Design and evaluation of rectal drug delivery systems of non-steroidal anti-inflammatory drug

The aim of the present study was to design and evaluate the suppositories of aceclofenac a non-steroidal anti inflammatory drug (NSAID). Aceclofenac, rectal suppositories were developed by employing various hydrophilic and hydrophobic polymeric bases like gelatin, PEG-400 and hydrogenated vegetable oil using propylene glycol as plasticizer and beeswax as hardening agent. The in-vitro release rate data was evaluated statistically and was found that from all the formulations the drug release is by diffusion mechanism (r = 0.9547 to 0.9967) according to Higuchis equation. All the prepared formulations have shown zero-order release kinetics except those prepared by utilizing 15% and 20 % of PEG-400. The formulation prepared using 7.5% beeswax in hydrogenated vegetable oil has displayed zero-order drug release (r = 0.9927) and has released 99.18% of the aceclofenac within 4h, hence, this formulation is considered as a promising formulation. The stability study on the promising formulation was conducted over a period of 6 months and found that there are no significant changes in the drug content and in-vitro drug release rate (p<0.05). The result suggests that the suppositories can be prepared by employing hydrophilic and hydrophobic polymers.DOI: http://dx.doi.org/10.3329/icpj.v1i7.10810International Current Pharmaceutical Journal 2012, 1(7): 165-170

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

Current Drug Therapy ◽

10.2174/1574885515666200331104440 ◽

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.

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EFFECT OF DIFFERENT NON IONIC SURFACTANTS ON THE IN-VITRO RELEASE RATE OF A NON STEROIDAL ANTI-INFLAMMATORY DRUG FROM SOME LIPOPHILIC SUPPOSITORY BASES

Zagazig Journal of Pharmaceutical Sciences ◽

10.21608/zjps.2011.161988 ◽

2011 ◽

Vol 20 (1) ◽

pp. 1-8

Author(s):

Sayed Auda ◽

Mahmoud Ahmed ◽

S. Abd El-Rasoul

Keyword(s):

Release Rate ◽

In Vitro Release ◽

Ionic Surfactants ◽

Inflammatory Drug ◽

Anti Inflammatory ◽

Vitro Release

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Disintegration, In vitro Dissolution, and Drug Release Kinetics Profiles of k-Carrageenan-based Nutraceutical Hard-shell Capsules Containing Salicylamide

Open Chemistry ◽

10.1515/chem-2020-0028 ◽

2020 ◽

Vol 18 (1) ◽

pp. 226-231

Author(s):

Pratiwi Pudjiastuti ◽

Siti Wafiroh ◽

Esti Hendradi ◽

Handoko Darmokoesoemo ◽

Muji Harsini ◽

...

Keyword(s):

Drug Release ◽

Rate Constant ◽

Release Rate ◽

Release Kinetics ◽

Zero Order ◽

Dissolution Profile ◽

Natural Polymers ◽

Drug Release Kinetics ◽

Hard Shell

AbstractThe release of drugs from solid drug delivery materials has been studied intently in recent years. Quantitative analyses achieved from in vitro dissolution becomes easier if a zero-order mathematical model is used. Non-gelatin nutraceutical hard-shell capsules of zero size (approximately 0.7-0.8 cm) were produced from carrageenan-based natural polymers, namely carrageenan-alginate (CA) and carrageenan-starch (CS). Disintegration, dissolution and zero-order drug release kinetics of hard-shell capsules containing 100 mg of salicylamide were studied. The disintegration time of CA and CS were observed to be less than 30 min for both CA and CS. In vitro dissolution profile showed that the percentage dissolution of CA capsules was better at pH 4.5, while that of CS was poor at pH 1.2, 4.5 and 6.8. Determination of drug release kinetics profiles of carrageenan-based hardshell capsules utilized the Noyes-Whitney and Peppas-Sahlin modification rules for zero-order. The drug release from carrageenan-based capsules followed zero-order kinetics, especially at pH 6.8, and was compared to the Higuchi model. Salicylamide in CA hard-shell capsules at a pH 6.8 had a release rate constant (kH) of 2.91 %(ppm/ ppm) min-1/2, while the release rate constant of CS was 0.36 %(ppm/ppm) min-1.

