scholarly journals Development of Orodispersible Tablets of Candesartan Cilexetil-β-cyclodextrin Complex

2013 ◽  
Vol 2013 ◽  
pp. 1-13 ◽  
Author(s):  
Maddukuri Sravya ◽  
Rajamanickam Deveswaran ◽  
Srinivasan Bharath ◽  
Basappa Veerbadraiah Basavaraj ◽  
Varadharajan Madhavan
Keyword(s):  
Inclusion Complex ◽  
Inclusion Complexes ◽  
Candesartan Cilexetil ◽  
Water Soluble ◽  
Molar Ratio ◽  
Spectral Studies ◽  
Dissolution Profile ◽  
Cyclodextrin Complex ◽  
Disintegration Time ◽  
Orodispersible Tablets

The aim of this study was to investigate the use of inclusion complexation technique employing β-cyclodextrin in improving the dissolution profile of candesartan cilexetil, a BCS class-II drug, and to formulate the inclusion complex into orodispersible tablets. The inclusion complexes were formed by physical mixing, kneading, coevaporation, and lyophilisation methods. Inclusion complexes were characterized by FTIR, DSC, XRD, NMR, and mass spectral studies. Inclusion complexes prepared using kneading, and lyophilisation techniques in the molar ratio 1 : 5 with β-cyclodextrin were used for formulating orodispersible tablets by direct compression with different superdisintegrants like croscarmellose sodium, crospovidone, sodium starch glycolate, and low substituted hydroxypropyl cellulose in varying concentrations. The directly compressible powder was evaluated for precompression parameters, and the prepared orodispersible tablets were evaluated for postcompression parameters. Drug-excipient compatibility studies showed no interaction, and characterization proved the formation of inclusion complex. In vitro disintegration time was found to be within 3 minutes, and all the formulations showed complete drug release of 100% within 20 minutes. The optimized formulation was found to be stable after 6 months and showed no significant change in drug content. This work proved β-cyclodextrins to be effective solubilizing agent in improving the solubility of poorly water soluble drugs.

Solubility Enhancement of the Poorly Water-Soluble Antiulcer Drug Famotidine by Inclusion Complexation

2013 ◽  
Vol 6 (1) ◽  
pp. 1983-1989 ◽  
Author(s):  
Shabnam Ain ◽  
V Gupta ◽  
Babita K ◽  
Q Ain ◽  
J Dahiya
Keyword(s):  
Inclusion Complex ◽  
Dissolution Rate ◽  
Phosphate Buffer ◽  
Physical Mixture ◽  
Water Soluble ◽  
Molar Ratio ◽  
Phase Solubility ◽  
Distilled Water ◽  
Physicochemical Interaction ◽  
Mixture Phase

Aqueous solubility is a critical factor for optimum drug delivery. In the present study, we investigated the potential of drug-cyclodextrin complexation as an approach for improving the solubility and bioavailability of famotidine, an H2-receptor antagonist and acid reducing drug which has poor solubility and bioavailability. Solubility improvement of drug by β-cyclodextrin was done by simple complexation approach using physical, kneading and co-precipitation methods and compared with physical mixture. Phase solubility profile indicated that the solubility of famotidine was significantly increased in presence of β-cyclodextrin and shows a linear graph with β-cyclodextrin indicating formation of inclusion complexes in a 1:1 molar ratio. β-Cyclodextrin-famotidine mixture have maximum stability constant 1477.6 M-1. The inclusion complex ratio 1:1 of kneading mixture was selected based on drug release profile and compared with physical mixture. Further characterization was done by  using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM) to identify the physicochemical interaction between drug and carrier and its effect on dissolution. Dissolution rate studies for selected inclusion complex was performed in 0.1 N HCl (pH 1.2), phosphate buffer (pH 7.5) and distilled water (pH 6.8) and compared these to pure drug profile which was found to be 2.34 fold increase in distilled water, 1.83 fold in HCl and 2.01 fold in phosphate buffer (pH 7.5). These results suggest that the kneaded complex of famotidine with β-cyclodextrin as hydrophilic complexation agent can substantially enhance the solubility and dissolution rate. Such complex has promising potential to improve the bioavailability of famotidine.  

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.

