PREPARATION AND CHARACTERIZATION OF LAFUTIDINE AS IMMEDIATE RELEASE ORAL STRIP USING DIFFERENT TYPE OF WATER-SOLUBLE POLYMER

Saba Abdulhadee Jabir,Halah Talal Sulaiman

doi:10.22159/ijap.2018v10i5.28292

Saba Abdulhadee Jabir, Halah Talal Sulaiman

Open Access

https://doi.org/10.22159/ijap.2018v10i5.28292

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Abstract

Objective: The objective of the present study was to design and optimize oral fast dissolving film (OFDF) of practically insoluble drug lafutidine in order to enhance bioavailability and patient compliance especially for a geriatric and unconscious patient who are suffering from difficulty in swallowing.Methods: The films were prepared by a solvent casting method using low-grade hydroxyl propyl methyl cellulose (HPMC E5), polyvinyl alcohol (PVA), and sodium carboxymethyl cellulose (SCMC) as film forming polymers. Polyethylene glycol 400 (PEG400), propylene glycol (PG) and glycerin were used as a plasticizer to enhance the film forming properties of the polymer. Tween 80 (1% solution) and poloxamer407 were used as a surfactant, citric acid as a saliva stimulating agent, and croscarmellose as a super disintegrant. Films were then tested for both physical (weight variation, thickness, surface pH, drug content) and mechanical (folding endurance, tensile strength, percent elongation, Young's modulus) characteristics. In vitro disintegration, time and drug release profile were also determined for each formula.Results: Films were found to be satisfactory when evaluated for both physical and mechanical characterizations. The surface pH of all the films was found to be within the range of salivary pH 6.8. The USP dissolution apparatus type II (paddle type) was used for in vitro drug release studies. The optimized formulation F13 gave 100 % of drug released at 2 min. It also showed satisfactory surface pH (6.2±0.2), drug content (100.1±0.01%), the disintegration time of (7.0±0.5) seconds and the time needed for 80% of medication to be released (T80%) was 0.96 min.Conclusion: Lafutidine OFDF was formulated using HPMC E5 as film-forming a polymer with PEG400 as a plasticizer. Combination of tween80 (1% solution) and poloxamer407 as a surfactant were used in the presence of croscarmellose as a super disintegrant. The chosen OFDF disintegrates within seven seconds, releases the drug rapidly and gives an action.

Highlights

Oral administration is one of the most crucial routes of administering a drug with high credit to obtain a systemic effect due to its simplicity, comfort ability by producing no pain compared with the systemic administration
All the prepared oral fast dissolving film (OFDF) which contain HPMC E5, polyvinyl alcohol (PVA), and sodium carboxymethyl cellulose (SCMC) showed homogenous and smooth surface properties, where as HPMC and PVA films were transparent, colorless, thin and soft while those prepared from SCMC were thin, soft, colorless and semi-transparent
The results indicate that no significant changes (p>0.05) were shown on the in vitro disintegration time (DT) of the OFDF upon changing of plasticizer type as shown in fig. 5, this may be due to the fact that penetration of fluid into the film was facilitated by the three types of plasticizer since the densely packed chains of HPMC were altered by the plasticizer through forming a polymer structure possess more pores and less densely that breaks at lower force, resulting in faster disintegration of the film [35]

Summary

Introduction

Oral administration is one of the most crucial routes of administering a drug with high credit to obtain a systemic effect due to its simplicity, comfort ability by producing no pain compared with the systemic administration. Disadvantages in case of certain oral dosage forms capsules and tablets, such as swallowing problems especially for children, infants and elderly leading to in compliance and disadherence to the treatment [1]. Oral fast dissolving films (OFDFs) are the most advanced form of an oral solid dosage form, which disintegrate or dissolve within a minute when placed in the mouth without drinking water or chewing. Oral films are formulated using polymers, plasticizer, flavors, colors, and sweeteners. Hydrophilic polymers are rapidly disintegrated or dissolved in the oral cavity delivering the drug to the systemic circulation that was used in the preparation of OFDFs. Plasticizer helps to enhance the flexibility and reduces the brittleness of the strip [4]

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Conclusion