Formulation and Evaluation of Osmotic Tablet of Lovastatin

Abstract

Lovastatin is one of the antihypertensive drug used to control the high blood pressure. Osmotically Controlled release tablet of Lovastatin was performed for reducing dosing frequency and patient compliance. Elementary osmotic tablets of Lovastatin were developed using Sodium chloride as a key ingredient which gives osmogent property which provides driving force inside the core tablet and which leads to release of drug. Microcrystalline cellulose used as a release retardant material in the present work. These formulations were evaluated for, Hardness, Flow property, Thickness, Friability, Drug content and In-vitro drug release. Tablets were coated with a semipermeable membrane using 5% w/v cellulose acetate(CA) in acetone and PEG 400(1%) used as Plasticizer. Coated Elementary osmotic tablets were drilled for delivery orifice using standard micro drill of diameter size 0.8mm. Drug release rate was increased as the increase in the concentration of sodium chloride and release rate decreased on increasing the concentration of MCC. Drug release rate was directly proportional to delivery orifice size. SEM Study carried out for detection of diameter size of delivery orifice. The FTIR studies demonstrate that there was no interaction between polymer and drug. The optimized formulation was stable for 3 months of accelerated stability study.

Introduction

• Oral drug delivery is the most preferred route due to convenience and patient compliance.

• Conventional oral systems release drugs immediately, often failing to maintain therapeutic levels.

• Modified release systems like delayed, extended, site-specific, and receptor-targeted releases aim to improve therapy by offering controlled and sustained drug release.

2. Objective & Approach:

• The study focuses on developing osmotic-controlled release tablets of Lovastatin using the elementary osmotic pump method.

• Wet granulation was used to prepare the core tablets with excipients like NaCl, polyethylene oxide, lactose, and PVP K30.

• Tablets were coated with cellulose acetate (semi-permeable membrane) using ethanol:acetone solution and drilled with a 0.8 mm orifice for controlled release.

3. Evaluation & Optimization:

a. Granules and Tablets:

• Granules evaluated for flow properties, bulk/tapped density, Carr’s Index, and Hausner’s Ratio.

• Tablets evaluated for weight variation, hardness, friability, porosity, and content uniformity.

• All formulations passed standard quality tests.

b. In-vitro Dissolution Study:

• Among all formulations (F1–F9), F6 showed the best drug release profile:

  • 96 ± 2.08% drug release over 24 hours, indicating effective controlled release.

c. Stability Study:

• Stability of F6 was assessed over 3 months as per ICH guidelines (40°C ± 2 / 75% RH ± 5).

• Drug content and release profile showed no significant variation, confirming the stability of the formulation.

d. FTIR Studies:

• FTIR analysis confirmed no interaction between Lovastatin and excipients, proving compatibility.

Conclusion

The results of osmotic tablet studies of Lovastatin tablets proved that the granules of Lovastatin showed good flow properties, tablet evaluation tests are within the acceptable limits, IR spectral analysis proved that there was no drug-excipients interaction, the kinetic studies revealed that optimized formulation followed First order release kinetics and stability studies revealed that all the formulations were found to be stable after storing at temperature of 45ºC ± 2ºC, 75% ± 5% relative humidity for 3 months. Thus the results of the above study clearly indicated that Developed Osmotically controlled release tablet of Lovastatin provide release of drug at a predetermined rate and for a predetermined time in controlled manner.

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Copyright © 2025 Mayuri Ashok Khobare, Dr. Pranav Parekh. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.