scholarly journals Taste Masked Orally Disintegrating Pellets of Antihistaminic and Mucolytic Drug: Formulation, Characterization, and In Vivo Studies in Human

2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Yasmeen Taj ◽  
Roopa S. Pai ◽  
V. Kusum Devi ◽  
Gurinder Singh
Keyword(s):  
Drug Formulation ◽  
Taste Perception ◽  
In Vivo Studies ◽  
Taste Masking ◽  
Disintegration Time ◽  
Ambroxol Hydrochloride ◽  
Average Size ◽  
Mouth Feel

The main aim of the present study was to evaluate the potential of orally disintegrating pellets (ODPs) as an approach for taste masking of bitter drugs, namely, Ambroxol hydrochloride (A-HCl) and Cetirizine dihydrochloride (C-DHCl). Pellets were prepared by extrusion/spheronization with Eudragit EPO, kyron T-134, Kyron T-314, mannitol, sorbitol, MCC (Avicel PH-101), sucralose, chocolate flavor, and 5% xanthum gum. The prepared pellets were characterized for percentage yield, drug content, particle size, in vitro drug release, and in vivo evaluation on humans for taste, mouth feel, and in vivo disintegration time. The results revealed that the average size of pellets was influenced greatly by the percentage of binder and extrusion speed. The optimized ODPs disintegrated in less than 20 s and showed more than 98% of drugs in ODPs dissolved within 15 min. Taste perception study was carried out on human volunteers to evaluate the taste masking ability of ODPs for taste, mouth feel, and in vivo disintegration time. Crystalline state evaluation of drugs in the optimized ODPs was conducted for X-ray powder diffraction. In conclusion, the study confirmed that ODPs can be utilized as an alternative approach for effective taste masking and rapid disintegration in the oral cavity.

scholarly journals FORMULATION, IN VITRO, AND IN VIVO EVALUATION OF TASTE-MASKED ORAL DISINTEGRATING TABLETS OF FEXOFENADINE HYDROCHLORIDE USING SEMISYNTHETIC AND NATURAL SUPERDISINTEGRANTS

2021 ◽  
pp. 99-108
Author(s):  
NAGADANI SWARNALATHA ◽  
VIDYAVATHI MARAVAJHALA
Keyword(s):  
Desirability Function ◽  
Research Work ◽  
In Vivo Studies ◽  
Taste Masking ◽  
Wet Granulation ◽  
Maximum Plasma ◽  
In Vivo Evaluation ◽  
Eudragit Epo

Objective: The aim of the present research work was to prepare and evaluate taste-masked oral disintegrating tablets (ODT) of Fexofenadine hydrochloride. Methods: In the present work, Eudragit EPO, a taste masking agent and Karaya gum (GK) (natural), Sodium starch glycolate, and Croscarmellose sodium (CCS) (semi-synthetic) super disintegrants in three ratios (3, 6,9%) were used. Taste masked granules were prepared by different ratios of the drug: Eudragit EPO (1:1, 1:1.5, 1:2) by wet granulation method. The optimized taste-masked granules (1:2) were selected by sensory evaluation test to prepare 9 Fexofenadine ODT (FH1-FH9) formulations. These were evaluated for different parameters. Then desirability function (DF) was calculated for all formulations using disintegration time (DT), time taken for the tablet to release 90% of the drug (t 90%), and % drug dissolved in 10 min (Q10) as significant parameters. Results: The best formulation (FH6) showed the highest DF value due to less DT and 100% in vitro drug release within 15 min. Thus, FH6 formulation containing 9% CCS was selected as the best among the prepared formulations to which in vivo studies were performed on rabbits to find maximum plasma concentration (Cmax), time taken to reach maximum concentration (tmax), area under the curve (AUC), rate of elimination (Kel), absorption rate (Ka) and half-life(t1/2) and compared with Fexofenadine (Allegra) marketed tablets. Total bioavailability was increased for the test formulation compared to the reference formulation. Conclusion: Fexofenadine was successfully prepared as ODT with increased AUC and decreased tmax to which stability studies were conducted which were found to be stable.

