scholarly journals Ciprofloxacin Release from Polymeric Films. Modeling and Pharmaceutical Parameters Determination

Proceedings ◽  
2020 ◽  
Vol 78 (1) ◽  
pp. 8
Author(s):  
Cintia A. Briones Nieva ◽  
Mercedes Villegas ◽  
Analia I. Romero ◽  
Alicia G. Cid ◽  
Santiago N. Campos ◽  
...  
Keyword(s):  
In Vitro Release ◽  
Absorption Efficiency ◽  
Physiological Solution ◽  
Dissolution Time ◽  
Uv Spectrophotometry ◽  
Lumped Model ◽  
Casting Technique ◽  
Orbital Shaking ◽  
Time Required

Ciprofloxacin (Cipro) is a broad-spectrum antibiotic used against both Gram (+) and Gram (−) bacteria. Its biological half-life is very short (4–5 h) and its conventional administration forms present a limited absorption efficiency. For this reason, the aim of this work was to study other administration strategies based on topical films. Sodium alginate (SA), a naturally occurring polymer, and a recombinant elastin-like polymer (rELP) produced by advanced genetic engineering techniques were evaluated as potential carrier systems. The films were obtained by the casting technique, adding the Cipro by direct dispersion in the polymer solution using 16.6% w/w rELP or 1.5% w/w SA. The in vitro release assays were performed at 37 °C in physiological solution and with orbital shaking at 90 rpm. Cipro concentration was determined by ultraviolet (UV) spectrophotometry at 276 nm. The release profiles were analyzed and adjusted using the Lumped model developed and validated by our research group. Pharmaceutical interest parameters were calculated and compared for both polymer-Cipro systems: the time required to reach 80% of the drug dissolved (t80%), the dissolution efficiency (DE) and the mean dissolution time (MDT). The SA-Cipro platform released the 80% of the drug in 35 min, while this parameter was 209 min for the rELP-Cipro system. The MDT80% was 8.9 and 53 min for the SA-Cipro and rELP-Cipro, respectively, while the DE, evaluated at 200 min, was 66.6 and 58.8 for each platform, respectively. These parameter values demonstrate that the rELP films were able to modulate the drug release rate and for the SA ones, release can be considered immediate. Therefore, both systems are promising strategies for the topical application of Cipro.

Formulation and Evaluation of Orodispersible Tablets Containing Taste Masked Mirabegron Resinate

2021 ◽  
pp. 4736-4742
Author(s):  
Sarika S. Malode ◽  
Milind P. Wagh
Keyword(s):  
Overactive Bladder ◽  
Bitter Taste ◽  
In Vitro Release ◽  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Disintegration Time ◽  
Orodispersible Tablets ◽  
Weight Variation

The objective of present work was to develop taste masked orodispersible tablets of mirabegron. Mirabegron is beta 3 adrenoceptor agonist used to treat overactive bladder. Overactive bladder (OAB) is defined as a symptom syndrome showing feeling of urgency to urinate, typically accompanied by frequent daytime and nocturnal urination, in the absence of proven infection or other obvious pathology. Over active bladders are generally common in geriatrics. Moreover, this drug has a very strong bitter taste. Frequent dosing requires frequent water intake, which further aggregates the condition of over active bladder and bitter taste of drug affects patient compliance. Hence a need arises to mask the bitter taste for development of an ODT which does not require consuming water with every dosage. In this work, the bitter taste of mirabegron was masked by forming a complex with an ion exchange resin tulsion 344. The drug resin complexation process was optimized for resin activation, drug: resin ratio, soaking time and stirring time. In –vitro release studies revealed complete drug elution from the complex within 10 minutes in pH 1.2 buffer. The taste-masked complex was then formulated into palatable orodispersible tablets using a direct compression approach by use of superdisintegrants to achieve a rapid disintegration. The tablets were evaluated for weight variation, hardness, friability, drug content, wetting time, In- vivo disintegration time and in-vitro dissolution time.

