26 research outputs found
Bahan Baku Fraksi Diterpen Lakton Herba Sambiloto sebagai Antimalaria
Sambiloto adalah lanaman yang banyak ditemukan di Indonesia. Sambiloto dikelahui memiliki kandungan beragam senyawa diterpen lakton terutama andrografolida dan senyawa flavonoj-d. Andrografolida merupakan senyawa diterpen lakton yang diketahui mempunyai banyak aktivitas yang telah ditunjukkan dan dibuktikan bahwa andrografolida menghambat pertumbuhan P. berghei secara in vivo dan P,falciparun secara jn vitro dengan mekanisme penghambatan pada stadi.um skizon dan gametosit. Sedangkan sambiloto telah lama dimanfaatkan sebagai bahan ramuan obat traditionat untuk mengobati berbagai penyakit termasuk malaria. para penemu dari invensi ini telah menemukan bahwa Fraksi DTL herba sambiloto dapat dijadikan sediaan obat, untuk menqobati penyakit malaria
The Development of tablet formulation of Artocarpus champeden Stembark extract as antimalarial drug
Parasite resistance to antimalarial drug, chloroquine and sulfadoxin-pirimetamin, still
e major problem in malaria control worldwide, thereforc, the cffort in developing a new
targct of antimalarial drug become a high priority. Our preliminary test revealed that
fuom A. chanpeden exhibiedt potent antimalarial activities againts P. lalciparum in vitro
brghci in vivo. Several isolaEd compounds from this plant exhibited antimalarial activity
drc isotated compound identified as hetcroflavon C, a prenylated flavooe, have a higher
activity than chloroquine. Therefore, it is potential to be developed as antimalarial
rcscarch was conducted to develop tablet formulation of ethanol extract of A.
stcmbark (EEAC). The formula that composed: EEAC 150 mg, lactose 140 mg, cabarnilum
46 mg, avicel PH l0l 79o, primogcl 57o, and Mg stcarat 1% was the selected
Th€ tablet hardness o[ the formula has span betwccn 9.0-12.27 kP and the averagc is
,
thc disintegration time of formula 12 minutcs 4? seconds. A standard fiays test oll P.
infected mice was used to evaluated in vrv, antimalarial activity of the tablet. This
rlvcalcd that EEAC tablet has antimalarial activity against parasite P. berghei in vivo.
ration ofEEAC tablet at a dose of 10 mg/kg body weight multiple dose (twice a day)
thc parasite growth better than 100 mg/kg body weight single dose (once a day)
activity of tablet in multiple dose pcr oral shqwed inhibition of parasite growth of
while at single dose per oral showed inhibition of parasite growth of 83.32
Dissolution Enhancement of Gendarusin A by Poloxamer 188 Addition in Justicia gendarussa Burm. f Ethanolic Extract Granule Matrix
Justicia gendarussa Burm. f (Acanthaceae) is often used as folk medicine for many purposes in Indonesian indigenous tribes. Preclinical studies on J. gendarussa leaves indicated that the extract possessed the activity of male contraception. Gendarusin A was found to be the compound responsible for the activity. The purpose of this study was to prove that poloxamer 188 can increase the dissolution rate of gendarusin A in Justicia gendarussa Burm. f ethanolic extract granule (JEG) matrix, in an effort to find male contraceptives phytopharmaceutical product. In this research, we had made three JEG matrix types, which were type 1 (without the addition of surfactant poloxamer 188); type 2 (with the addition of 1% surfactant poloxamer 188), and type 3 (with the addition of 2% surfactant poloxamer 188). The three types of JEG matrix then examined by dissolution test to obtain the dissolution rate of gendarusin A. HPLC instrument was utilized to analyse the concentration of gendarusin A from dissolution mediums. The results showed that the gendarusin A in JEG matrix type 3 dissolved much faster compared to JEG matrix type 1 and type 2. The score of dissolution efficiencies of gendarusin A in JEG matrix type 1, type 2, and type 3 were 15,72%; 24,22%; and 31,83% respectively. It can be concluded that poloxamer 188 addition can increase the dissolution rate of gendarusin A in JEG matrix
In vivo antimalarial activity of Andrographis paniculata Tablets
