Cc dng thuc rn

dng qua ng ung

solid oral dosage forms

Thuc bt, cm : 3h
Pellet:
1thuc Nang:
4Vin trn:
0Vin nn:
9GiI p:
1Cng:
18TS. P T M Hue- 2008

M u
1-V tr DTR:
-Xt v th cht: nhm 3
.lng: dd (tim, nh mt), hn dch,
nh dch
.mm (bn rn:semi-solid): nh tng,
m, t, cao
.rn: bt, ht (pellet), vin, nang (soft
cap.)
TS. P T M Hue- 2008

M u
1-V tr DTR:
-Xt v h phn tn: nhm 3
.phn t: dd tht
.keo: dd keo, siu vi nh tng
.c hc (tiu phn c hc):nhn thy, o
m c: bt, ht(pellet), vin, nang
-Xt v mt s dng: 2 nht
.LDA phc tp nht
.S dng rng rI nht ?

TS. P T M Hue- 2008

M u
2-u-nhc: (so vi thuc lng): 4-2
2.1-u: (p.132)
-mI trng kh (t xy ra p. ha hc):
n nh hn, tui th di hn, t tng tc
hn (d phi hp hn), t b nhim khun
hn
-C th bao: d che du mi v, d kim sot
GP-hp thu (bao tan rut, bao TDKD,)

TS. P T M Hue- 2008

M u
2-u-nhc:
-Th tch gn nh: tin vn chuyn,
bo qun, s dng (mang theo ngi)
-u t SX t tn km hn (so vi thuc
v khun)
2.2-Hn ch:
-LDA phc tp: pht huy td chm, d
pht sinh vn v SKD
-Quy trnh SX thng ko di (sy ht,
bao vin)
TS. P T M Hue- 2008

M u
3-Xu hng SX:
Vi DC t bn: lng rn (khng sinh,
vit,)
.Dd: bt, vin pha dd (ng kh, si
bt)
.Hn dch: bt, cm pha hn dch
.Siro: bt, cm pha siro (dry siryp): dd
hay hn dch, tin dng
TS. P T M Hue- 2008

Phn 1:

Thuc bt
Thuc cm v pellet
(p.129-151, 2006)

Mc tiu

1.

Trnh by c nh ngha, u-nhc ca thuc bt

(phn bit thuc bt- bt thuc)

2.

Nu c nh hng ca KTTP ti KTBC v SKD ca

DTR

3.

Vn dng c ngtc trn bt kp trong pha ch

thuc bt

4.

Phn tch c mt s v d thuc bt

5.

Nu c PP BC thuc cm v pellet
TS. P T M Hue- 2008

Thuc bt
I-Di cng
1-nh ngha:
Thuc bt

Bt thuc

DVN 3:
Dng rn, gm cc ht nh
Kh ti
C mn xc nh
Cha mt hay nhiu DC (c
hay k c t dc)
Thnh phm ung, dng
ngoi

Tp hp cc tiu phn
dc cht rn
C kch thc xc nh
Nguyn liu u vo
bo ch cc dng
thuc khc.

Thuc bt
2-Phn loi: t c
-Cch phn liu: phn liu-khng phn
-C bt: da theo c ry
.Th: 2000/355 (100/<40%)
.Na th: 710/250
.Na mn: 355/180
.Mn:
180 (100%)
.Rt mn: 125 (100%)
TS. P T M Hue- 2008

10

Thuc bt
3-u-nhc: t c (ging DTR)
LDA n gin nht trong cc DTR

TS. P T M Hue- 2008

11

Thuc bt
Ii-k thut ngin-ry (c bt): t c
1-Nghin bt: gim KTTP:
-Phn chia c hc
-Phn chia c bit:
.dmI bay hI ha tan DC
.mI trng nc (thy phi): lng gn, lc
.nhit: thng hoa, phun sy

TS. P T M Hue- 2008

12

Thuc bt
2- Ry:
-C ry: DDVN
-Ch khi ry: hiu sut, an ton
.bt kh
.lng v
.o nh
.y np

TS. P T M Hue- 2008

13

Thuc bt
3-Lin quan gia bt thuc-DTR :
Vin n
n

Vin trn

Bt thuc

H t

Thuc bt

Vin nang

Bo ch
Gii phng

4-Mt s tnh cht ca tiu phn vn dng

trong bo ch DTR
-Kch thc (KTTP)
-Hnh dng
-Lc lin kt

4.1-Kch thc tiu phn

+nh hng n SKD:
-KTTP gim lm tng SKD:
Phng trnh Noyes- Whitney:
Dc/ dt= K. S. (Cs- C)

