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VIN NN
MC TIU HC TP
1. Trnh by c vai tr, c ch tc dng v xu hng nh hng ti kh nng
gii phng dc cht ca 5 nhm t dc: n, dnh, r, trn, bao.
2. Nu c u nhc im v cch dng ca cc t dc c th thuc 5 nhm
ni trn.
3. La chn c t dc cho mt cng thc vin nn.
4. Vit c quy trnh bo ch vin nn theo 3 phng php: dp vin qua to
ht t, to ht kh v dp thng.
5. Nu c mc ch bao vin v cc phng php bao.
6. Trnh by c tiu chun cht lng vin nn v cch nh gi.
7. Trnh by c cc yu t nh hng n sinh kh dng vin nn v bin
php nng cao sinh kh dng.
I. I CNG
1. V tr vin nn
Xem nh ngha vin nn trong SGK v DVN IV.
2. Phn loi vin nn
Theo phng php sn xut:
+ Vin nn dp thng
+ Vin nn dp qua to ht: t, kh
Theo hnh thc bn ngoi:
+ Vin nn trn
+ Vin nn bao: ng, film
Theo cch s dng:
+ Vin nut, ngm cy, t, pha dung dch, hn dch...
3. u - nhc im ca vin nn: SGK
Vin nn l dng bo ch ph bin nht: ti sao?
Vin nn cng l dng bo ch c nhiu vn v sinh kh dng nht: ti sao?
II. K THUT BO CH VIN NN
1. La chn t dc xy dng cng thc dp vin
- Cc yu t cn xem xt?
- Yu cu chung ca t dc vin nn?
i vi mi t dc cn ch :
- Ngun gc, bn cht l, ho hc
- Tnh cht
- Cch s dng
- n nh
- Tng k vi cc thnh phn khc
- an ton
- Gi thnh
- nh hng ca t dc n c tnh vin nn, SKD v n nh ca
vin.
1.1. T dc n (fillers, diluents)
1.1.1. Nhm t dc n tan c trong nc
- Lactose
Manitol
Sorbitol
Bt ng (saccarose)
Emdex v Celutab: tinh bt thu phn (90 92% dextrose, 3 5%
maltose), trn chy tt, d ht m, phn ng vi cc cht c nhm amino.
Thng dng cho vin nhai (do c v ngt).
- Dextrates USP (Emdex): 93 99% dextrose. Vin nn cha dextrates tng
lc gy v vin sau vi gi sn xut nhng sau khng tng. Tng k:
cht cha nhm amino, tc nhn oxy ho.
- Inositol: hay dng cho vin nhai.
1.1.2. Nhm t dc n khng tan trong nc
- Tinh bt
- Dextrin
- Tinh bt bin tnh (cc loi...)
- Cellulose bt
- Cellulose vi tinh th (Avicel, Emcocel, Vivacel)
- Calci carbonat, magnesi carbonat
- Cc mui calci phosphat
Nng trong
cng thc vin (%)
25
15
15
25
2 25
5 20
25
15
2 25
2 10
1 10
14
2 5
MC
NaCMC ( nht thp)
EC
PVA
PEG 6000
Cch s dng ca mt s t dc r
T dc r
Tinh bt, USP
Starch 1500
Avicel PH 101, PH 102
Solka floc (cellulose g tinh ch)
Acid alginic
Explotab (sodium starch glycolate)
Gm guar
Polyclar AT (PVP, crosslinked PVP)
Amberlite IPR 88 (nha trao ion)
MC, Na CMC, HPMC
1.4. T dc trn
T dc trn c th chia lm 3 loi theo 3 cch tc dng:
- Cc cht lm gim ma st (lubricants): gim ma st gia ht v thnh ci.
Chy lm cn lc nn cao hn v nhiu t dc trn hn. Kch thc ht cng nh
cn cng nhiu t dc trn. Dng khng qu 1%.
- Cc cht chng dnh (antiadherents): chng dnh chy ci.
- Cc cht ci thin kh nng trn chy (glidants): ci thin kh nng trn chy
ca ht.
Nhng vn cn xem xt khi la chn t dc trn:
- Nhiu t dc trn c bn cht s nc, c th lm chm qu trnh thm
nc vo vin v lm gim r v ho tan dc cht.
- TD trn c th lm gim c tnh lin kt ca nhiu TD.
