Formulation, Development and evaluation of Nitrofurantoin tablets drug delivery systems

 Corresponding author: Prachi Nandkumar Padwal Copyright © 2025 Author(s) retain the copyright of this article. This article is published under the terms of the Creative Commons Attribution License 4.0. Formulation, Development and evaluation of Nitrofurantoin tablets drug delivery systems Prachi Nandkumar Padwal 1, *, Akanksha Dattatray Khore 2, Reema Chandrakant Londhe 1, Madhavi Baban Aher 2, Mujeba Rajjak Pathan 2 and Payal Hemant Padwal 2 1 Assistant Professor, Department of Quality Assurance Technique, Samarth Institute of Pharmacy, Belhe, Pune, Maharashtra. 2 Student, Samarth Institute of Pharmacy, Belhe, Pune, Maharashtra. World Journal of Biology Pharmacy and Health Sciences, 2025, 24(02), 054-058 Publication history: Received on 21 September 2025; revised on 01 November 2025; accepted on 03 November 2025 Article DOI: https://doi.org/10.30574/wjbphs.2025.24.2.0940 Abstract Nitrofurantoin is a synthetic nitrofuran derivative widely used for the treatment and prevention of urinary tract infections (UTIs). It exhibits both bacteriostatic and bactericidal properties depending on its concentration. The formulation of Nitrofurantoin tablets aims to achieve optimum bioavailability, stability, and patient compliance. This review summarizes various approaches to the formulation and evaluation of Nitrofurantoin tablets, focusing on excipient selection, manufacturing methods, quality control parameters, and recent advances in sustained or controlled release systems. Keywords: Nitrofurantoin; Hydroxyl Propyl Methyl Cellulose (HPMC K4M; HPMC K100M); Xanthan Gum; Sustained Release 1. Introduction The oral route is considered to be the most convenient for administration of drugs to patients. Oral administration of conventional dosage forms normally dissolves in the stomach fluid or intestinal fluid and absorption from these regions of gastro-intestinal tract (GIT) depends upon the physicochemical properties of the drug. It is a serious drawback in conditions where localized delivery of the drugs in the urinary tract is required or in conditions where a drug needs to be protected from the hostile environment of upper GIT. Dosage forms that deliver drugs into the urinary tract or colon rather than upper GIT prefers number of advantages. A traditional oral sustained release formulation releases most of the drug, after the dosage form pass from the stomach. Hence, the drug should have absorption window either in the duodenum or intestine or urinary tract [1]. The main goal of sustained drug delivery systems is to improve the effectiveness of drug therapies [2]. Sustained release drug system is “any drug or dosage form modification that prolongs the therapeutic activity of the drug”. Ideally a sustained release oral dosage form is designed to release rapidly some pre-determined fraction of the total dose in to GI tract. This fraction (loading dose) is an amount of drug, which will produce the desired pharmacological response as promptly as possible and the remaining fraction of the total dose (maintenance dose) is then release at a constant rate. Nitrofurantoin is a urinary tract antibiotic [3]. The short biological half-life (0.3 to 1 hour) and dosing frequency more than one per day make Nitrofurantoin an ideal candidate for sustained release [4]. To reduce the frequency of administration from four times daily to two times daily, to minimize the side effects of nausea and emesis and to improve patient compliance. World Journal of Biology Pharmacy and Health Sciences, 2025, 24(02), 054-058 55 2. Material and methods Material: Nitrofurantoin was obtained from QMED Pvt. ltd Bhaktapur, Nepal and the excipients present in the SR granules are: hydroxypropyl methylcellulose-K4M, HPMC K100M, Xanthan gum, Anhydrous Lactose, Magnesium stearate, Talc were obtained from Amtech Med. Pvt. Ltd. Katahari-4, Morang as a gift. All the chemicals used were of analytical grade and purchased from an authorized dealer. Drug-Drug and Drug-Excipient Compatibility DrugDrug and Drug-Excipient Compatibility was assured by FT-IR spectroscopy. Preparation of sustained release matrix tablet of nitrofurantoin tablets were prepared by direct compression method. Specified quantity of nitrofurantoin, polymers such as HPMC K4M, HPMC K100M, xanthan gum, other excipients like lactose, magnesium stearate and talc weighed accordingly to the formula given in table no.1. All the materials except magnesium stearate and talc were transferred in a mortar and pestle and mixed thoroughly. This powder was passed through sieve no #80. To this add weighed quantity of magnesium stearate and talc. Each batch formulation powder blend was weighed to accurate single total tablet weight (710mg). Tablet was compressed with Single head rotary tablet compression machine. Table 1 Material and Supplied By Nitrofurantoin QMED PVT ITD Bhaktapur, Nepal HPMC K4M Yarrow chem PVT ITD, Mumbai HPMC K100M Yarrow chem PVT ITD, Mumbai Xanthan gum Yarrow chem PVT ITD, Mumbai Anhydrous Lactose Mehta chemicals, Bangalore Magnesium stearate Signet Chemical Corporation Mumbai Talc Karnataka Fine Chem, Bangalore Table 2 Equipment Used Sr. No Equipment 1 Fourier Transform Infrared Spectrophotometer (IR. Thermoscientific Nicolet is 10) 2 UV/VIS Spectrophotometer (up Jasco 2016) No: Qc.cp-057 3 pH Meter H12216 pH/ ORP/ISE Meter 4 Ultra-sonic 5 Electronic Balance Sartorius No: Oc-Cp.059 6 Hardness Tester RimekIndia. No: cp.010. 