scholarly journals FORMULATION OF TETRANDRINE BEADS USING IONIC GELATION METHOD CA-PECTINATE COATED PH-SENSITIVE POLYMERS AS COLON-TARGETED DOSAGE FORM

2017 ◽  
Vol 10 (10) ◽  
pp. 90
Author(s):  
Raditya Iswandana ◽  
Kurnia Sari Setio Putri ◽  
Cindy Espreancelly Sandiata ◽  
Sisilia Triani ◽  
Santi Purna Sari ◽  
...  
Keyword(s):  
Targeted Drug Delivery ◽  
In Vitro Release ◽  
Chloride Concentration ◽  
In Vitro Drug Release ◽  
Eudragit L100 ◽  
Calcium Pectinate ◽  
Release Study ◽  
Vitro Release

Objectives Pectin, a natural polysaccharide, can be used as colon targeted drug delivery systems. Ionotropic gelation of pectin in the presence of certain divalent cations, such as calcium ions, protects drugs by producing insoluble hydrogels that can be used as a colon-targeted drug delivery carrier. In this study, calcium pectinate beads containing tetrandrine were made and were evaluated for in-vitro drug release and in-vivo study.Methods: Calcium pectinate beads were prepared by ionic gelation method with varied calcium chloride concentration (5%, 10%, and 15%). The best formula was coated with pH sensitive polymers, i.e. Eudragit L100-55, Eudragit L100, HPMCP (Hydroxypropylmethyl Cellulose Phthalate) HP-55 or CAP (Cellulose Acetate Phthalate).Results: Characterization results showed that the beads produced were quite spherical and have yellow-brownish color. After the coating process, beads were used in in-vitro drug release and targeted test. From in-vitro release study, beads coated with Eudragit L100 10% has shown good colon targeted dosage form with percent cumulative release 57.87%. This result also confirmed with the in-vivo test. Beads which were coated by Eudragit L100 10% could be found in the rat intestine.Conclusion: Formula 1 (5% calcium chloride concentration) was chosen as the best beads characterization. Formula 1C (5% beads coated with 10% Eudragit L100) showed an optimal protection from gastric acid in the in-vitro release study and able to deliver the beads to the intestine in the in-vivo targeted test.

Development, in vitro and in vivo Evaluations of Solid-Lipid Microparticles based on Solidified Micellar Carrier System for Oral Delivery of Cefepime

2017 ◽  
Vol 10 (1) ◽  
pp. 3582-3593
Author(s):  
Chukwuebuka Umeyor ◽  
Uchechukwu Nnadozie ◽  
Anthony Attama
Keyword(s):  
Oral Delivery ◽  
In Vitro Release ◽  
Carrier System ◽  
Solid Lipid ◽  
Solid Lipid Microparticles ◽  
Release Study ◽  
Lipid Microparticles ◽  
Vitro Release

This study seeks to formulate and evaluate a solid lipid nanoparticle-based, solidified micellar carrier system for oral delivery of cefepime. Cefepime has enjoyed a lot of therapeutic usage in the treatment of susceptible bacterial infections; however, its use is limited due to its administration as an injection only with poor patient compliance. Since oral drug administration encourage high patient compliance with resultant effect in improved therapy, cefepime was formulated as solid lipid microparticles for oral delivery using the concept of solidified micellar carrier system. The carrier system was evaluated based on particle yield, particle size and morphology, encapsulation efficiency (EE %), and thermal analysis using differential scanning calorimeter (DSC). Preliminary microbiological studies were done using gram positive and negative bacteria. In vitro release study was performed using biorelevant media, while in vivo release study was performed in white albino rats. The yield of solid lipid microparticles (SLM) ranged from 84.2 – 98.0 %. The SLM were spherical with size ranges of 3.8 ± 1.2 to 42.0 ± 1.4 µm. The EE % calculated ranged from 83.6 – 94.8 %. Thermal analysis showed that SLM was less crystalline with high potential for drug entrapment. Microbial studies showed that cefepime retained its broad spectrum anti-bacterial activity. In vitro release showed sustained release of cefepime from SLM, and in vivo release study showed high concentration of cefepime released in the plasma of study rats. The study showed that smart engineering of solidified micellar carrier system could be used to improve oral delivery of cefepime.

