scholarly journals Formulation, in vitro characterization and optimization of taste-masked orally disintegrating co-trimoxazole tablet by direct compression

PLoS ONE ◽  
2021 ◽  
Vol 16 (3) ◽  
pp. e0246648
Author(s):  
Chernet Tafere ◽  
Zewdu Yilma ◽  
Solomon Abrha ◽  
Adane Yehualaw
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Dosage Forms ◽  
Taste Masking ◽  
Direct Compression ◽  
Improve Patient Compliance ◽  
Preliminary Study ◽  
Improve Patient ◽  
Central Composite

Introduction Orally disintegrating tablet (ODT) is a dosage form that overcomes the problem of swallowing which is prevalent in about 35% of the general population. Co-trimoxazole (CTX) is given for patients with HIV for the prophylaxis of opportunistic infection (OI), commonly for pneumocystis carinii pneumonia. It was reported that CTX was associated with a 25–46% reduction in mortality among individuals infected with HIV in sub-Saharan Africa. Esophageal candidiasis which usually comes along with HIV/AIDS is one of AIDS defining illness affecting up to 1 in 5 of people with AIDS. This opportunistic illness is manifested by painful or difficulty of swallowing. In this respect, CTX ODT offer the advantages of both liquid dosage forms in terms of easy swallowing thereby improve patient compliance and solid dosage forms in terms of dose uniformity, stability, lower production, and transportation costs. The objective of this study was to formulate, characterize and optimize CTX ODT which could overcome swallowing problem and improve patient compliance. Co-trimoxazole ODTs were prepared by direct compression technique using a semi synthetic super disintegrant (crospovidone) along with other excipients. Two taste masking techniques were employed, addition of sweetening agent, and solid dispersion by using a pH sensitive polymer, Eudragit E-100 at different ratios (1:1, 1:2 and 1:3). Taste masking was determined by comparing taste threshold value and in vitro drug release. Preliminary study was used to investigate the effect of crospovidone, compression force (CF) and Hydroxypropyl cellulose (HPC) on disintegration time, friability and wetting time (WT). Factorial design was used as it enables simultaneous evaluation of formulation variables and their interaction effect. From the preliminary study, the factors that were found significant were further optimized using central composite design. Design-Expert 8.0.7.1 software was employed to carry out the experimental design. The bitterness threshold concentration of Trimethoprim was found to be 150 μg/ml and the in vitro drug release of the three batches of drug to polymer ratio (F1:1, 1:2 and 1:3) was 2.80±0.05, 2.77±0.00 and 2.63±0.00 respectively. From the optimization study, the optimal concentration for the superdisintegrant was 8.60% w/w and a CF of 11.25 KN which gave a rapid disintegration and WT of 13.79 and 23.19 seconds respectively and a friability of 0.666%. Conclusion In this study, co-trimoxazole ODT was formulated successfully. Central composite design was effectively used to model and optimize friability, DT and WT. The method was found effective for estimating the effect of independent variables on the dependent variables by using polynomial equation and surface plots. Optimization of the response variables was possible by using both numerical and graphical optimization and the predicted optimal conditions were confirmed experimentally and were found to be in good agreement within 5% of the predicted responses. The results of the study showed that CTX ODT had significantly rapid disintegration, less than 1% friability and enhanced dissolution profiles. The successful formulation of CTX ODT can solve difficulty of swallowing of conventional tablets for some group of patients which are unable to swallow solid oral dosage form.

scholarly journals Formulation and Evaluation of Ondansetron HCl Nanoparticles for Transdermal Delivery

2020 ◽  
Vol 29 (2) ◽  
pp. 70-79
Author(s):  
Amjed H Noor ◽  
Mowafaq M. Ghareeb
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Patient Compliance ◽  
Transdermal Delivery ◽  
Patient Adherence ◽  
In Vitro Release ◽  
Burst Release ◽  
Improve Patient Compliance ◽  
Improve Patient