KTTP

DTBM TX

Tc tan

ng dng:

Tc hp thu

bt siu mn (micronise/ micronis)

V d: Vin nn Griseofulvin
Micronize/ microcrystaline: 500 mg
Ultramicronize/ Ultramicrocrystaline: 330 mg

4.1-Kch thc tiu phn

+nh hng n SKD

-KTTP tng ko di tc dng: hthu thI tr chm
V d: Penicillin- Procain

KTTP
(m)

Nng mu trung
bnh (th) theo gi
(g/ml)
1h

24h

32h

150-250

1,37

0,86

0,31

58-105

1,54

0,47

0,12

< 35

2,4

0,33

0,07

17

4.1-Kch thc tiu phn

+nh hng n trn chy:

KTTP > 250m:

Bt chy tt

KTTP < 100 m: Kh chy

KTTP < 10 m:

KTTP
DTBM TX
Lc LKTP

Khng chy
trn chy

18

4.1-Kch thc tiu phn

Cch o trn chy:

Vc=m/t
(g/giy)

Gc
ngh

( ln: trn chy km)

TS. P T M Hue- 2008

19

4.2-hnh dngtiu phn

+nh hng n trn chy:
.Hnh cu: tng sI, phun sy
-Khc phc:
.sy
.Tng KTTP
.Td trn
.To ht

TS. P T M Hue- 2008

20

+nh hng n KLR v xp

L xp

L xp
VC

VCS

V cha trong bao

b

V cha trong bao

b -V bt

V tht = VC- VCS

-Hnh cu: (30%)
-Hnh hp: xp kht
21

+nh hng n KLR v xp

Ch s nn
I=D -D 100
D
f

.Df: KLR bk trc khi lc

.Do: KLR bk sau khi lc
( I < 20: Bt chu nn tt)

TS. P T M Hue- 2008

22

+nh hng n KLR v xp

Qu trnh nghin bt c th:

Gim KLR bk ca bt do lng khng kh,
tng xp.
Tng KLR bk do gim KT, khi bt c ng
cht.
Tng KLR tht: Gim KT, gim xp bn
trong tiu phn.

4.3-Lc lin kt tiu phn

- Lc kt dnh (cohesion): tiu phn- tiu
phn: KTTP nh, m: vn, kh chy (sy,
to ht)
- Lc bm dnh (adhesion): tiu phn- b
mt rn (ci, chy,): dng td trn
- Lc tnh in: trong qu trnh chy

25

c tnh ca tiu phn cht rn vn dng trong

bo ch
KTTP

Hnh dng TP

lc lkTP

Tc
ho tan

Tc

ho tan trn chy

Xt ht
Tc
hp thu

PP xt ht

Xt ht
Ry

dng th hnh

Tng
si

Ry
c l

TD dnh

TD trn
Tc
hp thu

III-k thut bo ch thuc bt

1. Nghin bt n
-Bt c khi lng ln nghin trc, khi lng nh
nghin sau
- Bt c t trng ln nghin mn hn bt c t
trng nh.
2. Trn bt kp
- Nguyn tc ng lng
- Bt bay bi (d nh) trn sau cng

27

 ng gi:
2 cch

Trong ti vi liu 1 ln

Chai c vch cha

th tch thm nc.

bi tp 1
PAPS
(Laboratoires M. RICHARD SA)
Lu hunh

8,5 g

Km undecylenat

1,0 g

Bismuth gallat base

0,5 g

Menthol

0,5 g

Camphor

1,0 g

Acid salicylic

0,5 g

Km oxyd

9,0 g

Acid boric

9,0 g

Tinh du thm

0,25 g

+ Trn bt kp

100,0 g

+ Phun cht thm

Talc

- CD: Bt dng
ngoi iu tr
eczema, nm da
- Pha ch:
+ Nghin bt n

bi tp

Bt pha hn dch

Scale (mg/Bottle) (7 g/60 ml)

Amoxicillin Trihydrate (equivalent to 1,250 of Amoxicillin)
1500.00
Potassium
393.60
Xanthan
150.00

Clavulanate
Gum

Hydroxypropyl
1800.00

Methylcellulose

Saccharin Sodium
Silicon Dioxide
300.00

Dried
150.00

Colloidal

Succinic Acid

10.00

Silica Gel

1500.00

30

IV-yu cu cht lng ca Thuc bt

+ Th cht
Kh ti ( m<9%)
- D bo qun
- D phn liu
- D s dng (thi, rc)
+ng nht
+Sai s phn liu
DVN III
31

Iv-yu cu cht lng ca Thuc bt

4. mn
Theo chuyn lun
Xc nh qua php th c bt v ry
R
y
K
nhhi
nvi
i
nt

K
nhhi
nvi quanghc

Siu ly t
m

Sa l
ng
Coulter counter

Hp ph

-4

10

-3

10

-2

10

-1

10

Thm kh

10

100

K
ch th c tiu ph
n

1000

10000 m

32

thuc cm (granules)
KhI nim:
- L cc ht nh xp (ng knh t 1- 2mm) hay
si ngn xp,
- c iu ch t bt thuc v t dc dnh,
- Thng dng ung: pha siro, si bt, pha
dung dch, pha hn dch.