EFFECT OF DRUG TO B-CYCLODEXTRIN RATIO AND METHOD OF COMPLEXATION IN THE DEVELOPMENT OF B-CYCLODEXTRIN INCLUSION COMPLEX OF OFLOXACIN

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (12) ◽  
pp. 34-40
Author(s):  
M Panchpuri ◽  
◽  
D Singh ◽  
A Semalty ◽  
M. Semalty
Keyword(s):  
Inclusion Complex ◽  
In Vitro Dissolution ◽  
Molar Ratio ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
Dissolution Study ◽  
Drug Content ◽  
Kneading Method ◽  
Made In

Ofloxacin, a second generation fluoroquinolone, shows poor aqueous solubility and dissolution profile. Thus, ofloxacin–β-cyclodextrin complexes were prepared to improve its dissolution by imparting an environment of improved hydrophilicity. Ofloxacin was complexed with β-cyclodextrin (in 1:1 and 1:2 molar ratio) by two different methods namely, solvent evaporation and kneading method. These inclusion complexes were evaluated for solubility, drug content, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X ray powder diffraction (XRPD) and in vitro dissolution study. The highest drug content (35.45%) was found in complex made by kneading method (OK1:1) in 1:1 molar ratio. All the complexes OSE1:1, OSE1:2, OK1:1, OK1:2 were found to be showing rough and porous surface morphology in SEM. Solubility as well as the dissolution of the complexes was found to be improved. Complex prepared by kneading method in 1:1 molar ratio (OK1:1) showed a marked improvement in percent drug release (88.94%) than that of pure drug (54.22%) at the end of 1 hour in dissolution study. FTIR, DSC and XRPD data confirmed the formation of inclusion complex. It was concluded that the complex made in 1:1 molar ratio (irrespective of the method) showed better solubility and dissolution profile as compared to complex made in 1:2 molar ratio.

scholarly journals Quality Enhancement by Inclusion Complex Formation of Simvastatin Tablets

2013 ◽  
Vol 59 (4) ◽  
pp. 223-225
Author(s):  
Rédai Emőke ◽  
Sipos Emese ◽  
Pocsai Zs ◽  
Tőkés B ◽  
Székely P
Keyword(s):  
Inclusion Complex ◽  
Inclusion Complexation ◽  
Molar Ratio ◽  
Physical Parameters ◽  
Quality Enhancement ◽  
Direct Compression ◽  
Dissolution Profile ◽  
Host Molecule ◽  
Inclusion Complex Formation ◽  
Dissolution Properties

Abstract Introduction: Simvastatin is an inhibitor of hydroxy-methyl-glutaryl-coenzyme A reductase, used in the treatment of hypercholesterolemia. To enhance its bioavailability by inclusion complexation, as host molecule randommethyl-β-cyclodextrin had been used. After evaluating the complexes we chose the kneading product in 1:2 molar ratio for incorporation of 10 mg simvastatin tablets. Materials and methods: We prepared homogenous mixtures of the inclusion complex and some excipients. The tablets were prepared by direct compression. The tablets were evaluated in regard to: weight uniformity, thickness, diameter, hardness, friability, disintegration and dissolution profile. Results: Weights are in the range of 196-208 mg, diameter 6.83-6.86 mm, height 3.86-4.01 mm, hardness 78.3-113.1 N, friability 0.75- 1.19 %, disintegration above 15 minutes. The dissolved amounts of simvastatin from the tablets are higher compared to the dissolution of pure simvastatin, but lower than the dissolution of the complex itself. Excipients, like disintegrants and lubricants greatly influence the dissolution properties of the tablets. Conclusions: According to our results, tablets containing inclusion complex of simvastatin exhibit better solubility, according to the dissolved amount of simvastatin, than pure drug alone. Proper physical parameters of the tablets are obtained by application of 5 % Primellose

Development of Pediatric Orodispersible Tablets Based on Efavirenz as a New Therapeutic Alternative

2020 ◽  
Vol 18 (5) ◽  
pp. 342-353
Author(s):  
José Lourenço de Freitas Neto ◽  
Ilka do Nascimento Gomes Barbosa ◽  
Camila Gomes de Melo ◽  
Matheus Alves Ângelos ◽  
Larissa Morgana dos Santos Mendes ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Aqueous Solubility ◽  
Dissolution Profile ◽  
Multicomponent Systems ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Orodispersible Tablets ◽  
Orodispersible Tablet ◽  
Immunodeficiency Syndrome

Background: Efavirenz is the most used medication in the treatment of Acquired Immunodeficiency Syndrome (AIDS). The limited number of pediatric antiretroviral formulations approved by regulatory agencies is the most significant obstacle to adequate and efficient pharmacotherapy for this group of patients. The efavirenz has excellent therapeutic potential, but has low aqueous solubility/bioavailability. Methods: To minimize these limitations, multicomponent systems with β-cyclodextrin and polyvinylpyrrolidone K-30 were obtained. Due to the limited number of pediatric antiretroviral formulations, the development of a pediatric orodispersible tablet is an alternative that is thought easy to administer, since it disintegrates rapidly in the oral cavity. The multicomponent systems were obtained by the method of kneading and characterized by solubility test, X-ray diffraction, differential scanning calorimetry and infrared absorption spectroscopy by Fourier transform. The orodispersible tablets were prepared by direct compression. The quality control of hardness, friability, disintegration, and dissolution was performed. The influence of the components of the formulation on the characteristics of the tablets was evaluated through a 22 factorial design added with three central points, to compare the effect of the dependent variables on the responses. Results: An increase in drug solubility was observed, with a decrease in crystallinity. Besides that, an excellent dissolution profile presented with more than 83% of the drug's content dissolved in less than 15 minutes. Satisfactory disintegration time and friability were observed. Conclusion: It was observed that reduced concentrations of mannitol decreased the hardness and disintegration time of the formulations. The orodispersible tablet composed of efavirenz: β- cyclodextrin: polyvinylpyrrolidone, favors greater absorption and bioavailability. It has several advantages for pediatric patients, as the dosage form disintegrates quickly in the mouth and does not require water for administration, thereby improving patient compliance with the treatment.