Ondansetron HCl (OND) is a potent antiemetic drug used for control of nausea and vomiting associated with cancer chemotherapy. It exhibits only 60 – 70 % of oral bioavailability due to first pass metabolism and has a relative short half-life of 3-5 hours. Poor bioavailability not only leads to the frequent dosing but also shows very poor patient adherence. Hence, in the present study an approach has been made to develop OND nanoparticles using eudragit® RS100 and eudragit® RL100 polymer to control release of OND for transdermal delivery and to improve patient compliance. Six formulas of OND nanoparticles were prepared using nanoprecipitation technique. The particles sizes and zeta potential were measured using zeta-plus analyzer. The particle morphology was also studied using scanning electron microscopy (SEM). The in-vitro release of the drug from the nanoparticles was carried out in phosphate buffer saline pH 7.4. The particle size of the prepared NPs were in nano size which ranged from (95.34 to 275.84 nm) with positive zeta potential. The drug entrapment efficiency was varied with the drug polymer ratio from 41.87% to 78.45%. The SEM showed uniform shape and regularly distributed particle sizes. The in-vitro drug release study exhibited the sustained release of OND with burst release. The cumulative percentage released after 12 hr. were between were 77.89 and 96.01%. Also the transdermal permeation study show that nanoparticles permeate more efficiently than aqueous solution of the drug through the skin by approximately two fold. OND nanoparticles were prepared successfully using nanoprecipitation method. The controlled drug release aimed for transdermal drug delivery could be obtained by using eudragit RS100 and eudragit RL100 polymers which can reduce dosing frequency, decrease side effects and improve patient compliance.

FORMULATION AND EVALUATION OF MICROSPHERE BASED ORO DISPERSIBLE TABLETS OF SUMATRIPTAN SUCCINATE

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (03) ◽  
pp. 28-38
Author(s):  
S. B. Baliga ◽  
B. P Manjula ◽  
M. Geetha ◽  
Keyword(s):  
Drug Release ◽  
Liquid Paraffin ◽  
Entrapment Efficiency ◽  
Taste Masking ◽  
Direct Compression ◽  
Disintegration Time ◽  
Sumatriptan Succinate ◽  
Dispersible Tablets ◽  
Effervescent Agents

Sumatriptan succinate (SS) is a drug used in the treatment of migraine headaches, but suffers from low patient compliance due to its unpalatable bitter taste. The purpose of the present work was to prepare taste-masked oro dispersible tablets (ODTs) of SS by incorporating drug loaded microspheres into tablets for use in patients experiencing difficulty in swallowing. Microspheres loaded with SS were prepared by solvent evaporation technique. Eudragit EPO, a pH-sensitive aminoalkylmethacrylate copolymer, was used for coating the drug particles, acetone as solvent for the polymer and light liquid paraffin as an encapsulating medium. Drug : polymer ratio of 1:1 was considered to be optimized formulation with a yield of 99.96%, entrapment efficiency of 61.55%, particle size ranging from 30.32 – 90.96μm and in vitro drug release of 85.06% within an hour. FTIR studies suggested absence of drug-excipient interaction. Tablets prepared by direct compression containing microspheres and effervescent agents were evaluated for pre-compression and post-compression parameters. The wetting time, in vitro dispersion time and in vitro disintegration time of the tablets were found to be 39 sec, 35 sec and 32 sec, respectively. The drug release from the tablet was about 85.44% within an hour. The SEM of final ODTs revealed that the microspheres remained intact even after compression. Stability studies indicated that the selected formulation was stable. The results obtained suggested that effective taste-masking was achieved for SS using the technique of microencapsulation and ODTs of acceptable characteristics were obtained by adding effervescent agents followed by direct compression.

