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The purpose of this study was to develop and evaluate a drug
delivery system in vitro based on a compression coated tablet
containing 5-fluorouracil (5-FU) in core and pectin Hydroxypropyl
Methylcellulose (HPMC) mixture in coat layer. The main reason for
selecting pectin was its biodegradation in colon by colonic flora.
On other hand, high molecular weight HPMC increases mechanical
strength of tablet coat around a drug core during its
transportation in gastro-intestinal tract. Multiple regression
analysis with two way ANOVA revealed that both factors had
statistically significant influence for the response studied (P
Indians are genetically more susceptible to diabetes and the W.H.O
predicts the number of diabetes in India would go up to 40 million
by 2010 and 74 million by 2025. Diabetes is associated with
long-term complications that affect almost every part of the body.
However Insulin administration is effective to some extent in
increasing the life expectation of diabetic patients, but there are
wide spectrum of limitations as well as draw backs for this
therapy. Some Oral hypoglycemic agents are also employed in this
regard, such as renal damage and neurological disturbances. There
are great deals of evidences to suggest that the use of carefully
chosen herbal remedies and dietary supplements to prevent and
control the diabetes.The leaves of the plant Actinodaphne hookeri
Meissn.(Lauraceae)have been traditionally claimed to be useful in
diabetic conditions but yet no scientific reports are available in
this regard. Hence the plant Actinodaphne hookeri Meissn leaves was
selected for Phytochemical investigations and Anti diabetic
activity.
Levocetrizine hydrochloride is an oral antihistamine and
antiallergic agent, which blocking histamine receptors. It does not
prevent the actual release of histamine from mast cells, but
prevents it binding to its receptors. This in turn prevents the
release of other allergy chemicals and increased blood supply to
the area, and provides relief from the typical symptoms of hey
fever and rhinitus allergic condition. The dose of Levocetrizine
hydrochloride ranges from 5 to 10 mg twice in a day and it
undergoes extensive first pass metabolism. Hence it has only 66%
bioavailability. The half life of the drug 8 to 10 hours indicates
the need for modified release dosage form. levocetrizine
hydrochloride was chosen as model drug with an aim to developed
fast dissolving tablet that improve bioavailability, patient
compliance and rapid action in rhinitus allergic condition.
The aim of this study was to develop a new intra-gastric oating in
situ gelling system for controlled delivery of levetiracetam for
the treatment of partial onset seizures.High dose of levetiracetam
(750 to 1000 mg) is di cult to incorporate in oating tablets but
can easily be given in liquid dosage form. Sodium alginate-based
in-situ gelling systems were prepared by dissolving various
concentrations of sodium alginate in deionized water, to which drug
and calcium carbonate were added. A 32 full factorial design was
used for optimization. The concentrations of sodium alginate (X1)
and calcium carbonate (X2) were selected as the independent
variables.The amount of the drug released after 1 h (Q1) and 6 h
(Q6) and 12 h (Q12), viscosity and Floating lag time of the liquid
formulation were selected as the dependent variables. The studies
indicate that the formulation was effective in providing in vitro
release for extended time up to 12 hrs and also convenient for
geriatric and paediatric patient and increase drug residency to the
GIT."
The purpose of this research was to formulate tasteless complexes
of Fexofenadine Hydrochloride with Kyron-134 and to formulate
tasteless complex into fast-Dispersible tablets (FDT) for the
treatment of allergic rhinitis & chronic idiopathic urticaria.
Drug release from FDT in salivary pH was insufficient to impart
bitter taste. Complete drug release was observed at gastric pH. The
studies indicate that the formulation was taste masked drug can be
formulated in to FDT with view to enhance patient compliance &
to obtain faster onset action of the drug which would be
advantageous in comparison to the currently available conventional
forms. Formulations D-5 was found to be palatable with in vitro
disintegration time of 20 s Dissolution studies showed complete
release of D-5 within 30 min.
