FORMULATION AND EVALUATION OF ANTIPARKINSON’S DRUG INCORPORATED TRANSDERMAL FILMS

Objective: Ropinirole suitable for transdermal delivery due to its small molecular size (260.37 g/mol), optimum log p (2.3), and low oral bioavailability (50%) due to first-pass metabolism, the short elimination half-life of 4–6 h. Dose of drug is 6 mg/day. Hence, in the present study, an attempt was made to deliver antiparkinson’s drug through transdermal route in the form of transdermal film to attain sustained release using different concentration of drug, polymers stabilizers. Methods: Among the different formulations of matrix type (F1 to F5), F2 and F4 formulations were optimized based on crystallinity. These formulations were carried out for in vitro permeation studies. Out of these two formulations, F4 formulation showed target drug release. Results and Discussion: The formulation F4 containing 2 mg drug, 600 mg hydroxypropyl methylcellulose E15 and 50 mg of Eudragit RS 100 was selected as optimized formulation, after considering its microscopic examination throughout stability, % drug content (98.4%), drug permeated through the cellophane membrane at the end of 72 h, and evaluation of physicochemical characterization parameters such as thickness, weight variation, flatness, folding endurance, moisture content, and tensile strength. Conclusion: The results of physicochemical characterization were ensured the stability of the films. The drug permeation profile was also found to follow Higuchi kinetic model.

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DESIGN AND EVALUATION OF CHITOSAN-HPMC POLYMERIC FILMS FOR TRANSDERMAL DELIVERY OF CAPTOPRIL

INDIAN DRUGS ◽

10.53879/id.57.06.12317 ◽

2020 ◽

Vol 57 (06) ◽

pp. 69-72

Author(s):

Rajesh Sreedharan Nair ◽

Manickam Balamurugan ◽

Meng Sheng Teng

Keyword(s):

Transdermal Delivery ◽

Moisture Absorption ◽

Hydroxypropyl Methylcellulose ◽

Physicochemical Characterization ◽

Scanning Calorimetry ◽

Drug Permeation ◽

Evaporation Technique ◽

Model Drug ◽

The Stability

Drug permeation through the skin layers remains a major challenge in transdermal drug delivery. In this study, the permeation enhancing property of chitosan together with its rate-controlling property has been utilized in the development of an efficient transdermal delivery system, using captopril as a model drug. Chitosan-hydroxypropyl methylcellulose (HPMC) films were developed by solvent evaporation technique. The films were characterized for appearance, thickness, weight uniformity, drug content, folding endurance and moisture absorption. Drug-polymer interaction was assessed using ATR-FTIR spectroscopy and Differential Scanning Calorimetry. The in vitro permeation carried out in Franz-type diffusion cells using synthetic Strat-M® membrane, demonstrated that the film coded F2 (Chitosan:HPMC = 50:50) showed a significant increase in drug permeation than F1 (Chitosan:HPMC = 90:10) with a flux value 86.7 µg/cm2/h. The physicochemical characterization and the stability studies confirmed that the formulated films were chemically and physically stable.

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DESIGN AND EVALUATION OF INTRAGASTRIC BUOYANT TABLETS OF VENLAFAXINE HYDROCHLORIDE

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i5.16948 ◽

2017 ◽

Vol 10 (5) ◽

pp. 166

Author(s):

