Under the Guidance of V.

Sampath Reddy

Presented by M.Sahadev B.Pharm

INTRODUCTION

LITERATURE SURVEY
AIM AND OBJECTIVE DRUG AND POLYMER PROFILE MATERIALS AND METHODS RESULTS AND DISCUSSION

SUMMARY AND CONCLUSION

REFERENCES

Georgarakis et al., Microcapsules of salbutamol sulphate with ethylcellulose were prepared using an emulsion-solvent evaporation technique and by the use of two different stirrer types, propeller and magnet. Different amounts of drug were added in order to obtain various drug to

polymer ratios. The physical properties, loading efficiency and dissolution rate depended on
the emulsion-solvent evaporation technique and on the drug to polymer ratio. Tween 80 was used as a dispersing agent. For a given drug to polymer ratio the percentage amount of Tween 80 affected the release of salbutamol sulphate and the size distribution of microcapsules. Tarun K. Mandal et al.,23 Preparation of biodegradable microcapsules of zidovudine using solvent evaporation: Effect of the modification of aqueous phase. The objective of the present investigation was to improve the efficiency of encapsulation of zidovudine (AZT) in poly

(lactide/gycolide) (PLGA 50:50) by modifying the secondary aqueous phase16.

Pao-Chu Wua et al.,
27

The water in soluble polymer ethylcellulose is used as a retardant

prepares sustained release of potassium chloride microspheres by drying in a liquid process. The effect of sustained release of potassium from ethyl cellulose microspheres was evaluated by the in vitro dissolution test.

Anne Andre-Abranta et al.,

28

Prepared microspheres of ethyl cellulose by solvent

evaporation process. The influence of the agitation rate, the viscosity of the dispersed phase, the molecular weight of the polymer and the volume ratio between the dispersed phase and

the continuous one on the drug release rate has been studied.
David s et al., 29 study the effects of the process variables, pH of a aqueous phase, rate of addition of organic, polymeric, drug-containing phase to aqueous phase, organic: aqueous phase volume ratio and aqueous phase temperature on the entrapment of propraonolol hydrochloride in ethylcellulose (N4) microspheres prepared by solvent evaporation method were using factorial design. S.S. Biju et al.,24 Dual coated erodible microcapsules for modified release of diclofenac sodium Diclofenac sodium was formulated as novel enteric microcapsules for improved delivery to the intestine using the polymers cellulose acetate phthalate (CAP) and ethyl cellulose (EC). The novel process was analysed for its capability to produce microcapsules of uniform size, good flowability, uniform drug loading and maximum entrapment efficacy and the absence of interaction between drug and process parameters as well as the polymers. In addition to sustained and uniform release of drug, the best formulation that contained cellulose acetate phthalate and ethyl cellulose in the concentration of 10:90 at 1:1.5 drug polymer ratio showed better anti-inflammatory activity than the marketed formulation and retarded drug release in the gastric medium.

1 Drug profile: Name: Venlafexin Structure:

IUPAC Name: 1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexan-1-ol Chemical Formula : C17H27NO Molecular Weight : Average-277.4018

Bioavailability: 45% Protein binding: 27%-30% Metabolism : Undergoes extensive first pass metabolism in the liver Half life Description : 5 hours : white to off white powder

Melting point : 215-217C State Solubility : solid : Slightly soluble

BCS classification: class I (highly solubility highly permeability) Dose : Tablet-100mg,25mg,37.5mg and 50mg capsule-150mg, 37.5mg and 75mg

Pharmacology:

