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Solubility enhancement technique of BCS Class II drug by Solvent Evaporatiom

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Solubility enhancement technique of BCS Class II drug by Solvent Evaporatiom

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I am very happy to share with you my B.Pharm Final semester Presentation. The topic of the presentation was “SOLUBILITY ENHANCEMENT TECHNIQUE OF BCS CLASS II DRUG BY SOLVENT EVAPORATION TECHNIQUE – FORMULATION & EVALUATION" which i have done under the esteemed guidance of Dr. Goutam Kumar Jena. It was a great experience to deliver this topic infront of the expert jury. I would also like thank all my teammates especially Agniv Masanta for his efforts. I hope everyone of you will like presentation and the research and efforts behind it.Thank you for giving your precious time. #research #science #thankyou #experience #share

I am very happy to share with you my B.Pharm Final semester Presentation. The topic of the presentation was “SOLUBILITY ENHANCEMENT TECHNIQUE OF BCS CLASS II DRUG BY SOLVENT EVAPORATION TECHNIQUE – FORMULATION & EVALUATION" which i have done under the esteemed guidance of Dr. Goutam Kumar Jena. It was a great experience to deliver this topic infront of the expert jury. I would also like thank all my teammates especially Agniv Masanta for his efforts. I hope everyone of you will like presentation and the research and efforts behind it.Thank you for giving your precious time. #research #science #thankyou #experience #share

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Solubility enhancement technique of BCS Class II drug by Solvent Evaporatiom