33

thuc cm (granules)

Phng php bo ch:

Xt ht qua ry
Phun sy
To ht tng si
Nho cao tc

thuc cm (granules)
v d 2: Cm pha hn dch azithromycin 5%

Azithromycin dihydrat
5g
Natri citrat
5g
Acid citric
2g
Bt ng
60 g
Natri cyclamat
0,5 g
Crospovidon
9g
Ethanol
9g
Menthol
0,5 g
Polyoxyl 40
0,3 g

(500 mg/10 ml)

lng gi
-Vit 1 n thuc bt dng ngoi
-Vit 1 n thuc bt dng ung (2 cch k
n)
-Nu cch xc nh c bt (th, na th, na mn,
mn,)
-KTTP nh hng n nhung tnh cht no ca bt
-GiI thich ngtac ngin bt n v trn bt kp

TS. P T M Hue- 2008

36

lng gi
Phn bit ng, sai
Ni dung
1

C hai cch k n thuc bt dng

ngoi

KTTP ch nh hng n tan ca dc

cht

Bt n c khi lng ln thi nghin mn

hn

Thuc bt dng ngoi cn phi nghin

mn hn

Bt vi cc tiu phn hinh cu c KLR

biu kin nh

Trong thnh phn ca thuc bt c th

c cht lng

lng gi

Chn mt cu tr li ng nht :
9. Trong mt cng thc thuc bt kp, khi nghin bt
n, phi bt u nghin t loi bt:
A- C khi lng nh
B- C khi lng ln
C- C t trng nh
D- C t trng ln
E- D ht m
10. Trong mt n bt kp, khi trn bt, phi trn t
bt:
A- C khi lng nh
B- C khi lng ln
C- C t trng nh
D- C t trng ln
38

pellet

1-KhI nim:
Ht nh (thng l hinh cu), ng knh t 0,25- 1,5
mm (vin trn nh: nhn n, LTH,)
c iu ch bng cch lin kt cc tiu phn dc
cht rn bi cc t dc dnh.
L bn thnh phm dng ng nang cng hay
dp thnh vin nn.
Mt s pellet tr (non- pareil sead) l cc gi mang
thuc.

39

pellet
2-u-nhc:
.SKD n nh hn vin nn: tho rng d dy
d hn
.D bao hn vin nn: hinh cu, bn c
hc cao, b mt nhn,
.D phi hp DC, hn ch tng k: ng nhiu
loi pellet trong 1 nang (vit B-C)

TS. P T M Hue- 2008

40

pellet
2-u-nhc:
.D kim sot GPDC: bao TDKD kt hp ctmng bao, ng nhiu loi pellet c thi
gian GPDC khc nhau trong 1 nang
(spansules),
.Hn ch : cn c my chuyn dng

TS. P T M Hue- 2008

41

pellet
3-t dc:
-T dc to cu:
Avicel: va to cu va to ct, va l ta n,
thng chim 20-80% khi lng pellet, c
nhiu loi Avicel,
-T dc dnh: to khi do (nh cm, vin): dng
dng rn hay lng ( dnh va phi): dd
HPMC, PVP,
-T dc n, r, to knh KT: Avicel, lactose,
-T dc trn: chng dnh thit b
TS. P T M Hue- 2008

42

4-phng php bo ch
- n v to cu
- Bi dn tng lp (layering)
- Phun sy

4.1-n v to cu
Trn bt kp
DC-TD
To khi do
n si (extrusion)
(Screen Extruder)

Ct on v to cu (spheronization)

Lm kh pellet/ bao

4.2-bi dn

Nhn
Td dnh
lng
Ht m
Bt
Ht bi
Bi
pelle
t
TS. P T M Hue- 2008

45

Pellet ibuprofen TDKD

Ibuprofen

60 g

Avicel PH102

30g

Lactose
HPMC
EC

10g
v
-

Magnesium stearate

Water purified

Phng
php bi
dn