scholarly journals Correlation between in vivo mean dissolution time and in vitro mean dissolution time of ampicillin products.

1982 ◽  
Vol 5 (5) ◽  
pp. 370-372 ◽  
Author(s):  
YUSUKE TANIGAWARA ◽  
KIYOSHI YAMAOKA ◽  
TERUMICHI NAKAGAWA ◽  
MUTSUMI NAKAGAWA ◽  
TOYOZO UNO
Keyword(s):  
Dissolution Time ◽  
Mean Dissolution Time

Synthesis and characterization of Chitosan-Catechol conjugates: Development and in vitro, in silico and in vivo evaluation of mucoadhesive pellets of lafutidine

2021 ◽  
pp. 088391152199784
Author(s):  
Loveleen Kaur ◽  
Ajay Kumar Thakur ◽  
Pradeep Kumar ◽  
Inderbir Singh
Keyword(s):  
Drug Release ◽  
In Silico ◽  
Ex Vivo ◽  
Strong Interactions ◽  
Dissolution Time ◽  
Sem Images ◽  
In Vivo Evaluation ◽  
Release Studies

Present study was aimed to synthesize and characterize Chitosan-Catechol conjugates and to design and develop mucoadhesive pellets loaded with lafutidine. SEM images indicated the presence of fibrous structures responsible for enhanced mucoadhesive potential of Chitosan-Catechol conjugates. Thermodynamic stability and amorphous nature of conjugates was confirmed by DSC and XRD studies respectively. Rheological studies were used to evaluate polymer mucin interactions wherein strong interactions between Chitosan-Catechol conjugate and mucin was observed in comparison to pristine chitosan and mucin. The mucoadhesion potential of Chitosan-Catechol (Cht-C) versus Chitosan (Cht) was assessed in silico using molecular mechanics simulations and the results obtained were compared with the in vitro and ex vivo results. Cht-C/mucin demonstrated much higher energy stabilization (∆E ≈ −65 kcal/mol) as compared to Cht/mucin molecular complex. Lafutidine-loaded pellets were prepared from Chitosan (LPC) and Chitosan-Catechol conjugates (LPCC) and were evaluated for various physical properties viz. flow, circularity, roundness, friability, drug content, particle size and percent mucoadhesion. In vitro drug release studies on LPC and LPCC pellets were performed for computing t50%, t90% and mean dissolution time. The values of release exponent from Korsmeyer-Peppas model was reported to be 0.443 and 0.759 for LPC and LPCC pellets suggesting Fickian and non-Fickian mechanism representing drug release, respectively. In vivo results depicted significant controlled release and enhanced residence of the drug after being released from the chitosan-catechol coated pellets. Chitosan-Catechol conjugates were found to be a promising biooadhesive polymer for the development of various mucoadhesive formulations.

Formulation and Evaluation of Orodispersible Tablets Containing Taste Masked Mirabegron Resinate

2021 ◽  
pp. 4736-4742
Author(s):  
Sarika S. Malode ◽  
Milind P. Wagh
Keyword(s):  
Overactive Bladder ◽  
Bitter Taste ◽  
In Vitro Release ◽  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Disintegration Time ◽  
Orodispersible Tablets ◽  
Weight Variation

The objective of present work was to develop taste masked orodispersible tablets of mirabegron. Mirabegron is beta 3 adrenoceptor agonist used to treat overactive bladder. Overactive bladder (OAB) is defined as a symptom syndrome showing feeling of urgency to urinate, typically accompanied by frequent daytime and nocturnal urination, in the absence of proven infection or other obvious pathology. Over active bladders are generally common in geriatrics. Moreover, this drug has a very strong bitter taste. Frequent dosing requires frequent water intake, which further aggregates the condition of over active bladder and bitter taste of drug affects patient compliance. Hence a need arises to mask the bitter taste for development of an ODT which does not require consuming water with every dosage. In this work, the bitter taste of mirabegron was masked by forming a complex with an ion exchange resin tulsion 344. The drug resin complexation process was optimized for resin activation, drug: resin ratio, soaking time and stirring time. In –vitro release studies revealed complete drug elution from the complex within 10 minutes in pH 1.2 buffer. The taste-masked complex was then formulated into palatable orodispersible tablets using a direct compression approach by use of superdisintegrants to achieve a rapid disintegration. The tablets were evaluated for weight variation, hardness, friability, drug content, wetting time, In- vivo disintegration time and in-vitro dissolution time.

