Doko - VN 202070 Ky Thuat Bao Che THUOC MO

K THU T BO CH
THU C M
(OINTMENT)
MC TIU
1. Nm c nh ngha, phn loi thuc m.
2. Phn tch c t dc: Phn loi, u nhc im,
ng dng.
3. Nm c k thut bo ch thuc m: m, kem, gel.
4. Nm c mt s ch tiu cht lng chnh.
5. Nm c SDH v cc cht lm tng hp thu thuc
qua da.
08/27/15
Bien soan: Nguyen Trong Diep
Ni dung
1. i cng
2. Thnh phn
3. K thut sn xut - iu ch
4. Kim tra cht lng
5. Sinh dc hc
08/27/15
PHN I
I CNG
08/27/15
1. nh ngha
Theo DVN III, TM c c im:
- Th cht: Mm.
- ng dng: Da, nim mc.
- Mc ch iu tr:
+ Bo v da.
+ a thuc thm qua da: Gy tc dng ti ch hoc ton thn.
- Bt nho bi da: Dcht rn khng tan trong t dc (>40%).
- Kem bi da: C cu trc kiu nh tng.
2. Phn loi
2.1. Theo th cht v thnh phn cu
to
Loi thuc m
c im
T dc
V d
- Thuc m mm Th cht mm
Thn du, td khan
Benzosali, methyl
salicylat
- Thuc m c
Dcht ko tan trong tdc
Thn du, thn nc
km oxyd
- Sp
Th cht do
Sp, alcol bo cao
Son mi
- Kem
Th cht mm, mn mng
Td nh tng
Deepheat
USP 23: Thuc m, thuc m tra mt, kem, gel, h tr liu qua da
2. Phn loi
2.2. Theo quan im ho l
TM thuc h phn tn ng th:
+ Tn khc: TM 1 pha, TM dng dd.
+ Dcht ho tan trong td thn du hoc thn nc:
vd: TM Methyl salicylat, cao sao vng, gel lidocain..
Thuc m thuc h phn tn d th:

+ Tn khc: TM hai pha.
+ Gm:
TM kiu HD: TM km oxyd.
TM kiu NT: ibuprofen cream, Deepheat cream
TM thuc nhiu h phn tn: Voltaren emugel,
dicloran gel.
2. Phn loi
2.3. Theo mc ch iu tr
TM dng bo v da v nim mc.
Vd: Kem chng nng, chng n, TM Maduxin
TM gy td ti ch: St khun, gim au, chng
vim
Vd: kem Deepheat, kem Mecylat, gel lidocain
TM gy hp thu hoc gy td ton thn: Cha
ni tit t, h huyt p
3. H TR LIU QUA DA
(Transdermal Therapeutic System-TTS)
nh ngha:
L dng thuc hp thu qua da c bit, dng dn vo vng
da ca c th gy c tc dng phng v iu tr bnh.
VD: Thuc dn chng say tu xe, gim au, chng vim, iu tr
co tht mnh vnh, ni tit t
3. H TR LIU QUA DA
Cu to
- Cht nn dnh
- Ct mang dc cht/polymer
- Mng bn thm
Phn loi
- DC gii phng qua mng
- DC k/tn vo ct tr
- DC phn tn trong nn dnh
- DC ha tan trong polyme thn nc
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10
3. H TR LIU QUA DA
u im :
- Trnh cc yu t bt li ca ng tiu ho: pH, men, thc n,
ung...
- Dcht -> h mch, t chc di da -> Trnh chuyn ho qua gan,
khu tr tc dng, hn ch TDKMM.
- Kim sot gii phng dcht: Thch hp vi bnh mn tnh.
- Gim s ln dng.
p dng: Dcht c td mnh, liu < 2mg/ngy, khng gy kch ng da.
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11
4. YU CU I VI THUC M
1. Hn hp ng nht dc & td, dc phi t phn tn cao.
2. Th cht mm, mn mng, khng chy lng T0 thng,
d bm dnh ln da & nim mc.
3. Khng gy kch ng, d ng vi da v nim mc.
4. Bn vng (L, ho, vi sinh)/bo qun.
5. C hiu qu iu tr cao, ng mc tiu, yu cu thit k.
Tu theo mc ch, ni s dng c cc yu cu

ring:Bo
bng.
08/27/15
v, hp thu, h tr liu, bi ln vt thng vt
12
5. CU TRC, NHIM V, CHC NNG SINH L CA DA

CU TRC
Sda = 2m2; 5%kl c th; 1/3 lng mu.

