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Nanosuspension-Based Repaglinide Fast-Dissolving Buccal Film for Dissolution Enhancement

Drug solubility and dissolution remain a significant challenge in pharmaceutical formulations. This study aimed to formulate and evaluate repanglinide (RPG) nanosuspension-based buccal fast-dissolving films (BDFs) for dissolution enhancement. RPG nanosuspension was prepared by the antisolvent-precipitation method using multiple hydrophilic polymers, including soluplus®, polyvinyl alcohol, polyvinyl pyrrolidine, poloxamers, and hydroxyl propyl methyl cellulose. The nanosuspension was then directly loaded into BDFs using the solvent casting technique. Twelve formulas were prepared with a particle size range of 81.6-1389 nm and PDI 0.002-1 for the different polymers. Nanosuspensions prepared with soluplus showed a favored mean particle size of 82.6 ± 3.2 nm. The particles were spherical and non-aggregating, as demonstrated by SEM imaging. FTIR showed no interaction between soluplus and RPG. Faster dissolution occurred for the nanosuspension in comparison with pure RPG (complete release vs 60% within 30 min). The nanosuspension was successfully incorporated into BDFs. The optimum film formula showed 28 s disintegration time, and 97.3% RPG released within 10 min. Ex-vivo permeation profiles revealed improved RPG nanosuspension permeation with the cumulative amount of RPG permeated is103.4% ± 10.1 and a flux of 0.00275 mg/cm2/min compared to 39.3% ± 9.57 and a flux of 0.001058 mg/cm2/min for pure RPG. RPG was successfully formulated into nanosuspension that boosted drug dissolution and permeation. The selection of the ultimate NP formula was driven by optimal particle size, distribution, and drug content. Soluplus NPs were shown to be the successful formulations, which were further incorporated into a buccal film. The film was evaluated for ex-vivo permeation, confirming successful RPG formulation with improved performance compared to pure drugs.

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Publication Date
Mon Jan 01 2018
Journal Name
Journal Of Pharmacy Research
Preparation and characterization of lacidipine as an oral fast dissolving film

Background: Fast dissolving oral drug delivery system is solid dosage form which disintegrates or dissolves within second when placed in the mouth without need of water or chewing. In present investigation, an attempt has been made to develop oral fast dissolving film of calcium channel blocker lacidipine. Method: Five formulas were prepared by solvent casting method using HPMC (METOLOSE)® as a film forming polymer and evaluated for their physical characteristics such as thickness, weight variation, folding endurance, drug content, disintegration time and in vitro drug release. The compatibility of the drug in the formulation was confirmed by FTIR and DSC studies. Result and Conclusion: The optimized formula F1 showed minimum in vitr

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Publication Date
Sun Dec 22 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Enhancement of Solubility and Improvement of Dissolution Rate of Atorvastatin Calcium Prepared as Nanosuspension

       Atorvastatin have problem of very slightly aqueous solubility (0.1-1 mg/ml). Nano-suspension is used to enhance it’s of solubility and dissolution profile. The aim of this study is to formulate Atorvastatin as a nano-suspension to enhance its solubility due to increased surface area of exposed for dissolution medium, according to Noyes-Whitney equation.

        Thirty one formulae were prepared to evaluate the effect of ; Type of polymer, polymer: drug ratio, speed of homogenization, temperature of preparation and inclusion of co-stabilizer in addition to the primary one; using solvent-anti-solvent precipitation method under high power of ultra-sonication.

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Publication Date
Thu Jan 04 2018
Journal Name
International Journal Of Applied Pharmaceutics
FORMULATION AND IN VITRO EVALUATION OF BROMOCRIPTINE MESYLATE AS FAST DISSOLVING ORAL FILM

Objective: The aim of this study was to formulate and in vitro evaluate fast dissolving oral film of practically insoluble bromocriptine mesylate to enhance its solubility and to improve its oral bioavailability by avoiding first pass effect as well as to produce an immediate release action of the drug from the film for an efficient management of diabetes mellitus type II in addition to an improvement of the patient compliance to this patient- friendly dosage form. Methods: The films were prepared by the solvent casting method using hydroxypropyl methylcellulose of grades (E3, E5, E15), polyvinyl alcohol (PVA), pectin and gelatin as film-forming polymers in addition to polyethene glycol 400 (PEG400), propylene glycol (PG) and glycerin were

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Publication Date
Fri Aug 02 2024
Journal Name
Farmacia
SOLUPLUS AND SOLUTOL HS-15 OLMESARTAN MEDOXOMIL NANOMICELLE BASED ORAL FAST DISSOLVING FILM: IN VITRO AND IN VIVO CHARACTERIZATION

Olmesartan medoxomil (OM) has low bioavailability and limited solubility. To enhance bioavailability, fast dissolving films (FDF) with mixed micelles of soluplus (SPL) and solutol HS15 (STL H15) were developed using solvent casting. The optimised formula, FM2, used polyvinyl alcohol (PVA) and showed high entrapment efficiency, rapid disintegration, and significant improvement in OM bioavailability compared to the market tablet (Olmetec®). FM2 also demonstrated stability and potential for enhanced drug delivery.

