Preparation of poly(sebacic anhydride) and polylactic acid pills used as drug carrier for levofloxacin controlled release

2013 ◽  
Vol 33 (7) ◽  
pp. 659-664 ◽  
Author(s):  
Zhuan Zhang ◽  
Liao-Bing Chen ◽  
Jie Gao ◽  
Feng Bao ◽  
Jing Yin ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Controlled Release ◽  
Drug Release ◽  
Polylactic Acid ◽  
Release Rate ◽  
Drug Carrier ◽  
Antibacterial Drug ◽  
Molecular Weights ◽  
Zero Order Release

Abstract A biodegradable local drug release system consisting of poly(sebacic anhydride) and polylactic acid was developed for the purpose of osteomyelitis therapy. Five kinds of poly(sebacic anhydride) with different molecular weights were synthesized, and levofloxacin was chosen as a model antibacterial drug in the in vitro release within 38 days. As the molecular weight of poly(sebacic anhydride) increased, the melting point (Tm) of the matrices increased and the surface morphology became smoother. Consequently, the initial burst effect was reduced and the release rate significantly decreased. In addition, the kinetics of pills containing poly(sebacic anhydride) (Mw=13,000) were close to zero order release. The release profile reveals that the thermodynamic properties and morphology of these matrices, which are affected by the molecular weight, are essential for developing controllable delivery systems. The drug release rate could be easily controlled by the molecular weight of the poly(sebacic anhydride). Finally, these prospective results allow the biodegradable controlled release systems to be employed as carriers for the treatment of chronic osteomyelitis, as well as for other medical applications.

Formulation Development and Characterization of controlled release core in cup matrix tablets of venlafaxine HCl

2020 ◽  
Vol 15 ◽  
Author(s):  
Balaji Maddiboyina ◽  
Vikas Jhawat ◽  
Gandhi Sivaraman ◽  
Om Prakash Sunnapu ◽  
Ramya Krishna Nakkala ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Rate ◽  
Zero Order ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Crystalline Cellulose ◽  
Hydrophobic Polymers

Background: Venlafaxine HCl is a selective serotonin reuptake inhibitor which is given in the treatment of depression. The delivery of the drug at a controlled rate can be of great importance for prolonged effect. Objective: The objective was to prepare and optimize the controlled release core in cup matrix tablet of venlafaxine HCl using the combination of hydrophilic and hydrophobic polymers to prolong the effect with rate controlled drug release. Methods: The controlled release core in cup matrix tablets of venlafaxine HCl were prepared using HPMC K5, K4, K15, HCO, IPA, aerosol, magnesium sterate, hydrogenated castor oil and micro crystalline cellulose PVOK-900 using wet granulation technique. Total ten formulations with varying concentrations of polymers were prepared and evaluated for different physicochemical parameters such FTIR analysis for drug identification, In-vitro drug dissolution study was performed to evaluate the amount of drug release in 24 hrs, drug release kinetics study was performed to fit the data in zero order, first order, Hixson–crowell and Higuchi equation to determine the mechanism of drug release and stability studies for 3 months as observed. Results: The results of hardness, thickness, weight variation, friability and drug content study were in acceptable range for all formulations. Based on the In vitro dissolution profile, formulation F-9 was considered to be the optimized extending the release of 98.32% of drug up to 24 hrs. The data fitting study showed that the optimized formulation followed the zero order release rate kinetics and also compared with innovator product (flavix XR) showed better drug release profile. Conclusion: The core-in-cup technology has a potential to control the release rate of freely water soluble drugs for single administration per day by optimization with combined use of hydrophilic and hydrophobic polymers.

scholarly journals Hydroxyapatite/nifuroxazide conjugate: Characterization, drug release and antimicrobial activity

2021 ◽  
pp. 40-40
Author(s):  
Zeljko Radovanovic ◽  
Katarina Mihajlovski ◽  
Lidija Radovanovic ◽  
Djordje Janackovic ◽  
Rada Petrovic
Keyword(s):  
Drug Release ◽  
Raw Materials ◽  
Drug Carrier ◽  
In Vitro Study ◽  
Inhibitory Effect ◽  
Antibacterial Drug ◽  
Stomach Acid ◽  
Poorly Soluble ◽  
Good Biocompatibility

