scholarly journals Development and Characterization of Novel Site Specific Hollow Floating Microspheres Bearing 5-Fu for Stomach Targeting

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Peeyush Bhardwaj ◽  
Deepti Chaurasia ◽  
Ranjit Singh ◽  
Anoop Swarup
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Drug Bioavailability ◽  
Gastric Residence Time ◽  
Evaporation Technique ◽  
Multiple Unit

Multiple-unit-type oral floating hollow microspheres of 5-fluorouracil (5-Fu) were developed using modified solvent evaporation technique to prolong gastric residence time, to target stomach cancer, and to increase drug bioavailability. The prepared microspheres were characterized for micromeritic properties, floating behavior, entrapment efficiency, and scanning electron microscopy (SEM). Thein vitrodrug release and floating behavior were studied in simulated gastric fluid (SGF) at pH 1.2. The yield of microspheres was obtained up to84.46±6.47%. Microspheres showed passable flow properties. Based on optical microscopy, particle size was found to be ranging from158.65±12.02to198.67±17.45 μm. SEM confirmed spherical size, perforated smooth surface, and a hollow cavity inside the microspheres. Different kinetic models for drug release were also applied on selected batches.

Floating Microsphere of Curcumin as Targeted Gastro-retentive Drug Delivery System

2021 ◽  
pp. 5202-5206
Author(s):  
Anupam K Sachan ◽  
Saurabh Singh ◽  
Kiran Kumari ◽  
Pratibha Devi
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sustained Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Entrapment Efficiency ◽  
Synthetic Polymers ◽  
Drug Bioavailability ◽  
Gastric Residence Time

Microspheres carrier system made from natural or synthetic polymers used in sustained release drug delivery system. The present study involves formulation and evaluation of floating microspheres of Curcumin for improving the drug bioavailability by prolongation gastric residence time. Curcumin, natural hypoglycemic agent is a lipophilic drug, absorbed poorly from the stomach, quickly eliminated and having short half-life so suitable to formulate floating drug delivery system for sustained release. Floating microspheres of curcumin were formulated by solvent evaporation technique using ethanol and dichloromethane (1:1) as organic solvent and incorporating various synthetic polymers as coating polymer, sustain release polymers and floating agent. The final formulation were evaluated various parameters such as compatibility studies, micrometric properties, In-vitro drug release and % buoyancy. FTIR studies showed that there were no interaction between drug and excipients. The surface morphology studies by SEM confirmed their spherical and smooth surface. The mean particles size were found to be 416-618µm, practical yield of microspheres was in the range of 60.21±0.052% - 80.87±0.043%, drug entrapment efficiency 47.4±0.065% - 77.9±0.036% and % buoyancy 62,24±0.161% - 88.63±0.413%. Result show that entraptmency increased as polymer (Eudragit RS100) conc. Increased. The drug release after 12 hrs. was 72.13% - 87.13% and it decrease as a polymer (HPMC, EC) concentration was decrease.

DEVELOPMENT AND CHARACTERIZATION OF NOVEL SITE SPECIFIC FLOATING-MUCOADHESIVE TABLETS BEARING 5-FLOUROURACIL FOR STOMACH TARGETING.

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (09) ◽  
pp. 23-30
Author(s):  
P Bhardwaj ◽  
◽  
R Singh ◽  
A Swarup
Keyword(s):  
Drug Release ◽  
Methyl Cellulose ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Wet Granulation ◽  
Prolonged Release ◽  
Mucoadhesive Tablets

Object of present investigation was to develop and characterize such a gastroretentive tablet, which provides the synergism effect of adhesiveness and floating property for prolonged release of 5-flourouracil within the stomach. The floating mucoadhesive tablets were prepared by the wet granulation method using different ratios of hydroxy propyl methyl cellulose (HPMC K4MCR) and Carbopol 934P as polymers. The prepared floating-mucoadhesive tables were characterized for hardness, detachment stress, floating properties, swelling index and surface morphology by SEM. The in vitro drug release and floating behaviour were studied in simulated gastric fluid (SGF) at pH 1.2. Different kinetic models for drug release were as well applied. Formulations of T-9 batch were furthermore subjected to stability and in vivo radiographic studies.

