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Novel drug delivery systems (NDDS) have recently gained importance
for delivering a variety of therapeutic agents for both local and
systemic administration. Delivery of drugs directly to targeted
sites of action provides several advantages over non-specific
delivery of drugs. Oral colon targeted drug delivery system is one
of that NDDS which directly deliver a drug in to the colon for
local treatment of a variety of colonic diseases as well as
systemic absorption of proteins and peptides. The Metronidazole is
the drug of choice in the treatment of the diseases like
Amoebiasis, Giardiasis, Trichomonosis and Bacterial Vaginosis. The
aim of the present research was to design, development and
optimization of swellable rupturable system taking account of local
action of the Metronidazole drug in the lower gastrointestinal
tract to kill the bacteria in the disease conditions like
Amoebiasis, Giardiasis and Trichomonosis.
Transdermal drug delivery systems are adhesive, dug containing
devices of defined surface area that deliver a pre-determined
amount of drug to the surface of intact skin at a pre-programmed
rate. These systems provide drug systemically at a predictable rate
and maintain the rate for extended periods of time. In this work an
attempt was made to formulate and evaluate TDDS for sustained
release Atorvastatin calcium by solvent casting method. Low
molecular weight, good permeability of Atorvastatin calcium made it
a suitable drug candidate for the development of transdermal
patches. The main objective of formulating the transdermal system
was to prolong the drug release time, reduce the frequency of
administration and to improve patient compliance. We sincerely hope
that this book will helpful to student as well as industry and
academic professionals involved in pharmaceutical and other related
science.
Sustained release drug system is any drug or dosage form
modification that prolongs the therapeutic activity of the drug.
Ideally a sustained release oral dosage form is designed to release
rapidly some predetermined fraction of the total dose in to GI
tract. This fraction (loading dose) is an amount of drug, which
will produce the desired pharmacological response as promptly as
possible and the remaining fraction of the total dose (maintenance
dose) is then release at a constant rate. The rate of the drug
absorption from the entire maintenance dose into the body should
equal to the rate of the drug removal from the body by all the
processes over the time for which the desired intensity of
pharmacological response is required. We sincerely hope that this
book will helpful to student as well as industry and academic
professionals involved in pharmaceutical and other related science.
The liquisolid systems are generally considered as acceptably
flowing and compressible powdered forms of liquid medications (that
implies liquid lipophilic (oily) drugs, or water-insoluble solid
drugs dissolved in suitable water-miscible nonvolatile solvent
systems). Such liquid medication may be converted into a dry
looking, non-adherent, free flowing, and readily compressible
powders by a simple admixture with selected powder excipients
referred to as the carrier and coating materials. We sincerely hope
that this book will helpful to student as well as industry and
academic professionals involved in pharmaceutical and other related
science.
Melt-In-mouth (MIM) technology is an innovative technology, which
allows tablet to disintegrate rapidly, usually in a matter of
seconds, without the need for water, providing optimal convenience
to the patient. Topiramate is antiepileptic drug prescribed
extensively for the patient of partial onset seizures, or primary
generalized tonic-clonic seizures in both children and adults, is
extremely bitter resulting in poor patient compliance. Recently, a
number of novel techniques for bitterness inhibition in
formulations intended for pediatric and geriatric patients need
acceptable taste. In the present study, an attempt was given to
mask bitter taste of topiramate by kyron T-114 (Cation exchange
resin). We sincerely hope that this book will helpful to student as
well as industry and academic professionals involved in
pharmaceutical and other related science.
The present study has been a satisfactory attempt to formulate
microparticulate system for colon targeted delivery of albendazole
using natural polysaccharides sodium alginate and chitosan.
Targeted drug delivery to the colon, by means of combination of one
or more controlled release mechanisms, hardly releases drug in the
upper part of the GIT but releases in the colon following oral
administration. Specifically delivering drug to the colon, a lot of
benefits would be acquired in terms of improving safety and
reducing toxicity when treating local or systemic chronic diseases.
We sincerely hope that this book will helpful to student as well as
industry and academic professionals involved in pharmaceutical and
other related science.
The present investigation is concerned with synthesis of new 2 and
6 - substituted 4H-chromen-4-One derivatives with the objectives of
discovering novel and potent anti-inflammatory agents and
anti-oxidants. The results of anti-inflammatory activity were
revealed that the compound has indole 2 substitution with
4-nitrophenyl amino methyl (at 6th position) on 4H- chromen-4-one
having more anti-inflammatory activity as compared to other
substituent's. While, indole 2 substituted 4-methoxy phenyl amino
methyl (at 6th position) 4H-chromen-4-one showed outperformed
anti-oxidant activity in different anti-oxidant model as compared
to other substituent's. The all newly synthesized compounds
displayed moderate to potent anti-inflammatory and anti-oxidant
activity and has therapeutic potential in combating this
devastating inflammatory and oxidative condition of the body, might
be deserve promising substances for further in vivo evaluation as
anti-inflammatory and anti-oxidant properties. However the
anti-inflammatory activity is not related to antioxidant potential.
Heterocycles bearing a triazole ring residue are reported to show
anticancer, anti-inflammatory, analgesic, antifungal,
antitubercular, antimicrobial, antiviral, antioxidant, CNS
depressant, and plant growth regulatory activity etc. Keeping in
view the importance of Triazole from the literature survey I found
various triazole derivatives & from that I planned to work the
substituted triazole derivatives from m-nitro benzoic acid, which
gives various anticipated biological activities. Among the all
synthesized compound, compound
6-(2-chloro-phenyl)-3-(4-nitro-phenyl)- 1,2,4]triazolo 3,4-b]
1,3,4]thiadiazole (PLP 105b) with MIC value of (16ug/ml) against
gram-positive (B.subtilis) and (16ug/ml) against gram-negative
(E.coli, p.aeroginosa)and the compound3,6-bis-(4-nitro-phenyl)-
1,2,4]triazolo 3,4-b] 1,3,4]thiadiazole (PLP 105d) with MIC value
of (16ug/ml) against gram-negative (p.aeroginosa) give better
antimicrobial activity than other synthesized compound."
The NSAIDs have known to cause serious problems such as gastric
ulceration, bleeding and renal disorders on long term medication.
These severe side effects are partially due to their nonselectivity
towards to COX-2 enzyme. Hence, newer, selective COX-2 enzyme
inhibitors have been developed to overcome the toxicity problems.
Recently, Rofecoxib and Celecoxib were withdrawn due to cardiac
toxicity.1,2-disubstituted five-membered heterocyclic compounds
have shown selectivity towards COX-2 inhibition. But, the toxicity
reports of drugs like Rofecoxib and Celecoxib in this category
prompted us to synthesize 1,2-diaryl diazepines (E) and their
derivatives as, survey of literature indicated the diazepine
heterocyclic system to have anti-inflammatory activity.
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