- Thi gian trn TD trn thng khng qu 10 pht.
- Cn xc nh lng TD trn ti u cho mi cng thc.
- TD trn phi c ry qua ry 125 180 m trc khi trn vo ht.
Vai tr ca t dc trn?
Cc cht lm gim ma st khng tan trong nc
T dc
Cc stearat (Mg, Ca, Na)
Acid stearic
Du thc vt hydrogen ho (Stearotex, Duratex)
Talc
Sp
Stearowet C (Ca stearat + Na lauryl sulfat)
Du khong nh
Tinh bt
T dc
Talc
Tinh bt ng
Cab-O-Sil
Syloid
DL Leucine
Na v Mg lauryl sulfat
Acid stearic, bt mn
Stearat
Stearowet C
Du hydrogen ho (Stearotex, Duratex)
Du khong nh
Natri benzoat
Natri clorid
PEG 4000 v 6000, bt mn
Bi tp p dng:
La chon t dc thch hp cho cc vin nn sau:
1.
Vin nn paracetamol 325 mg
2.
Vin nn vitamin C 100 mg
3.
Vin nn vitamin B1 10 mg
4.
Vin bao tan rut aspirin 100 mg
5.
Vin nn ampicilin 250 mg
6.
Vin pha hn dch Co - trimoxazol
2. Dp vin
- Cc giai on chnh trong qu trnh dp vin? Cc thng s cn kim sot
trong tng giai on? Cc thng s ny nh hng nh th no n cht lng
thnh phm?
- So snh u nhc im ca ba phng php dp thng, dp vin qua to ht
kh, dp vin qua to ht t v cc mt: kh nng chu nn, trn chy,
phn b kch thc ht dp vin, cht lng vin lng ca vin, phm vi p
dng, thit b s dng, t dc s dng.
- Nu mc ch to ht, cc giai on chnh ca hai phng php to ht.
- Cc kh khn khi dp vin v bin php khc phc? (Vin b bong mt, st
cnh, dnh chy ci, kh nh vin, mt vin khng bng, khng ng u khi
lng, c bn c hc thp, khng t r, ho tan...).
Bi tp p dng:
C th dng nhng phng php no bo ch cc vin nn sau? u nhc
im khi p dng cc phng php :
1. Vin nn paracetamol 0,325 g
2. Vin nn aspirin 0,5 g
3. Vin nn vitamin C 0,5 g
Dch bao nn
Bt bao nn
175 g
52,5 g
840 ml
v 1750 ml
60 g
60 g
1500 g
1000 ml
4,1 kg
0,12 kg
1,35 kg
0,23 kg
v
22,7 kg
136 kg
76 kg
0,09 kg
0,09 kg
0,02 kg
3,785 l
Sy kh vin.
Thit b: ni bao thng, ni bao ci tin, my tng si.
Kh khn khi bao vin:
Vin b dnh: xem li tc phun dch, tc sy kh, cng thc dch bao.
Mng bao b bong: dch bao khng lan rng trc khi sy kh do sy kh qu
nhanh hay nht dch bao cao Cn pha long dch bao.
- Mng bao x x: phun thnh git, nng polymer, cht rn cao.
- m vin, khng u mu.
- Mng bao b rch, nt, co ko: thm hoc thay i cht lm do.
- Mng bao m: nhit qu cao lm bin tnh polymer.
- Khuyt tt g: vin c g, mi mn cao, mng bao gin.
Mt s cng thc dch bao: phn tch vai tr ca cc thnh phn trong cng
thc? Nu cch pha ch v cch s dng dch bao ny bao vin?