Parasuram Rajam Radhika ◽

Nishala N ◽

Kiruthika M ◽

Sree Iswarya S

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Xanthan Gum ◽

Hydroxypropyl Methylcellulose ◽

Methyl Cellulose ◽

In Vitro Drug Release ◽

Weight Variation ◽

Floating Drug Delivery ◽

Venlafaxine Hydrochloride

Objective: The present study was undertaken to prolong the release of orally administered drug. The aim is to formulate, develop, and evaluate theintragastric buoyant tablets of venlafaxine hydrochloride, which releases the drug in a sustained manner over a period of 12 hrs. Different formulationswere formulated using the polymers Carbopol 934 P, xanthan gum, hydroxypropyl methylcellulose (HPMC K100M) with varying concentration ofdrug: Polymer ratio of 1:1, 1:1.5, 1:2, in which sodium bicarbonate acts as gas generating agent, and microcrystalline cellulose as a diluent.Methods: The tablets were prepared by direct compression and evaluated for tablet thickness, weight variation, tablet hardness, friability, in vitrobuoyancy test, in vitro drug release and Fourier transform infrared spectroscopy. Formulations were evaluated by floating time, floating lag time and in vitro drug release. Dissolution profiles were subjected for various kinetic treatments to analyze the release pattern of drug.Results: It was found that drug release depends on swelling, erosion, and diffusion, thus following the non-Fickian/anomalous type of diffusion.Formulation F8 was considered as an optimized formulation for gastro retentive floating tablet of venlafaxine hydrochloride. The optimizedformulation showed sustained drug release and remained buoyant on the surface of the medium for more than 12 hrs. As the concentration of HPMCK100M increases in the formulation the drug release rate was found to be decreased. The optimized formulation was subjected for the stability studiesand was found to be stable as no significant change was observed in various evaluated parameters of the formulation.Conclusion: It can be concluded that floating drug delivery system of venlafaxine hydrochloride can be successfully formulated as an approach toincrease gastric residence time, thereby improving its bioavailability.Keywords: Venlafaxine hydrochloride, Intragastric buoyant, Floating drug delivery systems, Hydroxypropyl methyl cellulose K100M, Carbopol 934 P,Xanthan gum.

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Formulation and investigation of crushed puffed rice-chitosan-HPMC based polymeric blends as carrier for sustained stomach specific drug delivery of piroxicam using 3(2) Taguchi mathematical design studies

International Current Pharmaceutical Journal ◽

10.3329/icpj.v6i11.36435 ◽

2018 ◽

Vol 6 (11) ◽

pp. 61-80 ◽

Cited By ~ 1

Author(s):

Shashank Soni ◽

Veerma Ram ◽

Anurag Verma

Keyword(s):

Drug Release ◽

Release Kinetics ◽

Drug Loading ◽

Hydroxypropyl Methylcellulose ◽

Research Work ◽

Pharmaceutical Journal ◽

Weight Variation ◽

Zero Order Release ◽

Puffed Rice

In the present experimental investigation an attempt has been made to assess the utility of Crushed Puffed Rice (CPR)-High Molecular Weight Chitosan (HMWCH)-Hydroxypropyl Methylcellulose K15M (HPMC K15M) as a polymeric carrier for the sustained stomach delivery of Piroxicam (PRX). A total of nine formulations were prepared by using 3 (2) Taguchi factorial design, physically blending drug and polymer(s) followed by encapsulation into hard gelatin capsules size 1. The prepared capsules were evaluated for various performance such as weight variation, drug contents, in vitro buoyancy and drug release in 0.1 M HCl. The effect of drug loading on in vitro performance of the formulations was also determined. Crushed puffed rice (CPR) remained buoyant for up to average time span of 06 hr as an unwetted irregular mass in 0.1 M HCl. However, when combined with HMWCH or HPMC K15M or HPMC K15M + HMWCH a low -density cylindrical raft type hydrogel was formed which remained buoyant for up to 12 hr and released up to 99% drug in a sustained manner from 8 to 12 hr following zero order release kinetics. It was also observed that drug release from drug + CPR matrices followed Fickian mechanism. Combination of CPR + HMWCH or HMWCH + HPMC K15M also follows Fickian mechanism. Obtained data from the research work suggests that CPR in combination with HMWCH or HPMC K15M or HPMC has sufficient potential to be used as a carrier for stomach specific delivery of gastric irritant drug like PRX.Soni et al., International Current Pharmaceutical Journal, April 2018, 6(11): 61-80http://www.icpjonline.com/documents/Vol6Issue11/01.pdf

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FORMULATION AND EVALUATION OF PROCHLORPERAZINE MALEATE SUSTAINED RELEASE FLOATING TABLET

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2017v9i2.15665 ◽

2017 ◽

Vol 9 (2) ◽

pp. 89 ◽

Cited By ~ 1

Author(s):

Ahmed Abdulameer Albadry ◽

Wedad K. Ali ◽

Fouad A. Al-saady

Keyword(s):