- Lp biu b (Epiderma):
+ Mng cht bo: c td bo v da.
+ Lp sng (Stratum corneum): Hng ro bo
v, ngn cn hp thu thuc, b dy khc nhau.
08/27/15
- Lp Trung b (Cornium): 3-5mm.

+ Gm cc protein thn nc (gelatin,
elastin, reticulin).
+ Cho dc thn nc i qua
- Lp H b (hypoderma): D cho dc thn
du di qua.
13
08/27/15
14
NHIM V, CHC NNG SINH L

Chc nng c hc: lm da do dai,
linh ng
Chc nng bo v:
- Bo v VSV.
- Bo v ho hc.
- Bo v cc tia.
- Bo v nhit v iu chnh nhit.
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15
PHN II
THNH PHN THUC M
08/27/15
16
Cu hi:
1. Thnh phn c bn ca mt dng thuc?
2. Vai tr ca t dc, dung mi trong cc cng thc thuc?
3. Vai tr cc cht ph?
1. DC CHT
c im: Rn, lng, tan hoc khng tan/td.
Arbutin
Mc ch:
Bo v da v nim mc
Gy td ti ch
Gy tc dng ton thn
Ngun gc:
Tng hp, bn tng hp.
Thin nhin
ibuprofen
2. T DC
Vai tr:
- Mi trng phn tn, tip nhn & bo qun thuc.
- Gii phng dc, dn thuc qua da & nim mc: KS tc & mc .
- m bo hiu qu iu tr.
Ch :
- Td khng hon ton tr.
- nh hng n gphng, hp thu v tr liu .
2.1. Yu cu i vi t dc
1. To vi dc thnh hh ng u, dc p/tn u trong td.

2. Ko c td dl ring, Ko cn tr td ca dc.
3. pH trung tnh hoc acid nh. pHda = ?
4. Ko nh hng n chc nng ca da.
5. Gphng dc vi tc v mc mong mun.
6. Bn vng: L, ho, vi sinh.
7. t gy bn da & q/o, d ra sch.
Tu vo m s dng, TM c yu cu ring
2.2.Phn loi t dc
- Thn du: Du m sp v dn cht

- Thn nc: td gel, PEG
PEG
- Khan (Hp ph, nh ho, ht): Lanolin, alcol bo

- Nh tng: td nh ho.
Alcol cetylic
Lanolin sp lng cu
Nhm t dc thn du
Du, m, sp
1. Bn cht: Triglycerid
2. u im
-
D bt dnh v hp thu tt trn da.
Dc cht ha tan v d hp thu.
Thm su.
3. Nhc im
-
Trn nhn, k nc, cn tr h sinh l bnh thng ca da.
Gii phng dc cht chm.
B i kht.
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22
T dc du
1. Tnh cht: th cht lng snh, d b i kht, cn
dng phi hp
2. ng dng:
- iu chnh th cht
- Lm pha du trong nh tng thuc
- Tng tnh thm
3. Cc loi:
- Du ng vt: du c, du iu: c td sinh hc
- Du thc vt: du lc, du thu du
Phng php iu ch du TV?
08/27/15
23
Thnh phn du iu
Emu %
Ostrich %
Nandu %
0.3
0.7
1.0
Palmitic
22.6
15
29.1
Palmitoleic
3.8
3.5
4.1
Stearic
9.8
3.9
7.5
Oleic
49.6
32
32.6
Linoleic
15.4
21.2
21.3
Linolenic
1.1
17.3
2.4
Loi acid
Myristic
Tc dng:
+ Tt cho tim mch thn kinh, chng OXH.