Development and In vitro Evaluation of Sustained Release Matrix Tablets of Theophylline using Hydrophilic Polymer as Release Retardant

2009 ◽  
Vol 2 (1) ◽  
pp. 450-456
Author(s):  
D. Nagasamy Venkatesh ◽  
Jawahar N. ◽  
Ganesh G.N.K. ◽  
R. Suresh Kumar ◽  
Senthil V. ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Matrix Material ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Hydrophilic Polymer ◽  
Improve Patient Compliance ◽  
In Vitro Drug Release ◽  
Improve Patient

In the present investigation, an attempt has been made to increase therapeutic efficacy, reduce frequency of administration and improve patient compliance by developing sustained release matrix tablets of theophylline. Sustained release matrix tablets of theophylline were developed by using drug and different concentrations of polymer such as 10, 20, 30, 40 and 50%. Hydroxypropylmethylcellulose (HPMC) was used as a matrix material and microcrystalline cellulose as diluent. All the lubricated formulations were compressed using 10 mm flat faced punches. Compressed tablets were evaluated for uniformity of weight, drug content, friability, hardness, thickness, in vitro dissolution and swelling index. All the formulations were found to be within pharmacopoeial standards. Among the different formulations, F1 showed sustained release of drug for 12 h with 84.23% release. The effect of release modifier (PEG 6000) on in vitro drug release was also studied. Thus, HPMC can be used as an effective matrix former, to extend the release of theophylline

Development and Evaluation of Acetaminophen Orodispersible Disc with Taste-Masking Property

2019 ◽  
Vol 819 ◽  
pp. 233-239
Author(s):  
Phirawat Trirattanapintusorn ◽  
Sirachai Leatpianpanit ◽  
Phurit Thanarangsarit ◽  
Srisagul Sungthongjeen ◽  
Worawut Kriangkrai
Keyword(s):  
Drug Release ◽  
Bitter Taste ◽  
Active Pharmaceutical Ingredient ◽  
Hydraulic Press ◽  
Taste Masking ◽  
Improve Patient Compliance ◽  
Orodispersible Tablet ◽  
Ft Ir ◽  
Co Precipitation ◽  
Improve Patient

Orodispersible tablet (ODT) provides rapid disintegration in the oral cavity. ODT improves the efficacy of using medicines especially in term of compliance in a patient with dysphagia. The major challenge of ODT is a bitter taste of active pharmaceutical ingredient (API); they can lead the patients to refuse medication. This study focused on the developing of the orodispersible disc (ODD) with a taste masking property by preparation of API particle that was taste-masked by polymers. The co-precipitation technique was used for the taste masking. Acetaminophen (APAP) taste-masked particles prepared with different grades of crospovidone were investigated for the taste-masking property. Kollidon® CL-SF exhibited the lowest drug release. An increasing amount of Kollidon® CL-SF caused increasing of APAP release. Particles consisted of APAP:crospovidone at ratio 3:1 showed the lowest drug release. It was probably due to the complexation which was shown by the FT-IR and DSC. Taste-masked particles were compressed as ODD by a hydraulic press machine. The disintegrating time of ODD was at the range of 12.62-17.35 s. The dissolution of ODD was focused on the taste-masking zone (drug release in 1 min). The ODD with ratio 3:1 particle (APAP: Kollidon® CL-SF) showed the highest taste-masking performance, the lowest drug release. All disc formulations completely released APAP after 30 min. Therefore, the preparation of ODD contains taste-masked particles was promising to improve patient compliance of bitter APIs.

scholarly journals Fabrication And In-Vitro Analysis Of Mouth Dissolving Tablets Of Ondansetron Using Water Insoluble Super Disintegrant

2021 ◽  
Vol 001 (01) ◽  
Author(s):  
Jayendrakumar Patel ◽  
Shalin Parikh ◽  
Shwetaben Patel
Keyword(s):  
Dosage Form ◽  
Research Work ◽  
Active Pharmaceutical Ingredient ◽  
Taste Masking ◽  
Direct Compression ◽  
Onset Of Action ◽  
Geriatric Population ◽  
Oral Tablet ◽  
Vitro Analysis