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Thermosensitive Drug Delivery System SBA-15-PEI for Controlled Release of Nonsteroidal Anti-Inflammatory Drug Diclofenac Sodium Salt: A Comparative Study

Materials ◽

10.3390/ma14081880 ◽

2021 ◽

Vol 14 (8) ◽

pp. 1880

Author(s):

Lubos Zauska ◽

Stefan Bova ◽

Eva Benova ◽

Jozef Bednarcik ◽

Matej Balaz ◽

...

Keyword(s):

Drug Release ◽

Sodium Salt ◽

Release Rate ◽

Diclofenac Sodium ◽

Simulated Gastric Fluid ◽

Release Mechanism ◽

Drug Release Rate ◽

Inflammatory Drug ◽

Vis Spectroscopy ◽

Anti Inflammatory

Mesoporous SBA-15 silica material was prepared by the sol–gel method and functionalized with thermosensitive polyethylenimine polymers with different molecular weight (g·mol−1): 800 (SBA-15(C)-800), 1300 (SBA-15(C)-1300) and 2000 (SBA-15(C)-2000). The nonsteroidal anti-inflammatory drug (NSAID) diclofenac sodium was selected as a model drug and encapsulated into the pores of prepared supports. Materials were characterized by the combination of infrared spectroscopy (IR), atomic force microscopy (AFM), transmission electron microscopy (TEM), photon cross-correlation spectroscopy (PCCS), nitrogen adsorption/desorption analysis, thermogravimetry (TG), differential scanning calorimetry (DSC) and small-angle X-ray diffraction (SA-XRD) experiments. The drug release from prepared matrixes was realized in two model media differing in pH, namely small intestine environment/simulated body fluid (pH = 7.4) and simulated gastric fluid (pH = 2), and at different temperatures, namely normal body temperature (T = 37 °C) and inflammatory temperature (T = 42 °C). The process of drug loading into the pores of prepared materials from the diclofenac sodium salt solutions with different concentrations and subsequent quantitative determination of released drugs was analyzed by UV-VIS spectroscopy. Analysis of prepared SBA-15 materials modified with polyethylenimines in solution showed a high ability to store large amounts of the drug, up to 230 wt.%. Experimental results showed their high drug release into the solution at pH = 7.4 for both temperatures, which is related to the high solubility of diclofenac sodium in a slightly alkaline environment. At pH = 2, a difference in drug release rate was observed between both temperatures. Indeed, at a higher temperature, the release rates and the amount of released drug were 2–3 times higher than those observed at a lower temperature. Different kinetic models were used to fit the obtained drug release data to determine the drug release rate and its release mechanism. Moreover, the drug release properties of prepared compounds were compared to a commercially available medicament under the same experimental conditions.

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Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2016.9.3.8 ◽

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.

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Gastroretentive Floating Capsules of Risedronate Sodium: Development, Optimization, in vitro and in vivo Evaluation in Healthy Human Volunteers

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2015.8.2.6 ◽

2015 ◽

Vol 8 (2) ◽

pp. 2835-2842

Author(s):

Bhikshapathi D. V. R. N. ◽

Arun Kumar Jarathi ◽

Suresh Gande ◽

Viswaja Medipally ◽

Ramesh Bomma

Keyword(s):

Drug Release ◽

Sustained Release ◽

Zero Order ◽

Wet Granulation ◽

Capsule Formulation ◽

In Vivo Evaluation ◽

Healthy Human ◽

X Ray ◽

Human Volunteers

Background and the purpose of the study: Risedronate sodium inhibits osteoclast bone resorption and modulates bone metabolism. Risedronate has a high affinity for hydroxyapatite crystals in bone and is a potent antiresorptive agent. In the present investigation efforts were made to improve the bioavailability of risedronate sodium by increasing the residence time of the drug through sustained-release matrix capsule formulation via gastroretentive mechanism. Capsules were prepared by wet granulation technique. The influence of gel forming agents, amount of risedronate and total weight of capsules on physical properties, in vitro buoyancy, drug release, FTIR, DSC, X-ray studies were investigated. The release mechanisms were explored and explained by applying zero order, first order, Higuchi and Korsmeyer equations. The selected formulations were subjected to stability study at 40 °C/75% RH, 25 °C/60% RH for the period of three months. For all formulations, kinetics of drug release from capsules followed Higuchi’s square root of time kinetic treatment heralding diffusion as predominant mechanism of drug release. Formulation containing 25 mg HPMC K4M and 75 mg HPMC K100 LV (F-8) showed zero order release profile. There was no significant change in the selected formulation, when subjected to accelerated stability conditions over a period of three months. X-ray imaging in six healthy human volunteers revealed a mean gastric retention period of 5.60 ± 0.77 hrs for the selected formulation. Stable, sustained release effervescent floating capsules of risedronate sodium could be prepared by wet granulation technique.