Publication Date
Sat Apr 23 2022
Journal Name
Research Journal Of Pharmacy And Technology
Effect of Natural/ Synthetic Polymers and Super disintegrants on the Formulation of Zafirlukast Fast Dissolving Film

Fast-dissolving films are one of the interested delivery systems for oral solid dosage forms to overcome swallowing difficulty for geriatric and pediatric patients. Zafirlukast (ZLK) is one of the most commonly used oral medication for treatment of asthmatic patients particularly mild to moderate cases. Oral fast dissolving films of ZLK were prepared using two different filming forming polymers, hydroxypropyl methylcellulose (HPMC) and sodium carboxymethyl cellulose (SCMC). Different concentrations of the 2 polymers were used to prepare 10 formulas. Other excipients were also added at various ratios to produce 10 different formulations. These were maltodextrin, crosspivodone, polyvinylpyrrolidone (PVP), and banana powder. In vitro c

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Publication Date
Sat Jun 19 2021
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Characterization of Isradipine Nanoparticle for Dissolution Enhancement

Isradipine belong to dihydropyridine (DHP) class of calcium channel blockers (CCBs). It is  used in the treatment of hypertension, angina pectoris, in addition to Parkinson disease. It goes under the BCS class II drug (low solubility-high permeability). The drug will experience extensive first-pass metabolism in liver, therefore, oral bio-availability will be approximately15 to 24 %.

 

 The aim of this study was to formulate and optimize a stable  nanoparticles of a highly hydrophobic drug, isradipine by anti-solvent microprecipitation Method to achieve the higher in vitro dissolution rate, so that it will be absorbed by intestinal lymphatic transport in order to avoid hepatic first-pass metabolism&nbs

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Publication Date
Thu Jun 09 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Improvement of the Solubility and Dissolution Characteristics of Risperidone via Nanosuspension Formulations

Risperidone is an atypical antipsychotic drug that is used for treating schizophrenia, bipolar mania, and autism. Risperidone rebalances dopamine and serotonin to improve thinking, mood, and behavior by working on dopamine and serotonin α2receptor antagonism. Risperidone has poor solubility and high permeability through the intestine, so it belongs to Biopharmaceutical Classification System (BCS) class II exhibits poor oral biopharmaceutical properties.

 The aim of the present work was to improve solubility and dissolution of Risperidone by preparing nanosuspension using different stabilizers and different solvents‎ in a method known as solvent-antisolvent precipitation method.  Twenty-eight formulas were prepared

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Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Optimization of Oral Fast Dissolving Prochloperazine Maleate Tablets

Prochloperazine maleate (PCM) is one of the most prescribed phenothiazine. The purpose of the present research was to develop fast dissolving tablets of PCM with β-cyclodextrin inclusion complex. Tablets prepared  by wet granulation with sublimation and by using  different superdisintegrants type [ low-hydroxypropylcellulose LH21 (L-HPC LH21), carboxymethylcellulose calcium (ECG505), crospovidone (CP)], and different type of subliming agents (urea and ammonium bicarbonate (AB)). Tablets evaluated for its % friability, disintegration time, wetting time, hardness, content uniformity, weight variation, in vitro dissolution studies. For further enhancement of disintegration and dissolution, PCM orodispersible tablet were formula

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Publication Date
Sun Dec 22 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Characterization of Itraconazole as Nanosuspension Dosage Form for Enhancement of Solubility

Abstract

            Itraconazole is a triazole antifungal given orally for the treatment of oropharyngeal and vulvovaginal candidiasis, for systemic infections including aspergillosis, candidiasis,  and for the prophylaxis of fungal infections in immunocompromised patients.

           The study aimed to formulate a practical water-insoluble Itraconazole, with insufficient bioavailability as nanosuspension to increase aqueous solubility and improve its dissolution and oral bioavailability.

          Itraconazole nanosuspension was produced by a

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Enhancement of Atorvastatin Tablet Dissolution Using Acid Medium

         In this study some generic commercial products of Atorvastatin tablets were evaluated by dissolution test in acid medium by comparing with that of parent drug Lipitor of Pfizer Company. Some of solubilizing agents were studied in formulation  of Atorvastatin tablet including;  surface active agent  and PEG 6000 .The most effective factor was the  use of PEG6000 in formulation of Atorvastatin tablet which improved the dissolution and the results of dissolution profile of formulated tablet in this work  was bioequivalent to that of Lipitor .The quantitative analysis of this work was performed by using reversed phase liquid chromatography and a proper mixture of &nbsp

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