TASTE MASKING OF OXYBUTYNIN CHLORIDE USING LIPID EXCIPIENTS AND FORMULATION AS ORODISPERSIBLE TABLETS FOR GERIATRIC POPULATION

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (10) ◽  
pp. 39-46
Author(s):  
V Prakash ◽  
◽  
L. Keshri ◽  
V. Sharma ◽  
K. Pathak
Keyword(s):  
In Vitro Release ◽  
In Vitro Dissolution ◽  
Taste Masking ◽  
Dissolution Time ◽  
Disintegration Time ◽  
Geriatric Population ◽  
Orodispersible Tablets ◽  
Lipid Excipients

The aim of the present study was to mask the bitter taste of oxybutynin chloride by lipid excipients and to develop its fast disintegrating tablet. For this purpose, a blend of two lipids, glyceryl behenate and glyceryl palmitostearate was utilized for taste masking by solvent evaporation method. The evaporation of solvent was accomplished by freeze drying and taste masked granules were characterized for their micromeritic and rheological properties. The state of dispersion was analyzed by SEM and DSC. Orodispersible tablets were then formulated (F1- F6) using Polyplasdone XL as extragranular superdisintegrant and evaluated for hardness, disintegration time, in vitro dissolution time and in vivo disintegration time. Results indicated that the formulation F6 exhibited minimum in vivo disintegration time of 8 sec with effective taste masking. In vitro release analysis indicated %DE10 and %DE25 of 51.48 and 76.53 respectively. Conclusively, taste masked orodispersible formulation of oxybutynin chloride was developed that could be beneficial for geriatric population.

scholarly journals STATISTICAL INTERPRETATION AND OPTIMIZATION OF VALSARTAN FLOATING TABLETS USING BOX-BEHNKEN DESIGN

2019 ◽  
pp. 44-53
Author(s):  
SANKHA BHATTACHARYA
Keyword(s):  
Akaike Information Criterion ◽  
Bayesian Information Criterion ◽  
Information Criterion ◽  
Stability Study ◽  
Therapeutic Window ◽  
Dissolution Time ◽  
Floating Tablets ◽  
Mean Dissolution Time ◽  
Styrene Divinylbenzene

Objective: The main purpose of this study was to formulate and statistically evaluate 300 mg floating tablets of valsartan. Methods: Floating tablets of valsartan was prepared in 16 station rotary punching machine by considering 300 mg of valsartan as drug, 40-60 mg of hydroxypropyl methylcellulose (HPMC) K100M and 20-40 mg of poly (styrene-divinylbenzene) as polymers and 20 mg of sodium bicarbonate as gas generating agents. Since upper stomach has maximum therapeutic window for valsartan absorption, hence Gastroretentive Floating Tablets (GRFTs) was prepared by implementing Box-Bentham Design. The pre and post compression parameters were optimized using Statistica 10 software. From the in vitro buoyancy and drug release studies and interpretation of statistical outcomes viz. Akaike Information Criterion (AIC), Bayesian Information Criterion (BIC), Root Mean Squared Error (RMSE), Dissolution Efficiency (DE), Mean Dissolution Time (MDT), desirability study, it was concluded that batch VF5 formulation was found to be the most optimized formulation. Results: The floating time of VF5 was found to be 132±0.33 sec, in vitro buoyancy time was 18 h, Akaike Information Criterion (AIC) was 54.97, Bayesian Information Criterion (BIC) was 5.13, percentage dissolution efficacy was 56.39%, mean dissolution time was 5.19hr. Further, six-month stability study was performed as per ICH QIA guideline. After performing two-way ANOVA within stability study response variables, it was confirmed that the interaction was most significant. Conclusion: Valsartan floating drug delivery system was successfully developed by considering HPMC K100M and poly (styrene-divinylbenzene) as polymers. Among all the nine batches, VF5 was found to be the best-optimized batch.