TASTE MASKING OF OXYBUTYNIN CHLORIDE USING LIPID EXCIPIENTS AND FORMULATION AS ORODISPERSIBLE TABLETS FOR GERIATRIC POPULATION

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (10) ◽  
pp. 39-46
Author(s):  
V Prakash ◽  
◽  
L. Keshri ◽  
V. Sharma ◽  
K. Pathak
Keyword(s):  
In Vitro Release ◽  
In Vitro Dissolution ◽  
Taste Masking ◽  
Dissolution Time ◽  
Disintegration Time ◽  
Geriatric Population ◽  
Orodispersible Tablets ◽  
Lipid Excipients

The aim of the present study was to mask the bitter taste of oxybutynin chloride by lipid excipients and to develop its fast disintegrating tablet. For this purpose, a blend of two lipids, glyceryl behenate and glyceryl palmitostearate was utilized for taste masking by solvent evaporation method. The evaporation of solvent was accomplished by freeze drying and taste masked granules were characterized for their micromeritic and rheological properties. The state of dispersion was analyzed by SEM and DSC. Orodispersible tablets were then formulated (F1- F6) using Polyplasdone XL as extragranular superdisintegrant and evaluated for hardness, disintegration time, in vitro dissolution time and in vivo disintegration time. Results indicated that the formulation F6 exhibited minimum in vivo disintegration time of 8 sec with effective taste masking. In vitro release analysis indicated %DE10 and %DE25 of 51.48 and 76.53 respectively. Conclusively, taste masked orodispersible formulation of oxybutynin chloride was developed that could be beneficial for geriatric population.

scholarly journals ENHANCEMENT OF SOLUBILITY AND OPTIMIZATION OF ORALLY DISINTEGRATING FILMS OF ACYCLOVIR

2018 ◽  
Vol 11 (9) ◽  
pp. 280 ◽  
Author(s):  
Bikash Pandey ◽  
Arshad Bashir Khan
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Antiviral Agent ◽  
Disintegration Time ◽  
Casting Technique ◽  
Accelerated Stability ◽  
Full Factorial

Objective: The objective of this work was to prepare and optimize orally disintegrating films of acyclovir (ACV), which is a known antiviral agent. To enhance the solubility of ACV, solid dispersions of ACV were made.Methods: The films were prepared using a solvent casting technique. Full factorial design was utilized for the optimization of the effect of independent variables such as the amount of hydroxypropyl methylcellulose 5 cps, sodium starch glycolate, and propylene glycol on the disintegration time. Other evaluation tests such as drug release, drug content, thickness, and folding endurance of film were also conducted.Results: Compatibility studies by Fourier transform infrared showed that there was no significant interaction between the drug and excipients used. Disintegration time was found to be 43 s for the optimized batch. The in vitro release profile of formulation response disintegrating time in phosphate buffer pH 6.8 revealed that there was a significant increment in drug release of the optimized batch in comparison to the screening batches. Further, short-term accelerated stability studies carried out for 4 weeks for the optimized formulation which proved that the formulated films were stable at the accelerated conditions of temperature and humidity (40±2°C/75±5% RH).Conclusions: It was concluded that such ACV solid dispersion films could be beneficial in enhancement of dissolution and consequently the oral bioavailability of ACV.

FORMULATION AND EVALUATION OF CAFFEINE-LOADED SOLID LIPID NANOPARTICLES TO TREAT CLINICAL MASTITIS

2020 ◽  
pp. 79-85
Author(s):  
B. SURENDRA ◽  
M. NAVEEN KUMAR ◽  
PADMINI IRIVENTI
Keyword(s):  
Sustained Release ◽  
Solid Lipid Nanoparticles ◽  
Evaluation Studies ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Clinical Mastitis ◽  
In Vitro Dissolution ◽  
Uv Spectrophotometry ◽  
Solid Lipid

Objective: The objective of the present study was to formulate and evaluate caffeine-loaded solid lipid nanoparticles (SLNs) in the treatment of clinical mastitis. Methods: These were prepared by homogenization technique using stearic acid, Tween 80, and chloroform as excipients. Pre-formulation studies such as UV spectrophotometry, Fourier transform infrared (FTIR), and differential scanning calorimetry (DSC) were performed for the drug. Entrapment efficiency and in vitro dissolution studies were carried out for prepared SLNs and the optimum formulation (F2) was taken for further studies such as FTIR, DSC, SEM, particle size, and zeta potential analysis. Results: Obtained results stated that prepared SLNs are roughly spherical in nature and are in nano range. These were incorporated in Carbopol gel and further evaluation studies such as pH, spreadability, viscosity, homogenicity, and in vitro drug diffusion studies were carried out. All the results stated that prepared nanogel has shown sustained release of drug. Antimicrobial study was carried out using Staphylococcus aureus and it was confirmed by the appearance of zone of inhibition. Conclusion: Nanogel that contains caffeine SLNs with 1:2 ratio drug:lipid has shown good in vitro release. Sustained release of caffeine drug till 12 h was achieved by delivering it in the form of nanogel.

