scholarly journals FORMULATION AND EVALUATION OF PROCHLORPERAZINE MALEATE SUSTAINED RELEASE FLOATING TABLET

Author(s):  
Ahmed Abdulameer Albadry ◽  
Wedad K. Ali ◽  
Fouad A. Al-saady

<p><strong>Objective: </strong>The objective of this study was to formulate once daily sustained oral release floating tablet of prochlorperazine maleate, this floating tablet has many advantages like reduction in dosing frequency, increase bioavailability, enhance patient compliance, and improve drug solubility.</p><p><strong>Methods: </strong>The prochlorperazine maleate floating tablets were formulated by using hydrophilic swellable polymer and gas generating agent. In this study, 15 formulas were prepared with many variables in order to achieve an optimum dissolution and floating behaviour for the floating tablet. The all prepared formulas were tested for bulk density, tap density, angle of repose, Carr's Index, thickness, weight variation, hardness, friability, drug content, <em>in vitro</em> dissolution test, <em>in vitro </em>buoyancy, and swelling index.</p><p class="Default"><strong>Results: </strong>Formula (F2) that contain 55% (w/w) <a href="https://www.google.iq/url?sa=t&amp;rct=j&amp;q=&amp;esrc=s&amp;source=web&amp;cd=3&amp;ved=0ahUKEwjh383ow9LPAhWF6RQKHRChCVgQFggpMAI&amp;url=https%3A%2F%2Fwww.ulprospector.com%2Fen%2Fna%2FFood%2FDetail%2F895%2F563462%2FBenecel-Hydroxypropylmethylcellulose-HPMC-K4M&amp;usg=AFQjCNGgfyJECkumK5cpU_6luVwwJ2fKxA&amp;bvm=bv.135258522,d.d24">hydroxypropyl methylcellulose</a> k4M (HPMCK4M), 5 % (w/w) sodium bicarbonate (NaHCO<sub>3</sub>) have acceptable flow properties and compressibility index and good physical properties with floating lag time (16±0.57) seconds and total floating time (32±0.29) h with 100% release of prochlorperazine maleate at the end of 24 h. Fourier transform infrared spectroscopy (FTIR) study of optimum formula (F2) showed no chemical interaction between the drug and the excipients that used in the formula.<strong></strong></p><p><strong>Conclusion: </strong>It can be concluded that that the selected formula (F2) can be a promising formula for the preparation of gastro retentive floating drug delivery systems of prochlorperazine maleate.</p>

2018 ◽  
Vol 10 (6) ◽  
pp. 119 ◽  
Author(s):  
Anas T. Alhamdany ◽  
Ali Khidher Abbas

Objective: The aim of this study was to formulate a developed floating tablet of amlodipine using different concentrations and types of hydrophilic and hydrophobic polymers to be conserved in the stomach for modulating solubility and bioavailability, diminishes drug waste and decline side effects.Methods: Through this study, eleven innovative formulations of amlodipine floating tablets were prepared [mixture of amlodipine, sodium bicarbonate (NaHCO3), hydroxypropyl methylcellulose (HPMC) E50, HPMC K100M, ethylcellulose (EC) 5 mp. a. s.] by direct compression method. The pre-compressed mixtures were then evaluated for numerous parameters such as angle of repose, bulk density, tapped density, Carr's compressibility index and Hausner's ratio. After compression, tablets were subjected to several tests like; floating behavior of tablets, tablet thickness, hardness test, friability test, weight variation, in vitro dissolution test. In addition, the optimum formulation was evaluated for Fourier transform-infrared (FT-IR) and differential scanning calorimetry (DSC) tests. Results: From in vitro dissolution tests and kinetic assessments; F8 was selected as an optimum formula, depending on the R2 value of zero order kinetics (0.9915) and (n) value of Korsmeyer-Peppas (0.9635) which indicate purely relaxation zero order kinetic with good delaying in drug release that was reached to 14 h.Conclusion: It can be concluded that the developed formulation of a certain combination of low viscosity grades of HPMC and EC was considered an efficient floating tablet.


