scholarly journals Development and Evaluation of Ginkgo biloba L. Extract Loaded into Carboxymethyl Cellulose Sublingual Films

2020 ◽  
Vol 11 (1) ◽  
pp. 270
Author(s):  
Laura Rimkiene ◽  
Juste Baranauskaite ◽  
Mindaugas Marksa ◽  
Laurynas Jarukas ◽  
Liudas Ivanauskas
Keyword(s):  
Mechanical Properties ◽  
Carboxymethyl Cellulose ◽  
In Vitro Release ◽  
Release Profile ◽  
Flavonoid Glycosides ◽  
Disintegration Time ◽  
Chemical Complexity ◽  
Freeze Dried ◽  
Physicochemical Evaluation

Oral bioavailability of flavonoids, including G. biloba extract, is limited due to their chemical complexity, which determines slow dissolution in vitro behavior of the extract. The overall research objective was to compare the effect of increasing freeze-dried G. biloba extract (GFD) concentrations in carboxymethyl cellulose (CMC) films on their mechanical properties, release profile of flavonoid glycosides, stability and disintegration time. Physicochemical evaluation of films was performed by SEM and FTIR. The mechanical properties and in vitro release profile of flavonoid glycosides from the prepared films were characterized in the study. The higher elongation at break and tensile strength values, quick release of flavonoids and good stability were observed in formulation, coded FRG—15 (the film contained 0.4 g of GFD, 0.3 g of glycerol and 2 g of 2% CMC), (p < 0.05). Dissolution rate tests showed that approximately 85% of loaded flavonoid glycosides had been released; the release profile of flavonoid glycosides from FRG-15 had levelled off after only 15 min. The results could lay the groundwork for further studies, concerning the development of sublingual films as G. biloba extract-based dosage forms, which might increase the multifunctional properties and pharmacological activity closer to the desired level.

scholarly journals The Mechanical and In vitro Release Properties of Diazepam from Tablets Containing Fluid Bed Dried and Lyophilized Cocos nucifera Microcrystalline Cellulose

2019 ◽  
pp. 1-14
Author(s):  
Nkemakolam Nwachukwu ◽  
Sabinus Ifeanyi Ofoefule
Keyword(s):  
Mechanical Properties ◽  
Drug Release ◽  
Microcrystalline Cellulose ◽  
Cocos Nucifera ◽  
In Vitro Release ◽  
Disintegration Time ◽  
British Pharmacopoeia ◽  
Fluid Bed ◽  
Vitro Release

Aim: This study aimed to evaluate the mechanical and in vitro release properties of diazepam from tablets containing fluid bed dried and lyophilized microcrystalline cellulose (MCC) obtained from the matured fruit husks of Cocos nucifera (CN). Study Design: Method of experiment. Place and Duration of Study: Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka from March 2015 to September, 2016 Methods:  Dried CN fruit husks were digested in sodium hydroxide to obtain alpha (α) cellulose which on hydrolysis with mineral acid (Hydrochloric acid) solution gave CN-MCC. The dry MCC obtained by either fluid bed or lyophilized drying of the wet CN-MCC were coded MCCF-Cocos and MCCL-Cocos respectively. Both MCCs were used in the formulation of diazepam tablets at 20, 30 and 40% w/w. Avicel PH 102 (AVC-102), was used as comparing standard. The tablets were evaluated for physical and dissolution properties using standard methods. Results: Results show the tablets passed the British Pharmacopoeia specifications for weight uniformity, crushing strength, disintegration time, friability and dissolution. Diazepam tablets containing MCCL-Cocos (coded DCL) were mechanically stronger than those containing MCCF-Cocos (coded DCF). Disintegration time was in the order of DCF > DCL tablets while friability was in the order of DCL < DCF tablets. Diazepam tablets containing AVC-102 (coded DAV) were mechanically stronger than DCL and DCF tablets. The dilution potential was in the order DAV > DCL > DCF. More than 80% of the diazepam content was released from DAV, DCL and DCF tablets. Conclusion: Generally, DAV, DCL and DCF tablets met the British Pharmacopoeia limits for mechanical properties and in vitro drug release with DCL tablets showing significantly (P = .05) superior mechanical properties while DCF showed faster drug release.