7 Disintegration Tester (disintegration tester -bj-3) 8 HPIC 2020 9 Dissolution Tester (Rc-80C) No: Qc-cp-071 10 Tablet Machine World Journal of Biology Pharmacy and Health Sciences, 2025, 24(02), 054-058 56 Rotary tablets press machine Zp-7 11 Friability Tester (Cjy-300D Tablets friability tester) 12 Thickness Tester Vernier (Stainless hardened) 13 Oven Incubator) Accelerate Stability Study Champer 2.1. Formulation And Evaluation of Nitrofurantoin Table 3 Formulation Table Ingredient in mg F1 F2 F3 F4 F5 Nitrofurantoin 200 200 200 200 200 Xanthine gum 300 _ _ _ 150 HPMC K4M _ 300 _ 150 150 HPMC K100M _ _ 300 150 _ Anhydrous lactose 200 200 200 200 200 Magnesium starts 7 7 7 7 7 Talc 3 3 3 3 3 Total weight 710 710 710 710 710 2.2. Evaluation of Nitrofurantoin • Evaluation of pre-compression flow properties of powderblend • Organoleptic properties -Organoleptic properties of API like color, odor and stability • were observed a recorded. Solubility was observed in • methanol and sodium hydroxide. • Bulk Density -Bulk density was measured using bulk density apparatus. Fixed weight of powder was poured in the measuring cylinder and volume was recorded. • Bulk density = Bulk weight/Bulk volume Tapped Density -Fixed weight of powder was poured in the measuring cylinder and tapped 50 cycles multiple times. Volume was recorded after each 50 tapping cycles until fixed (concurrent) reading was obtained. The tapped density was obtained by using following equation: Tapped Density = Bulk weight/Tapped volume. • Weight variationThe weight variation test would be satisfactory method of determining the drug content uniformity. Twenty tablets randomly were taken from each batch and weighted individually, calculating the average weight, and comparing the individual tablet weights to the average. The average weight of one tablet was calculated. • Diameter test -The diameter test one of tests which used for determination of the tablets size, it is done by taking five tablets from each batch randomly. Diameter may obtain by using suitable micrometer. • Thickness test -The thickness test of five tablets was picked from each batch randomly and thickness was measured individually using “Verniercaliper” (Electronic Digital Caliper). It is expressed in millimeter and average was calculated. • Hardness test -The hardness test or tablet crushing strength. The force required to break a tablet in a diametric compression was measured using digital tablet hardness tester. It is expressed in kg/cm. Five tablets were randomly selected from each batch and hardness of tablets was determined by using digital hardness tester. The mean values and standard deviation for each batch were calculated. • Friability test -The friability test is performed to assess the effect of friction and shocks, which may often cause tablet to chip, cap or break. Roche fryolator was used for the purpose. Pre-weighed sample of five tablets from each batch were placed in the fryolator, which was then operated for 100 revolutions. After 100 revolutions the tablets were dusted and reweighed. Compressed tablets should not lose more than 1% of their weighed. World Journal of Biology Pharmacy and Health Sciences, 2025, 24(02), 054-058 57 • In-vitro disintegration timeThe in-vitro disintegration time was determined using disintegration test apparatus. A tablet was placed in each of the six tubes of the apparatus and one disc was added to each tube. The time in seconds taken for complete disintegration of the tablet with no palatable mass remaining in the apparatus was measured in seconds. 3. Result and discussion Table 4 Evaluation parameters of Nitrofurantoin Formulation Code Hardness Thickness Friability% Average Weight Drug Content F1 7.5 ± 0 5.5 0.74 710.3 98.29 ± 0.05 F2 6.66 5.5 0.47 710.17 99.54 ± 0.64 F3 6.5 ±0 5.4 0.72 710.42 99.05 ± 0.4 F4 6±0 5.48 0.70 709.36 100.35 ± 0.16 F5 7.33 ± 0.288 5.01 0.50 709.4 101.76 ±0.52 F6 6.5 ±0 5.02 0.83 710.5 100.63 ± 0.09 4. Conclusion Matrix tablet of nitrofurantoin was successfully prepared by direct compression method, using different types of matrixes forming polymers like HPMC K4M, HPMC K100M, Xanthan gum. Matrix tablets are easy to prepare. They are cost effective and exhibit predictable release behavior. So, the ultimate aim of the present study was to prepare twice daily sustained release matrix tablets of Nitrofurantoin for improved patient compliance, better therapeutic efficacy, less side effects and reduced dosage regimen with less toxicity for treatment of urinary tract infection. In conventional dosage form it undergoes First pass metabolism, that is way it shows poor bioavailability of 45-56%. So, due to this disadvantage to improve bioavailability sustained release matrix tablet was formulated. Following conclusions have been drawn from the present study. Ø Compatibility of drug and polymer was confirmed by FTIR studies. Ø the formulation blend was subjected for pre-compressional evaluations such as angle of repose, bulk and tapped density, compressibility index and Hausner’s ratio and was found to be in the specified limit. Ø the evaluation data for properties such as hardness, thickness, friability, weight variation, drug content indicated that the prepared matrix tablet was within the specified standards. Compliance with ethical standards Acknowledgments We sincerely acknowledge the continuous guidance, motivation, and constructive feedback provided by our mentor, Ms. Prachi Nandkumar Padwal Their expertise and patience have been instrumental in shaping this review paper. We also extend our gratitude to Samarth Institute of Pharmacy, Belhe for providing the necessary academic environment and resources that supported this work. Disclosure of conflict of interest No conflict of interest to be disclosed. References [1] Sustained-Release Matrix Tablets of Nitrofurantoin: Formulation and Optimization. (2013) — using HPMC K-100 LV Premium and other excipients in wet granulation technique. 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