Formulation and Evaluation of Loperamide Liquisolid Compacts

Dibu, S Babu (2017) Formulation and Evaluation of Loperamide Liquisolid Compacts. Masters thesis, R.V.S College of Pharmaceutical Sciences, Coimbatore.


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INTRODUCTION: DRUG DELIVERY SYSTEM: Dosage forms are also referred to as “Drug Delivery Systems” or “Finished Drug Products”. A drug delivery system (DDS) is defined as a formulation or a device that enables the introduction of a therapeutic substance into the body and improves its efficacy and safety by controlling the rate, time, and site of release of drugs in the body. The goal of any drug delivery system is to provide a therapeutic amount of drug in the proper site in the body to achieve promptly and then to maintain the desired drug concentration. That is, the drug delivery system should deliver drug at a rate dedicated by the needs of the body over a specified period of treatment. Oral route of drug administration is most appealing route for delivery of drugs for various dosage forms. The tablet is one of the most preferred dosage forms, because of its ease of administration, accurate dosing and stability as compared to oral liquid dosage forms. Tablets may be defined as solid unit pharmaceutical dosage forms containing drug substance with or without suitable excipients and prepared by either compression or molding methods. AIM AND OBJECTIVE OF THE WORK: The aim and objective of the present study is to develop a pharmaceutically stable, cost effective and quality improved robust formulation of Loperamide tablets using liquisolid technique. Oral route still remains the convenient route of drug administration in many diseases. That the major problem in oral drug formulations is low and erratic bioavailability, which mainly results from poor aqueous solubility of certain drugs. Incase of poorly water soluble drugs, dissolution is the rate limiting step in the process of drug absorption. So, bioavailability problems are prevalent with extremely hydrophobic drugs (aqueous solubility <3.4 mg /ml at 37 ͦC). The enhancement of oral bioavailability of poorly water soluble drugs like LOPERAMIDE could be improved by enhancing aqueous solubility. Among numerous ways of enhancing drug dissolution, liquisolid compacts are the promising techniques to enhance the dissolution poorly water soluble drugs. To achieve this goal various prototype formulation trials will be taken and evaluated with respect to the various quality control parameters such as dissolution, assay. The formula will be finalized by dissolution profile. The objective includes providing a robust formulation for the production of the dosage form for which the influence of various factors like concentration and nature of non volatile solvents along with type of disintegrates used on disintegration time and dissolution parameters are to be studied and also analyzed.SUMMARY: The major problem in oral drug formulations is low and enteric bioavailability, which mainly results from poor aqueous solubility. Liquisolid compacts is the techniques are the most attractive processes to improve solubility of poorly soluble drugs . Loperamide hydrochloride an oral Anti-diarreheal agent used for the treatment of diarrheal. Loperamide is a Piperidine derivative. Loperamide is an opioidreceptor agonist and acts on the μ-opioid receptors in the myenteric plexus of the large intestine.  Slows intestinal motility and affects water and electrolyte movement through the bowel.Inhibits peristaltic activity by a direct effect on circular and longitudinal muscles of the intestinal wall.  Prolongs the transit time of intestinal contents; reduces fecal volume, increases fecal viscosity and bulk density, and diminishes loss of fluid and electrolytes.  Inhibits peristalsis of intestinal wall musculature and intestinal co ntents. Also reduces fecal volume, increases fecal bulk, andminimi zes fluid and electrolyte loss. Here the solubility of Loperamide is enhanced by liquisolid compacts with propylene glycol as liquid medication. Then the formed liquisolid compact is characterized and evaluated by FT-IR , drug content and In Vitro dissolution studies. Among the various liquisolid compacts were prepared, the formulation F2 i.e., the liquisolid compacts of Loperamide with PG 2% shows faster dissolution rate. The prepared tablets of LOPERAMIDE were evaluated for precompession parameters like angle of repose, bulk density, tapped density, carr’s index and post compression parameters like hardness, friability, weight variation, drug content, In Vitro disintegration time and In Vitro dissolution studies. Accelerated stability studies was carried out for selected formulations F2 which showed no significant difference in the drug content, disintegration time , hardness, friability and In vitro dissolution studies which confirm the stability of product.CONCLUSION: The Following conclusions were drawn from the Liqisolid compacts studies: The solubility studies of Loperamide in presence of Propylene Glycol was high when compared with PEG and Tweens & spans. The liquisolid technique was found to be a promising approach for improving the dissolution of poorly soluble drugs like lopermide. The Dissolution of loperamide was significantly increased in liquisolid formulation compared to the marketed product. The IR spectra indicate there was no interaction between the drug and excipients. The increased dissolution rate may be due to increased wetting and increased surface area of the particles. From the XRD, FT-IR, Drug content & In Vitro dissolution studies of loperamide liquisolid compacts it was concluded that the formulation F2 is the best formulation. The following conclusions were drawn from the Liquisolid compacts formulated to tablets: The powder blend was subjected to various physical characteristics such as bulk density, tapped density, Hausner’s ratio, compressibility index. The powder was compressed and the core tablets were evaluated for weight variation, hardness, disintegration time, drug content, dissolution studies, powder analysis like XRD, FT-IR studies & stability studies is concluded the best formulation is F2.

Item Type: Thesis (Masters)
Additional Information: Reg.No.261510751
Uncontrolled Keywords: Loperamide Liquisolid Compacts
Subjects: PHARMACY > Pharmaceutics
Depositing User: Ravindran C
Date Deposited: 23 Mar 2018 10:20
Last Modified: 23 Mar 2018 10:20

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