scholarly journals CINNARIZINE LIQUID SOLID COMPACTS: PREPARATION EVALUATION

2019 ◽  
Vol 11 (1) ◽  
pp. 150
Author(s):  
Sreenivas Patro Sisinthy ◽  
Shubbaneswarei Selladurai

Objective: The objective of this research was to formulate cinnarizine tablets using the liquid-solid compact technique to enhance its solubility and dissolution rate.Methods: Cinnarizine liquid-solid compacts were formulated using propylene glycol as the non-volatile solvent, Neusilin US2 as the carrier material, Aerosil 200 as the coating material and croscarmellose sodium as the disintegrant. The interaction between drug and excipients were characterized by Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) studies. Different batches of liquid, solid compacts were prepared by using varying carrier-coating excipient ratio and different concentration of liquid medication. Flow parameters such as bulk density, tapped density, Carr’s Index, Hausner’s Ratio as well as an angle of repose were used to test the flowability of the powder blend. The liquid-solid compacts were produced by direct compression method and were evaluated for tests such as weight variation, drug content, hardness, thickness, friability, wetting time, disintegration time as well as the in vitro dissolution studies.Results: The results of the preformulation studies of liquisolid compacts showed acceptable flow properties. The results of FTIR and DSC studies showed that there is no drug-excipient interactions. The different R values and concentrations were found to have a marked effect on the dissolution profile. Formulations with higher carrier: coating ratio (R-value) and lower drug concentrations displayed a better dissolution profile. The percentage of drug release of F3 with an R-value of 20 and a drug concentration of 10% was found to be 88.11% when compared to the conventional marketed tablet which released only 44.07% at the end of 2 h.Conclusion: From this research, it is inferred that liquid-solid technique is a promising and effective approach that can be used to enhance the dissolution rate of cinnarizine.

Author(s):  
Y. Shravan Kumar ◽  
Prashanthi Patel ◽  
Sravanthi Ch ◽  
Rashmi B

Aripiprazole is an atypical antipsychotic agent used for treatment of schizophrenia, bipolar disorder and major depressive disorders. In the present work, oral  disintegrating tablets of aripiprazole were developed to  enhance the patient compliance and provide rapid onset of  action. The efficacy of aripiprazole is mediated through a combination of partial agonist activity at dopamine D2 and serotonin 5HT-1A receptors and antagonist activity at 5HT-2A receptors. It has a bitter taste and poor-solubility in water. Thus, the main objective of the study is to formulate taste masked oral disintegrating tablets of aripiprazole by using inclusion complex beta-cyclodextrin to achieve a better dissolution rate and further improving the bioavailability of the drug. Oral disintegrating tablets were   prepared by direct compression method using  super disintegrant like crospovidone, croscarmellose sodium,  sodium starch glycolate and combinations of  cros-povidone with croscarmellose sodium, and crospovidone with sodium  starch glycolate in different concentrations. They were evaluated for the pre-compression parameters such as bulk density, compressibility, Hausner ratio and angle of repose. The prepared batches of tablets were evaluated for hardness, weight variation, thickness, friability, drug content, disintegration time, wetting time,    in vitro dispersion time, and in vitro dissolution profile. All these parameters were found to be satisfactory. Among all, the formulation F15 containing crospovidone 5% + cros-povidone with croscarmellose sodium 5% was considered to be the optimum formulation, which released nearly 99% of the drug in 20 minutes with a disintegration time of 10. 20 seconds. These studies indicate the viability and benefits of oral disintegrating tablets of aripiprazole. 


