Mahendra Babu, J (2015) Formulation and Evaluation of Epalrestat Microspheres. Masters thesis, Arulmigu Kalasalingam College of Pharmacy, Krishnankoil.
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Abstract
INTRODUCTION: Oral route has been one of the most popular routes of drug delivery due to its ease of administration, Patient’s compliance, least sterility constraints and flexible design of dosage form. Time release technology, also known as sustained release (SR), sustained-action (SA), extended-release (ER, XR or XL), time release or timed release, Controlled release (CR), modified release (MR) or continuous release (CR) is a mechanism used in pill tablets or capsules to dissolve slowly and release a drug over a prolonged period of time. Different polymers are employed due to their In situ gel forming characteristics and their ability to release entrapped drug in the specific medium by swelling and cross linking. OBJECTIVE OF THE RESEARCH WORK:Epalrestat is an effective diabetic neuropathy drug used for reliving nerve pain. Because of relatively short biological half life, it needs frequent administration to the patient. Hence controlled release of this drug is highly desirable. Epalrestat when formulated as microspheres eliminate the disadvantages of the controlled release tablets such as Absorption of drug irrespective of the feeding state, Minimal potential for dose dumping, shorter lag time and lower variability. Selection of right excipient is crucial and important during the development of matrix system because there is a chance of drug dumping. Hence different polymers were used to control the drug release from the matrix system. In the present study different polymer were used. The present study was aimed to prepare the micro spheres of Epalrestat using various Eudragit and Ethyl cellulose polymer at different drug to polymer concentrations.Eudragit RL 100 and Eudragit RS 100 are two copolymers synthesized from acrylic and methacrylic acid esters, containing a low level of quaternary ammonium groups. Eudragit RS 100 has a lower content of charged groups (4.5–6.8%), and it is considered less permeable to water with respect to the more readily permeable Eudragit RL 100 (8.8–12% ammonium groups). Higher permeability of Eudragit RL 100 is due to maximum number of quaternary ammonium substitution present in the structure of Eudragit RL 100 compared to RS 100 which affects the release behaviour of the drug. Ethyl cellulose is hydrophobic in nature; thus, the hydrophobic polymer encapsulates larger amount of the drug and hence was used in combination with Eudragit RL and RS 100 to increase the encapsulation efficiency and for a better controlled release. Eudragit S- 100 being a pH dependent polymer may reduce the impermeability of Ethyl cellulose by the formation of pores in the matrix. Hence the study was aimed to study the controlling effect of Epalrestat using the aforementioned polymers in the microspheres. The micro spheres prepared were evaluated for assay encapsulation efficiency, average particle size, in vitro drug release kinetics. The micro spheres were evaluated for drug excipient compatibility studies by FT-IR. SUMMARY: The prepared microspheres were analyzed for various Physico chemical properties such as entrapment efficacy, particle size , in-vitro dissolution studies, FT-IR, SEM. The entrapment efficacy can be varied to the changing the different kinds of polymers. The entrapment efficacy depends upon the some factors such as, nature of the polymer, RPM of the propeller, solubility of the drug , and concentration of surfactant. Highest proportion of the microspheres was obtained in the range of 389 nm for all the formulations. The average percent of microspheres obtained at 389 nm not varied with the type of polymer used. The drug release from the F1 formulation microspheres releases the more amount of drug in phosphate buffer solution. The kinetics showed that the release was followed Zero order and it was best fitted koresmeyer - Peppas model clearly indicates that the mechanism was erosion mechanism. The drug release from the micro spheres prepared with Eudragit S 100 was found between 1 to 8 hours for the micro spheres prepared at (F1). The drug release for the micro spheres prepared at (f2) to (F4) was found more than 12 hours. The drug release from the micro spheres prepared with Eudragit RS 100 was found between 1 to 10 hours for the micro spheres prepared at (F5). The drug release for the micro spheres prepared at (f6) to (F8) was found more than 12 hours. The drug release from the micro spheres prepared with Eudragit RL 100 was found between 1 to 12 hours for the micro spheres prepared at F(9). The drug release for the micro spheres prepared at (F10) to (F12) was found more than 12 hours. FT-IR Study on the selected formulations prepared with different polymers such as Ethyl cellulose , Eudragit S 100, Eudragit R 100 and Eudragit RL 100. The Spectrum peak points of the formulation were similar with that of pure Epalrestat, this clearly indicating that there is no drug polymer interaction. In the SEM photograph , the microspheres prepared with different polymers found spherical/round. The surface of the microspheres was rough and observed some particles.CONCLUSION:Epalrestat microspheres were prepared using Ethyl cellulose, Eudragit S 100 & Eudragit RL 100. The result of drug release kinetics show zero order with erosion mechanism. From the FTIR study, it is observed that there was no interaction between the drug and polymers. Dissolution studied study showed that all the polymer combinations gave sustained release. Maximum drug release was from the formulation (Drug: Ethyl cellulose: Eudragit S 100) (F1). From the SEM, the morphological characterization of the microspheres was studied . The prepared microspheres were spherical and free flowing by flow property studies and particle size distribution. The research work gives some preliminary idea about the release of Epalrestat embedded in the core system of microspheres.
| Item Type: | Thesis (Masters) |
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| Uncontrolled Keywords: | Epalrestat Microspheres ; Formulation ; Evaluation. |
| Subjects: | PHARMACY > Pharmaceutics |
| Depositing User: | Ravindran C |
| Date Deposited: | 14 Mar 2018 10:56 |
| Last Modified: | 16 Mar 2018 06:51 |
| URI: | http://repository-tnmgrmu.ac.in/id/eprint/6196 |
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