For evaluation of granules containing different herb parameters
tested for raw material were organoleptic, physicochemical,
physical, phytochemical etc. Parameters for finished product
(granules) include pH, LOD, angle of repose, tapped density, bulk
density, Carr's index, Hausner's ratio. Marketed formulation
consists of aqueous extract of G. glabra, Z. officinalis and A.
vasica indicated for sore throat, cough, cold and flu. Results
indicated that Raw material of Marketed formulation and Developed
formulation were identical with respect to all organoleptic,
physicochemical, physical, and phytochemical parameters. All three
batches of marketed formulation were uniform in colour, size, loss
on drying, angle of repose, bulk and tap density and also showed
uniformity with developed formulation. HPTLC fingerprinting
indicated presence of peaks at Rf in respective solvent system were
matched with Raw material, Marketed formulation and Developed
formulation confirm.
Venlafaxine Hydrochloride is an oral antidepressant agent of the
Serotonin-Norepinephrine Reuptake Inhibitor class. Venlafaxine
Hydrochloride has been studied for the treatment of panic disorder,
post-traumatic stress disorder, and the treatment of hot flashes in
patients who cannot or do not want to take hormone replacement
therapy. The dose of Venlafaxine hydrochloride ranges from 75 to
225 mg three times a day and it undergoes extensive first pass
metabolism hence it has only 45% bioavaibility. The short half life
of the drug 5 hr indicates the need for modified release dosage
form. Venlafaxine HCl was chosen as model drug with an aim to
developed mucoadhesive buccal tablet that minimize dose related
side effects and reducing the dosing frequency of drug and finally
improve the bioavaibility.
Itopride, a novel prokinetic agent is unique and different from the
available prokinetics because of its dual mode of action and lack
of significant drug interaction potential. Itopride is a newly
developed prokinetic agent, which enhances gastric motility through
both anti-dopaminergic and anti-acetylcholinesterage actions. It is
best candidate for Gastro Esophageal Reflux Disease. Itopride 50mg
can be given thrice in a day for Treatment of GERD. By developing
the sustain release formulation of Itopride hydrochloride, the
frequency of drug can be reduce to once only to obtain good
therapeutic response. The prepared formulation is usually taken on
an empty stomach about an hour before meals. Sustained release
tablet of Itopride Hydrochloride was prepared by using combination
of HPMC grade as matrix forming material. The influence of amount
of Hydroxypropyl Methylcellulose K15M and Hydroxypropyl
Methylcellulose K100M on release of Itopride hydrochloride was
studied using Central composite design. The optimized Formulation
FB7 had given prolonged drug release up to 24 hr. It also had
desired drug release kinetics and it was found to be stable after 1
month at accelerated conditions.
Nicotinic acid (NA) as lipid lowering agent drug has not become a
first-line treatment due to the strong side effect called flushing
occurs when given in immediate release dosage form. The tablets
were prepared by wet granulation method using HPMC K-15M, polymer
as retardant and the prepared tablets of NA will remain intact up
to 2 hrs in pH 1.2 due to Eudragit L 100-55 and its release is not
only initiated but tact fully retarded up to 12 hrs and were found
to be superior in physical properties, dissolution characteristics,
and drug content uniformity. The drug release from the matrix
tablet Fitted to the Higuchi model and Zero order release which
indicates non-Fickian diffusion.N8 showed good similarity with
theoretical profile of nicotinic acid. Excipients has significant
effect on drug release, because DCP retarded the release due to
hydrophobic nature, on the contrary MCC increased drug release for
its swelling property and causing burst release, and lactose
moderately affected drug release due to channeling action and hence
causing drug release at desired rate and amount. The studies
indicate that the formulation was effective in providing in vitro
release for extended perio
Metoprolol Tartrate is a -blocker drug indicated for the treatment
of angina, prevention of myocardial infarction, Essential
hypertension; It has low bioavailability of about 40% due to
hepatic metabolism. The purpose of this research was to improve the
bioavailability by preparing a fast dissolving tablet using
superdisintegrants method. Because pregastric absorption of drug
improves bioavailability, gives rapid onset of action when needed."