+ Gau, chng vim, cha vt thng, vt bng.
+ T dc tng hp thu thuc qua da.
+ Dng da, xo np nhn
08/27/15
24
M, SP
M ln:
- Tnh cht: Th cht mm, c kh nng nh ha.
- u im: pH trung tnh, du vi da & nim mc, thm su.
- Nhc im: d b i kt.
Sp:
ester ca acid bo cao vi alcol bo cao, alcol thm.
- Tnh cht: th cht do, rn, t b bin cht & i kt, t 0nc cao.
- ng dng: td TM, iu chnh th cht, tng t0nc, tng kh ht.
- Cc loi: Sp ong, lanolin (sp lng cu).
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25
DN CHT CA DU, M, SP
Acid bo:
- Acid stearic: C18H36O2:
+ Th cht rn, bt hoc ht.
+ Td pha du, to cht nh ho x phng kim, iu
chnh th cht.
- Acid oleic: C18H34O2
+ Th cht lng, mu vng.
+ Td pha du, tng hp thu thuc qua da.
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26
DN CHT CA DU, M, SP
Dn cht ca acid bo: p ester ho
- Ester vi glycerol: Khng tan trong nc, th cht rn.
vd: Glycerin momostearat.
- Ester vi polyethylenglycol (PEG): Tan trong nc, th
cht lng.
Glycerin momostearat:
+ Td pha du, cht nh ho cho nh tng N/D.
+ Phi hp vi cht din hot (Tween, Na laurylsulphat)
cho nh tng D/N.
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27
DN CHT CA DU, M, SP
Alcol bo:
- Th cht rn hoc mm, un chy trn u vi cc td thn
du.
- td pha du, iu chnh th cht, tng mn, n nh cho
nh tng, du vi da & nim mc.
- Cht in hnh:
+ Alcol cetylic.
+ Alcol cetostearic.
+ Cholesterol
Hydrocarbon:
+ Vaselin: T0nc = 38-600C.
+ Parafin: rn, lng
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28
V d:
VD 1: t dc thn du
Lanolin
10%
Sp ong
5%
Vaselin
85%
Vd 2: t dc nh ho
Alcol cetylic
26%
Natri laurylsulphat3%
Nc ct
1%
Du parafin
35%
Vaselin
35%
T DC THN NC
Bn cht: Cao phn t c kn ho tan hay trng n/nc & cht
lng phn cc.
u im:
+ Ho tan hoc trn u vi nc v cht lng phn cc -> thn nc.
+ Gii phng dcht nhanh.
+ Th cht tng i n nh.
+ Khng cn tr hot ng SL bnh thng ca da.
+ Khng trn nhn, d ra sch.
Nhc im:
+ D b vk, nm mc gy hng -> cn thm cht bo qun.
+ D b kh cng.
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T DC THN NC
1. Dn cht cellulose
MC
Na CMC
c im
- Trng n trong nc to gel.
Cc cht hay dng:
- Bn vng vi nhit, pH.
MC; CMC, Na.CMC; HPMC
- D b nhim khun.
Ch : Nng s dng.
- Tng k vi mt s hot cht.

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31
T DC THN NC
2. Gel carbomer (carbopol)
Bn cht: Sn phm trng hp ca acid
acrylic.
c im: Trng n/nc to gel, pH
acid, thng c trung ho vi cc kim
-> d/chnh pH, tng nht.
Cht hay dng: carbopol 934, 940.
08/27/15
Use
Concentration (%)
Emulsifying agent
0.10.5
Gelling agent
0.52.0
Suspending agent
0.51.0
Tablet binder
5.010.0
32
T DC THN NC
3. PEG (macrogol, carbowax)
Bn cht: Sn phm trng hp
ca ethylen oxyd.
c im:
+ Tng tan & tc ho tan cho nhiu
dcht t tan.
+ Bn vng, c td st khun nh.
+ Thm qua da km.
+ Thng dng phi hp.
+ Ch tng k
08/27/15
Grade
Average molecular weight
PEG 200
4.2
190210
PEG 300
6.4
285315
PEG 400
8.7
380420
PEG 900
15.3
855900
PEG 1000
22.3
9501 050
PEG 2000
40.050.0
1 8002 200
PEG 3000
60.075.0
2 7003 300
PEG 4000
69.084.0
3 0004 800
PEG 8000
181.4
7 0009 000
lng snh
sp
rn
33
T DC HP PH
c im: Ht nc, clng phn cc -> nh tng N/D
u im:
Nhc im:
+ Kh bn vng, c kh ht.
+ Trn nhn, kh ra sch.
+ Phi hp vi dcht k nc
v thn nc.
+ C th cn tr hot ng SL
bnh thng ca da.
+ Gphng dcht nhanh hn td

thn du.
Vd 3:
+ C kn thm su.
+ Thng phi dng phi hp.
08/27/15
Du parafin 10%.
Lanolin khan 40%
Vaselin
50%
34
T DC NH TNG HON CHNH

c im: L mt nh tng hon chnh (D/N hay N/D)
u im
Nhc im
- Gii phng dc nhanh
- Km bn vng, d tch lp
- C kh nng thm su.
- D b nm mc pht trin.
- Th cht mn mng.
- Kh ra sch (N/D).
- D bm dnh, d ra sch.
Cu hi:
- Cch nhn bit mt nh tng?
- Dc cht phn tn trong pha no ca nh tng? Ti sao?
08/27/15
35
v d 4:
08/27/15
1. Alcol cetylic
17g
2. Vaselin
25g
3. Tween 80
7g
4. Glycerin
15g
5. Nc ct v
100g
36
T DC
Vd 5:
08/27/15
Acid stearic
20g
Triethanolamin
2g
Glycerin
10g
Nc ct v
100g
37
v d 6:
STT
Thnh phn
KL
STT Thnh phn
KL
Natri
diclofenac
1,0g
Span 80
0,6g
Propylen
glycol
12,0g
Tween 80
7,4g
Alcol cetylic
24,0g
Cn paraben 10%
2,0g
Vaselin
8,0g
Nc ct v
100g
Ch phm tng t: Voltarel emugel, Dicloran gel, Osapain cream