1. CT 1:
HPMC 2910, USP, 15 cps
4%
Propylen glycol
1,2 %
Ethanol
45 %
Methylen clorid
v
100 %
2. CT2:
Eudragit E100
30 g
Talc
42 g
Magnesi stearat
6g
Titan dioxyd
18 g
Amaranth E 123
1g
PEG 6000
6g
Tween 80
2g
Nc
200 g
Isopropanol
700 g
Aceton
480 g
3. CT 3:
Eudragit L 100
30 g
Dibuthyl phtalat
3g
Talc
42 g
Magnesi stearat
6g
Yellow lake E 104
18 g
PEG 6000
6g
Isopropanol
900 g
Nc
12 g
Aceton
480 g
4. CT 4:
CAP
12 %
Propylen glycol
3%
Sorbitan monooleat
1%
Ethanol
45 %
Aceton
v
100 %
5. CT 5:
Cng thc Aquacoat:
Tng lng cht rn
29 32 %
Ethylcellulose
24,5 29,5 %
Natri lauryl sulfat
0,9 1,7 %
Alcol cetylic
1,7 3,3 %
pH
4,0 7,0
nht
150 cP
Kim loi nng
10 ppm
Tng s vi khun hiu kh
100 cfu/g
Tng s nm men v mc
20 cfu/g
S dng Aquacoat bao vin:
Aquacoat
450,00 g
Dibuthyl sebacat
33,48 g
Dung dch HPMC E-5 14%
132,71 g
Nc
149,97 g
6. CT 6:
Eudragit L 100-55
12,5 %
PEG 6000
1,0 %
Triethyl citrat
1,2 %
Talc
3,1 %
Titan dioxyd
2,1 %
Nc
79,9 %
Natri hydroxyd
0,2 %
7. CT7:
Cellulose acetat phthalat
6,00 %
Propylen glycol
1,86 %
Sorbitan monooleat (Span 80)
0,66 %
Du thu du (khng mi)
0,12 %
FD&C Blue Dye No.1
0,85%
FD&C Yellow Dye No. 5 lake
3,11%
Titan dioxyd
5,33%
Methylen clorid
21,58 %
Aceton
va
100 %
8. CT8:
Hydroxy propyl methyl cellulose 2910 (15 cps)
4,5%
Hydroxy propyl cellulose
0,5%
Titan dioxyd
2%
Propylen glycol
2%
Ethanol
45%
Methylen clorid
v 100%
Lactose monohydrat
55,23 mg
Pregelatinized starch (Starch 1500)
15,00 mg
Butyl hydroxy anisol
0,02 mg
Acid ascorbic
2,50 mg
Acid citric
1,25 mg
Cellulose vi tinh th (Avicel PH 102)
15,00 mg
Magnesi stearat
0,60 mg
Colloidal silicon dioxide (Aerosil 200)
0,30 mg
Nc tinh khit
12,00 mg
Ethanol tuyt i
5,00 mg
7. Vin nn amoxicilin trihydrat v kali clavulanat
Amoxicilin trihydrat (compacted)
587,50 mg 500 mg amoxicilin khan
Hn hp kali clavilanat v Avicel (1:1) 305,00 mg 125,00 mg clavulanat
Sodium starch glycolate
25,00 mg
Aerosil 200
30,00 mg
Sodium carmellose
10,00 mg
Talc
10,00 mg
Magnesi stearat
5,00 mg
Bao vin bng dung dch HPMC trong dung mi hu c.
8. Vin nn acid ascorbic
Acid ascorbic
250 mg
Explotab
15 mg
Dung dch EC (50 cps) 10% trong ethanol v ( 4 mg)
Calci silicat
10 mg
9. Vin nn hydroclorothiazid
Hydroclorothiazid
50 mg
Lactose monohydrat
422 mg
Kollidon 90 F
8 mg
Isopropanol
0,038 ml
Kollidon CL
15 mg
Magnesi stearat
2 mg
10. Vin nn meprobamat
Meprobamat
400,0 mg
Tinh bt ng
100,0 mg
PVP K-25
15,0 mg
PEG 400
4,5 mg
Isopropanol
va
Talc
2,0 mg
Aerosil 200
0,2 mg
Calcium arachinat
0,3 mg
11. Vin si paracetamol
Paracetamol, KTTP < 300 m
500 mg
Natri hydrocarbonat
500 mg
Acid tartaric, bt mn
430 mg
Dextrose
200 mg
Cht thm
va
PVP K30
20 mg
Isopropanol
0,1 ml
Polyethylen glycol 6000, bt mn
60 mg
12. Vin nn amoxiclin kali clavulanat
Amoxicilin trihydrat
Hn hp kali clavulanat : Avicel (1:1)
587,5 mg
( 500,0 mg amoxicilin khan)
305,0 mg
( 125,0 mg acid clavulanic)
25,0 mg
30,0 mg
10,0 mg
10,0 mg
5,0 mg
Magnesi stearat
Nc tinh khit
VI. MT S VIN NN C BIT
T c SGK
0,6 mg
va