Author(s):  
Parasuram Rajam Radhika ◽  
Nishala N ◽  
Kiruthika M ◽  
Sree Iswarya S

Objective: The present study was undertaken to prolong the release of orally administered drug. The aim is to formulate, develop, and evaluate theintragastric buoyant tablets of venlafaxine hydrochloride, which releases the drug in a sustained manner over a period of 12 hrs. Different formulationswere formulated using the polymers Carbopol 934 P, xanthan gum, hydroxypropyl methylcellulose (HPMC K100M) with varying concentration ofdrug: Polymer ratio of 1:1, 1:1.5, 1:2, in which sodium bicarbonate acts as gas generating agent, and microcrystalline cellulose as a diluent.Methods: The tablets were prepared by direct compression and evaluated for tablet thickness, weight variation, tablet hardness, friability, in vitrobuoyancy test, in vitro drug release and Fourier transform infrared spectroscopy. Formulations were evaluated by floating time, floating lag time and in vitro drug release. Dissolution profiles were subjected for various kinetic treatments to analyze the release pattern of drug.Results: It was found that drug release depends on swelling, erosion, and diffusion, thus following the non-Fickian/anomalous type of diffusion.Formulation F8 was considered as an optimized formulation for gastro retentive floating tablet of venlafaxine hydrochloride. The optimizedformulation showed sustained drug release and remained buoyant on the surface of the medium for more than 12 hrs. As the concentration of HPMCK100M increases in the formulation the drug release rate was found to be decreased. The optimized formulation was subjected for the stability studiesand was found to be stable as no significant change was observed in various evaluated parameters of the formulation.Conclusion: It can be concluded that floating drug delivery system of venlafaxine hydrochloride can be successfully formulated as an approach toincrease gastric residence time, thereby improving its bioavailability.Keywords: Venlafaxine hydrochloride, Intragastric buoyant, Floating drug delivery systems, Hydroxypropyl methyl cellulose K100M, Carbopol 934 P,Xanthan gum.


2019 ◽  
Vol 9 (4-A) ◽  
pp. 415-424
Author(s):  
Eknath B Thakare ◽  
Prashant S. Malpure ◽  
Avish D. Maru ◽  
Yashpal M. More

The aim of present investigation was formulation and evaluation of mucoadhesive buccal tablet of Repaglinide to study the effect of different polymers on release profile of drug for prolonged release. In this study mucoadhesive buccal tablet were prepared by direct compression method. Various rheological characteristics of the powder bed like bulk density, compressibility index, and angle of repose were evaluated and studied. Mucoadhesive buccal tablets were compressed on a 8 station mini press using 10 mm flat faced punches and were all assessed for weight variation, hardness, thickness, percent swelling index, mucoadhesive strength and in vitro release of the drug by using USP TDT 08L dissolution testing apparatus method II using a paddle at 50 rpm. Data was optimized by using 32 full factorial design by using software named as design expert and with the help of kinetic study. The stability studies showed that there is no decrease in the drug content of all formulations for the period of 2 months. Keywords: Buccal tablet, Repaglinide, HPMC K100M, Xanthan gum.


2020 ◽  
Vol 10 (1) ◽  
pp. 5-10
Author(s):  
Muhammad Abbas ◽  
Musharraf Abbas ◽  
Fatima Tariq ◽  
Rabiya Yasin ◽  
Muhammad Nabeel

In the modern era, chewable tablets are preferred over conventional dosage forms by pediatric, geriatric and bedridden patients due to difficulty in swallowing, lesser amount of water for swallowing medications as well as unable to tolerate the bitter taste of certain drugs. Chewable tablets of Desloratadine (DS) were formulated by aqueous and non-aqueous granulation method using water paste and Isopropyl alcohol (IPA) as a wetting agents respectively. Desloratadine is used to treat the symptoms of allergy such as sneezing, watery eyes. In the recent research, we have formulated eight trials by various concentrations of excipients. For instance; lactose, talcum, magnesium stearate, blue color, flavor, aspartame, mannitol, avicel 101 and polyvenylpyrollidine (PVP). Pre-compression and post compression parameters (thickness, hardness, friability weight variation and drug content) of the formulations were evaluated. B3 was our optimum dosage form because its Hausner’s ratio, compressibility index, bulk density, tap density, angle of repose have optimum values i.e. 1.01, 5.1%, 0.66(g/cc), 0.69(g/cc), 26.1º respectively and post-compression i.e. thickness, hardness, friability weight variation and drug content have values, 2.9mm, 3.9(kg/cm²), 0.6%, 99.5% respectively. Tablets prepared by wet granulation technique showed reasonable release profile i.e. 100% within the required time i.e. 2 hours.  Moreover, organoleptic evaluation of all formulations were performed. Keywords: Desloratadine, chewable, magnesium stearate, aspartame, compressibility, granulation.