Author(s):  
Hemant A. Deokule ◽  
Smita S. Pimple ◽  
Praveen D. Chaudhari ◽  
Ajit S. Kulkarni

Fast dissolving strips are used as novel approaches, as it dissolves rapidly in mouth and directly reaches the systemic circulation. In present research work, an attempt has been made to prepare mouth dissolving strips of Metoclopramide hydrochloride by using a novel film former Pullulan by solvent casting method. A33 full factorial design was utilized for the optimization of the effect of independent variables such as the amount of Pullulan, amount of PEF 400, amount of SSG on mechanical properties, and % drug release of strips. The drug compatibility studies using FTIR and DSC studies formulated strips were characterized for their physicochemical parameter like weight variation, visual appearance, folding endurance, thickness, disintegration time, drug content, and in vitro dissolution studies. FTIR and DSC studies revealed that the polymer is compatible with the drug. It was found that the optimum levels of the responses for a fast release strip could be obtained at low levels of Pullulan, PEG400, and SSG. The prepared strip was clear transparent and had a smooth surface. The surface pH was found 4.8 to 5.2 be in the range of to which is close to salivary pH, which indicates that strips may have less potential to irritate the oral mucosa, thereby they are comfortable. The drug release was found to be between 90.94 to 100.5% in 2 min. The in-vitro disintegration time of strips prepared with Pullulan was in the range of 19 to 57 sec. As the concentration of SSG increases the decrease in the disintegration time of strips a decrease. The dissolution rate increased with an increase in the concentration of SSG. Hence, it can be inferred that the fast dissolving oral strips of Metoclopramide hydrochloride may produce rapid action thereby improving bioavailability and enhance the absorption by avoiding the first-pass effect.


2021 ◽  
Vol 10 (1) ◽  
pp. 59-67
Author(s):  
Mahipal Shakkarwal ◽  
Dr. Mukesh Sharma ◽  
Dr. Ram Garg ◽  
Shankar Lal Soni ◽  
Gopal Kumar Paswan ◽  
...  

The demands for fast dissolving tablets have received ever increasing day by day during the last 10-15 years for the onset of action. In the present study, the effect of superdisintegrant was compared with synthetic super disintegrants and other conventional super disintegrants in the of fast dissolving tablet formulation of Meclofenamate. Meclofenamate is an antihypertensive drug and in case of hypertension immediate treatment is required so the proposed investigation is totally based to provide the suitable treatment for hypertension. In the present work 9 formulations of Fast dissolving tablets of Cilnidipine were prepared by using Synthesized Co-proceed was evaluated and compiles with the official standards, parameters and specifications. Various formulations were prepared using four different superdisintegrant namely- kyron T-304, sodium starch glycolate, cross carmelose sodium with three concentrations (2%, 4%, 6%) by direct compression method. The blend was evaluated for pre-compression parameters like Angle of repose , bulk density , tapped density , and then tablet  evaluated post-compression parameters like thickness , drug content , hardness , weight variation  , wetting time , friability , disintegration time , dissolution time, drug release study. Formulation A8 showed the lowest disintegration time and in-vitro dissolution studies recorded that formulation A8 showed 98.64% drug release at the end of 3 minutes. The best formulations were also found to be stable and optimized formulations were subjected to the stability studies as per ICH guideline and standards.


2019 ◽  
Vol 9 (4-s) ◽  
pp. 462-468
Author(s):  
Mohd. Razi Ansari ◽  
Sumer Singh ◽  
M.A. Quazi ◽  
Yaasir Ahmed Ansari ◽  
Jameel Abbas

Among the different type of route of administration oral route for drug administration is most common route in which Orodispersible tablet is preferred for the patient which are unconscious, week or for immediate control. The tablet gets dispersed in mouth cavity without water, present study deals with formulation of Naproxen sodium mouth dissolving tablets using super disintegrants. Naproxen sodium is analgesic and NSAID, used for the treatment of pain and inflammation caused by different condition such as osteoarthritis, rheumatoid arthritis and menstrual cramps. However gastric discomfort caused by naproxen sodium result in poor patient compliance associated with it conventional doses form but now days Naproxen sodium MDTs produces rapid onset of action and minimise gastric discomfort associated with it. Thus improves patient compliance, enhance bioavailability and reduces the dose of drug. MDTs are formulated by direct compression method using super disintegrants in different proportion. The powder blend is subjected to pre-compression evaluation parameters like bulk density, true density, and tapped density and angle of repose. Formulations are evaluated for weight variation, hardness, wetting time, water absorption time, disintegration time. And in vitro dissolution studies and all formulations complies Pharmacopoeias standards. The tablets are evaluated and result compared for all five formulation the most efficacious super disintegrants for MTDs of Naproxen sodium as suggested by the dispersion time, disintegration time and drug dissolution profiles. Keywords: - MDT, Naproxen Sodium, crosscarmellose Sodium, Sodium starch glycolate, Cross-povidone.