FORMULATION AND EVALUATION OF MOUTH DISSOLVING TABLETS OF RANITIDINE HYDROCHLORIDE

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (09) ◽  
pp. 13-20
Author(s):  
V Arora ◽  
◽  
S Kumar ◽  
P. B Mishra ◽  
N. Vashisht
Keyword(s):  
Research Work ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Taste Masking ◽  
Dissolution Profile ◽  
Cyclodextrin Complex ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Ranitidine Hydrochloride ◽  
Weight Variation

In present research work, taste masked Mouth Dissolving Tablets (MDTs) of Ranitidine Hydrochloride were designed with a view to enhance the patient compliance and provide a quick onset of action. Taste masking of the drug was done by formation of complex with β cyclodextrin. Tablets were prepared by direct compression, using superdisintegrants like crosscarmellose sodium and crosspovidone in different proportion and evaluated for the pre-compression parameters such as bulk density, compressibility, angle of repose etc. In view of the better taste palatability of such a bitter API, taste masking was carried out via making the cyclodextrin complex and sucralose was used as the sweetener to impart a palatable taste to the formulation. The prepared batches of tablets were evaluated for hardness, weight variation, friability, drug content, disintegration time and in vitro dissolution profile and found satisfactory. Among all, the formulation F7 containing 5% w/w proportion of both crosscarmellose sodium and crosspovidone was considered to be best formulation, which disintegrated completely in 19 seconds and released up to 98.38% of the drug.

scholarly journals Preparation of Amylose-Oligo[(R)-3-hydroxybutyrate] Inclusion Complex by Vine-Twining Polymerization

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2595
Author(s):  
Jun-ichi Kadokawa ◽  
Yuki Wada ◽  
Kazuya Yamamoto
Keyword(s):  
Inclusion Complex ◽  
Inclusion Complexes ◽  
Water Soluble ◽  
Enzymatic Polymerization ◽  
X Ray Diffraction ◽  
Mechanism Of Formation ◽  
X Ray ◽  
Partial Formation ◽  
Glucan Phosphorylase ◽  
Polymerization Conditions

In this study, we attempted to prepare an amylose-oligo[(R)-3-hydroxybutyrate] (ORHB) inclusion complex using a vine-twining polymerization approach. Our previous studies indicated that glucan phosphorylase (GP)-catalyzed enzymatic polymerization in the presence of appropriate hydrophobic guest polymers produces the corresponding amylose–polymer inclusion complexes, a process named vine-twining polymerization. When vine-twining polymerization was conducted in the presence of ORHB under general enzymatic polymerization conditions (45 °C), the enzymatically produced amylose did not undergo complexation with ORHB. However, using a maltotriose primer in the same polymerization system at 70 °C for 48 h to obtain water-soluble amylose, called single amylose, followed by cooling the system over 7 h to 45 °C, successfully induced the formation of the inclusion complex. Furthermore, enzymatic polymerization initiated from a longer primer under the same conditions induced the partial formation of the inclusion complex. The structures of the different products were analyzed by X-ray diffraction, 1H-NMR, and IR measurements. The mechanism of formation of the inclusion complexes discussed in the study is proposed based on the additional experimental results.

scholarly journals Intercalation of Aceclofenac/Sulfobutyl Ether-β-cyclodextrin Complex into Layered Double Hydroxides through Swelling/Restoration Reaction and Its Controlled-Release Properties

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Shifeng Li ◽  
Tan Zhang ◽  
Min Xiao ◽  
Zhigang Zhang ◽  
Wenxiu Li ◽  
...  
Keyword(s):  
Controlled Release ◽  
Inclusion Complex ◽  
Layered Double Hydroxides ◽  
Dissolution Profile ◽  
Cyclodextrin Complex ◽  
Release Process ◽  
Buffer Solutions ◽  
Sulfobutyl Ether ◽  
Restoration Method ◽  
Double Hydroxides