Chemical Interaction ◽

Hydroxypropyl Methylcellulose ◽

Angle Of Repose ◽

Weight Variation ◽

Compressibility Index ◽

Floating Drug Delivery ◽

Tap Density ◽

Floating Tablet ◽

Optimum Formula

Objective: The objective of this study was to formulate once daily sustained oral release floating tablet of prochlorperazine maleate, this floating tablet has many advantages like reduction in dosing frequency, increase bioavailability, enhance patient compliance, and improve drug solubility.Methods: The prochlorperazine maleate floating tablets were formulated by using hydrophilic swellable polymer and gas generating agent. In this study, 15 formulas were prepared with many variables in order to achieve an optimum dissolution and floating behaviour for the floating tablet. The all prepared formulas were tested for bulk density, tap density, angle of repose, Carr's Index, thickness, weight variation, hardness, friability, drug content, in vitro dissolution test, in vitro buoyancy, and swelling index.Results: Formula (F2) that contain 55% (w/w) <a href="https://www.google.iq/url?sa=t&rct=j&q=&esrc=s&source=web&cd=3&ved=0ahUKEwjh383ow9LPAhWF6RQKHRChCVgQFggpMAI&url=https%3A%2F%2Fwww.ulprospector.com%2Fen%2Fna%2FFood%2FDetail%2F895%2F563462%2FBenecel-Hydroxypropylmethylcellulose-HPMC-K4M&usg=AFQjCNGgfyJECkumK5cpU_6luVwwJ2fKxA&bvm=bv.135258522,d.d24">hydroxypropyl methylcellulose</a> k4M (HPMCK4M), 5 % (w/w) sodium bicarbonate (NaHCO3) have acceptable flow properties and compressibility index and good physical properties with floating lag time (16±0.57) seconds and total floating time (32±0.29) h with 100% release of prochlorperazine maleate at the end of 24 h. Fourier transform infrared spectroscopy (FTIR) study of optimum formula (F2) showed no chemical interaction between the drug and the excipients that used in the formula.Conclusion: It can be concluded that that the selected formula (F2) can be a promising formula for the preparation of gastro retentive floating drug delivery systems of prochlorperazine maleate.

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Design, Development and Evaluation of Instant Release Oral Thin Films of Flunarizine

International Journal of Pharmaceutical Sciences Review and Research ◽

10.47583/ijpsrr.2021.v71i01.016 ◽

2021 ◽

Vol 71 (1) ◽

Author(s):

Asfiya Fatima ◽

Mamatha Tirunagari ◽

Divya Theja Chilekampalli

Keyword(s):

Thin Films ◽

Drug Release ◽

Hydroxypropyl Methylcellulose ◽

Rapid Onset ◽

In Vitro Dissolution ◽

Design Development ◽

Onset Of Action ◽

Weight Variation ◽

Accelerated Stability

The main objective of the present study was to prepare and evaluate the instant release oral thin films of Flunarizine, in order to enhance the bioavailability of the drug and to provide rapid onset of action thereby improving patient compliance. The instant release oral thin films of Flunarizine were prepared by solvent casting method using film forming polymer like Hydroxypropyl Methylcellulose E-15. The film was evaluated for various physicochemical parameters that include thickness, weight variation, folding endurance, tensile strength, drug content and in vitro drug release studies. No differences were observed in in vitro dissolution of drug from the formulated film F1-F9 as the film instantly gets wet by dissolution medium. The drug release for F5 formulations was about 98.1%. The accelerated stability studies for the optimized film formulations F5 were performed that indicates that the formulated instant release oral thin films were unaffected after initial and 3 months storage under accelerated conditions.