The formulation of three phytopharmaceutical products of Andrographispaniculata fractions (AP fraction A and B) containing diterpene lactones as an active substance were developed and their antimalarial activities against Plasmodium bergheihas been examined. In vivo antimalarial assay on P. berghei infected mice was carried out by oral administration,twice a dayfor four consecutive days of the AP fractions product, which were Tablet I: wet granulated formula of AP fraction A; Tablet II: wet granulated formula of AP fraction B; Tablet III: solid dispersion formula of AP fraction B.. The results revealed that three phytopharmaceutical products of A.paniculata were inhibited parasite's growth with inhibition range of 70.15% to 80.35%. There was no significant difference of antimalarial activities between Tablet II and III, meanwhile there was significant difference among Tablet I with Tablet II and Tablet III.It was concluded that antimalarial activity depending on raw material form of A. paniculata active substance
KINETICS STUDY COCRYSTALS KETOCONAZOLE-SUCCINIC ACID PREPARED WITH SLURRY METHOD BASED ON POWDER X-RAY DIFFRACTION (PXRD)
The compounds with low solubility drugs can
be a problem in the development of drugs for
the pharmaceutical industry. Group of drugs
that are included in the Biopharmaceutical
Classification System (BCS) class II drugs can
be a challenge for the preparations of pharmaceutical
development
because
of
low
solubility
drugs
as
well
as
the
rate
of
dissolution.
In
this
case
to
increase
the solubility of
drugs
besides
salts,
pharmaceutical
cocrystals
opened
a
new
dimension
to
search
for
solid
forms
such as
solubility,
dissolution rate, stability, and shelf
life of active pharmaceutical ingredients (APIs)
without affecting their inherent pharmacological
properties1.
Pharmaceutical
co crystals are materials or
crystalline materials consisting of at least two
different components (multicomponent crystals
or mixed crystals)2-3. Co crystal could be
prepared by several methods, such as solvent
evaporation, slurry, melt, and grinding. Co
crystals formed between ketoconazole (KTZ)
as an active pharmaceutical and succinic acid
(SA) as a co crystal former (co-former)4 was increased
dissolution
rate
of
pure
ketoconazole
in
equimolar ratio (1:1)1. Physical characterization
of
co
crystal
was
performed
by
physical
mixture
of
binary
system
with
molar
ratio
using
different
thermal
analyzer
(DTA)
data
from
KTZ
and SA. Besides that, physicochemical
characterizations of cocrystal were performed
by using PXRD and infrared spectroscopy (IR).
Active solid materials in the manufacture of
pharmaceutical preparation suffered in various
thermic or
machanical
proccessed
such
as grinding, milling, granulations (wet and dry granulations), tabletasi, and storage at
various temperature, so the materials can
occure transformation polymorph or hidrat/
solvat5. Kinetic study of cocrystal KTZ-SA prepared
with slurry
method
at
various
solvent
concentrations
a
follows
2%,
3%,
4%,
5%
and
6%
(w/w).
Therefore, the aim of the present
study was determined the kinetics of co crystals
KTZ-SA prepared with slurry method by
using Powder X-ray Diffraction (PXRD) data
such as the research of co crystalline phase
transformation of binary mixture of trimethoprim
(TMP)
and
sulfamethoxazol
(SMZ)
by
slurry
technique5
In vivo antimalarial activity of Andrographis paniculata Tablets
The formulation of three phytopharmaceutical products of Andrographispaniculata fractions (AP fraction A and B) containing diterpene lactones as an active substance were developed and their antimalarial activities against Plasmodium bergheihas been examined. In vivo antimalarial assay on P. berghei infected mice was carried out by oral administration,twice a dayfor four consecutive days of the AP fractions product, which were Tablet I: wet granulated formula of AP fraction A; Tablet II: wet granulated formula of AP fraction B; Tablet III: solid dispersion formula of AP fraction B.. The results revealed that three phytopharmaceutical products of A.paniculata were inhibited parasite's growth with inhibition range of 70.15% to 80.35%. There was no significant difference of antimalarial activities between Tablet II and III, meanwhile there was significant difference among Tablet I with Tablet II and Tablet III.It was concluded that antimalarial activity depending on raw material form of A. paniculata active substance
Peningkatan kelarutan dan bioavailabilitas kurkumin (Curcuma Xanthoriza Linn) dengan membentuk senyawa inklusi kurkumin-hidroksipropil-B-siklodekstrin
Tujuan penelitian ini adalah untuk memperbaiki kelarutan dan meningkatkan disolusi
serta bioavailabilitas kurkumin. Kurkumin adalah bahan baku yang diperoleh dari
rimpang temu lawak (Curcumin xanthoriza Linn) yang aktifitas terapinya cukup luas,
praktis tidak lamt dalam air dan bioavailabilitasnya rendah.