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 Formulation and Evaluation of Fast Dissolving Film of Losartan Potassium

2021 ◽  
Vol 68 (1) ◽  
Author(s):  
Bhageerathy A ◽  
Sandhya Murali ◽  
eny Sara Thomas ◽  
Sigi Vasanthkumar ◽  
Prasanth V V
Keyword(s):  
Drug Release ◽  
Physical Stability ◽  
Losartan Potassium ◽  
In Vivo Studies ◽  
Disintegration Time ◽  
Drug Content ◽  
Weight Variation ◽  
Significant Difference

A total of nine formulations of fast dissolving films of Losartan Potassium were developed by solvent casting method using film forming polymers such as HPMC E5, E15 and E50 and other film modifiers. The appearances of films were transparent, thin, flexible, elastic, smooth and transparent. The weight variation ranged between 16.14 ± 0.192 and 17.31 ± 0.313 and showed that there was no significant difference in the weight of individual formulations. All the formulations showed more than 150 of folding endurance. The drug content was found to be in an acceptable range for all the formulations which indicated uniform distribution of drug. A rapid dissolution of all the film was observed by the dissolution test, in which above 90% of Losartan Potassium was released within 5 min. The formulation F1 showed maximum drug release (98.73) within 5 minutes. Based on the in vitro drug release, drug content and in vitro disintegration time it is found that F1 was selected as the best formulation. The formulations showed satisfactory physical stability at 40°C at 75 % RH. Losartan Potassium (LOSAR-25) is shown in Figure 4. From the results of comparative studies of marketed product and it found that F1 showed 98.73% release within 5 min and LOSAR 25 showed 90.76% release in 30 min. In vitro studies indicate that this potential drug delivery system has considerably good stability and release profile. Nevertheless, further in vivo studies are warranted to confirm these results.

scholarly journals FORMULATION AND IN VITRO EVALUATION OF EZETIMIBE RAPIDMELTS

2020 ◽  
pp. 97-103
Author(s):  
T NEELIMA RANI ◽  
Y INDIRA MUZIB
Keyword(s):  
Solid Dispersions ◽  
Ammonium Bicarbonate ◽  
In Vivo Studies ◽  
Direct Compression ◽  
Compression Method ◽  
Disintegration Time ◽  
Weight Variation ◽  
Sublimation Method

Objective: The main objective of the present research was formulation and evaluation of ezetimibe rapidmelts. Methods: As ezetimibe comes under Class II drug, solubility of the drug should be increased before formulation. For that solid dispersions were prepared with β-CD and PVP K-30 using coevaporation and kneading method. Among those solid dispersions prepared with β-CD (1:1.5) using coevaporation method has given better drug entrapment values compared to other solid dispersions. Those solid dispersions were formulated as rapidmelts using direct compression. In direct compression method, rapidmelts were prepared using superdisintegrants such as crospovidone, croscarmellose sodium, and starch 1500. Those are evaluated for both pre-compression and post-compression parameters. Rapidmelts of ezetimibe were prepared using sublimation method with subliming agents camphor, urea, and ammonium bicarbonate. The concentrations of subliming agents were found to be 2.5, 5.0, and 7.5%. Results: Rapidmelts prepared using direct compression and sublimation methods were evaluated for weight variation, hardness, friability, % drug content, and disintegration time. The best formulation was subjected to stability testing for 6 months at 25°C/60% RH and 40°C/75% RH. All the prepared formulations compiled with the pharmacopeial limits. In all the formulations, results suggest that E12 formulation has given the best results. Conclusion: From the result, it was concluded that rapidmelts prepared using sublimation method which has given better result than direct compression method. That final formulation was further evaluated for in vivo studies using rabbits.

scholarly journals Formulation, in vitro and Bioavailability Assessments of Ranitidine Rectal Suppositories

2019 ◽  
pp. 1-10
Author(s):  
Khaled Shalaby ◽  
Ahmed M. Samy ◽  
Alaa Kassem ◽  
Mohamed F. Ibrahim ◽  
Nabil K. Alruwaili ◽  
...  
Keyword(s):  
Dosage Form ◽  
Oral Solution ◽  
Water Soluble ◽  
Oral Dosage ◽  
In Vivo Studies ◽  
Content Uniformity ◽  
Melting Points ◽  
Disintegration Time