Effect of Processing Parameters on Release Profiles of Donepezil Hydrochloride-Loaded Microparticles

2020 ◽  
Vol 859 ◽  
pp. 283-288
Author(s):  
Lalinthip Sutthapitaksakul ◽  
Pornsak Sriamornsak
Keyword(s):  
Drug Release ◽  
Double Emulsion ◽  
Processing Parameters ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Stirring Time ◽  
Evaporation Technique ◽  
Donepezil Hydrochloride ◽  
Release Profiles

The purpose of this study was to examine the effect of processing parameters on drug release profiles of microparticles. Double emulsion solvent evaporation technique was utilized to encapsulate donepezil hydrochloride which is a hydrophilic drug. The processing parameters examined were polymer amount, stirring time and volume of external aqueous phase. The morphology of microparticles was observed under light microscope and scanning electron microscope. After that, in vitro drug release testing was conducted in simulated salivary fluid (pH6.75) and simulated gastric fluid (pH1.2). The results showed that these three parameters were the significant parameter affecting drug release profiles of the microparticles.

scholarly journals Development and Characterization of Novel Floating-Mucoadhesive Tablets Bearing Venlafaxine Hydrochloride

Scientifica ◽  
2016 ◽  
Vol 2016 ◽  
pp. 1-13 ◽  
Author(s):  
Raghvendra Misra ◽  
Peeyush Bhardwaj
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Methyl Cellulose ◽  
Simulated Gastric Fluid ◽  
Drug Bioavailability ◽  
Hydroxypropyl Methyl Cellulose ◽  
Detachment Force ◽  
Gastric Residence Time ◽  
Venlafaxine Hydrochloride

The present investigation is concerned about the development of floating bioadhesive drug delivery system of venlafaxine hydrochloride which after oral administration exhibits a unique combination of floating and bioadhesion to prolong gastric residence time and increase drug bioavailability within the stomach. The floating bioadhesive tablets were prepared by the wet granulation method using different ratios of hydroxypropyl methyl cellulose (HPMC K4MCR) and Carbopol 934PNF as polymers. Sodium bicarbonate (NaHCO3) and citric acid were used as gas (CO2) generating agents. Tablets were characterized for floating properties,in vitrodrug release, detachment force, and swelling index. The concentration of hydroxypropyl methyl cellulose and Carbopol 934PNF significantly affects thein vitrodrug release, floating properties, detachment force, and swelling properties of the tablets. The optimized formulation showed the floating lag time72±2.49seconds and duration of floating24.50±0.74 hr. Thein vitrorelease studies and floating behavior were studied in simulated gastric fluid (SGF) at pH 1.2. Different drug release kinetics models were also applied. Thein vitrodrug release from tablets was sufficiently sustained (more than 18 hr) and the Fickian transports of the drug from the tablets were confirmed. The radiological evidence suggests that the tablets remained buoyant and altered position in the stomach of albino rabbit and mean gastric residence time was prolonged (more than > 6 hr).

scholarly journals THE USE OF CLINOPTILOLITES AS CARRIER OF METFORMIN HYDROCHLORIDE IN DRUG DELIVERY SYSTEM: IN VITRO DRUG RELEASE STUDY

2018 ◽  
Vol 11 (11) ◽  
pp. 285
Author(s):  
Putra Imwa ◽  
Kusumawati Igaw
Keyword(s):  
Drug Release ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Metformin Hydrochloride ◽  
Simulated Intestinal Fluid ◽  
In Vitro Drug Release ◽  
Encapsulation Process ◽  
N2 Sorption ◽  
Metformin Hcl

Objective: As an antidiabetic drug, metformin hydrochloride (HCl) has been well known to possess low oral bioavailability and short half-life. In this study, we prepared the drug delivery system (DDS) of metformin HCl and clinoptilolite as its carrier. The in vitro drug release profile was further investigated.Methods: DDS was made by encapsulating metformin HCl on clinoptilolite using the wet impregnation method at various pH and initial concentration of metformin HCl. Fourier transform infrared spectrometer (FTIR), X-ray diffractometer (XRD), and N2 Sorption Analyzer were used to characterize the as-synthesized DDS. Drug release study was conducted by stirring the DDS in simulated gastric fluid and simulated intestinal fluid over 12 h.Results: The encapsulation process was achieved optimally at pH 7.0 and initial concentration of metformin HCl of 300 mg/l (CLI2-300 denoted DDS). The results of FTIR and N2 sorption analyzer confirmed the existence of metformin HCl on clinoptilolites. Meanwhile, the XRD result showed that the crystallinity of clinoptilolites remained unchanged after the encapsulation process. The cumulative drug release in the simulated gastric fluid was found to be higher than that in the simulated intestinal fluid, which indicated the potent influence of pH on the release properties of the drugs. The drug release kinetics of metformin HCl from clinoptilolite was best fitted into the Korsmeyer-Peppas model with non-Fickian transport mechanism.Conclusion: We found that clinoptilolite was suitable for DDS application, particularly as a carrier of metformin HCl.

scholarly journals Crushed Tablets: Does the Administration of Food Vehicles and Thickened Fluids to Aid Medication Swallowing Alter Drug Release?