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

Pharmaceutics ◽

10.3390/pharmaceutics11060260 ◽

2019 ◽

Vol 11 (6) ◽

pp. 260 ◽

Cited By ~ 4

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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FORMULATION AND EVALUATION OF CHLOROTHALIDONE LOADED MOUTH DISSOLVING FILM-A BIOAVAILABILITY ENHANCEMENT APPROACH USING MULTILEVEL CATEGORIC DESIGN

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2020v12i3.36067 ◽

2020 ◽

pp. 34-41

Author(s):

SHUBHAM BIYANI ◽

SARANG MALGIRWAR ◽

RAJESHWAR KSHIRSAGAR ◽

SAGAR KOTHAWADE

Keyword(s):

Drug Release ◽

Hydroxypropyl Methylcellulose ◽

Aqueous Dispersion ◽

Onset Of Action ◽

Polyethylene Glycol 400 ◽

Bioavailability Enhancement ◽

Disintegration Time ◽

Peg 400 ◽

Folding Endurance

Objective: The intension of the present study includes fabrication and optimization of mouth dissolving film loaded with Chlorothalidone by solvent evaporation techniques using two components and their three levels as multilevel Categoric design. Methods: Major problem associated with the development of film loaded with BCS class II drug is to increase its solubility. Here the Chlorothalidone solubility achieved by co-solvents, such as methanol. After dissolving the drug in co-solvent, this drug solution is poured into an aqueous dispersion of Hydroxypropyl Methylcellulose E5 (HPMC E5) and Polyethylene glycol 400 (PEG 400). The two independent variables selected are factor A (concentration of HPMC E5) and factor B (concentration of PEG 400) was selected on the basis of preliminary trials. The percentage drug release (R1), Disintegration time in sec (R2) and folding endurance (R3) were selected as dependent variables. Here HPMC E5 used as a film former, PEG 400 as plasticizer, mannitol as bulking agent, Sodium starch glycolate as a disintegrating agent, tween 80 as the surfactant, tartaric acid as saliva stimulating agent, sodium saccharin as a sweetener and orange flavour etc. These fabricated films were evaluated for physicochemical properties, disintegration time and In vitro drug release study. Results: The formulation F6 has more favorable responses as per multilevel categoric design is % drug release about 98.95 %, average disintegration time about 24.33 second and folding endurance is 117. Thus formulation F6 was preferred as an optimized formulation. Conclusion: The present formulation delivers medicament accurately with good therapeutic efficiency by oral administration, this mouth dissolving films having a rapid onset of action than conventional tablet formulations.

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Preparation, evaluation, and in vitro release of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules

Technology and Health Care ◽

10.3233/thc-202529 ◽

2020 ◽

pp. 1-9

Author(s):

Yunhong Wang ◽

Rong Hu ◽

Yanlei Guo ◽

Weihan Qin ◽

Xiaomei Zhang ◽

...

Keyword(s):

Drug Release ◽

Sustained Release ◽

Release Rate ◽

Orthogonal Design ◽

Drug Loading ◽

In Vitro Release ◽

Core Material ◽

Evaluation Indexes ◽

Vitro Release

OBJECTIVE: In this study we explore the method to prepare tanshinone self-microemulsifying sustained-release microcapsules using tanshinone self-microemulsion as the core material, and chitosan and alginate as capsule materials. METHODS: The optimal preparation technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules was determined by using the orthogonal design experiment and single-factor analysis. The drug loading and entrapment rate were used as evaluation indexes to assess the quality of the drug, and the in vitro release rate was used to evaluate the drug release performance. RESULTS: The best technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules is as follows: the concentration of alginate is 1.5%, the ratio of tanshinone self-microemulsion volume to alginate volume to chitosan mass is 1:1:0.5 (ml: ml: g), and the best concentration of calcium chloride is 2.0%. To prepare the microcapsules using this technology, the drug loading will be 0.046%, the entrapment rate will be 80.23%, and the 24-hour in vitro cumulative release rate will be 97.4%. CONCLUSION: The release of the microcapsules conforms to the Higuchi equation and the first-order drug release model and has a good sustained-release performance.

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