scholarly journals FABRICATION OF BIOADHESIVE OCUSERT WITH DIFFERENT POLYMERS: ONCE A DAY DOSE

2018 ◽  
Vol 10 (6) ◽  
pp. 309
Author(s):  
Aya M. Dawaba ◽  
Hamdy M. Dawaba ◽  
Amal S. M. Abu El-enin ◽  
Maha K. A. Khalifa
Keyword(s):  
In Vitro Release ◽  
Methyl Cellulose ◽  
Storage Period ◽  
Poly Vinyl Alcohol ◽  
Release Kinetic ◽  
Casting Technique ◽  
Process Characterization ◽  
Vitro Release

Objective: The objective of this current study is to fabricate ocuserts to control the drug release from chosen bioadhesive polymeric matrixes to enhance patient compliance. Ciprofloxacin HCl (CFX HCl) was selected as a model drug.Methods: Different bioadhesive polymers with different film forming capabilities namely Hydroxy Propyl Methyl Cellulose (HPMC K4M), Poly Vinyl Alcohol (PVA), Sodium Carboxy Methyl Cellulose (Na CMC), Hydroxy Propyl Cellulose (HPC), Sodium Alginate (Na Alg.), pullulan and Xanthan Gum (XG) in different ratios were used in fabricating ocuserts using solvent-casting technique. Propylene Glycol (PG) was used as a plasticizer to facilitate the fabrication process. Characterization tests of the developed ocuserts were performed as well as bioadhesive tests and in vitro release studies of the incorporated drug. The obtained results were analysed using different release kinetic models. Stability of the selected ocuserts was investigated at 40±0.5 °C and 75±5% Relative Humidity (RH) for three months’ storage period. In vivo ocular irritation test was performed to investigate the safety of the formula in rabbits’ eyes as well as to test the release profile and thus to estimate In vitro In vivo correlation.Results: All the prepared ocuserts showed the uniformity of film characterization and bioadhesion strength ranged from 240±66 and 158±52dyne/cm2. Selected formula from the in vitro release study tested for in vivo study showed the slow release of ciprofloxacin drug up to 24 h with no signs of eye irritancy. Results for In vitro In vivo correlation showed an excellent correlation with R2 value of 0.9982.Conclusion: PVA based ocuserts proven to be a promising once-daily, effective and safe ocular delivery system of the drug.

scholarly journals IN VITRO RELEASE STUDIES OF CARBAMAZEPINE TABLETS AND BENZOYL METRONIDAZOLE SUSPENSIONS USING THE FLOW-THROUGH CELL APPARATUS AND SIMULATED GASTROINTESTINAL FLUIDS

2017 ◽  
Vol 9 (4) ◽  
pp. 54 ◽  
Author(s):  
Jose Raul Medina ◽  
Jonathan Hernandez ◽  
Marcela Hurtado
Keyword(s):  
In Vitro Release ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Dissolution Time ◽  
Intestinal Fluid ◽  
Simulated Intestinal Fluid ◽  
Release Studies ◽  
Flow Through ◽  
Vitro Release

Objective: To characterize the in vitro release of carbamazepine tablets and benzoyl metronidazole suspensions using the flow-through cell apparatus and simulated gastrointestinal fluids.Methods: Tegretol® tablets, Flagyl® suspension, and generic formulations of each were tested. Release studies were performed using an automated flow-through cell apparatus. Simulated gastric fluid (with and without pepsin) and simulated intestinal fluid (without pancreatin) at 16 ml/min and fasted state simulated intestinal fluid at 8 ml/min, all at 37.0±0.5 °C, were used as dissolution media. The quantity of dissolved carbamazepine and benzoyl metronidazole was determined at 5-min intervals until 60 min at 285 and 278 nm, respectively. Percentage dissolved at 60 min, mean dissolution time, dissolution efficiency values, and t10%, t25%, t50% and t63.2% were calculated. Mean values for all parameters were compared between the reference and generic formulations using Studentʼs t-test. Dissolution data were fitted to different kinetic models.Results: Simulated gastric fluid without pepsin showed no discriminative capability for carbamazepine tablets. Significant differences were observed between the reference and generic formulations for almost all parameters (*P<0.05). In some cases, the logistic model best described the in vitro release of both drugs.Conclusion: Using an apparatus and media that best simulates the gastrointestinal environment, we identified differences in the rate and extent of dissolution of both drugs that could help to optimise the design of interchangeable formulations. Based on the physicochemical characteristics of carbamazepine and benzoyl metronidazole and the conditions in which the formulations were tested, these differences could be of clinical relevance. 