2014 ◽  
Vol 17 (2) ◽  
pp. 207 ◽  
Author(s):  
Yady Juliana Manrique-Torres ◽  
Danielle J Lee ◽  
Faiza Islam ◽  
Lisa M Nissen ◽  
Julie A.Y. Cichero ◽  
...  
Keyword(s):  
Drug Release ◽  
Orange Juice ◽  
Immediate Release ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Simulated Gastric Fluid ◽  
Drug Bioavailability ◽  
Thickening Agents

Purpose. To evaluate the influence of co-administered vehicles on in vitro dissolution in simulated gastric fluid of crushed immediate release tablets as an indicator for potential drug bioavailability compromise. Methods. Release and dissolution of crushed amlodipine, atenolol, carbamazepine and warfarin tablets were tested with six foods and drinks that are frequently used in the clinical setting as mixers for crushed medications (water, orange juice, honey, yoghurt, strawberry jam and water thickened with Easythick powder) in comparison to whole tablets. Five commercial thickening agents (Easythick Advanced, Janbak F, Karicare, Nutilis, Viscaid) at three thickness levels were tested for their effect on the dissolution of crushed atenolol tablets. Results. Atenolol dissolution was unaffected by mixing crushed tablets with thin fluids or food mixers in comparison to whole tablets or crushed tablets in water, but amlodipine was delayed by mixing with jam. Mixing crushed warfarin and carbamazepine tablets with honey, jam or yoghurt caused them to resemble the slow dissolution of whole tablets rather than the faster dissolution of crushed tablets in water or orange juice. Crushing and mixing any of the four medications with thickened water caused a significant delay in dissolution. When tested with atenolol, all types of thickening agents at the greatest thickness significantly restricted dissolution, and products that are primarily based on xanthan gum also delayed dissolution at the intermediate thickness level. Conclusions. Dissolution testing, while simplistic, is a widely used and accepted method for comparing drug release from different formulations as an indicator for in vivo bioavailability. Thickened fluids have the potential to retard drug dissolution when used at the thickest levels. These findings highlight potential clinical implications of the addition of these agents to medications for the purpose of dose delivery and indicate that further investigation of thickened fluids and their potential to influence therapeutic outcomes is warranted. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

Design, development and characterization of ketorolac tromethamine polymeric nanosuspension

2019 ◽  
Vol 10 (9) ◽  
pp. 585-597 ◽  
Author(s):  
Pankaj A Jadhav ◽  
Adhikrao V Yadav
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Slight Reduction ◽  
Ketorolac Tromethamine ◽  
Design Development ◽  
In Vitro Drug Release ◽  
Sustained Effect ◽  
Eudragit Rl

Aim: At present, various ophthalmic formulations show low bioavailability. The rationale of present work was to design and develop stable ketorolac tromethamine nanosuspension with sustained effect and greater permeability for ocular drug delivery and increased ocular residence. Materials & methods: Formulations were designed by using central composite design, developed by combined nanoprecipitation and probe sonication method. Results & discussion: Nanosuspensions depicted the size range of the particles in between 199 and 441 nm with slight reduction in crystallinity of drug. In vitro drug release revealed that higher % entrapment efficiency of drug in nanosuspension delays the drug release. Conclusion: Eudragit RL-100-based nanosuspension increases viscosity and avoids problems like drug loss from precorneal surface and rapid drainage through nasolacrimal areas.

scholarly journals Development and Characterization of Elastic Liposomes of Metronidazole for the Treatment of Bacterial Infection

2020 ◽  
Vol 10 (6-s) ◽  
pp. 83-88
Author(s):  
Priyam Chaurasiya ◽  
Ritesh Agarwal ◽  
Kavita R. Loksh
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Topical Administration ◽  
Stability Study ◽  
Vesicle Size ◽  
Rotary Evaporation ◽  
Span 60