The objective of the current work was to develop and evaluate suppository dosage form in order to improve ranitidine bioavailability as a substitute to the oral administration. Suppocire (different grades), Witepsol W25 and polyethylene glycol (PEG) were used as suppository bases and prepared by molding method. The prepared formulations were examined for hardness, disintegration time, melting point, content uniformity, drug release, stability and bioavailability. The hardness ranged from 3.82 to 12.53 kg and disintegration time from 13.32 to 28.22 min. The melting points of fatty bases had values from 33.94 to 36.82±0.36ºC while PEG based suppositories melting points were directly proportional chain length. Higher content uniformity was observed in PEG based suppositories due to easy incorporation of RT into water soluble base. Release was affected by hydroxyl value and molecular weight (in cases of fatty and PEG bases respectively). All formulations were relatively stable after 12 months. In vivo studies of all formulations exhibited double peak phenomena. PEG based formula (S8) showed significant higher Cmax (10.05±1 μg/ml) and AUC0-12 (58.313±3.9 µg.h/mL) than fatty bases and oral solution. In conclusion, rectal administration of S8 could be prepared as an alternative to the oral dosage form to improve bioavailability and overcome the first-pass metabolism.

scholarly journals ORAL DELIVERY OF ZOLMITRIPTAN LOADED FAST DISINTEGRATING FILM: FORMULATION DEVELOPMENT, STATISTICAL OPTIMIZATION, IN-VITRO AND IN-VIVO EVALUATION

2019 ◽  
pp. 13-22 ◽  
Author(s):  
Iti Chauhan ◽  
Mohammad Yasir ◽  
Madhu Verma
Keyword(s):  
Oral Delivery ◽  
Stability Study ◽  
In Vivo Studies ◽  
Pharmacokinetic Parameters ◽  
Albino Rats ◽  
Formulation Development ◽  
In Vivo Evaluation ◽  
Disintegration Time

Introduction: Fast dissolving film technology has been developed out as a alternative drug delivery system that gives an exception advantage for taking medications. Objective: The aim of this study was to formulate and evaluate the Zolmitriptan loaded fast disintegrating oral film by solvent casting method. Material and methods:  A preliminary study was conducted to select a suitable film forming polymer and plasticiser concentration.The formulation was optimized with the help of 22 factorial designs in which polymer and plasticizer concentration at two levels was taken as independent factors and disintegration time, tensile strength and % elongation were taken as dependent factors. The optimized formulation OP1 was subjected to stability study as per the ICH guidelines at 40 ± 0.50C / 75 ± 5% RH for six months. In vivo studies were conducted on Wister albino rats and concentration of drug in blood was analysed by HPLC technique. Various pharmacokinetic parameters for OP1 were determined and compared with reference formulation (drug sol.). Result and Discussion: For optimized formulation various parameters were found to be in acceptable range and it was stable under specified conditions. The value of AUC0–t (ng h/ml), AUC0–∞ (ng h/ml) of the OP1 was found to be 723.91± 84.21, 770.90 ± 104.32, respectively, for the drug sol 468.56 ± 79.36, 500.37 ± 95.43 respectively. Relative bioavailability of OP1 was 1.55 time than that of drug sol. Conclusion: The formulation not only increases the bioavailability of drug but also produce the quick action for the migraine patients. 

In vitro and in vivo studies of new cationic Zn(II)‐benzonaphthoporphyrazines as photosensitizers for PDT

2001 ◽  
Vol 5 (8) ◽  
pp. 645-651
Author(s):  
M. Peeva ◽  
M. Shopova ◽  
U. Michelsen ◽  
D. Wöhrle ◽  
G. Petrov ◽  
...  
Keyword(s):  
In Vivo Studies

Effect of caffeine on theophyliine on cerebral blood flow response to brain activation: In vitro and in vivo studies

2005 ◽  
Vol 25 (1_suppl) ◽  
pp. S198-S198
Author(s):  
Joseph R Meno ◽  
Thien-son K Nguyen ◽  
Elise M Jensen ◽  
G Alexander West ◽  
Leonid Groysman ◽  
...  
Keyword(s):  
Blood Flow ◽  
Cerebral Blood Flow ◽  
Brain Activation ◽  
In Vivo Studies ◽  
Blood Flow Response ◽  
Flow Response
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