PharmSciTech. 2007;8(1):Article 13

nh hng ca t dc r n skd ca vin nn

Dissolution profile of ibuprofen tablets

AAPS PharmSciTech. 2007;8(1):Article 13

nh hng ca t dc n skd ca vin nn

-T dc trn
VD: nh hng ca t dc trn n tc ho tan
ca vin nn acid salicylic
3% natri lauryl sunfat
0% TD trn
3% Mg stearat

nh hng ca k thut bo ch n skd ca vin

nn
VD: Tc ho tan ca Dexamethason t vin nn c to ht
khc nhau
% ho tan

To ht tng si
Xt ht t
Xt ht kh

T (pht)

nh hng ca k thut bo ch n skd

ca vin nn

nh hng ca k thut bo ch n skd ca vin

nn

Tiu chun cht lng vin nn

v phng php nh gi
- SS v khi lng
- SS v hm lng
- nh lng
- r
- ho tan
- cng
- mi mn/b

 r
- nh gi bng thi gian vin r hon ton thnh
cc ht hoc cc kt t nh c th lt qua li ry
ca thit b th
-Qui nh:
Giai
S vin
on
S1

Yu cu
Tt c 6 vin phi t, nu 1-2
vin khng t th th tip

S2
12
t nht 16 vin (S1+S2) u phi
+ Qui nh ca cc Dc in l khng ging nhau
t
VD: D VN qui nh thi gian r ca vin cha bao l
15 pht trong mi trng nc ct;
USP qui nh thi gian v mi trng th tu theo
chuyn lun. (Vin Promazin HCL, t=30 pht Vin
Scopolamin HBr, t= 15 pht)

Thit b th r

-Nhit mi tr
ng th: 36-38oC
-Tc chuyn
ng ca ng
th: 28-32 ln/ph,
khong
cch
chuyn ng: 5-6
cm

 ho tan
ho tan: % DC ho tan sau 1 thi im
theo qui nh ca dc in
VD: theo USP 26, vin paracetamol c % DC
ho tan sau 30 pht phi 80%
Tc ho tan: Lng DC hoc % DC ho tan
trong mt n v thi gian
Thng dng nghin cu, so snh cc cng
thc

iu kin th ho tan:
Thit b
Mi trng ho tan: Dung mi, th tch,
nhit
Thi gian ly mu
Phng php nh lng dc cht
Phng php tnh, nh gi lng DC ho tan
(gii phng)

Thit b th ho tan

Gi quay

(TB s 1)

A
C

A: Cnh khuy (TB s 2), B: Mi trng ho tan, C: B iu

nhit

Gii hn th ho tan (USP)

Giai
on

S vin
th

S1

Mi vin: khng t hn Q+5%

Trung bnh ca 12 vin (S1+S2)

Q, khng c vin no <Q-15%

S2
S3

12

Yu cu

Trung bnh 24 vin

(S1+S2+S3) Q, khng qu 2
vin < Q-15%, khng c vin
no < Q-25%

Gii hn th ho tan (USP)

VD: Vin nn paracetamol
- Thit b: s 2 (cnh khuy)
- Mi trng: 900 ml m phosphat pH 5,8
- Thi gian th: 30 pht
- Phng php nh lng DC: Ph t ngoi,
= 243 nm
- Q= 80%

nguyn tc o lc gy v vin

n v: Strong Cobb (SC), Kilopond

(Kp) or Newton (N)

thit b o lc gy v vin

nguyn tc th b (friability)

Thit b th b (friability apparatus)

Tiu chun b/ mi mn
USP 30:
- p dng cho vin nn khng bao (tr vin si
bt, nhai)
- Lng mu th:
Khi lng 1 vin
650 mg
> 650 mg

Mu th
6,5 g
10 vin

- Trng quay 100 vng

- mi mn/ b F (%)= M0-Mt/M0.100
- Yu cu F 1%