Aceclofenac (AC)/sulfobutyl ether-β-cyclodextrin (SBE-β-CD) inclusion complex intercalated layered double hydroxides (LDHs) composite were prepared by swelling/restoration method. After swelling/restoration, thed-spacing of LDHs is expanded to 2.23 nm, which clearly demonstrates the successful intercalation of AC/SBE-β-CD into LDHs layer. AC/SBE-β-CD inclusion complex in the interlayer has monolayer arrangement based on thed-spacing of LDHs and torus thickness of SBE-β-CD. The AC release performances were also studied in buffer solutions with different pH values. The results show AC/SBE-β-CD intercalated LDHs not only enhance the dissolution profile of AC but also exhibit a controlled-release process, which indicates that the AC/SBE-β-CD-LDHs have a potential application in drug delivery agent.

scholarly journals Research Article. Kinetics and Mechanism of Drug Release from Loratadine Orodispersible Tablets Developed without Lactose

2017 ◽  
Vol 63 (1) ◽  
pp. 23-26
Author(s):  
Adriana Ciurba ◽  
Emőke Rédai ◽  
Ioana Pop ◽  
Paula Antonoaea ◽  
Nicoleta Todoran
Keyword(s):  
Zero Order ◽  
Order Kinetic ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Research Article ◽  
Orodispersible Tablets ◽  
Orally Disintegrating Tablets ◽  
Dissolution Properties ◽  
Gelatinized Starch ◽  
Croscarmellose Sodium

Abstract Objective: The aim of this study is to develop lactose-free orodispersible tablets with loratadine for patients with lactose intolerance. Materials and methods: Seven compositions (F1-F7) of 10 mg loratadine were prepared in form of orally disintegrating tablets, by direct compression, using croscarmellose sodium and pre-gelatinized starch in various concentrations as superdisintegrants, diluted with microcrystalline cellulose and combined with mannitol and maltodextrin as binder agents. The tablets had been studied in terms of their pharmacotechnical characteristics, by determining: the weight uniformity of the tablets, their friability, breaking strength and disintegration time, drug content and the dissolution profile of loratadine. The statistical analyses were performed with GraphPad Prism Software Inc. As dependent variables, both the hardness of the tablets and their disintegration ability differ between batches due to their compositional differences (as independent variables). DDSolver were used for modeling the kinetic of the dissolution processes by fitting the dissolution profiles with time-dependent equations (Zero-order, First-order, Higuchi, Korsmeyer-Peppas, Peppas-Sahlin). Results: All proposed formulas shows rapid disintegration, in less than 15 seconds, and the dissolution loratadine spans a period of about 10 minutes. Akaike index as well as R2 adjusted parameter have demonstrated that the studied dissolution profiles are the best fitted by Zero-order kinetic. Conclusion: In conclusion, association of croscarmellose sodium (7.5%) with pre-gelatinized starch (6%) as superdisintegrants and mannitol as the binder agent (35%), positively influences the dissolution properties of loratadine from orally fast dispersible tablets.

scholarly journals DEVELOPMENT AND OPTIMIZATION OF ORODISPERSIBLE TABLETS OF CARVEDILOL BY COMBINATION OF SUPER-DISINTEGRANTS ADDITION AND SUBLIMATION TECHNIQUES

2017 ◽  
Vol 9 (7) ◽  
pp. 155
Author(s):  
Vijayanand P. ◽  
Sridevi P. ◽  
Bhagavan Raju M.
Keyword(s):  
Research Work ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Orodispersible Tablets ◽  
Orodispersible Tablet ◽  
Drug Sample ◽  
Croscarmellose Sodium ◽  
Model Drug ◽  
Hypertensive Drug ◽  
Dysphagic Patients

Objective: Objective of the present research work was to prepare orodispersible tablets of carvedilol (CDL) for dysphagic patients.Methods: Carvedilol, an anti-hypertensive drug, was chosen as a model drug in this study. Orodispersible tablets of carvedilol were prepared using different super-disintegrating agents such as crospovidone, croscarmellose sodium and sodium starch glycolate at different concentrations. The best formulation was selected based on disintegration and dissolution profile that was further taken for sublimation studies using camphor, menthol and thymol. Drug-excipients interaction studies were carried out by fourier transform infra-red (FTIR) spectrophotometer with pure drug sample and optimized formulation.Results: The orodispersible tablet formulation having 4% croscarmellose sodium disintegrated in 92 sec. Hence this formulation was considered best formulation and taken further for sublimation studies. A formulation containing 10% w/w of menthol showed disintegration time of 16 sec with more than 96.64% drug release within 15 min. Menthol leaves the porous structure as it sublimates from the tablet. This might have contributed to the decrease in disintegration time. Hence, this formulation was considered optimized.Conclusion: From this study, it can be concluded that orodispersible tablets of carvedilol may prove to be more efficacious in the treatment of hypertension particularly in dysphagic patients.

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