08/27/15
38
PHN III
K THUT IU CH - SN XUT
THUC M
08/27/15
39
K THUT IU CH THUC M
Cc phng php:
1. Phng php ho tan -> dng bo ch?
2. Phng php trn u n gin -> dng bo ch?
3. Phng php trn u nh ho -> dng bo ch?
Cn c la chn pp bo ch:
1. Tnh cht ca dc cht v t dc.
2. Dng bo ch: TM mm, kem, gel.
3. Cu trc ca TM to thnh: DD, HD, NT.
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40
1. PHNG PHP HO TAN

a. iu kin p dng:
- DC: Tan trong t dc, ho tan/DM c th trn ln vi td.
- TD: Thn du, thn nc hoc td khan.
-> TM dng dd, thuc h phn tn ng th.
b. Cc giai on chnh:
- Chun b dc.
- Chun b td.
- Phi hp dc vi td.
Ch : La chn thit b, iu kin BC ph hp vi dng thuc.
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1. PHNG PHP HO TAN

Chun b
T dc
Dc cht
Bao b
Ha tan
Thuc m
ng thuc
Tup thuc
Dn nhn, ng gi
Thnh phm
KNSP
S cc g iu ch
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42
1. PHNG PHP HO TAN

Vd 7: Cao sao vng
Menthol
Long no
12,5 g
12,5 g
Tinh du bc h
17,0 ml
Tinh du long no
10,5 ml
Tinh du khuynh dip
5 ml
Tinh du hng nhu
2,5 ml
Tinh du qu
T dc v
100 g
( Vaselin, cerezin, lanolin, sp ong, parafin rn)
08/27/15
43
Vd 8: Bch h hot lc cao (White Tiger Balm):

Menthol
1,6
g
Long no
3,18 g
Tinh du bc h
2,18
g
Long no
3,18 g
Tinh du khuynh dip
0,98
g
Tinh du inh hng
0,4 g
Tinh du qu
0,3
Methyl
salicylat
4,0
g
08/27/15
T dc v
20 g
44
1. PHNG PHP HO TAN

Vd 9: Diclofenac gel 1%
KTBC:
1. Cn, ho tan natri diclofenac vo hn hp dung mi EtOH-PG.
2. Ngm carbomer 934/nc n trng n hon ton.
3. Cho dd dc vo gel carbopol, khuy u.
4. Cho tip triethanolamin vo, khuy u.
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1. PHNG PHP HO TAN

Vd 10: Diclofenac gel 1%
Diclofenac sodium.......................................1 g
Propylene glycol Pharma. .......................20 g
Lutrol F 127 ...........................................20 g
Water............................................................59 g
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46
1. PHNG PHP HO TAN

Vd 11: Betamethasone gel
Betamethasone valerate ..................0.1 g
Ethanol 96% ........................................10.0 g
Propylene glycol Pharma....................15.0 g
Lutrol F 127..........................................20.0 g
Water ...................................................54.0 g
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47
2. PHNG PHP TRN U N GIN

a. iu kin p dng:
- DC: Khng hoc t tan/td, cc dc tng k khng tan/td.
- TD: Thn du, thn nc, td khan, td nh tng.
-> TM thuc h phn tn d th.
b. Cc giai on chnh:
- Chun b dc: Lm bt n, hh bt kp. Ch : mn, ng nht.
- Chun b td:
- Phi hp dc vi td:
+ Lm TM c.
+ Phi hp TM c vi t dc cn li.
+ Lm ng nht.
+ ng gi, dn nhn.
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Chun b
Dc cht
Lm m c
T dc
Bao b
M c
Phi hp td
Thuc m
Cn ng nht
TM ng nht
ng tup
ng hp
KNSP
Tup
Thnh phm
S cc g bo ch
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49
Vd 12: TM benzosali
Cng thc cho 20g:
T dc nh ho 20g:
Sp nh ho 10.4g:
08/27/15
Acid benzoic
1.2g
Acid salicylic
0.6g
T dc nh ho v
20g
Sp nh ho
6g
Du parafin
7g
Vaselin
7g
Alcol cetostearylic
9g
Natri laurylsulphat
1g
Nc ct
0.4g
50
Vd 13: TM km oxyd:
Km oxyd
3g
Lanolin
12g
Vaselin85g
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51
3. PHNG PHP TRN U NH HO