scholarly journals Optimized Taste-Masked Microparticles for Orally Disintegrating Tablets as a Promising Dosage Form for Alzheimer’s Disease Patients

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 1046
Author(s):  
Lalinthip Sutthapitaksakul ◽  
Kasitpong Thanawuth ◽  
Crispin R. Dass ◽  
Pornsak Sriamornsak
Keyword(s):  
Particle Size ◽  
Water Phase ◽  
In Vitro Dissolution ◽  
Simulated Gastric Fluid ◽  
Dissolution Time ◽  
Orally Disintegrating Tablets ◽  
Stirring Time ◽  
Outer Water

The objective of this research was to optimize the tasted-masked microparticles for orally disintegrating tablets containing donepezil hydrochloride using quality risk assessment and design of experiment approaches. The double emulsion solvent evaporation technique using aminoalkyl methacrylate copolymer (AMC) was used to prepare taste-masked microparticles. Factors affecting the quality of the taste-masked microparticles were analyzed using an Ishikawa diagram. A risk-ranking approach was used to rank the formulation and process risks. Furthermore, the effect of AMC quantity, stirring time, and volume of outer water phase on various responses, such as particle size, the amount of drug dissolved at 5 min (Q5) in simulated saliva fluid, and mean dissolution time (MDT) in simulated gastric fluid, was investigated using the Box-Behnken design. The optimized microparticles were then used to prepare orally disintegrating tablets (ODTs) and evaluated by in vitro and in vivo testing. The results demonstrated that particle size was influenced by the AMC amount and stirring time. Q5 was significantly affected by the amount of AMC and the volume of the outer water phase. On the other hand, these two factors had a positive effect on MDT. The optimized microparticles had a particle size of 174.45 ± 18.19 µm, Q5 of 5.04%, and MDT of 5.97 min. The ODTs with taste-masked microparticles showed acceptable in vitro dissolution with an MDT of 5 min. According to the results of a panel of six human volunteers, they greatly improved palatability.

In Vitro and In Vivo Evaluation of Taste Masked Chlorhexidine-Releasing Oral Films

2017 ◽  
Vol 7 (03) ◽  
Author(s):  
Palekar – Shanbhag P. ◽  
Belatikar S. ◽  
Sahane C.
Keyword(s):  
In Vitro Dissolution ◽  
Taste Masking ◽  
Dissolution Time ◽  
Dissolution Profile ◽  
In Vivo Evaluation ◽  
Activity Effect ◽  
Arginine Hydrochloride ◽  
Oral Films

The present investigation was undertaken with the objective of formulating chlorhexidine diacetate containing fast dissolving oral films to serve as superior alternative to mouthwash, aiming at consumer compliance. Various film forming agents, plasticizers and taste masking agents were evaluated for optimizing the composition of fast dissolving oral films. The potential of arginine hydrochloride as taste masking agent for fast dissolving oral films containing hydroxypropylmethylcellulose E5 (HPMC E5), propylene glycol and sucralose were formulated. Fast dissolving oral films of chlorhexidine diacetate were evaluated for the in vitro dissolution profile and in vitro microbiological assay. Oral films exhibited satisfactory in vitro dissolution profile and in vitro antimicrobial activity. Effect of incorporation of eugenol on the in vivo performance of oral films was evaluated in human volunteers. Arginine hydrochloride and eugenol containing oral films improved effectiveness and acceptability of films with respect to taste masking, mouth feel and mouth freshening without compromising the in vivo dissolution time.

scholarly journals EVALUATION OF DISINTEGRATION AND DISSOLUTION TEST OF METOCLOPRAMIDE ORALLY DISINTEGRATING TABLET USING MALTODEXTRINS FROM BANANA STARCH (MUSA PARADISIACA L) AS SUPERDISINTEGRANT

2018 ◽  
Vol 11 (13) ◽  
pp. 210 ◽  
Author(s):  
Minda Sari Lubis
Keyword(s):  
Dissolution Time ◽  
Dissolution Test ◽  
Test Results ◽  
Orally Disintegrating Tablet ◽  
Musa Paradisiaca ◽  
In Vitro Disintegration ◽  
Better Than