In the present time, a mouth dissolving tablets become popular over conventional oral solid dosage form as it overcome common problem associated with conventional oral tablet dosage form such as issue in swallowing tablets in paediatric as well as geriatric population as well as avoid first pass metabolism and provide quick onset of action as it starts to absorb directly from oral cavity. Ondansetron HCl is used to prevent nausea and vomiting. In case of vomiting as well as in nausea, drug must require to act quickly to treat therapeutic condition of patient in need thereof. Therefore, combining Mouth dissolving technology with Ondansetron HCl as active pharmaceutical ingredient could be potential strategy to provide quick onset of action without swallowing entire tablet. Therefore, aim of the present research work is to fabricate mouth dissolving tablets of Ondansetron HCl using different concentration, i.e. 3%, 5% and 9%w/w, of different water insoluble super-disintegrants, namely Kollidon CL-SF, croscarmellose sodium and sodium starch glycolate. Batch F2 prepared using 6% Kollidon CL-SF with 2.5% sodium saccharine by direct compression method shown better taste masking as well as satisfied all mouth dissolving tablet criteria’s. Thus, it was concluded that taste masked mouth dissolving tablets of Ondansetron HCl could be successfully formulated by direct compression methods using 6% Kollidon CL-SF as water insoluble super-disintegrant that can effectively provide quick onset of action by eliminating need of administration of entire dosage form.

Formulation and In vitro Release Characterization of Metoprolol Succinate Extended Release Tablets

2012 ◽  
Vol 4 (4) ◽  
pp. 1537-1543
Author(s):  
Sakthikumar T ◽  
Rajendran N N ◽  
Natarajan R
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Wet Granulation ◽  
Direct Compression ◽  
Metoprolol Succinate ◽  
Extended Release Formulations ◽  
Vitro Release

The present study was aimed to develop an extended release tablet of metoprolol Succinate for the treatment of hypertension.  Four extended release formulations F1-F4 were developed using varying proportions of hydroxylpropyl-methylcellulose K100M, sodium carboxy methyl cellulose and Eudragit L30 D55 by wet granulation. Five extended release formulations F5-F9 containing HPMC K100M and HPMC 5 cps in varying concentration were developed by direct compression. The physicochemical and in vitro release characteristics of all the formulations were investigated and compared. Two formulations, F7 and F8 have shown not more 25% drug release  in 1st h, 20%-40% drug release at 4th hour, 40%-60% drug release at 8th hour and not less than 80% at 20th hour and the release pattern conform with USP specification for 24 hours extended release formulation. It can be conclusively stated that optimum concentration of HPMC K100M (58%-65%) by direct compression method can yield an extended release of metoprolol succinate for 24 hours.

scholarly journals FORMULATION AND EVALUATION OF ORAL FAST DISINTEGRATING TABLET OF IBUPROFEN USING TWO SUPER DISINTEGRANTS

2017 ◽  
Vol 9 (4) ◽  
pp. 92
Author(s):  
Hrishav Das Purkayastha ◽  
Bipul Nath
Keyword(s):  
Drug Release ◽  
Magnesium Stearate ◽  
Direct Compression ◽  
Compression Method ◽  
Disintegration Time ◽  
Orally Disintegrating Tablet ◽  
Rapid Release ◽  
Weight Variation ◽  
Fast Disintegrating Tablet