a. iu kin p dng:
-
DC CHT:
+ Lng phn cc, bn phn cc, khng tan v kh trn u vi td.
Vd: dd ng, km sulphat
+ Rn, mm ho tan/dm tr phn cc: Nc, gl, pg
Vd: cao thuc, dd thuc, khng sinh dng mui
+ Dc rn ch pht huy td di dng dd nc nh: iod, bc keo
T DC: nhm td khan.
TM kiu NT N/D, thuc h phn tn d th.

08/27/15
52

b. KTBC
- Tu theo tcht dc -> KTBC thch hp.
- Ch :
+ Dc lng cn thm t t vo td khan, trn u.
+ Td rn cn ho tan vi dm ti thiu thch hp.
+ Cc cao thuc (cao mm, cao kh) cn ho tan nng vi dm
thch hp.
+ Nu l hh cc dc cn phi hp tng phn phn tu theo tnh
cht dc & td.
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53

Chun b
T dc khan
Dd dc cht
Bao b
Phi hp
Thuc m
ng tup
Tup thuc
ng hp
KNSP
Thnh phm
S cc g bo ch
08/27/15
54

Vd 14: TM dalibuor
ng sulfat
Km sulfat
Nc ct
Lanolin khan
Vaselin
08/27/15
0,3 g
0,5 g
30 ml
50 g
100 g
55

Vd 15: Thuc m iu tr
bng
Cao c c lo
5g
Cao l hi (5:1)
10g
Nc ct
10g
Cht bo qun
Lanolin
30g
Vaselin
40g
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56
4. PHNG PHP NH HO TRC TIP

a. iu kin p dng:
- DC: rn, mm, lng htan trong tng du hoc tng nc ca NT
- TD: Cc nh tng hon chnh.
- TM kiu NT D/N, thuc h phn tn d th.
08/27/15
57
b. Cc giai on
+ Ho tan cc DC, cht nh ho, cht ph trong pha
du hoc pha nc, tu theo tnh cht ca dc cht.
+ un nng pha du khong 65-700C, pha nc cao
hn pha du khong 3-50C.
+ Cho pha du vo pha nc, khuy trn trong thit
b thch hp n ngui thu c cream ng nht.
+ ng gi, dn nhn.
+ Kim nghim thnh phm.
+ Nhp kho.
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58
S cc g bo ch
Dc cht v cc cht
ph ho tan trong
Pha nc
un nng 70-750c
Pha du
un nng 65700c
Khuy trn
ng nht ho
ng tup
ng gi
08/27/15
Kim nghim thnh

phm
59
Vd 16: kem natri diclofenac 1%
08/27/15
Natri diclofenac
1,0g
Propylen glycol
10,0g
Alcol cetylic
20,0g
Vaselin
4,0g
Acid stearic
4,0g
Span 80
0,6g
Tween 80
5,4g
Cn paraben 10%
2,0g
Nc ct va
100g
60
Vd 17: kem Chloramphenicol 1%

Chloramphenicol
1,0g
Propylen glycol
10,0g
Alcol cetylic
8,0g
Acid stearic
8,0g
Du parafin
6,0g
Cn paraben 10%
2ml
Triethanolamin
4,0g
Nc tinh khit v
100g
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61
Vd 18: Miconazole Cream (2%)

I.
Cetylstearyl alcohol.................7.0 g
Cremophor A 6 [1] .................1.5 g
Cremophor A 25 [1] ...............1.5 g
Liquid paraffin .....................12.0 g
Parabene(s).........................0.1 g
II. Water ..............................67.8 g
III. Propylene glycol [1] ................8.0 g
Micronazole nitrate ................2.0 g
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62
Vd 19: Ketoconazol Cream (2%)

Ketoconazol bt mn
2,0g
Propylene glycol
20,0g
Alcol cetostearylic
10,0g
Span 60
2,0g
Tween 60
1,5g
Isoprpyl myristat
1,0g
Natri sulfit khan
0,2g
Tween 80
0,1g
Nc ct va
100g
08/27/15
63
Vd 20
Australian Emu Oil
Cream
Thnh phn
08/27/15
10
Tocopherol acetate
55.35
11
Fragrance
% kl/kl
0.1
vua du
Deinonised water
Stearic acid
12
Phenoxyethanol
0.5
Cetearyl Alcohol
13
Methyl paraban
0.1
Mineral Oil
14
Ethyl paraben
0.1
Sorbitol
15
Butyl paraben
0.05
Emu oil
20
16
Isobutyl paraben
0.05
Lanolin oil
17
Propyl paraben
0.1
Carbomer
0.1
18
Disodium EDTA
0.05
Triethanolamine
0.5
64
Vd 21: ALOE VERA NIGHT CREAM