  Objective: The objective of this study was to know maltodextrin can be used as a superdisintegrant and to know the dissolution time and to know disintegration and dissolution test of metoclopramide orally disintegrating tablet (ODT) better than conventional metoclopramide tablets.Methods: The methods used in this study include the formulation of banana starch, formulation of maltodextrin, and then maltodextrin formulated into ODT with metoclopramide drug model, and evaluated the disintegration and dissolution test of ODT metoclopramide.Results: The results of the evaluation of 5 ODT formulas studied, showed ODT with maltodextrin 15% (ODT 4) gave the fastest in vitro disintegration of 22.2 s, the in vivo disintegration averaged between 55.38 s and 75.72 s, and dissolution test results against ODT 4 and metoclopramide tablets (positive comparator) showed statistically significant differences (p<0.05).Conclusion: Maltodextrin can be formulated superdisintegrant on metoclopramide ODT by giving disintegration, and dissolution was better than the conventional tablets.

scholarly journals Estimation of the In Vivo Release of Amiodarone From the Pharmacokinetics of Its Active Metabolite and Correlation With Its In Vitro Release

2021 ◽  
Vol 11 ◽  
Author(s):  
Maytham Razaq Shleghm ◽  
Constantin Mircioiu ◽  
Victor A. Voicu ◽  
Ion Mircioiu ◽  
Valentina Anuta
Keyword(s):  
Active Metabolite ◽  
Water Solubility ◽  
In Vitro Release ◽  
Dissolution Time ◽  
Pharmacokinetic Data ◽  
Square Root ◽  
Reference Drug ◽  
Time Scaling

Due to its very low water solubility and complex pharmacokinetics, a reliable point-to-point correlation of its in vitro release with its pharmacokinetics has not been achieved so far with amiodarone. The correlation of the in vitro dissolution of a drug with the pharmacokinetics of one of its metabolites was recently proposed by the authors of the article as an additional or alternative analysis to the usual in vitro correlations in vivo, mainly in the case of fast-absorbing drugs that have metabolites with a significant therapeutic effect. The model proposed by the authors considers that amiodarone has a slow dissolution, rapid absorption, and rapid metabolism, and before returning to the blood from other compartments, its pharmacokinetics is determined mainly by the kinetics of release in the intestine from the pharmaceutical formulation. Under these conditions, the rate of apparition of desethylamiodarone in the blood is a metric of the release of amiodarone in the intestinal fluid. Furthermore, it has been shown that such an estimated in vivo dissolution is similar, after time scaling, to the dissolution measured experimentally in vitro. Dissolution data of amiodarone and the pharmacokinetic data of its active metabolite desethylamiodarone were obtained in a bioequivalence study of 24 healthy volunteers. The elimination constant of the metabolite from plasma was estimated as the slope of the linear regression of logarithmically transformed data on the tail of plasma levels. Because the elimination of desethylamiodarone was shown to follow a monoexponential model, a Nelson–Wagner-type mass equilibrium model could be applied to calculate the time course of the “plasma metabolite fraction.” After Levi-type time scaling for imposing the in vitro–in vivo correlation, the problem became that of the correlation between in vitro dissolution time and in vivo dissolution time, which was proven to follow a square root model. To validate the model, evaluations were performed for the reference drug and test drug separately. In both cases, the scaled time for in vivo dissolution, t*, depended approximately linearly on the square root of the in vitro dissolution time t, with the two regression lines being practically parallel.

Induction and Differentiation of Dental Epithelium in Vivo and in Vitro

1982 ◽  
Vol 40 ◽  
pp. 142-145
Author(s):  
E. J. Kollar
Keyword(s):  
Connective Tissue ◽  
Oral Mucosa ◽  
Basal Lamina ◽  
Functional Derivatives ◽  
Specific Source ◽  
Dental Epithelium ◽  
Connective Tissue Stroma

The differentiation and maintenance of many specialized epithelial structures are dependent on the underlying connective tissue stroma and on an intact basal lamina. These requirements are especially stringent in the development and maintenance of the skin and oral mucosa. The keratinization patterns of thin or thick cornified layers as well as the appearance of specialized functional derivatives such as hair and teeth can be correlated with the specific source of stroma which supports these differentiated expressions.

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