Categories:
Antidepressants Analgesics Serotonin Uptake Inhibitors Antidepressive Agents, Mechanism of action: The exact mechanism of action of venlafaxine is unknown, but appears to be associated with the its potentiation of neurotrasmitter activity in the CNS. Venlafaxine and its active metabolite, O-desmethylvenlafaxine (ODV), inhibit the reuptake of both serotonin and norepinephrine with a potency greater for the 5-HT than for the NE reuptake process. Both venlafaxine and the ODV metabolite have weak inhibitory effects on the reuptake of dopamine but, unlike the tricyclics and similar to SSRIs, they are not active at histaminergic, muscarinic, or alpha(1)-

aIM To design and Evaluate Micro capsules of Venlafexin Objective of the study Venlafaxine is a water soluble drug with a bitter taste. Venlafaxine was used in the treatment of antidepresent where an ultra rapid onset of action required. Marketed conventional Venlafaxine formulations are unpleasant, strong bitter taste and bioavailability is 45% only. CR formulations that would maintain plasma levels of drug 8 to 15 hrs might be

sufficient for once a day dosing for venlafaxine. CR products are needed for
venlafaxine to prolong its duration of action and to improve patience compliance.

The polymer selected for the present work was Eudragit rs100 and

Eudragit rl 100. The effect of polymer types and drug: polymer ratio on

release also studied. These polymers were sed for controlled release of drugs.

In this formulation method Solvent evaporation method were used for

procuction of micro capsules.

Materials used

S.N o 1

Materials

Manufacturer

Venlafaxine

Reddys labs Ltd,

Hyderabad
2 3 Eudragit-Rl Eudragit-Rs
100

Colorcon Asia Pvt Ltd Colorcon Asia Pvt Ltd

100

Equipments used

S.No 1 2

Equipments Electronic digital balance Double beam UVspectrophotometer

Company Shimadzu corp., Japan Elico pvt India Ltd, Hyderabad. Electro Lab TDT-08L Remi Equipments Ltd Mitutoyo Corp, Kawasaki,japan

3 4 5

Dissolution tester ( USP ) Rotary shaker Digital vernier calipers

method

Solvent evaporation method were used for procuction of micro capsules. Preparation of venlafaxine micro capsule includes first the polymer of different grades and drug was dissolved in tween80 solvent And it is been droped in to sodium carboxy mehyl cellulose (or)

in 0.1 N hydro chloride solution.

EVALUATION TEST Particle size analysis Encapsulation efficiency In-vitro dissolution studies Morphological study

Differential scanning calorimetric study(DSC)

Fourier transform infrared spectroscopy(FTIR

The standard graph of Venlafexine 0.01N HCl

Concentration (g/ml) 0 5 10 15 20 25 30 40

y = 0.0239x + 0.0098

0 0.148 0.271 0.385 0.478 0.604 0.721 0.944

Absorbance (nm)

Absorbance

R = 0.9982

0.5

0 0 10 20 30 40

Concentration mcg/ml

SUMMARY AND CONCLUSION

The prepared microcapsules were spherical and free flowing. The prepared microcapsules were analyzed for various physico chemical properties such as, entrapment efficiency, particle size distribution, in vitro dissolution studies, differential scanning clorimetry, FTIR, scanning electron microscopy. The entrapment efficiency was increased with the decrease in the polymer content. Highest proportion of the microcapsules was obtained in the range of 445 m for all the formulations. The drug release form the microcapsules prepared with Eudragit RS 100 was found between 13 hours and Eudragit RL 100 was found to be 12 hrs The release kinetics showed that the release was followed first order. The kinetics were best fitted to the higuchi model clearly indicates that the release mechanism was

diffusion controlled. Peppas n values suggests that the release was Fickian
diffusion.

The spectrum peak points of the formulation were similar with that of the pure
venlafaxine, this clearly indicating that there is no drug polymer interaction. DSC study was conducted on the pure drug and microcpasules. This clearly

indicates that there is no drug polymer interaction.

The surface of the microcapsule was rough and observed some particles. The surface was layered and some pores were observed between the layers.

Conclusions
Venlafaxine microcapsules were prepared using various polymers. The results of drug release kinetics shows first order with diffusion mechanism. The prepared

microcapsules were spherical and free flowing. DSC and FTIR study shows no drug
polymer interaction. This research work gives some preliminary idea about the release of Venlafaxine embedded in the matrix system as microcapsules.

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Expanded,

Marcel Dekker, INC. New York, Basel, Hong Kong, 139-196.