  1. 1. “SOLUBILITY ENHANCEMENT TECHNIQUE OF BCS CLASS II DRUG BY SOLVENT EVAPORATION TECHNIQUE – FORMULATION & EVALUATION PRESENTED BY – MR.KAUSTAV DEY REGD. NO. – 1703267065 SEMESTER- 8TH UNDER THE ESTEEMED GUIDANCE OF - DR. GOUTAM KUMAR JENA M.PHARM , Ph.D. ASSOCIATEPROFESSORCUMPLACEMENTOFFICER
  2. 2. C O N T E N T S 1. Introduction 2. Literature Review 3. Aim of the Study 4. Objectives of the Study 5. Plan of Work • Pharmaceutical Buffer preparation • Formulation • Dissolution study • Solubility study 6. Results & Conclusion 7. References ROLAND INSTITUTE OF PHARMACEUTICAL SCIENCES 1
  3. 3. I N T R O D U C T I O N • The enhancement of oral bioavailability of poorly water- soluble drugs remains one of the most challenging aspects of drug development. • The most commonly used techniques to increase dissolution rate are particle size reduction, salt formation and lyophilization, but all these methods have practical limitations like improper enhancement of solubility and all the drugs are not suitable for these techniques. • To overcome all these, solid dispersion technique by solvent evaporation approach is successfully applied to improve the solubility and dissolution rate, there by bioavailability. ROLAND INSTITUTE OF PHARMACEUTICAL SCIENCES 2
  4. 4. L I T E R A T U R E R E V I E W Sr. No. Drugs Additives Preparation Technique Solubility/dissolution improvement Reference 1 Glimepiride Arginine Neat grinding A significant increase in the solubility of glimepiride in phosphate buffer pH 6.8 was observed for the eutectic mixture when compared to the drug alone. An increase in the dissolution rate was also observed. (Park et al., 2020) 2 Celecoxib Adipic acid or Saccharin Liquid-assisted grinding The eutectic samples showed improved solubility in distilled water compared to pure drug. In the IDR assay, the dissolved amounts of celecoxib in eutectic mixtures were higher than the isolated drug and revealed the eutectic’s dissolution rate. Powder dissolution studies showed that both eutectics presented a significant higher dissolution profiles than raw celecoxib and physical mixtures, in different media (Hyun et al., 2019) 3 Nimesulide Nicotinamid Solvent Evaporation Drying) The solubility rise of eutectic sample was almost 14 times in distilled water compared to pure drug. A significant improvement of solubility of the mixture was also observed in other media (0.1 N HCl, phosphate buffer pH and simulated gastric fluid). Comparison of dissolution profiles revealed that prepared eutectic showed higher drug release (43.49%) compared to pure drug (24.30%) within one hour (Patel et al., 2019) 4 Ibuprofen Poloxamer Melting/cooling followed by grinding In vitro dissolution studies showed dissolution rate enhancement for eutectic mixtures in different media. The most pronounced effect was seen for mixture of ibuprofen: poloxamer (1:0.75) in acidic medium where the cumulative drug release was 58.27% while for drug, it was 3.67%. (Dugar et al., 2016) 5 Glicazide Succinic Acid Electrospray deposition and liquid-assisted grinding Dissolution profiles obtained in acidic medium pH 1.2 showed that the eutectic mixtures performed better than raw gliclazide. DE90min values were significantly higher for eutectic samples. The dissolution rate of formulated eutectic mixtures with Pluronic F68 and mannitol markedly was improved. (Emami et al., 2018) .
  5. 5. A I M O F T H E S T U D Y • The aim of this present investigation is to enhance solubility of Ibuprofen by formulating as solid dispersions. • To effectuate this formulation, solubility trials are performed with carrier like Ethyl Cellulose (EC) to enhance the solubility, dissolution rate and consequently bioavailability of the drug. • Further various molecular weight grades of these polymers are used to prepare the solid dispersion. ROLAND INSTITUTE OF PHARMACEUTICAL SCIENCES 3
  6. 6. O B J E C T I V E S O F T H E S T U D Y Solubility and Dissolution enhancement of Ibuprofen by using Ethyl Cellulose (EC) polymer with the help of Solvent evaporation method Comparing dissolution of formulated Drug-polymer complex with raw drug To evaluate the drug release from the tablets prepared with solid dispersion by invitro dissolution studies. Choosing appropriate Drug-polymer complex ratio among various ratios. The study is intended to select the best possible ratio of drug and polymer. The impact of polymers ratio on various properties of the tablet will be determined ROLAND INSTITUTE OF PHARMACEUTICAL SCIENCES 4
  7. 7. P L A N O F W O R K ROLAND INSTITUTE OF PHARMACEUTICAL SCIENCES Pharmaceutical Buffer Preparation Formulation of Various Drug Polymer complex 1.Dissolution Study 1.Solubility Study 5
  8. 8. PHARMACEUTICAL BUFFER PREPARATION ROLAND INSTITUTE OF PHARMACEUTICAL SCIENCES KH2PO4 (28.2 g) K2HPO4 (11.45 g) Distilled Water (1000 ml) Standard Phosphate Buffer Stock Solution (pH 6.8) Buffer Solution (10 ml) + Drug(10 mg) 2 ml was taken out Volume made upto 1000 ml (50 times dilution= 20 µg/ml) 2 µg/ml 4 µg/ml 6 µg/ml 8 µg/ml 10 µg/ml Blank Solution 6
  9. 9. PHARMACEUTICAL BUFFER PREPARATION (contd.) ROLAND INSTITUTE OF PHARMACEUTICAL SCIENCES Concentration Absorbance 10 0.022 20 0.044 30 0.065 40 0.087 50 0.109 y = 0.0022x + 0.0003 R² = 0.9999 0 0.02 0.04 0.06 0.08 0.1 0.12 0 10 20 30 40 50 60 Absorbance Concentration Standard Calibration Curve of Ibuprofen in Phosphate Buffer(pH 6.8) 7
  10. 10. F O R M U L A T I O N ROLAND INSTITUTE OF PHARMACEUTICAL SCIENCES Drug + Polymers in different ratios Sieved through Sieve #100 1.Mixed with solvent 1.Kept in Hot air Oven 2.(40°-45°C for 30 min) 1.Trituration of solid mass 1.Kept in Dessicator for 48 hrs 8