Famotidine is histamine -H2 receptor antagonist. It has
bioavailability of 40 to 45% and it has shorter plasma half life of
2.5 to 3.5 hrs. The effective treatment of erosive esophagitis and
Zolinger-Elisons syndrome requires administration of 20 mg of
Famotidine 4 times a day. A conventional dose of 20 mg can inhibit
gastric acid secretion up to 5 hours but not up to 10 hours. An
alternative dose of 40 mg leads to plasma fluctuations; thus a
sustained release dosage form of famotidine is desirable. Direct
access to the systemic circulation bypasses drugs from the hepatic
first pass metabolism leading to high bioavailability. Moreover,
the buccal route is easily accessible, has a good patient
compliance and can be used in patients who can't swallow. Bilayer
buccal tablet was prepared by using mucoadhesive polymer
combination of Sodium CMC and Carbopol934P, by direct compression
with backing layer of Ethyl cellulose. The optimized formulation F1
had given release of 102.57% in 8hrs and it had optimum swelling,
mucoadhesive property and permeation from buccal mucosa. It also
had desired drug release kinetics and found to be stable for the
period of 1 month.
Tolperisone hydrochloride has a short elimination half- life and
rapidly absorbed from gastrointestinal tract.2 If it is formulated
by conventional tablets, it will require multiple daily
administrations (2-3 times daily) which ultimately results into in
conveniency to the patients and possibility of reduced compliance
with prescribed therapy. Tolperisone HCl is more stable in acidic
medium (pH > 4.5), and in alkaline medium (pH 4 to 7)
tolperisone breaks down into 4-MMPPO and piperidine. Thus, the
patient is exposed to an uncontrollable quantity of 4-MMPPO
2methyl-1-(4methylphenyl)-propanone]. Proposed are floating
tolperisone tablets with the controlled release of the active
substance tolperisone in the stomach at pH 1 to 2.
In the present investigation, solid dispersion of olanzapine has
been prepared to improve its solubility. Further, using solid
dispersion, mouth dissolving tablet was prepared to overcome the
problem of swallowing. A Simplex Lattice design was applied using
three factors, i.e. superdisintegrants like croscarmellose
sodium(X1) crospovidone(X2), and sodium starch glycolate(X3) in
tablet formulation. Disintegration time, Wetting time, Water
absorption, T50 (Time required to 50% drug release) and Q10
(percentage of drug released in 10 min.) taken as responses. Solid
dispersion showed significant enhancement in solubility of
olanzapine. For mouth dissolving tablet, batch containing 5%
croscarmellose sodium alone had minimum disintegration time (44
sec.) and faster drug release(T50: 40 sec) compared to other
batches.
To develop sustained release matrix tablet of Tramadol HCl that
deliver drug for 24 hr and to be taken once in a day. Drug having
high solubility and relatively shorter half-life suggests its
suitability for an extended formulation. If it is formulated by
conventional tablets, it will require multiple daily
administrations which ultimately results into inconveniency to the
patients and possibility of reduced compliance with prescribed
therapy. Also fluctuation in plasma drug concentration leads to
exaggerated side effects, this all limitations can be minimized by
adopting extended release formulation. To reduce the frequency of
administration and to improve the patient compliance, Once in a day
sustained release formulation is desirable. It describes the
influence of the concentration of HPMC K4M, HPMC K15M and HPMC
K100M on Tramadol HCl sustained release formulations using
box-behnken design.These Polymers were selected as an independent
variables. Drug release after 8 hr, 12 hr and 16 hr were selected
as a dependent variables. Optimized formulation found by similarity
and dissimilarity factor follow zero order kinetic with non-fickian
diffusion as a drug release mechanism.
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