Objective: The aim of the present investigation was to design and evaluate orally disintegrating tablet (ODT) of Ibuprofen, a NSAID drug used for the treatment of arthritis with a view to improve its oral bioavailability. The focus of the current study was to develop ODT of Ibuprofen using super disintegrants for ease of administration and its physicochemical characterization.Methods: Tablets were made from blends by direct compression method. All the ingredients were passed through mesh no. 80. All the ingredients were co-ground in a pestle motor. The resulting blend was lubricated with magnesium stearate and compressed into tablets using the Cadmach single punch (round shaped, 8 mm thick) machine.Results: Physicals parameters of the prepared tablets like Hardness, Weight variation, Friability, thickness, drug content etc. found within the limits. The disintegration time of prepared ODTs was in the range of 45 to 55 seconds. In vitro dispersion time was found to be 22 to 52 seconds which may be attributed to faster uptake of water due to the porous structure formed by super disintegrants. Short disintegration and faster release of ibuprofen were observed with Cross carmellose sodium as compared to sodium starch glycollate.Conclusion: It is concluded that F3 offered the relatively rapid release of Ibuprofen when compared with other formulations. The increase in the concentrations of super disintegrants may lead to increase in the drug release. The formulation prepared with cross carmellose sodium was offered the relatively rapid release of Ibuprofen when compared with other concentrations of both the super disintegrant. 

Preparation and Characterization of Mucoadhesive Microcapsules of Gliclazide with Natural Gums

1970 ◽  
Vol 4 (1) ◽  
pp. 38-48 ◽  
Author(s):  
Santhosh Kumar Mankala ◽  
Nishanth Kumar Nagamalli ◽  
Ramakrishna Raprla ◽  
Rajyalaxmi Kommula
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Guar Gum ◽  
Release Kinetics ◽  
Insulin Dependent Diabetes Mellitus ◽  
Dependent Diabetes Mellitus ◽  
Release Mechanism ◽  
Ionic Gelation ◽  
Release Formulation

Gliclazide is an oral hypoglycemic agent used in management of non-insulin dependent diabetes mellitus. Among people who are suffering from long term disorders, the major were categorized under diabetes so, a dosage form is needed to provide continuous therapy with high margin of safety & such dosage form can be achieved by microencapsulation. Gliclazide microspheres with sodium alginate (coat material, gum kondagogu, gum guar and xanthan gum (mucoadhesive agents) were prepared by orifice-ionic gelation and emulsification ionic gelation techniques varying concentrations (1:0.25, 1:0.5, 1:0.75 and 1:1). Formulations were then evaluated for surface morphology, particle shape, Carr’s index, microencapsulation efficiency, drug release, mucoadhesion studies. Compatibility studies were performed by FTIR, DSC, and XRD techniques and no interactions were found between drug and excepients used. The microspheres were found spherical and free flowing with emulsion ionic gelation technique with a size range 400-600μm. % drug content and encapsulation efficiency found in the range of 55%-68% and, 86.23%-94.46% respectively. All microspheres showed good mucoadhesive property in in-vitro wash of test. In vitro drug release studies showed that the guar gum has more potentiality to retard the drug release compared to other gums and concentrations. Drug release from the microspheres was found slow following zero order release kinetics with non-fickian release mechanism stating release depended on the coat: core ratio and the method employed. The concentration of 1:1 of SA: GG (EMG 4) found suitable for preparing the controlled release formulation of gliclazide stating emulsification gelation technique is the best among followed.   Key words: Gliclazide; Natural gums; orifice ionic gelation technique; emulsification ionic gelation technique DOI: http://dx.doi.org/10.3329/sjps.v4i1.8865 SJPS 2011; 4(1): 38-48

scholarly journals Development and Evaluation of Clove and Cinnamon Supercritical Fluid Extracts-Loaded Emulgel for Antifungal Activity in Denture Stomatitis

Gels ◽  
2022 ◽  
Vol 8 (1) ◽  
pp. 33
Author(s):  
Meenakshi Srinivas Iyer ◽  
Anil Kumar Gujjari ◽  
Sathishbabu Paranthaman ◽  
Amr Selim Abu Lila ◽  
Khaled Almansour ◽  
...  
Keyword(s):  
Drug Release ◽  
Cure Rate ◽  
In Vitro Drug Release ◽  
Promising Alternative ◽  
Denture Stomatitis ◽  
Antifungal Effects ◽  
The Common ◽  
Central Composite