Development and In Vitro Characterization of Paclitaxel Loaded Solid Lipid Nanoparticles

2019 ◽  
Vol 9 (1) ◽  
pp. 76-85 ◽  
Author(s):  
R. Nithya ◽  
K. Siram ◽  
R. Hariprasad ◽  
H. Rahman
Keyword(s):  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Release Profile ◽  
Mcf7 Cells ◽  
Solid Lipid ◽  
Cancerous Cells ◽  
Vitro Release

Background: Paclitaxel (PTX) is a potent anticancer drug which is highly effective against several cancers. Solid lipid nanoparticles (SLNs) loaded with anticancer drugs can enhance its toxicity against tumor cells at low concentrations. Objective: To develop and characterize SLNs of PTX (PSLN) to enhance its toxicity against cancerous cells. Method: The solubility of PTX was screened in various lipids. Solid lipid nanoparticles of PTX (PSLN) were developed by hot homogenization method using Cutina HR and Gelucire 44/14 as lipid carriers and Solutol HS 15 as a surfactant. PSLNs were characterized for size, morphology, zeta potential, entrapment efficiency, physical state of the drug and in vitro release profile in 7.4 pH phosphate buffer saline (PBS). The ability of PTX to enhance toxicity towards cancerous cells was tested by performing cytoxicity assay in MCF7 cell line. Results: Solubility studies of PTX in lipids indicated better solubility when Cutina HR and Gelucire 44/14 were used. PSLNs were found to possess a neutral zeta potential with a size range of 155.4 ± 10.7 nm to 641.9 ± 4.2 nm. In vitro release studies showed a sustained release profile for PSLN over a period of 48 hours. SLNs loaded with PTX were found to be more toxic in killing MCF7 cells at a lower concentration than the free PTX.

scholarly journals Antimicrobial Properties and Release Profile of Ampicillin from Electrospun Poly(εepsilon;-caprolactone) Nanofiber Yarns

2010 ◽  
Vol 5 (4) ◽  
pp. 155892501000500 ◽  
Author(s):  
Hang Liu ◽  
Karen K. Leonas ◽  
Yiping Zhao
Keyword(s):  
In Vitro Release ◽  
Antimicrobial Properties ◽  
Fiber Surface ◽  
Electrospun Nanofibers ◽  
Release Profile ◽  
Burst Release ◽  
Spun Yarns ◽  
Surgical Sutures ◽  
Release Model

Poly(εepsilon;-caprolactone) (PCL) electrospun fibers containing ampicillin sodium salt have been produced and twisted into nanofiber yarns. The fiber diameters and crystallinity, the in vitro antimicrobial properties of the yarns, and the in vitro release of ampicillin from yarns containing various ampicillin concentrations are studied. Decreased fiber diameters and reduced diameter variation are observed with the addition of ampicillin salt into the polymer solution. The results from the zone of inhibition test of the yarns against both gram-positive Staphylococcus aureus and gram-negative Klebsiella pneumoniae indicate that the released ampicillin retains its effectiveness after the production processes, therefore the as-spun yarns are antimicrobial active. A burst release of ampicillin from the yarns has been observed in the first hour, and the release is almost completed in 96 hours. The burst release is believed to be due to the low compatibility of ampicillin with PCL, the accumulation of ampicillin on fiber surface and the small fiber diameters. An empirical release model is developed to describe the release profile. The results indicate that the electrospun nanofibers yarns will have a great potential to be used for biomaterials, such as surgical sutures, to decrease the surgical site infection rate.