Penelitian yang sekarang dilakukan adalah membuat kompleksasi inklusi antara
kurkumin dan HP~CD. Kompleks kurkumin-HP~CD disiapkan dengan cara koevaporasi,
sementara campuran fisik diperoleh dengan pencampuran sederhana. Analisis kelarutan setimbang dilakukan untuk menentukan konstante stabilitas kompleks inklusi. Studi kelarutan fase menunjukkan diagram tipe AL dengan kompleksasi perbandingan molar
1 : 1 dan konstante stabilitasnya 30,09 mM-I. Kompleks inklusi padat ini selanjutnya dikarakterisasi dengan DTA, difraksi sinar-X, SEM dan FTIR. Analisis DTA dan difraksi sinar-X menunjukkan bahwa kurkumin berada sebagai bentuk kompleks amorf dalam kompleks koevaporasi. Studi disolusi menunjukkan bahwa kurkumin berada dalam kompleks terkoevaporasi yang disolusinya lebih besar daripada kurkumin murni dan campuran fisiko Temuan penelitian ini memberi bukti kurkumin berhasil ditingkatkan disolusi dan kemungkinan bioavailabilitasnya
Peningkatan kelarutan dan bioavailabilitas kurkumin (Curcuma Xanthoriza Linn) dengan membentuk senyawa inklusi kurkumin-hidroksipropil-B-siklodekstrin
Tujuan penelitian ini adalah untuk memperbaiki kelarutan dan meningkatkan disolusi serta bioavailabilitas kurkumin. Kurkumin adalah bahan baku yang diperoleh dari rimpang temu lawak (Curcumin xanthoriza Linn) yang aktifitas terapinya cukup luas, praktis tidak lamt dalam air dan bioavailabilitasnya rendah. Penelitian yang sekarang dilakukan adalah membuat kompleksasi inklusi antara kurkumin dan HP~CD. Kompleks kurkumin-HP~CD disiapkan dengan cara koevaporasi, sementara campuran fisik diperoleh dengan pencampuran sederhana. Analisis kelarutan setimbang dilakukan untuk menentukan konstante stabilitas kompleks inklusi. Studi kelarutan fase menunjukkan diagram tipe AL dengan kompleksasi perbandingan molar 1 : 1 dan konstante stabilitasnya 30,09 mM-I. Kompleks inklusi padat ini selanjutnya dikarakterisasi dengan DTA, difraksi sinar-X, SEM dan FTIR. Analisis DTA dan difraksi sinar-X menunjukkan bahwa kurkumin berada sebagai bentuk kompleks amorf dalam kompleks koevaporasi. Studi disolusi menunjukkan bahwa kurkumin berada dalam kompleks terkoevaporasi yang disolusinya lebih besar daripada kurkumin murni dan campuran fisiko Temuan penelitian ini memberi bukti kurkumin berhasil ditingkatkan disolusi dan kemungkinan bioavailabilitasnya
In vivo Antimalarial Activity of Andrographis paniculata Tablets
The formulation of three phytopharmaceutical products of Andrographispaniculata fractions (AP fraction A and B) containing
diterpene lactones as an active substance were developed and their antimalarial activities against Plasmodium bergheihas been
examined. In vivo antimalarial assay on P. berghei infected mice was carried out by oral administration,twice a dayfor four
consecutive days of the AP fractions product, which were Tablet I : wet granulated formula of AP fraction A; Tablet II : wet
granulated formula of AP fraction B; Tablet III : solid dispersion formula of AP fraction B.. The results revealed that three
phytopharmaceutical products of A.paniculata were inhibited parasite’s growth with inhibition range of 70.15% to 80.35%. There
was no significant difference of antimalarial activities between Tablet II and III, meanwhile there was significant difference
among Tablet I with Tablet II and Tablet III.It was concluded that antimalarial activity depending on raw material form of A.
paniculata active substance