  11. 11. F O R M U L A T I O N ( c o n t d . ) ROLAND INSTITUTE OF PHARMACEUTICAL SCIENCES Formulation Drug: Polymer Ratio Drug Polymer Total Weight F1 1:1 400 mg 400 mg 800 mg F2 1:2 400 mg 800 mg 1200 mg F3 1:3 400 mg 1200 mg 1600 mg F4 1:4 400 mg 1600 mg 2000 mg 9
  12. 12. D I S S O L U T I O N S T U D Y ROLAND INSTITUTE OF PHARMACEUTICAL SCIENCES 100 mg Equivalent Solid dispersions obtained from each formulation Mixed with standard Phosphate buffer stock solution (pH 6.8) USP Dissolution Apparatus- II (37°±0.5°C/60 min/50 rpm) At every 15 min intervals for the next 1 hour, solution was withdrawn & replaced with 5ml PB 6.8 solution Filtered & 1ml solution is procured and diluted to 10 ml with PB 6.8 solution UV Absorbance measured % cumulative drug release was calculated Compared with raw drug by data visualization 10
  13. 13. D I S S O L U T I O N S T U D Y ( c o n t d . ) ROLAND INSTITUTE OF PHARMACEUTICAL SCIENCES Time(in minutes) Pure Drug F1 F2 F3 F4 15 0.106 0.141 0.142 0.174 0.138 30 0.087 0.051 0.088 0.104 0.089 45 0.096 0.029 0.051 0.051 0.103 60 0.083 0.082 0.058 0.105 0.058 Time (in minutes) Pure Drug F1 F2 F3 F4 0 0 0 0 0 0 15 49 55 65 75 66 30 51 59 68 79 71 45 62 65 70 87 73 60 65 69 71 93 81 Time v/s Absorbance Chart of Dissolution % Cumulative drug release of Various Formulations 11
  14. 14. D I S S O L U T I O N S T U D Y ( c o n t d . ) ROLAND INSTITUTE OF PHARMACEUTICAL SCIENCES 12 0 10 20 30 40 50 60 70 80 90 100 0 10 20 30 40 50 60 70 % RELEASE TIME (IN MINUTES) % CUMMULATIVE DRUG RELEASE Pure Drug F1 F2 F3 F4
  15. 15. S O L U B I L I T Y S T U D Y ROLAND INSTITUTE OF PHARMACEUTICAL SCIENCES 10 mg Equivalent Solid dispersions Mixed with 20 ml water Kept in Mechanical Shaker for 24 hrs at 25°C Filtered & 1ml solution is procured and diluted to 10 ml with PB 6.8 solution UV Absorbance measured & compared with raw drug 13
  16. 16. S O L U B I L I T Y S T U D Y ( c o n t d . ) ROLAND INSTITUTE OF PHARMACEUTICAL SCIENCES Solution Absorbance Pure drug 0.101 F1 0.137 F2 0.156 F3 0.178 F4 0.166 14 0.101 0.137 0.156 0.178 0.166 0 0.02 0.04 0.06 0.08 0.1 0.12 0.14 0.16 0.18 0.2 Pure drug F1 F2 F3 F4 Solubility Study
  17. 17. R E S U L T S & C O N C L U S I O N • The drug release from solid dispersions were in the order of F3>F4>F2>F1>Pure Drug. • In case of physical mixtures prepared in the ratio of 1:3 of drug polymer (Ibuprofen: Ethyl cellulose) ratio shows better release than other drug polymer ratios. Thus, F3 is the best suitable formulation among all other formulations. • The result of present study clearly indicated promising potential of solid dispersion of Ibuprofen and ethyl cellulose by solvent evaporation method in enhancing the solubility and from these methods could be viewed as alternative to conventional method of solubility enhancement of poorly soluble drugs. ROLAND INSTITUTE OF PHARMACEUTICAL SCIENCES 15
  18. 18. R E F E R E N C E S 1. . Alex, R., & Bodmeier, R. (1990). Encapsulation of water-soluble drugs by a modified solvent evaporation method. I. Effect of process and formulation variables on drug entrapment. Journal of Microencapsulation, 7(3), 347-355. https://doi.org/10.3109/02652049009021845 2. Amasya, G., Badilli, U., Aksu, B., & Tarimci, N. (2016). Quality by design case study 1: Design of 5-fluorouracil loaded lipid nanoparticles by the W/O/W double emulsion - Solvent evaporation method. Eur J Pharm Sci, 84, 92-102. https://doi.org/10.1016/j.ejps.2016.01.003 3. Arabi, H., Hashemi, S. A., & Fooladi, M. (1996). Microencapsulation of allopurinol by solvent evaporation and controlled release investigation of drugs. Journal of Microencapsulation, 13(5), 527-535. https://doi.org/10.3109/02652049609026038 4. Asghari-Varzaneh, E., Shahedi, M., & Shekarchizadeh, H. (2017). Iron microencapsulation in gum tragacanth using solvent evaporation method. Int J Biol Macromol, 103, 640-647. https://doi.org/10.1016/j.ijbiomac.2017.05.047 5. Assimopoulou, A. N., Papageorgiou, V. P., & Kiparissides, C. (2003). Synthesis and release studies of shikonin-containing microcapsules prepared by the solvent evaporation method. Journal of Microencapsulation, 20(5), 581-596. https://doi.org/10.3109/02652040309178348 6. Badmeier, R., & Chen, H. (1993). Hydrolysis of Cellulose Acetate and Cellulose Acetate Butyrate Pseudolatexes Prepared by a Solvent Evaporation-Microfluidization Method. Drug Development and Industrial Pharmacy, 19(5), 521-530. https://doi.org/10.3109/03639049309062964 7. Bodmeier, R., & McGinity, J. W. (1987). Polylactic acid microspheres containing quinidine base and quinidine sulphate prepared by the solvent evaporation technique. I. Methods and morphology. Journal of Microencapsulation, 4(4), 279-288. https://doi.org/10.3109/02652048709021820 8. Choi, J. S., Lee, S. E., Jang, W. S., Byeon, J. C., & Park, J. S. (2018). Solid dispersion of dutasteride using the solvent evaporation method: Approaches to improve dissolution rate and oral bioavailability in rats. Mater Sci Eng C Mater Biol Appl, 90, 387-396. https://doi.org/10.1016/j.msec.2018.04.074 9. Deng, Y., Yang, F., Zhao, X., Wang, L., Wu, W., Zu, C., & Wu, M. (2018). Improving the skin penetration and antifebrile activity of ibuprofen by preparing nanoparticles using emulsion solvent evaporation method. Eur J Pharm Sci, 114, 293-302. https://doi.org/10.1016/j.ejps.2017.12.024 10. Deshmukh, R., Wagh, P., & Naik, J. (2016). Solvent evaporation and spray drying technique for micro- and nanospheres/particles preparation: A review. Drying Technology, 34(15), 1758-1772. https://doi.org/10.1080/07373937.2016.1232271 ROLAND INSTITUTE OF PHARMACEUTICAL SCIENCES
  19. 19. THANK YOU 17

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