Author(s):  
Rosy Fatema ◽  
Sumaiya Khan ◽  
A. S. M. Roknuzzaman ◽  
Ramisa Anjum ◽  
Nishat Jahan

Loratadine, a second generation H1-receptor antagonist, works by blocking the action of histamine and is widely prescribed for itching, runny nose, watery eyes, and sneezing from "hay fever" and other allergic conditions. To ensure quality the main requirements for a medicinal product are safety, potency, efficacy and stability. This research work aimed to compare and assess the quality levels of different local brands of loratadine tablets available in the drug market of Bangladesh. Six different brands of loratadine 10 mg tablet manufactured by the local companies were used for the analysis. The evaluation was performed through the determination of weight variation, hardness, friability, percent potency, disintegration time, and dissolution profile in accordance with USP-NF specifications. All brands showed acceptable weight variation and % friability. The percent potency for tested samples by UV method ranges from 97.02%-108%, showing none of the brands contains less than 90% of the active principle as per the specification. The result of the physical and chemical studies, such as in-vitro dissolution, disintegration, hardness, etc., has been found to differ but lie within the specified limit. After analyzing the data obtained from the tests, it can be claimed that loratadine 10 mg tablets manufactured and marketed by several local companies in Bangladesh meet the quality standard required to achieve the desired therapeutic outcomes.


2020 ◽  
Vol 13 (5) ◽  
pp. 100
Author(s):  
Blasco Alejandro ◽  
Torrado Guillermo ◽  
Peña M Ángeles

This work proposes the design of novel oral disintegrating tablets (ODTs) of loperamide HCl with special emphasis on disintegration and dissolution studies. The main goal was augmenting the adherence to treatment of diseases which happen with diarrhea in soldiers who are exposed to diverse kinds of hostile environments. Optimized orally disintegrating tablets were prepared by the direct compression method from galenic development to the industrial scale technique, thanks to strategic and support actions between the Spanish Army Force Lab and the Department of Biomedical Sciences (UAH). The results show that loperamide HCl ODT offers a rapid beginning of action and improvement in the bioavailability of poorly absorbed drugs. The manufactured ODTs complied with the pharmacopeia guidelines regarding hardness, weight variation, thickness, friability, drug content, wetting time, percentage of water absorption, disintegration time, and in vitro dissolution profile. Drug compatibility with excipients was checked by DSC, FTIR, and SEM studies.


INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (09) ◽  
pp. 13-20
Author(s):  
V Arora ◽  
◽  
S Kumar ◽  
P. B Mishra ◽  
N. Vashisht

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.


2014 ◽  
Vol 50 (4) ◽  
pp. 799-818 ◽  
Author(s):  
Tariq Ali ◽  
Muhammad Harris Shoaib ◽  
Rabia Ismail Yousuf ◽  
Sabahat Jabeen ◽  
Iyad Naeem Muhammad ◽  
...  

The aim of the present study was to develop tizanidine controlled release matrix. Formulations were designed using central composite method with the help of design expert version 7.0 software. Avicel pH 101 in the range of 14-50% was used as a filler, while HPMC K4M and K100M in the range of 25-55%, Ethylcellulose 10 ST and 10FP in the range of 15 - 45% and Kollidon SR in the range of 25-60% were used as controlled release agents in designing different formulations. Various physical parameters including powder flow for blends and weight variation, thickness, hardness, friability, disintegration time and in-vitro release were tested for tablets. Assay of tablets were also performed as specified in USP 35 NF 32. Physical parameters of both powder blend and compressed tablets such as compressibility index, angle of repose, weight variation, thickness, hardness, friability, disintegration time and assay were evaluated and found to be satisfactory for formulations K4M2, K4M3, K4M9, K100M2, K100M3, K100M9, E10FP2, E10FP9, KSR2, KSR3 & KSR9. In vitro dissolution study was conducted in 900 ml of 0.1N HCl, phosphate buffer pH 4.5 and 6.8 medium using USP Apparatus II. In vitro release profiles indicated that formulations prepared with Ethocel 10 standard were unable to control the release of drug while formulations K4M2, K100M9, E10FP2 & KSR2 having polymer content ranging from 40-55% showed a controlled drug release pattern in the above mentioned medium. Zero-order drug release kinetics was observed for formulations K4M2, K100M9, E10FP2 & KSR2. Similarity test (f2) results for K4M2, E10FP2 & KSR2 were found to be comparable with reference formulation K100M9. Response Surface plots were also prepared for evaluating the effect of independent variable on the responses. Stability study was performed as per ICH guidelines and the calculated shelf life was 24-30 months for formulation K4M2, K100M9 and E10FP2.