% kl/kl
Qs 100
0.075
3.50
2.00
2.00
4.00
2.00
0.70
1.00
7.00
3.00
3.00
1.00
0.10
0.20
08/27/15
Phase A:
Water
Tetrasodium EDTA
Propylene Glycol
Phase B:
Cetyl Alcohol (Ado1 52 NF)
Cetearyl Alcohol (and) Polysorbate 60
Stearic Acid (Emersol 132)
Polysorbate-40
Sorbitan Palmitate
Mineral Oil (and) Lanolin Alcohol (Ritachol)
Mineral Oil
Aloe Vera Oil
Petrolatum (and) Lanolin (and) Dimethicone 200
BHA
Propylparaben
Phase C
Aloe Vera Gel
65
5. DNG C & THIT B

- Quy m PTN: chy ci, my nh kem.
- Quy m cng nghip: dng cc my.
Thit b nh kem kiu khuy trn qui m PTN

08/27/15
66
5. DNG C & THIT B
H thng Kalwerka
08/27/15
67
5. DNG C & THIT B
Thit b nh ho cao tc qui m CN

08/27/15
68
5. DNG C & THIT B
Thit b nh ho cao tc qui m CN

08/27/15
69
5. DNG C & THIT B

LABSONIC
Ultrasonic homogenizers for every application
Thit b nh ho bng sng siu m lm nh tng, kem thuc

08/27/15
70
5. DNG C & THIT B
Thit b ng tup & hn tup
08/27/15
71
Bao b & sn phm
08/27/15
72
PHN IV
KIM TRA CHT LNG &

SINH DC HC THUC M
08/27/15
73
KIM TRA CHT LNG THUC M

1. KIM TRA TNH CHT VT L CA TM & TD
ng nht ca thuc m:
Theo pp ca DVN III, PL 14.
Xc nh im nh git.
Xc nh im ng c.
Xc nh ch s nc ca t dc.
08/27/15
74
2. KIM TRA TNH CHT LU BIN CA TM

1. Xc nh nht.
2. Xc nh th cht:
- Xc nh bng my o xuyn su.
- Xc nh dn mng ca TM.
- Xc nh dnh ca TM.
3. Xc nh kh nng gii phng hot cht.
08/27/15
75
PP XC NH KN GII PHNG THUC

1.PP khuych tn gel
2.PP khuych tn qua mng:
- Mng thng dng:
+ Mng nhn to: Celophan, dn cht cellulose, silicon
+ Mng t nhin: da chut, da ln, da th, da ngi cht...
- MT ktn: Nc ct, dd m, hh dung mi...
- Dng c: M hnh bnh Franz.
- nh gi kq: o mc , tc thm ca thuc qua mng.
08/27/15
76
THIT B KHUYCH TN QUA MNG
08/27/15
77
Thit b o khuych tn thuc qua mng
08/27/15
78
08/27/15
79
Thit b o khuych tn thuc qua

mng
08/27/15
80
Thit b o khuych tn thuc qua

mng
08/27/15
81
SINH DC HC THUC M
Khi nim sinh dc hc ?
YU T SINH HC
YU T DC HC
QT HP THU DCHT/DNG THUC
C TH
NNG CAO HIU QU IU TR
08/27/15
82
NG HP THU THUC
Dc cht hp thu ch yu qua:
1. Qua biu b:
+ Qua khe ca cc tb.
+ Xuyn trc tip qua tb.
2. Qua TG cc b phn ph: L chn
lng, tuyn m hi, tuyn b nhn
CC GIAI ON HP THU THUC