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.

scholarly journals DESIGN AND IN VITRO/IN VIVO EVALUATION OF EXTENDED RELEASE MATRIX TABLETS OF NATEGLINIDE

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Mohini Sihare ◽  
Rajendra Chouksey
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Release Profile ◽  
Matrix Tablets ◽  
In Vivo Studies ◽  
Release Mechanism ◽  
In Vivo Evaluation

Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily. Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies. Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for. Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release

scholarly journals Enhancement of Solubility and Improvement of Dissolution Rate of Atorvastatin Calcium Prepared as Nanosuspension

2019 ◽  
Vol 28 (2) ◽  
pp. 46-57
Author(s):  
Ahmed H. Ali ◽  
Shaimaa N. Abd-Alhammid
Keyword(s):  
Particle Size ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Precipitation Method ◽  
Size Analysis ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Atorvastatin Calcium ◽  
Freeze Dried

       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. In this study five types of stabilizers (TPGS, PVP K30, HPMC E5, HPMC E15, and Tween80) were used in three different concentrations 1:1, 1:0.75 and 1:0.5 for preparing of formulations. At the same time, tween80 and sodium lauryl sulphate have been added as a co-stabilizer.          Atorvastatin nano-suspensions were evaluated for particle size, PDI, zeta potential, crystal form and surface morphology. Finally, results of particle size analysis revealed reduced nano-particulate size to 81nm for optimized formula F18 with the enhancement of in-vitro dissolution profile up to 90% compared to 44% percentage cumulative release for the reference Atorvastatin calcium powder in 6.8 phosphate buffer media. Furthermore, saturation solubility of freeze dried Nano suspension showed 3.3, 3.8, and 3.7 folds increments in distilled water, 0.1N Hcl and 6.8 phosphate buffers, respectively. Later, freeze dried powder formulated as hard gelatin capsules and evaluated according to the USP specifications of the drug content and the disintegration time.        As a conclusion; formulation of poorly water soluble Atorvastatin calcium as nano suspension significantly improved the dissolution of the drug and enhances its solubility.

scholarly journals QUALITY BY DESIGN (QBD) AS A TOOL FOR THE OPTIMIZATION OF INDOMETHACIN FREEZE-DRIED SUBLINGUAL TABLETS: IN VITRO AND IN VIVO EVALUATION

2021 ◽  
pp. 160-171
Author(s):  
MERVAT SHAFIK IBRAHIM ◽  
NIHAL MOHAMED ELMAHDY ELSAYYAD ◽  
ABEER SALAMA ◽  
SHEREEN H. NOSHI
Keyword(s):  
Response Surface ◽  
Quality By Design ◽  
Drug Dissolution ◽  
Disintegration Time ◽  
Optimization Study ◽  
Freeze Dried ◽  
Screening Study ◽  
Wetting Time

Objective: This study aims to prepare and optimize indomethacin freeze-dried sublingual tablets (IND-FDST) by utilizing a quality by design (QbD) approach to achieve rapid drug dissolution and simultaneously bypassing the GIT for better patient tolerability. Methods: A screening study was utilized to determine the most significant factors which the quality attributes, namely disintegration time and % friability. Then an optimization study was conducted using a full response surface design to determine the optimized formula by varying the amount of the matrix-forming polymer (gelatin) and super disintegrant (croscarmellose sodium (CCS)). The variables' effect on the % friability, disintegration time, wetting time, and amount of drug release after 10 min (%Q10) was studied. The optimized formula was tested for compatibility, morphology as well as stability studies under accelerated conditions in addition to the in vivo pharmacodynamics in rats. QbD was adopted by utilizing a screening study to identify the significant formulation factors followed by a response surface optimization study to determine the optimized IND-FDST formulation. Results: Optimized IND-FDST comprised of gelatin/CCS combination in a ratio of 1:1 possessed adequate %friability (0.73±0.03%), disintegration time (25.40±1.21 seconds), wetting time (3.49±0.68 seconds), and % Q10 (100.99±5.29%) as well as good stability under accelerated conditions. IND-FDST also showed significant inhibition of edema, tumour necrosis factor-alpha, and interleukin-6 release in vivo compared to the oral market product by 70%, 42%, and 65%, respectively. Conclusion: QbD presents a successful approach in the optimization of a successful IND-FDST formula that showed superior in vivo and in vitro characteristics.

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.

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