Under the Guidance of V.

Sampath Reddy

Presented by M.Sahadev B.Pharm

INTRODUCTION


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

SUMMARY AND CONCLUSION
REFERENCES

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.. Tween 80 was used as a dispersing agent.Georgarakis et al. 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. loading efficiency and dissolution rate depended on the emulsion-solvent evaporation technique and on the drug to polymer ratio.. . The physical properties. Microcapsules of salbutamol sulphate with ethylcellulose were prepared using an emulsion-solvent evaporation technique and by the use of two different stirrer types. Mandal et al. 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. Tarun K.23 Preparation of biodegradable microcapsules of zidovudine using solvent evaporation: Effect of the modification of aqueous phase. 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. Pao-Chu Wua et al. Different amounts of drug were added in order to obtain various drug to polymer ratios. propeller and magnet. The effect of sustained release of potassium from ethyl cellulose microspheres was evaluated by the in vitro dissolution test.

S. drug-containing phase to aqueous phase. polymeric. uniform drug loading and maximum entrapment efficacy and the absence of interaction between drug and process parameters as well as the polymers. The novel process was analysed for its capability to produce microcapsules of uniform size. the best formulation that contained cellulose acetate phthalate and ethyl cellulose in the concentration of 10:90 at 1:1. . David s et al. pH of a aqueous phase.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). 28 Prepared microspheres of ethyl cellulose by solvent evaporation process. the viscosity of the dispersed phase.Anne Andre-Abranta et al. 29 study the effects of the process variables. 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. good flowability. rate of addition of organic.. 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.S..5 drug– polymer ratio showed better anti-inflammatory activity than the marketed formulation and retarded drug release in the gastric medium. In addition to sustained and uniform release of drug. The influence of the agitation rate.. Biju et al.

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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 .

37.25mg. 37.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 : 215-217°C State Solubility : solid : Slightly soluble BCS classification: class I (highly solubility highly permeability) Dose : Tablet-100mg.5mg and 75mg .5mg and 50mg capsule-150mg.

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

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CR formulations that would maintain plasma levels of drug 8 to 15 hrs might be sufficient for once a day dosing for venlafaxine. strong bitter taste and bioavailability is 45% only. .aIM To design and Evaluate Micro capsules of Venlafexin Objective of the study Venlafaxine is a water soluble drug with a bitter taste. Marketed conventional Venlafaxine formulations are unpleasant. CR products are needed for venlafaxine to prolong its duration of action and to improve patience compliance. Venlafaxine was used in the treatment of antidepresent where an ultra rapid onset of action required.

These polymers were sed for controlled release of drugs. The effect of polymer types and drug: polymer ratio on release also studied.  In this formulation method Solvent evaporation method were used for procuction of micro capsules. The polymer selected for the present work was Eudragit rs100 and Eudragit rl 100. .

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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 .Materials used S.

Hyderabad.Equipments used S. Electro Lab TDT-08L Remi Equipments Ltd Mitutoyo Corp. Kawasaki. Japan Elico pvt India Ltd.japan 3 4 5 Dissolution tester ( USP ) Rotary shaker Digital vernier calipers ..No 1 2 Equipments Electronic digital balance Double beam UVspectrophotometer Company Shimadzu corp.

1 N hydro chloride solution. •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. .method Solvent evaporation method were used for procuction of micro capsules.

EVALUATION TEST Particle size analysis  Encapsulation efficiency  In-vitro dissolution studies  Morphological study Differential scanning calorimetric study(DSC) Fourier transform infrared spectroscopy(FTIR .

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604 0.01N HCl Concentration (μg/ml) 0 5 10 15 20 25 30 40 y = 0.0239x + 0.721 0.The standard graph of Venlafexine 0.5 0 0 10 20 30 40 Concentration mcg/ml .0098 0 0.148 0.271 0.9982 2 0.944 Absorbance (nm) Absorbance 1 R = 0.478 0.385 0.

SUMMARY AND CONCLUSION .

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 prepared microcapsules were spherical and free flowing. The entrapment efficiency was increased with the decrease in the polymer content. in vitro dissolution studies. entrapment efficiency. differential scanning clorimetry. The kinetics were best fitted to the higuchi model clearly indicates that the release mechanism was diffusion controlled. Highest proportion of the microcapsules was obtained in the range of 445 μm for all the formulations. . The prepared microcapsules were analyzed for various physico chemical properties such as. particle size distribution. scanning electron microscopy. FTIR. 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. The prepared microcapsules were spherical and free flowing. DSC study was conducted on the pure drug and microcpasules. Conclusions Venlafaxine microcapsules were prepared using various polymers. This research work gives some preliminary idea about the release of Venlafaxine embedded in the matrix system as microcapsules. This clearly indicates that there is no drug polymer interaction. The results of drug release kinetics shows first order with diffusion mechanism. The surface of the microcapsule was rough and observed some particles. . this clearly indicating that there is no drug polymer interaction. The surface was layered and some pores were observed between the layers. DSC and FTIR study shows no drug polymer interaction.

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Hollow microsphere: a review.AL. Microsphere As A Novel Drug Delivery System A Review. 213216. Madhu Sudana Chetty et al. International Journal of ChemTech Research. Cross-linked chitosan microspheres: Preparation and evaluation as a matrix for the controlled release of pharmaceuticals. Banarjee SK. [6]Agusundaram M. . [7] Dr. 2 (5) .s.A. J Pharm Pharmacol.2010. [3] Ei –Bagory .[1] http://www.2007. Fishers Microsphere Selection Bangs laboratories inc.suwaych . International Journal of Pharmaceutical Sciences Review and Research. Mahrous G M effect of spheres size. Tech Notes 1-201A . [4] Thanoo BC.1:10-15. Hosney .909-911.1(3):526-534. 15.merriam-webster. E. polymer to drug ratio and plastisizer concentration on the release of theophilin from ethyl cellulose microspheres . Gaikwad DD. 2009. Jadhav SL and Thorat RM. 1992. [5] Gholap SB. Ibrahom M.44:283-286. Sunny MC and Jayakrishnan A.com/dictionary/microsphere [2] European pharmacopeia 01/2005. Saudi pharm Journal.

139-196. . International journal of pharmaceutics. [10] Kalyan Shweta. 2010. [13] Yie W. Second Edition. New York. Basel. Novel Drug Delivery Systems. 218.1(3):195-210. preparation of microspheres by solvent evaporation technique . Revised and Expanded. 2010. Raje Veera Ashwani et al. [9] Kavita Kunchu. vol. Pelagia Research Library. James W Mc Ginity .10. 1998. [11] Perumal D. INC. microencapsulation of Ibuprofen and Eudragit RS 100 by solvent diffusion technology . Chein. [12] Patrick B O Donnell. Hong Kong. Marcel Dekker. 28 . 1-30. Recent Advancement InChitosan Best Formulation And Its Pharmaceutical Application.1998. 111. 2001. Sharma Parmod Kumar et al. Albumin Microspheres: A Unique system as drug delivery carriers for non steroidal anti-inflammatory drugs. 25-42.[8] Encyclopedia of pharmaceutical technology.5(2):12. Advanced drug delivery review.