Development of Polymeric Nanocarriers for Brain Targeted Delivery of Atorvastatin: A Quality-By-Design Approach

2020 ◽  
Vol 10 (2) ◽  
pp. 149-158
Author(s):  
Guilherme A.G. Martins ◽  
Fabio S. Murakami ◽  
Mauro S. Oliveira ◽  
Ana F. Furian ◽  
Helen Treichel ◽  
...  
Keyword(s):  
Quality By Design ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Physicochemical Characteristics ◽  
In Vivo Studies ◽  
Mean Size ◽  
Release Study ◽  
Vitro Release

Objective: Atorvastatin (ATV) is effective in reducing total cholesterol and low-density lipoprotein levels. Furthermore, it produces pleiotropic effects in neurodegenerative conditions such as Parkinson's, Alzheimer's, and epilepsy. However, due to the effective defense system of the central nervous system (CNS), the development of new medicines for clinical conditions has proven difficult. In this context, nanotechnology was applied as a promising solution to promote drug vectorization to the brain. Methods: The solvent emulsification-diffusion method was used to develop nanoparticles (NPs) based on polylactic acid and coated with polysorbate 80 containing ATV. Quality-by-Design (QbD) was used in the optimization of nanoparticles production through the application of the experimental design Box-Behnken Design. Results: After optimizing the independent factors including sonication time, surfactant concentration and surfactant volume, the NPs presented physicochemical characteristics such as entrapment efficiency of 86.4 ± 2.4%, mean size of 225.2 ± 4.8 nm, and zeta potential of -14.4 ± 0.36 mV. In the in vitro release study, approximately 20% of the encapsulated ATV was released. Conclusion: The application of QbD was very useful in demonstrating its applicability in the nanotechnological pharmaceutical area for controlling and predicting the influence of the variables in the production of NPs. The NPs developed in this study presented adequate physicochemical characteristics, which is promising for future in vivo studies. The physicochemical characteristics included entrapment efficiency of 86.4 ± 2.4%, mean size of 225.2 ± 4.8 nm, and zeta potential of -14.4 ± 0.36 mV. In the in vitro release study, approximately 20% of the encapsulated ATV was released. The application of QbD was very useful in demonstrating its applicability in the nanotechnological pharmaceutical area for controlling and predicting the influence of the variables in the production of NPs. The NPs developed in this study presented adequate physicochemical characteristics, which is promising for future in vivo studies.

scholarly journals FORMULATION DEVELOPMENT OF COLON TARGETED MESALAMINE PELLETS: IN VITRO-IN VIVO RELEASE STUDY

2019 ◽  
pp. 125-132 ◽  
Author(s):  
JAGAN BAHEKAR ◽  
SHAILESH WADHER
Keyword(s):  
In Vitro Release ◽  
Pharmacokinetic Parameters ◽  
High Dose ◽  
Aminosalicylic Acid ◽  
Formulation Development ◽  
In Vivo Release ◽  
Release Study ◽  
Vitro Release

Objective: This study was intended to investigate the potential of the colon specificity approach comprising of use of pH-sensitive and time-dependent polymers in combination for precise colonic release of Mesalamine or 5-Aminosalicylic acid (5-ASA). Methods: The extrusion and spheronization method, preferably employed in industry for allowing high dose capacity to formulate, was used to prepare drug pellets. The Wurster coating technique used for aqueous coatings of Eudragit NE 40D as an inner coat and Eudragit FS30D as outer coat. The changing pH media used for in vitro release study of optimization batches for both the coating levels. A scanning electron microscope (SEM) was used to evaluate coating thickness and surface morphology. Results: The pharmacokinetic parameters of formulation evaluated by in vivo study in rabbits revealed that the uncoated formulation released the drug too early in the gastrointestinal tract (GIT) with a mean Cmax of 1205.28±0.37 µg/ml at 2 h after administration, whereas desired lag time was achieved in case of coated pellets exhibiting mean Cmax 465.94±0.21 µg/ml and tmax of 8 h. Conclusion: The in vitro and in vivo release study divulge the reliability of approach involving the use of pH sensitivity and time dependency of polymer for drug release in a single formulation for the treatment of colonic diseases. Hence, the present study provides constructive results for colon targeting of 5-ASA pellets with industrially feasible processes.