Synthetic hydroxyapatite (Ca10(PO4)6(OH)2, HAp) is very similar to the inorganic part of the bones and teeth of mammals. It is a well-known biomaterial with good biocompatibility, osteoconductivity and bioactivity. Nifuroxazide (C12H9N3O5, NFX) is a broad-spectrum antibacterial drug and poorly soluble in water. In order to increase the solubility of NFX, nanosized HAp powder and raw NFX drug were mixed giving, as a result, HAp/NFX conjugate. Characterization of the raw materials and the obtained conjugate confirmed the integration of NFX on the HAp surface. The in vitro study of drug release in simulated stomach acid and intestinal fluid showed a much faster release of NFX from HAp surface than those of raw drug. HAp/NFX conjugate showed an excellent inhibitory effect against Gram-positive bacterium Staphylococcus aureus, Gram-negative bacterium Escherichia coli and yeast Candida albicans, proving the nanosized HAp powder as a promising drug carrier.

scholarly journals Development and Evaluation of Alprazolam Controlled Release tablets

2014 ◽  
Vol 1 (1) ◽  
pp. 8-23 ◽  
Author(s):  
Sarmila Shrestha ◽  
Dharma Prasad Khanal ◽  
Panna Thapa
Keyword(s):  
Molecular Weight ◽  
Controlled Release ◽  
Drug Release ◽  
Drug Formulation ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Significant Difference ◽  
Model Independent ◽  
Tablet Formulations

Twenty three different tablet formulations of alprazolam were prepared using Polymer like hydroxypropylmethyl cellulose (HPMC K4M, HPMC K15M and HPMC K100M) in the concentration of 5 – 50 % of total weight of tablets and combination of HPMC K15M and HPMC K100M with ethyl cellulose (EC) was formulated by using wet granulation method. Drug formulation containing 1.0 mg, 1.5 mg, 5 mg, 10 mg and 15 mg alprazolam per tablet maintaining constant HPMC K15M concentration was also developed.The in-vitro dissolution studies of the formulated and marketed product in USP type II apparatus showed that the drug release is dependent upon the drug: polymer ratio; also molecular weight of the polymer and solubility of loaded drug. With increasing concentration and molecular weight of polymer, drug release was found to be decreased. When formulating the tablets the method used whether direct compression or wet granulations also affect the release of the drug from matrix. Wet granulation method by using 40 % HPMC K15M in combination with 5 % EC was found to be most suitable controlled release alprazolam tablet as drug release was found to be appreciable in this formulation. When loading dose of alprazolam was increased, drug release was found to be tremendously decreased because of the poor solubility of alprazolam in water. When one-way ANOVA was applied for various formulated and marketed tablets it was found that there is no significant difference (p > 0.05) in drug release rate among formulation similarly model independent methods was also applied such as similarity and dissimilarity factor and found that there is no significant difference between these formulations.DOI: http://dx.doi.org/10.3126/jmmihs.v1i1.9896 Journal of Manmohan Memorial Institute of Health Sciences Vol.1(1) 2011; 8-23

scholarly journals Noncytotoxic polycaprolactone-polyethyleneglycol-ε-poly(l-lysine) triblock copolymer synthesized and self-assembled as an antibacterial drug carrier

RSC Advances ◽  
2017 ◽  
Vol 7 (63) ◽  
pp. 39718-39725 ◽  
Author(s):  
Chuncai Zhou ◽  
Xinyu Zhou ◽  
Xiaokai Su
Keyword(s):  
Antibacterial Activity ◽  
Drug Release ◽  
Triblock Copolymer ◽  
Drug Carrier ◽  
Antibacterial Drug ◽  
Self Assembled ◽  
Low Cytotoxicity

The PCL35-b-PEG45-b-EPL23 vesicles perform well in vitro drug release and antibacterial activity against Gram− and Gram+ bacteria with low cytotoxicity.

scholarly journals Formulation and Evaluation of Controlled Release Maintenance Dose Loaded Niosomes of Anti-Hypertensive Drug