Development of Mucoadhesive Buccal Films of Glipizide

1970 ◽  
Vol 1 (2) ◽  
pp. 177-183
Author(s):  
Mona Semalty ◽  
Ajay Semalty ◽  
Ganesh Kumar ◽  
Vijay Juyal
Keyword(s):  
Controlled Release ◽  
Residence Time ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Potential Candidate ◽  
Sodium Carboxymethylcellulose ◽  
Casting Technique ◽  
Buccal Films

For improving bioavailability in controlled release fashion and to circumvent the hepatic first pass effect of glipizide mucoadhesive buccal films of glipizide were prepared by solvent casting technique. Buccal films were prepared using hydroxy propylmethylcellulose, sodium carboxymethylcellulose, carbopol-934P and Eudragit RL-100. Films were evaluated for their weight, thickness, surface pH, swelling index,       in vitro residence time, folding endurance, in vitro release, ex vivo permeation studies and drug content uniformity. The films exhibited controlled release over more than 6 h. From the study it was concluded that the films containing 5 mg glipizide in 4.9 % w/v hydroxy propylmethylcellulose and 1.5 % w/v sodium carboxymethylcellulose exhibited satisfactory swelling, an optimum residence time and promising drug release thus proved to be potential candidate for the development of buccal films for therapeutic use.

Formulation and In vitro Evaluation of Mucoadhesive Buccal Patches of Ondansetron Hydrochloride

2010 ◽  
Vol 3 (1) ◽  
pp. 860-866
Author(s):  
Shayeda ◽  
Sathish Dharani
Keyword(s):  
Moisture Absorption ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Thickness Variation ◽  
Content Uniformity ◽  
Casting Technique ◽  
Weight Variation ◽  
Ondansetron Hydrochloride

The goal of the present investigation was to design and evaluate mucoadhesive buccal patches of Ondansetron Hydrochloride (OND) which is used for nausea and vomiting associated with cancer chemotherapy and radiotherapy. Permeation of OND was calculated ex vivo using porcine buccal membrane. Buccal films were developed by solvent-casting technique using Hydroxy Propyl Methyl Cellulose(HPMC E15) as mucoadhesive polymer. The patches were evaluated for weight variation, thickness variation, surface pH, moisture absorption, in vitro residence time, mechanical properties, in vitro release, ex vivo permeation studies and drug content uniformity. The formulation F3 was found to give the better results and obeys first order kinetics. 

Development of Mucoadhesive Patches for Buccal Administration of Prochlorperazine: Evaluation of In Vitro Release and Mechanical Properties

1970 ◽  
Vol 1 (1) ◽  
pp. 64-70
Author(s):  
Chandra Sekhar Kolli ◽  
Ramesh Gannu ◽  
Vamshi Vishnu Yamsani ◽  
Kishan V ◽  
Madhsudan Rao Yamsani
Keyword(s):  
Mechanical Properties ◽  
Drug Release ◽  
Moisture Absorption ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Work Of Adhesion ◽  
Casting Technique ◽  
Vitro Release