scholarly journals Comparative Study of Herbal Extract of Piper Nigrum, Piper Album and Piper Longum on Various Characteristics of Pyrazinamide and Ethambutol Microspheres

2019 ◽  
Vol 9 (4-A) ◽  
pp. 72-78
Author(s):  
Prashant L Pingale ◽  
R. P. Ravindra
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Herbal Extract ◽  
Piper Nigrum ◽  
Equal Proportion ◽  
In Vitro Drug Release ◽  
Piper Longum ◽  
Release Study ◽  
Vitro Release

Bioenhancers are the ‘bioavailability enhancers’; they do not show any therapeutic effect, but when used in combination enhances the activity of drug molecule. In a cited research paper, the effect of various species of piper used as bioenhancer singly and in combination in an equal ratio. The methods used for preparation of microspheres are Complex Coacervation and Modified Emulsion Method. The prepared microspheres were evaluated for various parameters like in-vitro release, drug entrapment efficiency, percent bioadhesion, permeability study using intestinal sac method. The in-vitro drug release of drugs from formulations where Piper nigrum was used as bioenhancers was found to be about 66-70% in 12 hrs. when used singly. When bioenhancers used in combination the in-vitro drug release of drugs was increased up to 85-90% for combination of Piper album and Piper longum in an equal proportion, the same was about 35-40% in case of formulations where no bioenhancers was used. The microspheres found to be less than 130 micron in size. The DEE was found to be in the range of 27-67%. The bioadhesion of the microsphere were found to be 20-76% (increased in formulations where bioenhancers incorporated). The in- vitro release study by USP paddle apparatus, the important results from in-vitro release study relates to the very significant enhancement in drug release, due to presence of bioenhancers. Keywords: Microspheres, Bioenhancer, Piper nigrum, Piper album, Piper longum, Pyrazinamide, Ethambutol

scholarly journals Recent Progress in Drug Release Testing Methods of Biopolymeric Particulate System

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1313
Author(s):  
Yejin Kim ◽  
Eun Ji Park ◽  
Tae Wan Kim ◽  
Dong Hee Na
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Testing Methods ◽  
In Vitro Drug Release ◽  
Particulate System ◽  
Vitro Release ◽  
Release Testing

Biopolymeric microparticles have been widely used for long-term release formulations of short half-life chemicals or synthetic peptides. Characterization of the drug release from microparticles is important to ensure product quality and desired pharmacological effect. However, there is no official method for long-term release parenteral dosage forms. Much work has been done to develop methods for in vitro drug release testing, generally grouped into three major categories: sample and separate, dialysis membrane, and continuous flow (flow-through cell) methods. In vitro drug release testing also plays an important role in providing insight into the in vivo performance of a product. In vitro release test with in vivo relevance can reduce the cost of conducting in vivo studies and accelerate drug product development. Therefore, investigation of the in vitro–in vivo correlation (IVIVC) is increasingly becoming an essential part of particulate formulation development. This review summarizes the principles of the in vitro release testing methods of biopolymeric particulate system with the recent research articles and discusses their characteristics including IVIVC, accelerated release testing methods, and stability of encapsulated drugs.

scholarly journals Research on Magnetically Targeted Drug Delivery System Based on Fullerene Derivatives

2021 ◽  
pp. X
Author(s):  
Ying WANG ◽  
Li SU ◽  
Bing LI ◽  
Ningning JIN ◽  
Riji LU ◽  
...  
Keyword(s):  
Targeted Drug Delivery ◽  
Water Solubility ◽  
In Vitro Release ◽  
Dipolar Cycloaddition ◽  
Effective Synthesis ◽  
Ft Ir ◽  
Bonding Method ◽  
Vitro Release