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Development and evaluation of miconazole mucoadhesive tablets for oropharyngeal candidiasis

Tropical Journal of Pharmaceutical Research ◽

10.4314/tjpr.v16i10.3 ◽

2017 ◽

Vol 16 (10) ◽

pp. 2325-2330

Author(s):

Qiong Jin ◽

Wei Chen ◽

Wan Wu

Keyword(s):

Drug Release ◽

Factorial Design ◽

Hydroxypropyl Methylcellulose ◽

Extended Period ◽

Content Uniformity ◽

Oropharyngeal Candidiasis ◽

In Vitro Drug Release ◽

Weight Variation ◽

Mucoadhesive Tablets

Purpose: To develop mucoadhesive tablets containing miconazole (MCZ) for the treatment of oropharyngeal candidiasis, using chitosan and hydroxypropyl methylcellulose (HPMC) as mucoadhesive polymers.Methods: Mucoadhesive tablets were formulated and optimized using a 23 factorial design and direct compression method. The independent variables were compression force and concentrations of chitosan and HPMC, while mucoadhesion time and in vitro drug release were dependent variables. Tablet characterization was carried out by evaluating hardness, thickness, tablet weight variation, content uniformity, friability and in vitro drug release at salivary pH (pH 6.8).Results: The tablets showed good mucoadhesion for an extended period (8 h), and their physical characteristics were within acceptable ranges. Drug release ranged from 60.5 % to 80.8 %.Conclusion: These results indicate that the mucoadhesive MCZ tablets formulated with chitosan and HPMC possess potential for the development of therapeutic preparations for management of oropharyngeal candidiasis.Keywords: Miconazole, Oropharyngeal candidiasis, Factorial design, Mucoadhesion, Chitosan, Drug release

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FABRICATION AND CHARACTERIZATION OF FAST DISSOLVING FILMS OF ECLIPTA PROSTRATE LEAVES EXTRACT TO TREAT MOUTH ULCERS

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i5.41597 ◽

2021 ◽

pp. 263-271

Author(s):

MANIKIRAN S. S. ◽

NAGAM SANTHI PRIYA ◽

B. AUBINE MOLLY ◽

LAKSHMI PRASANTHI NORI

Keyword(s):

Drug Release ◽

Moisture Loss ◽

Disintegration Time ◽

Weight Variation ◽

Eclipta Prostrata ◽

Release Studies ◽

Study Results ◽

The Stability ◽

Oral Films

Objective: This research focused on the design of fast dissolving herbal film of Eclipta Prostrate leaves extract for mouth ulcers. Methods: The extract of Eclipta Prostrata leaves was formulated as films by solvent casting method using various polymers viz., HPMC E5, HPMC E15, sodium alginate and PVA. The films were designed by using propylene glycol as a plasticizer, SSG as super disintegrate and honey as a sweetener. Furthermore, the films were evaluated for thickness, folding endurance, weight variation, % elongation, surface pH, % moisture uptake, % moisture loss, disintegration and in vitro drug release study. Results: The revealed that all the films were good in appearance and had a smooth texture. Out of all ten formulations, F3 and F5 disintegrated rapidly with a disintegration time of 27 and 32 seconds. The drug release studies revealed that all the formulations had a good release profile, but the F3 formulation showed rapid release i.e. 83.57% in 4 min. The stability studies revealed that the formulations F3 and F5 were found good with non-tackiness, easily separable and disintegrated at 29 and 33 sec respectively with no appearance and drug release. Conclusion: The research revealed that Eclipta prostrate leaves extract can be formulated into oral films for the treatment of mouth ulcers with improved bioavailability and expected patient compliance.

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Design and evaluation of Pulsatile drug delivery of Losartan Potassium

Dhaka University Journal of Pharmaceutical Sciences ◽

10.3329/dujps.v12i2.17610 ◽

2014 ◽

Vol 12 (2) ◽

pp. 119-123

Author(s):

MS Ashwini ◽

Mohammed Gulzar Ahmed

Keyword(s):

In Vitro Release ◽

Losartan Potassium ◽

Stability Studies ◽

In Vitro Drug Release ◽

Drug Content ◽

Weight Variation ◽

Release Studies ◽

The Stability ◽

Vitro Release

The study was designed for the investigation of pulsatile device to achieve time or site specific release of Losartan potassium based on chronopharmaceutical considerations. The basic design involves the preparation of cross linked hard gelatin capsules by using formaldehyde, then the drug diluent mixture were prepared and loaded in, which was separated by using hydrogel plugs of different polymers of different viscosities. Prepared formulations were subjected to evaluation of various parameters like weight variation, percentage drug content, in vitro drug release and stability studies. Weight variation and percentage drug content results showed that they were within the limits of official standards. The in-vitro release studies revealed that the capsules plugged with polymer HPMC showed better pulsatile or sustained release property as compared to the other formulations. The stability studies were carried out for all the formulations and formulations F1 & F2 were found to be stable. Dhaka Univ. J. Pharm. Sci. 12(2): 119-123, 2013 (December) DOI: http://dx.doi.org/10.3329/dujps.v12i2.17610