Denture stomatitis (DS), usually caused by Candida infection, is one of the common denture-related complications in patients wearing dentures. Clove and cinnamon oils have been acknowledged for their anti-inflammatory, antimicrobial activity, and antifungal effects in the oral cavity. The aim of this study, therefore, was to prepare clove/cinnamon oils-loaded emulgel and to assess its efficacy in treating Candida albicans-associated denture stomatitis. Central composite design was adopted to formulate and optimize clove/cinnamon extracts-loaded emulgel. The formulated preparations were assessed for their physical appearance, particle size, viscosity, spreadability, and in-vitro drug release. In addition, in-vivo therapeutic experiments were conducted on 42 patients with denture stomatitis. The prepared emulgel formulations showed good physical characteristics with efficient drug release within 3 h. In addition, in-vivo antifungal studies revealed that the optimized formula significantly (p < 0.001) reduced Candida colony counts from the denture surface, compared to commercially available gel (240.38 ± 27.20 vs. 398.19 ± 66.73 CFU/mL, respectively). Furthermore, the optimized formula and succeeded in alleviating denture stomatitis-related inflammation with a better clinical cure rate compared to commercially available gel Collectively, herbal extracts-loaded emulgel might be considered an evolution of polyherbal formulations and might represent a promising alternative to the existing allopathic drugs for the treatment of denture stomatitis, with better taste acceptability and no side effects.

scholarly journals Formulation and In Vitro Evaluation of Sustained Release Floating Matrix Tablet of Levofloxacin by Direct Compression Method

2019 ◽  
Vol 9 (4-s) ◽  
pp. 398-403
Author(s):  
Nidhi Kumari Pandey ◽  
Sailesh Kumar Ghatuary ◽  
Amit Dubey ◽  
Prabhat Kumar Jain
Keyword(s):  
Drug Release ◽  
Acute Infection ◽  
Methyl Cellulose ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Compression Method ◽  
Weight Variation

The objective of the present work was to develop Gastro retentive dosage forms which would remain in the stomach and upper part or GIT for a prolonged period of time thereby maximizing the drug release at desired site within the time before GRDFs left the stomach and upper part of the GIT, has provoked a great deal of increased interest in the formulation of such drug as floating drug delivery systems. Levofloxacin, (BCS class I) is a fluoroquinolone anti-bacterial agent. The rationale for the formulation of floating matrix tablet are acidic solubility of levofloxacin, residence of Halicobactor pylori mainly in sub region of stomach and the overdosing associated adverse effect due to continuous intake of drug in acute infection. A simple visible spectrophotometric method was employed for the estimation of levofloxacin at 294 nm and Beer’s law is obeyed in the concentration range of 2-10 μg /ml. Floating matrix tablet of levofloxacin was prepared by direct compression method using different polymers like hydroxyl propyl methyl cellulose (HPMC K4) and carbopol 934 as matrix formation polymers, sodium bicarbonate and citric acid was used as gas generating agents. The FTIR spectra of the levofloxacin and other excipients alone and in combination show the compatibility of the drug and excipients. Six formulations of different polymer percentages were formulated (F1-F6). Pre-compression parameters were evaluated. The influence of matrix forming agents and binary mixtures of them on levofloxacin release was investigated. The formulated tablets were characterized by hardness, friability, thickness, weight variation and in vitro drug release. The formulated tablets had acceptable physicochemical characters. The data obtained from the in-vitro dissolution studies of optimized batch F4were fitted in different models. The optimized formulation F4 showed 99.25% drug content and swelling index of 79.85 %. Drug release mechanism was found to be first order kinetics. Levofloxacin floating tablets exhibited increased gastric residence time, there by improved bioavailability and therapeutic effect of the drug.  

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