The aim of this investigation was to develop and evaluate mucoadhesive buccal patches of prochlorperazine (PCPZ). Permeation of PCPZ was calculated in vitro using porcine buccal membrane. Buccal formulations were developed by solvent-casting technique using hydroxy propylmethyl cellulose (HPMC) as mucoadhesive polymer. The patches were evaluated for in vitro release, moisture absorption and mechanical properties. The optimized formulation, based on in vitro release and moisture absorption studies, was subjected for bioadhesion studies using porcine buccal membrane. In vitro flux of PCPZ was calculated to be 2.14 ± 0.01 µg. h–1.cm–2 and buccal absorption was also demonstrated in vivo in human volunteers.             In vitro drug release and moisture absorbed was governed by HPMC content. Increasing concentration of HPMC delayed the drug release. All formulations followed Zero order release kinetics whereas the release pattern was non-Fickian. The mechanical properties, tensile strength (10.28 ± 2.27 kg mm–2 for formulation P3) and elongation at break reveal that the formulations were found to be strong but not brittle. The peak detachment force and work of adhesion for formulation P3 were 0.68 ± 0.15 N and 0.14 ± 0.08 mJ, respectively. The results indicate that suitable bioadhesive buccal patches of PCPZ with desired permeability and suitable mechanical properties could be prepared

scholarly journals Preparation and Evaluation of Rebamipide Film using Casting Technique for Local Action

2019 ◽  
Vol 28 (1) ◽  
pp. 24-36
Author(s):  
Zainab Abdulmohsin Hadi Radhi ◽  
Mowafaq Mohammed Ghareeb
Keyword(s):  
Mechanical Properties ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Physical And Mechanical Properties ◽  
Moisture Loss ◽  
Solvent Casting ◽  
Casting Technique ◽  
Solubility Study ◽  
Poly Ethylene

Abstract The aim of this study was to prepare rebamipide ocular inserts in order to extend its release on the ocular surface for dry eye treatment. Solubility study was applied to the drug with or without l-arginine using different solvents. Solvent casting technique was used to prepare the inserts; l-arginine was used to solubilize the drug, hydroxypropyl methylcellulose grades (E5 and K15M) and poly ethylene glycol 200 were used as excipients. The inserts were evaluated for their physical and mechanical properties, moisture loss% and absorption %, surface pH, and in-vitro drug release. The use l-arginine exhibited an enhancement of rebamipide solubility in both deionized water and phosphate buffer (pH 7.4) by approximately 250 times and 3 times, respectively. The formulations showed uniform weight and thickness except for F1, and all showed uniform drug content. The absence of plasticizer in F1 caused haziness in its appearance and brittleness of the inserts. F3 which contain hydroxypropyl methylcellulose K15M showed good physical and mechanical properties thus was selected for in vitro release and was compared to the marketed brand Mucosta® suspension eye drop; F3 showed significant enhancement in extending the release of rebamipide compared to the reference marketed brand. Keywords: Rebamipide, L-arginine, Ocular insert, Solvent casting technique     ???????                         ????? ?? ??? ??????? ?? ????? ?????????? ?????? ???? ???? ????? ??????????? ??? ??? ????? ????? ????? ?????. ??? ?????  ??????? ?????? ????? ???????? ? ???? ????? ???????? ?????? ??????. ??????? ????? ??????? ? ???? ?????? ??????? ? ?????? ???????? ?????? ?????? ? ?? ??????? ??????????? ?????? ???? ???????? ?????? (K15M  ? E5 ) ? ?????? ?????? ??????? ?????. ?? ????? ?????? ?????????? ? ?????????? ??????? ? ???? ?????? ??????? ??????? ????? ? ?????? ??????? ? ???? ???? ??????????? ???? ??????? ????? ?????  ????? ??????  ?? ???????. ????? ??????? ?? ???????? ???? ??? ????? ??????? ???????????? ?? ?? ?? ????? ??????? ???????? ? ????? ???????? ?????? (?? ??????????? 7.4 ), ?????? ????? 250 ??? ? ???? ???? ??? ???????. ???????? ????? ??? ? ????? ??????? ???? ??? (F1 ) ? ?? ???????????? ????? ????? ?????? ????????.  ??? ???? ???? ??(F1 ) ??? ??? ?????? ??????? ? ??????. ( F3) ???? ????? ??? ??????????? ?????? ???? ?????????? (M 15 K) ???? ???? ???????? ? ????????? ???? ? ??? ?? ??????? ?????? ??????? ?????? ?????? ?? ??????? ? ??????? ??????? ?????? ? ?? ????? ????? ????? ?????? ???? (????????) ? ?? ???? ?? ??????? F3 ???? ????? ???? ?? ????? ????? ???????????? ?????? ??????? ?????? ?????? ?????.                          ??????? ?????????: ??????????, ????????, ??????? ??????, ????? ??????? ? ????         

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