1. | ENHANCEMENT OF SOLUBILITY & DISSOLUTION RATE OF
PRAVASTATIN USING SOLID DISPERSION |
| Mohammad Masud Alam, Vivek Patel |
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The solubility and dissolution rate of pravastatin, a drug used for the treatment of hyperlipidaemia. Pravastatin is a selective
competitive inhibitor of HMG Co A reductase. However its absolute bioavailability is 5%. To increase the solubility of drug
solid dispersion was prepared. Solid dispersion preliminary solubility analysis was carried out for the selection of the carrier
and solid dispersion was prepared with Hydroxy Propyl Methyl Cellulose (HPMC) and Methyl Cellulose (MC). These solid
dispersions were analyzed for the solubility and in-vitro dissolution profile solid dispersion of drug with polymer has shown
enhanced solubility with improved dissolution rate. Further FTIR, X-Ray studies were carried out. Solid dispersion prepared
with polymer in 1:5 ratios shows the presence of amorphous form confirmed by the characterization study. The present
investigations showed that solubility of Pravastatin sodium was markedly increased by its solid dispersion using PVP K30
as carrier. The formulation SDF8 containing (1:8) shows highest dissolution rate. Hence the solid dispersion a way is useful
technique in providing fastest onset of action of Pravastatin sodium as well as enhanced dissolution rate. The study also
shows that dissolution rate of pravastatin can be enhanced to considerable extent by solid dispersion technique with
Polymer
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2. | PHYTOCHEMICAL INVESTIGATION OF TAGETES ERECTA FOR
ANTI-DIARRHOEAL ACTIVITY |
| Zeeba Fatima, Safdar Husan Quraishi |
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The object of the present investigation is to be screening of aqueous extract of Tagetes erecta (200 mg/kg and 400 mg/kg)
administered by orally were selected on anti-diarrhoeal action. In this investigation, screening by castor oil induced
diarrhoeal model, charcoal meal test model and PGE2 induced test model also dose of standard drugs is Loperamide (2
mg/kg) as well as atropine (0.1 mg/kg) were used in this study. Plant extract in dose of 200 and 400 mg/kg used followed by
Phytochemical and acute toxicity study. In results of extract formed significant anti-diarrhoeal active against castor oil
induced diarrhoea, charcoal meal test as well PGE2 induced diarrhoea. It also cause dose linked anti-diarrhoeal result.
Results propose that it may proceed centrally and may inhibition of PGE2 to give anti-diarrhoeal action. Result of charcoal
meal test also suggests its anti-muscarnic activity
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3. | FORMULATION DEVELOPMENT AND EVALUATION OF
VALSARTAN FLOATING MICROSPHERES USING PSYLLIUM HUSK
POWDER BY MODIFIED EMULSION SOLVENT DIFFUSION METHOD |
| Boda Veeru Naik1*, Balla Rmakrishna1, Purushothaman M |
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A sustained release system for Valsartan designed to increase its residence time in the stomach without contact with the
Microspheres was achieved through the preparation of floating Microspheres by the Modified Emulsion solvent Diffusion
method. In the present study attempt has been made to develop sustained released drug delivery system by formulating the
floating Microspheres of Valsartan using psyllium husk powder as a natural polymer which is biodegradable, biocompatible,
nontoxic, economically cheap cost, devoid of adverse and side effects and easily availability. Valsartan N-(1-oxopentyl)-N-
[[2-(1H-tetrazol-5-yl) [1,1’-biphenyl] -4[ -yl] methyl] L Valine used as an Anti-hypertensive agent. The 12 batches of
floating Microspheres (VF1 to VF12) were formulated by Modified Emulsion solvent Diffusion method using different ratio
of polymers like Psyllium husk power, HPMC K4M and Carbopal. The formulated Microspheres were evaluated by means
of different parameters like shape and density of Microsphere, drug content uniformity, Invitro buoyancy, swelling Index,
Invitro dissolution studies. The formulation VF7 has better sustained release when compared other formulations, hence we
conclude that the combination of Psyllium husk powder, HPMC K4M shows better Gastric retention time which sustains the
release of the dosage form
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4. | FORMULATION AND EVALUATION OF SOLID LIPID
NANOPARTICLES CONTAINING CELECOXIB |
| Rahul Verma, Pushpendra Singh |
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The oral administration of Celecoxib causes gastrointestinal ulcers and bleeding in chronic use. Due to
gastrointestinal bleeding it may cause anaemia. Also, use of Celecoxib is limited by its poor solubility and low
bioavailability. Thus, the present study aimed at design and development of a drug delivery system which could enhance
the solubility of Celecoxib. Lipid based drug delivery has attracted much attention during recent years as innovative
strategy to overcome insufficient bioavailability of hydrophobic drugs. S-SLN can also offer better patient compliance.
One of the most popular and commercially viable formulation approaches for solving these problems is SLN which have
been shown to be reasonably successful in improving the oral bioavailability of various poorly water-soluble SLN are
isotropic mixtures of drug, oil/lipid, surfactant, and/or cosurfactant, which form fine emulsion/lipid droplets, ranging in
size from approximately 100 nm on dilution with physiological fluid. The drug, therefore, remains in solution in the gut,
avoiding the dissolution step that frequently limits the absorption rate of hydrophobic drugs from the crystalline state SLN
can be optimized with the help of phase diagram, when such a system is released in the lumen of the GIT, it disperses to
form a fine emulsion with the aid of GIT fluid
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5. | FORMULATION AND DEVELOPMENT OF SELFMICROEMULSIFYING DRUG DELIVERY SYSTEM OF SIMVASTATIN |
| Dheeraj Singh, Aditya Tiwari, NK Sahu |
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Self-micro emulsifying drug delivery system (SMEDDS) is a promising system for the Biopharmaceutics
Classification System (BCS) class II drugs. The current research aimed to improve the dissolution of poorly water-soluble
anti-diabetic drug simvastatin by formulating it in SMEDDS. Liquid SMEDDS of simvastatin were formulated with
Capmul MCM C8 and oleic acid as oil phase, Cremophor RH 40 and Tween 80 as surfactant phase, and Transcutol P as
cosurfactant phase after screening various vehicles. The prepared formulations were evaluated for self-emulsifying ability
and phase diagram was constructed to optimize the system. These systems were further characterized for globule size,
effect of pH and robustness, zeta potential, drug content, viscosity, self-emulsification time, poly dispersity index, %
transmittance, thermodynamic stability, surface morphology, and drug release. The system was robust to different pH
media and dilution volumes. The optimized system possessed a mean globule size of 122.2 nm, zeta potential around -
22.9 mV, drug content 99.66 ± 0.47%, viscosity 0.8874 ± 0.026 cP, emulsification time 38 s, poly dispersity index value
of 0.5, and transmittance value of 99.3 ± 0.6%. Drug release in hydrochloric acid buffer pH 2 was found to be 99.35 ±
0.38%. More than three-fold increase in dissolution characteristics of simvastatin in SMEDDS was observed as compared
to pure and marketed formulation. Liquid SMEDDS filled in hard gelatin capsule (HGC) shell was found to be
compatible. Stability studies show there was no sign of phase separation or precipitation and no change in drug content
was observed.
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