A carboxyl-terminated fullerene pyrrolidine derivative was synthesized by 1, 3-dipolar cycloaddition of imine ylide (FP-COOH). UV-Vis, FT-IR and MALDI-TOF respectively verified the effective synthesis of compounds. The compound (FP-COOH) was used as an intermediate, and then the hydrothermal chemical bonding method was used to load ferric oxide on the compound (FP-COOH). Its purpose was to form a magnetic targeting carrier system (FP-IONP-COOH). Then use the non-covalent method to combine FP-IONP-COOH with doxorubicin. The ultimate goal was to improve the side effects of doxorubicin. The solubility experiments showed that both FP-IONP-COOH and FP-IONP-COOH/DOX had good water solubility. The investigation of magnetism showed that FP-IONP-COOH has good magnetism. Finally, in vitro release experiments further verified the targeting of FP-IONP-COOH/DOX. The cumulative release of DOX at 48 h could be as high as 82 %, whereas the accumulated release of FP-IONP-COOH/DOX at 48 h was only 48 %, and was able to continuously release for more than 120 h, demonstrating its good sustained release in vivo.

Reliability of a Single β-Thromboglobulin Measurement in a Diabetic Population : Importance of PGE1 in Anticoagulant Mixture

1987 ◽  
Vol 57 (02) ◽  
pp. 201-204 ◽  
Author(s):  
P Y Scarabin ◽  
L Strain ◽  
C A Ludlam ◽  
J Jones ◽  
E M Kohner
Keyword(s):  
In Vitro Release ◽  
Mean Value ◽  
Reliable Estimate ◽  
Diabetic Patients ◽  
Single Measurement ◽  
Diabetic Population ◽  
The Difference ◽  
Vitro Release

SummaryDuring the collection of samples for plasma β-thromboglobulin (β-TG) determination, it is well established that artificially high values can be observed due to in-vitro release. To estimate the reliability of a single β-TG measurement, blood samples were collected simultaneously from both arms on two separate occasions in 56 diabetic patients selected for a clinical trial. From each arm, blood was taken into two tubes containing an anticoagulant mixture with (tube A) and without (tube B) PGE!. The overall mean value of B-TG in tube B was 1.14 times higher than in tube A (p <0.01). The markedly large between-arms variation accounted for the most part of within-subject variation in both tubes and was significantly greater in tube B than in tube A. Based on the difference between B-TG values from both arms, the number of subjects with artifically high B-TG values was significantly higher in tube B than in tube A on each occasion (overall rate: 28% and 14% respectively). Estimate of between-occasions variation showed that B-TG levels were relatively stable for each subject between two occasions in each tube. It is concluded that the use of PGEi decreases falsely high B-TG levels, but a single measurement of B-TG does not provide a reliable estimate of the true B-TG value in vivo.

Formulation and Evaluation of Itopride Hydrochloride Floating Beads for Gastroretentive Delivery

2013 ◽  
Vol 6 (4) ◽  
pp. 2269-2280
Author(s):  
Nagratna Dhople ◽  
P N Dandag ◽  
A P Gadad ◽  
C K Pandey ◽  
Masthiholimath V S
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Sustained Release Formulation ◽  
Prokinetic Drug ◽  
Drug Entrapment Efficiency ◽  
Itopride Hydrochloride ◽  
Vitro Release

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.

Formulation and Evaluation of Sustained Release Dosage Forms of Norfloxacin

2018 ◽  
Vol 11 (6) ◽  
pp. 4331-4337
Author(s):  
C Suja ◽  
Sismy C
Keyword(s):  
Sustained Release ◽  
Guar Gum ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
Prolonged Release ◽  
Weight Variation ◽  
Sustained Release Tablets ◽  
Release Study ◽  
Vitro Release

The goal of this study was to formulate and evaluate norfloxacin sustained release tablets. Norfloxacin sustained release tablets were prepared by wet granulation method using two polymers such as HPMC K 100 M (hydrophilic polymer) and guar gum (natural polymer) and with three polymer ratios (0.5, 1.0 and 1.5). The prepared granules were evaluated to preformulation studies such as angle of repose, bulk density, tapped density, bulkiness, compressibility index and Hauser’s ratio. All the parameters shows that the granules having good flow properties. Then the formulated tablets were taken to evaluation studies such as hardness, weight variation, friability, drug content and thickness. All the parameters were within the acceptable limits. IR spectral analysis showed that there was no interaction between the drug and polymers. The in vitro release study was performed in phosphate buffer pH 7.4 at 293 nm. The in vitro release study showed that if the polymer ratio is increased, then the release of the drug is prolonged. HPMC K 100M shows a prolonged release when compared to guar gum.

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