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
Chandani Makvana ◽  
Satyajit Sahoo
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Zeta Potential ◽  
Drug Carrier ◽  
Entrapment Efficiency ◽  
Drug Carriers ◽  
Vesicle Size ◽  
Drug Content ◽  
Span 60

The present study was aimed to formulate, comparatively evaluate and optimize multiple lipid drug carriers of valsartan for oral controlled release to overcome the problems associated with the drug such as bioavailability, to reduce the dosage regimen, half life and to determine the appropriateness of niosomal formulation as a drug carrier. Ether injection method was chosen for the formulation of physically and chemically stable niosomes of valsartan. The formulation and process parameters were optimized by manufacturing placebo niosomes. Than drug loaded niosome was prepared by varying the concentration of span 60. The prepared nine formulations were evaluated for various parameters. Placebo niosomes were evaluated for appearance, odour, texture, creaming volume, pH and changes after 15 days. The medicated nine formulations were evaluated for organoleptic properties (appearance/color, odour), pH, total drug content, entrapment efficiency, mean particle size and polydispersibility index, zeta potential and In-vitro drug release. All formulations were off-white in color, odourless, and fluid in nature. It was stable and did not show sedimentation. The pH was found to be in the range of 4.6-5.4. Drug content was found in the range of 89.13 to 99.52. The Entrapment efficiency was found in range of 79.05 to 98.24. The mean vesicle size of drug loaded niosomes of the different batches ranged between 2.52-3.42μm. The polydispersvity index was in the range of 0.325 to 0.420 which indicates a narrow vesicle size distribution. The values of zeta potential were in the range of -20.29 mV to -30.55 mV which indicates that niosome had sufficient charge and mobility to inhibit aggregation of vesicles. All the nine formulations shows constant drug release in controlled manner up to 24 h. Formulation V7 was considered to be the best formulation as the % drug content (99.52 ± 0.97), % entrapment efficiency (98.24 ± 1.50) and % drug release at the end of 24th h (98.55) were high for V7. The optimized formulation V7 showed higher degree of correlation coefficient (r2) 0.9805 which indicates process of constant drug release from dosage form. The present study concludes that the prepared niosome is a convenient and efficiency carrier for the delivery of antihypertensive drug. Besides this, it provided controlled delivery of drug.

scholarly journals Drug release rate in vitro and bioavailability of new controlled release suspension of spherical matrix of ibuprofen.

1989 ◽  
Vol 4 (2) ◽  
pp. 100-104
Author(s):  
Yoshiaki Kawashima ◽  
Taro Iwamoto ◽  
Toshiyuki Niwa ◽  
Hirofumi Takeuchi ◽  
Tomoaki Hino ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Rate ◽  
Drug Release Rate

Development of resistant corn starch for use as an oral colon-specific nanoparticulate drug carrier

2018 ◽  
Vol 90 (6) ◽  
pp. 1073-1084 ◽  
Author(s):  
Norul Nazilah Ab’lah ◽  
Nagarjun Konduru Venkata ◽  
Tin Wui Wong
Keyword(s):  
Molecular Weight ◽  
Drug Release ◽  
Resistant Starch ◽  
Corn Starch ◽  
Drug Carrier ◽  
Scanning Calorimetry ◽  
Native Starch ◽  
Heat Moisture Treatment ◽  
Moisture Treatment

Abstract Starch is constituted of amylose and amylopectin. Debranching of amylopectin converts it into amylose thereby producing resistant starch which is known to be less digestible by the amylase. This study designed resistant starch using acid hydrolysis and heat-moisture treatment methods with native corn starch as the starting material. Both native and processed starches were subjected to Fourier transform infrared spectroscopy, X-ray diffractometry, differential scanning calorimetry and molecular weight analysis. They were nanospray-dried into nanoparticles with 5-fluorouracil as the drug of interest for colon cancer treatment. These nanoparticles were subjected to size, zeta potential, morphology, drug content and in vitro drug release analysis. Heat-moisture treatment of native corn starch enabled the formation of resistant starch through amylopectin debranching and molecular weight reduction thereby enhancing hydrogen bonding between the starch molecules at the amorphous phase and gelatinization capacity. The nanoparticles prepared from resistant starch demonstrated similar drug release as those of native starch in spite of the resistant starch had a lower molecular weight. The resistant starch is envisaged to be resistant to the digestive action of amylase in intestinal tract without the formed nanoparticles exhibiting excessively fast drug release in comparison to native starch. With reduced branching, it represents an ideal precursor for targeting ligand conjugation in design of oral colon-specific nanoparticulate drug carrier.