2018 ◽  
Vol 13 (2) ◽  
pp. 79
Author(s):  
Bassam Abduh Ali ◽  
Mohammed Gameel Al-haddad ◽  
Abdullah Ahmed Areqi

Clopidogrel is a medication to reduce the risk of heart disease and taken orally. Quality of drug characterizes the production process and every phamaceutical company strives for it but often it is very difficult to achieve. This study was to investigate quality control parameters of some marketed Clopidogrel tablets. To assess the quality, eight different marketed brands of Clopidogrel 75 mg tablets available in Yemeni market collected from different pharmacies in Hodeida city. Different quality parameters like weight variation, hardness, thickness and friability were determined according to established protocols. Then the in-vitro dissolution test, potency, disintegration time were also carried out. UV-spectrophotometer was used to determine the percentage released and assay at 218 nm. All the brands comply the requirements of Pharmacopoeia as they showed acceptable weight variation range. Friability of all brands was less than 1% and no significant differences in disintegration times as they disintegrated within 15 minutes. In case of dissolution profile, all brands except C6 showed acceptable dissolution time as they released more than 60% of drug in 45 minute. The hardness of only two brands was within the range. All brands also meet the potency specifications. This study suggested that most commercially Clopidogrel tablets in Yemen maintain the quality and comply with the pharmacopeia specifications.


Author(s):  
JOGABRATA TRIPATHY ◽  
SUBHASHREE SAHOO ◽  
AFRASIM MOIN ◽  
SIDDARAMAIAH ◽  
D. V. GOWDA

Objective: The study aimed to develop and evaluate an orally disintegrating tablet that contains pilocarpine and 2-hydroxy propyl β-cyclodextrin as an inclusion complex that is prepared by lyophilization used for treatment for dry mouth. Pilocarpine is utilized to treat dry mouth disorder. The inclusion complex lowers the taste of pilocarpine through the oral mucosa by the use of 2-hydroxy propyl β-cyclodextrin. Methods: The in vitro release from the insertion complex is also been studied. The parameters like differential scanning calorimetry (DSC), Fourier transformer infrared spectroscopy (FTIR), X-ray diffraction (XRD), and morphological study have been evaluated. The design of an experiment is carried out based on the concentration of croscarmellose sodium (CCS) and microcrystalline cellulose (MCC). Evaluation of the prepared orally disintegrating tablets have been carried out by different test methods like weight variation, thickness, drug content, disintegration, and in vitro dissolution study. Results: Orally disintegrating tablets are studied by utilizing the immediate pressure technique. Pilocarpine indicates the anhydrous crystalline medication, displaying sharp endothermic top at 120.2 °C, bend of 2-HPβCD demonstrates an exceptionally wide endothermal wonder among 55-100 °C for DSC. In pilocarpine spectra, characteristic band of aromatic C-H stretch at 3277 cm-1, C=C stretching at 1608 cm-1, C-N stretching at 1445 cm-1 and methoxy (CH3-O-) stretch at 2921 cm-1 was observed. The investigation shows that tablet hardness of 4.3N, breaking downtime of 12 sec and mean disintegration time is 1.562 min. Conclusion: The different diluents and super disintegrating have been applied for the quick elevation of dry mouth that helps us for patient compliance.


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