QT hp thu thuc qua cc g sau:
1. DC gii phng khi td (ct t dc).
2. DC thm qua lp biu b.
3. DC xuyn thm qua cc lp tip theo
ca da.
4. DC hp thu vo h mch.
08/27/15
83
Tc hp thu dc cht qua da c xc

nh bi:
1. Tc gii phng DC ra khi td hoc ct
td.
2. Tc thm ca thuc qua lp biu b.
3. Tc xuyn thm ca thuc qua cc lp
ca da.
C
ch:
ktnhp
th ng
thun
theo
l Fick.
4. Tc
thu vo
h
mch
ca c th.
V=
D.K.S.c
Js ADKCv
h
V: Tc ktn;
D: Hs ktn.
K: Hs phn b;
c: Chnh lch nng
x: B dy mng.
08/27/15
84
CC YU T NH HNG
1. Cc yu t sinh l:
- nh hng ca nhit & knng gin mch ca da.
- nh hng ca mc hydrat lp sng.
2. nh hng ca cc yu t cng thc, k thut.
- nh hng ca dcht: tan, HSKT, HSPB, pH, ion ho,
Cthuc, cc dn cht.
- nh hng ca td.
- nh hng ca cc cht lm tng hp thu.
08/27/15
85
nh hng ca vng da n hp
thu hydrocortison
08/27/15
86
nh hng ca tui n hp thu thuc

% thuc hp thu sau 7 ngy
Permeant
Testosterone
Estradiol
Hydrocortisone
Benzoic acid
Acetylsalicylic acid
Caffeine
log Ka
2240
3.32 19.0 4.4
2.49 7.1 1.1
1.61 1.5 0.6
1.83 36.2 4.6
1.26 31.2 7.3
0.01 48.2 4.1
yr
>65 yr
16.6 2.5
5.4 0.4
0.54 0.15
19.5 1.6
13.6 1.9
25.2 4.8
Thnh phn (4 mg/cm2) pha trong 20 mL acetone bi vo pha

trong cng tay (n= 38), theo pp ca Roskos et al. (1989).
08/27/15
87
PHN LOI THEO SINH DC HC
Nhm
tan
Tnh
thm
tt
tt
Doxycyclin HCl,
Fluconazol...
II
km
tt
Ibuprofen, griseofulvin...
III
tt
km
Acyclovir, aspirin...
IV
km
km
Furosemid, Ritonavir,
Saquinavir...
08/27/15
V d
88
nh hng ca tnh cht ti mc gii phng v

thm qua da ca mt s NSAID
Dc cht
HSPB
(p)
tan/nc
(g/ml)
tan/m
(g/ml)
Indomethacin
57,1
11
1010
Ketoprofen
5,2
294
8900
Diclofenac
116,9
3,5
1130
Piroxicam
5,3
53,3
110
Tenoxicam
0,4
61,9
880
Ketorolac
0,9
183
6890
Aceclofenac
6,2
32
8300
08/27/15
89
nghin cu nh hng ca mt s dn cht

ti tnh thm qua da ca acid salicylic
08/27/15
Hp cht
Flux
(nm/cm2.h-1)
Lag time
(h)
T l % DC thm
qua da
Acid salicylic
143
3,5
95,8
Butyl salicylat
86
1,7
64,8
Salicylamid
105
2,0
79,0
Dimethylamin
salicylat
51
5,0
79,0
90
bin php ci thin tan, tnh thm Ca dc cht
1) Lm gim kch thc tiu phn DC rn (microsize, ultramicrosize)
2) S dng hn hp dung mi, v d: propylen glycol, PEG,

DMA, DMF, DMSO, transcutol, 2-pyrolidon..
3) S dng cht din hot: acid v mui mt, din hot ion
ho (natri laurylsulfat, benzalkonium clorid..), khng ion ho
(tween, cremophor...)
4) Ch to h phn tn rn (solid dispersion system)
08/27/15
91
Cc cht lm tng hp thu

C ch tng hp thu theo Bary & CS:
- Ph v hng ro bo v ca lp sng.
- Tng tc vi cc protein t bo.
- Lm tng phn b ca dcht hoc dmi
trong lp sng.
08/27/15
92

STT
Nhm cht
Cht in hinh
Sulfoxid
Dimethylsulfoxid (DMSO), decylmethylsulfoxid
Alcol
- Alkanol: Ethanol, isopropanol, butanol,

pentanol, alcol benzylic, decanol
- Alcol bo: Caprylic, lauric, cetylic, stearilic
Acid bo
- Mch thng: Oleic, linoleic, linolenic,

myristic
- Mch nhnh: Isovaleric, neodecanoic
Ester ca acid Isopropyl myristat(IPM), isopropyl palmitat,

bo
ethyl acetat
Polyol
Propylen glycol, polyethylen glycol, ethylen

glycol, diethylen glycol
Amid
- Ure, dimethyl acetamid (DMA), dimethyl

formamid (DMF)
- Dn cht ca pyrolidon, cc amid vng
- Amin kim: monoethanolamin,
diethanolamin, triethanolamin
08/27/15
93