Toxicity of Heparinoids, with Special Reference to the Precipitation of Fibrinogen

1964 ◽  
Vol 12 (01) ◽  
pp. 232-261 ◽  
Author(s):  
S Sasaki ◽  
T Takemoto ◽  
S Oka
Keyword(s):  
Molecular Weight ◽  
Dextran Sulfate ◽  
Anticoagulant Activity ◽  
Molecular Structures ◽  
Severe Reaction ◽  
Clinical Use ◽  
Molecular Weights ◽  
Close Relationship

SummaryTo demonstrate whether the intravascular precipitation of fibrinogen is responsible for the toxicity of heparinoid, the relation between the toxicity of heparinoid in vivo and the precipitation of fibrinogen in vitro was investigated, using dextran sulfate of various molecular weights and various heparinoids.1. There are close relationships between the molecular weight of dextran sulfate, its toxicity, and the quantity of fibrinogen precipitated.2. The close relationship between the toxicity and the precipitation of fibrinogen found for dextran sulfate holds good for other heparinoids regardless of their molecular structures.3. Histological findings suggest strongly that the pathological changes produced with dextran sulfate are caused primarily by the intravascular precipitates with occlusion of the capillaries.From these facts, it is concluded that the precipitates of fibrinogen with heparinoid may be the cause or at least the major cause of the toxicity of heparinoid.4. The most suitable molecular weight of dextran sulfate for clinical use was found to be 5,300 ~ 6,700, from the maximum value of the product (LD50 · Anticoagulant activity). This product (LD50 · Anticoagulant activity) can be employed generally to assess the comparative merits of various heparinoids.5. Clinical use of the dextran sulfate prepared on this basis gave satisfactory results. No severe reaction was observed. However, two delayed reactions, alopecia and thrombocytopenia, were observed. These two reactions seem to come from the cause other than intravascular precipitation.

Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

1970 ◽  
Vol 9 (3) ◽  
pp. 3318-3329
Author(s):  
Kranthi Kumar Kotta ◽  
L. Srinivas
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Content Uniformity ◽  
In Vitro Drug Release ◽  
Mucoadhesive Tablets

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.

scholarly journals Development and In Vitro-In Vivo Evaluation of a Novel Sustained-Release Loxoprofen Pellet with Double Coating Layer

Pharmaceutics ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 260 ◽  
Author(s):  
Dongwei Wan ◽  
Min Zhao ◽  
Jingjing Zhang ◽  
Libiao Luan
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Diffusion Rate ◽  
Immediate Release ◽  
Pharmacokinetic Studies ◽  
Release Tablet

This study aimed to develop a novel sustained release pellet of loxoprofen sodium (LXP) by coating a dissolution-rate controlling sub-layer containing hydroxypropyl methyl cellulose (HPMC) and citric acid, and a second diffusion-rate controlling layer containing aqueous dispersion of ethyl cellulose (ADEC) on the surface of a LXP conventional pellet, and to compare its performance in vivo with an immediate release tablet (Loxinon®). A three-level, three-factor Box-Behnken design and the response surface model (RSM) were used to investigate and optimize the effects of the citric acid content in the sub-layer, the sub-layer coating level, and the outer ADEC coating level on the in vitro release profiles of LXP sustained release pellets. The pharmacokinetic studies of the optimal sustained release pellets were performed in fasted beagle dogs using an immediate release tablet as a reference. The results illustrated that both the citric acid (CA) and ADEC as the dissolution- and diffusion-rate controlling materials significantly decreased the drug release rate. The optimal formulation showed a pH-independent drug release in media at pH above 4.5 and a slightly slow release in acid medium. The pharmacokinetic studies revealed that a more stable and prolonged plasma drug concentration profile of the optimal pellets was achieved, with a relative bioavaibility of 87.16% compared with the conventional tablets. This article provided a novel concept of two-step control of the release rate of LXP, which showed a sustained release both in vitro and in vivo.

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