Objective: The objective of present study is to develop and evaluate the elastic liposomes of metronidazole so as to provide the sustained release and improve its bioavailability. Methods: Elastic liposomes were prepared by rotary evaporation method using Span 80 and Span 60 as a surfactants. The prepared elastic liposomes were evaluated for entrapment efficiency, vesicle size, In vitro drug release. Results: The drug release profiles from different elastic liposomes-in-vehicle formulations were in agreement with the physicochemical properties of the formulations. The formulation prepared showed an average vesicle size 185.4nm. The amount of drug entrapped into the elastic liposomes formulations was determined. The entrapment efficiency was found to be 73.45±0.78 %. A good amount of drug was entrapped in the liposome formulations prepared. Based on different parameters formulations of batch TG2 was found to be the best formulations. Stability study was performed on the selected formulation TG2. When the regression coefficient values of were compared, it was observed that ‘r’ values of first order was maximum i.e. 0.993 hence indicating drug release from formulations was found to follow Korsmeyer Peppas model release kinetics Conclusion: These results indicate that elastic liposome can function as probable drug delivery systems to enhance transdermal permeation of metronidazole for treating the topical infections. Keywords: Metronidazole, Elastic liposomes, Topical administration, Skin infection

scholarly journals Crystal products of lamotrigine-citric acid for improvement of in vitro drug release in simulated gastric fluid

2020 ◽  
pp. 49-49
Author(s):  
Bhabani Satapathy ◽  
Asuprita Patel ◽  
Rudra Sahoo ◽  
Subrata Mallick
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Crystal Engineering ◽  
Oral Absorption ◽  
Gastric Fluid ◽  
In Vivo Studies ◽  
Simulated Gastric Fluid ◽  
Drug Development Research

Crystal engineering is an integral part of the drug development research. Crystal forms can modify the physicochemical properties of the parent drug molecule. The present work was aimed at the synthesis and characterization of crystalline product of lamotrigine (LT), a FDA approved anti-epileptic drug, with citric acid (CA) to improve its release in gastric region and oral absorption. The crystalline products of LT-CA were developed by solvent evaporation method using ethanol-water as the solvent system. Appearance of new charac-teristic peaks in the FTIR spectra for the crystal products indicated formation of new crystal state. In DSC thermogram, melting point of the experimental crystal products was different than that of the pure drug. Further, formation of new crystalline phase was confirmed from XRD data through the identification of new sharp peaks for the selected crystal products. A higher cumulative percen-tage of drug release was observed for the crystal products than the free drug within 60 min of drug release in simulated gastric fluid. However, in vivo studies are warranted for the future technology transfer of the product at industrial scale.

scholarly journals Development of dissolution test method for a telmisartan/amlodipine besylate combination using synchronous derivative spectrofluorimetry

2014 ◽  
Vol 50 (2) ◽  
pp. 329-336
Author(s):  
Panikumar Durga Anumolu ◽  
Sirisha Neeli ◽  
Haripriya Anuganti ◽  
Sathesh Babu Puvvadi Ranganatham ◽  
Subrahmanyam Chavali Venkata Satya
Keyword(s):  
Drug Release ◽  
Gastric Fluid ◽  
Test Method ◽  
Simulated Gastric Fluid ◽  
Dissolution Test ◽  
Amlodipine Besylate ◽  
Dissolution Method ◽  
Quality Control Testing ◽  
Tablet Dosage

The dissolution process is considered an important in vitro tool to evaluate product quality and drug release behavior. Single dissolution methods for the analysis of combined dosage forms are preferred to simplify quality control testing. The objective of the present work was to develop and validate a single dissolution test for a telmisartan (TEL) and amlodipine besylate (AML) combined tablet dosage form. The sink conditions, stability and specificity of both drugs in different dissolution media were tested to choose a discriminatory dissolution method, which uses an USP type-II apparatus with a paddle rotating at 75 rpm, with 900 mL of simulated gastric fluid (SGF without enzymes) as the dissolution medium. This dissolution methodology provided good dissolution profiles for both TEL and AML and was able to discriminate changes in the composition and manufacturing process. To quantify both drugs simultaneously, a synchronous first derivative spectrofluorimetric method was developed and validated. Drug release was analyzed by a fluorimetric method at 458 nm and 675 nm for AML and TEL, respectively. The dissolution method was validated as per ICH guidance.

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