STT
Nhm cht
Cht in hinh
Cht din hot
- Anion: Natri laurat, natri laurylsulphat

-Cation: Benzalkonium clorid, cetyltrimethyl
amoni bromid
- Khng ion ho: Tween (20, 40, 60, 80), Span
(20, 40, 60, 80), polyxamer
- Mui mt: natri clorat, natri taurocholat
- Lecithin
Terpen
d-limonen,
-pinen,
-terpeneol,
carvrol,
menthol, limonen
Tinh du khuynh dip, tinh du bc h
Alkan
n-heptan, n-octan
10
Acid hu c
Acid citric, succinic, acid salicylic
11
Cyclodextrin
-CyD, -CyD, CyD, HP-CyD, M-CyD, DM(CyD) v dn CyD
cht
08/27/15
94
nh hng ca td n hp thu diclofenac

Thnh phn
Cng thc
DD
M3
M4
M5
M6
Natri diclofenac
Transcutol
19
19
59,2
59,2
59,2
m pH 7,4
80
Plutrol oleique
19,5
Nc
19,9
19,9
19,9
Isostearyl isostearat
Labrasol
Acid oleic
14,9
19,9
d-Limonene
5,0
Acid lauric
19,9
08/27/15
95
TI LIU THAM KHO

DVN III, Dc th QG.
TS. Hong Ngc Hng, T dc v cc cht ph gia NXB YHc
Handbook of Pharmaceutical excipients
Martindale
The merck Index
http://en.wikipedia.org
http://www.dav.gov.vn Cc QL dc Vn
08/27/15
96
Cm n s theo di &
lng nghe !
Chc cc bn
thnh cng !
08/27/15
97

Doko - VN 202070 Ky Thuat Bao Che THUOC MO

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K THU T BO CH

Bien soan: Nguyen Trong Diep

Bien soan: Nguyen Trong Diep

Bien soan: Nguyen Trong Diep

Thn du, td khan

Dcht ko tan trong tdc

Thn du, thn nc

Sp, alcol bo cao

Th cht mm, mn mng

Thuc m thuc h phn tn d th:

Bien soan: Nguyen Trong Diep

Bien soan: Nguyen Trong Diep

Tu theo mc ch, ni s dng c cc yu cu

v, hp thu, h tr liu, bi ln vt thng vt

Bien soan: Nguyen Trong Diep

5. CU TRC, NHIM V, CHC NNG SINH L CA DA

Sda = 2m2; 5%kl c th; 1/3 lng mu.

- Lp Trung b (Cornium): 3-5mm.

Bien soan: Nguyen Trong Diep

Bien soan: Nguyen Trong Diep

NHIM V, CHC NNG SINH L

Bien soan: Nguyen Trong Diep

THNH PHN THUC M

Bien soan: Nguyen Trong Diep

1. To vi dc thnh hh ng u, dc p/tn u trong td.

- Thn du: Du m sp v dn cht

- Khan (Hp ph, nh ho, ht): Lanolin, alcol bo

D bt dnh v hp thu tt trn da.

Dc cht ha tan v d hp thu.

Trn nhn, k nc, cn tr h sinh l bnh thng ca da.

Gii phng dc cht chm.

Bien soan: Nguyen Trong Diep

Bien soan: Nguyen Trong Diep

+ Tt cho tim mch thn kinh, chng OXH.

Bien soan: Nguyen Trong Diep

ester ca acid bo cao vi alcol bo cao, alcol thm.

Bien soan: Nguyen Trong Diep

Bien soan: Nguyen Trong Diep

Bien soan: Nguyen Trong Diep

Bien soan: Nguyen Trong Diep

Bien soan: Nguyen Trong Diep

Cc cht hay dng:

- Bn vng vi nhit, pH.

MC; CMC, Na.CMC; HPMC

- Tng k vi mt s hot cht.

Bien soan: Nguyen Trong Diep

Bien soan: Nguyen Trong Diep

Average molecular weight

Bien soan: Nguyen Trong Diep

+ Trn nhn, kh ra sch.

+ Gphng dcht nhanh hn td

+ Thng phi dng phi hp.

Bien soan: Nguyen Trong Diep

T DC NH TNG HON CHNH

- Gii phng dc nhanh

- C kh nng thm su.

Bien soan: Nguyen Trong Diep

Bien soan: Nguyen Trong Diep

Bien soan: Nguyen Trong Diep

STT Thnh phn

Ch phm tng t: Voltarel emugel, Dicloran gel, Osapain cream

Bien soan: Nguyen Trong Diep

Bien soan: Nguyen Trong Diep