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FORMULATION AND EVALUATION OF GASTRORETENTIVE TABLETS OF ANTIULCER DRUG

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2016.v9i6.10360 ◽

2016 ◽

Vol 9 (6) ◽

pp. 48

Author(s):

Pranali Shivaji Salunkhe

Keyword(s):

Drug Release ◽

Extended Period ◽

Lag Time ◽

In Vitro Dissolution ◽

Content Uniformity ◽

In Vitro Drug Release ◽

Gastric Residence Time ◽

Target Drug ◽

Weight Variation

ABSTRACTGastroretentive floating drug delivery system is utilised to target drug release in the stomach or to the upper part of intestine. Lansoprazole is proton pump inhibitor intended for oral administration used as antiulcer agent. The present investigation involved formulation and evaluation of Gastroretentive floating tablets of Lansoprazole for prolongation of gastric residence time with a view to deliver the drug at sustained and controlled manner in gastrointestinal tract. The tablets of Lansoprazole were prepared by direct compression method using gas generating agent and different polymer combinations (HPMCK4M, HPMC K100M, Psyllium husk) . The prepared tablets of Lansoprazole were evaluated for hardness, thickness, friability, weight variation, drug content uniformity, buoyancy lag time, total floating time, swelling index, in-vitro dissolution study. The varying concentration of gas generating agent and polymers were found to affect on in-vitro drug release, floating lag time and swelling index. In vitro drug release of floating Gastroretentive tablet of Lansoprazole shown that the formulation F2 was found to be the best formulation as it releases 97.9% Lansoprazole in a controlled manner for extended period of time (upto 12 hrs.)Keywords: Lansoprazole, Gastroretentive, floating tablet, total floating time.

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DEVELOPMENT, FORMULATION AND EVALUATION OF MECLOFENAMATE FAST DISSOLVING TABLETS

Journal of Biomedical and Pharmaceutical Research ◽

10.32553/jbpr.v10i1.838 ◽

2021 ◽

Vol 10 (1) ◽

pp. 59-67

Author(s):

Mahipal Shakkarwal ◽

Dr. Mukesh Sharma ◽

Dr. Ram Garg ◽

Shankar Lal Soni ◽

Gopal Kumar Paswan ◽

...

Keyword(s):

Drug Release ◽

Angle Of Repose ◽

In Vitro Dissolution ◽

Dissolution Time ◽

Onset Of Action ◽

Disintegration Time ◽

Weight Variation ◽

Suitable Treatment ◽

The Stability

The demands for fast dissolving tablets have received ever increasing day by day during the last 10-15 years for the onset of action. In the present study, the effect of superdisintegrant was compared with synthetic super disintegrants and other conventional super disintegrants in the of fast dissolving tablet formulation of Meclofenamate. Meclofenamate is an antihypertensive drug and in case of hypertension immediate treatment is required so the proposed investigation is totally based to provide the suitable treatment for hypertension. In the present work 9 formulations of Fast dissolving tablets of Cilnidipine were prepared by using Synthesized Co-proceed was evaluated and compiles with the official standards, parameters and specifications. Various formulations were prepared using four different superdisintegrant namely- kyron T-304, sodium starch glycolate, cross carmelose sodium with three concentrations (2%, 4%, 6%) by direct compression method. The blend was evaluated for pre-compression parameters like Angle of repose , bulk density , tapped density , and then tablet evaluated post-compression parameters like thickness , drug content , hardness , weight variation , wetting time , friability , disintegration time , dissolution time, drug release study. Formulation A8 showed the lowest disintegration time and in-vitro dissolution studies recorded that formulation A8 showed 98.64% drug release at the end of 3 minutes. The best formulations were also found to be stable and optimized formulations were subjected to the stability studies as per ICH guideline and standards.

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