Author(s):  
Ashish Masih ◽  
Ajay Kumar Tiwari

Objective: The present work is aimed to formulate fast dissolving stable tablet formulation a preferred combination of Amoxycillin trihydrate (Beta-lactum antibiotic) and Potassium clavulanate (Beta-lactum inhibitor) by using various super disintegrants.Methods: Fast dissolving tablets are prepared by direct compression method using super disintegrants i.e. sodium starch glycolate, crospovidone, croscarmellose sodium. Aspartame as a sweetener and trusil mango flavor were used to increase palatability. Reduction in the dose of Amoxycillin trihydrate and Potassium clavulanate tablet was possible by developing fast dissolving tablet. Results: The powder blends were subjected to various pre-formulation evaluations such as, tapped density, bulk density, hausner’s ratio, the angle of repose and compressibility index. The prepared Amoxycillin trihydrate and Potassium clavulanate fast dissolving tablets were evaluated for thickness, weight variation, friability, disintegration time, hardness, wetting time and in vitro drug release. All fast dissolving tablet formulations shown uniform weight, hardness and friability data indicates the good mechanical resistance of the fast dissolving tablet. Fast dissolving tablets were disintegrated between 25-50 second and in vitro disintegration time of the best fast disintegrating tablets was found to be 25 second. Conclusion: Amoxycillin trihydrate and Potassium clavulanate fast dissolving tablets were found to be of good quality fulfilling all the needs for fast dissolving tablets. The optimised (F-4) formulation had shown best disintegration time and released profile with a maximum in vitro drug release as compare to marketed preparation at all time intervals of in vitro drug release.


INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (04) ◽  
pp. 21-27
Author(s):  
V Ramya ◽  
◽  
Z Abbas ◽  
NGN Swamy

The aim of this study was to improve the bioavailability by enhancing the solubility of efavirenz, a poor water soluble, anti-viral drug by using liquisolid technique. Different liquisolid formulations were prepared by using various non-volatile hydrophilic solvents. Microcystalline cellulose (Avicel PH 102) and Aerosil 200 were used as carrier and coating materials respectively. Additives such as polyvinyl pyrrolidone, hydroxypropyl methylcellulose and hydroxypropyl guar were incorporated into the formulations, to improve dissolution characteristics. The prepared liquisolid compacts were evaluated for hardness, friability, weight variation, drug content and in vitro dissolution studies. FT-IR studies were carried out to rule out the drug-excipient interactions. It was observed that there was no chemical interaction between the drug and excipients. DSC and X-ray diffraction studies were performed to evaluate the physicochemical properties of the liquisolid tablets, which would enable us to confirm the conversion of the crystalline form of the drug to the amorphous form in the formulation. The dissolution profiles of the liquisolid tablets were compared with that of the directly compressed tablets. The results obtained showed the liquisolid tablets of efavirenz, to exhibit a higher percentage of drug release than the directly compressed tablets.


Author(s):  
Ganesh kumar Gudas ◽  
Manasa B ◽  
Senthil Kumaran K ◽  
Rajesham V V ◽  
Kiran Kumar S ◽  
...  

Promethazine.HCl is a potent anti-emetic. The central antimuscarinic actions of antihistamines are probably responsible for their anti-emetic effects. Promethazine is also believed to inhibit the medullary chemoreceptor trigger zone, and antagonize apomorphine -induced vomiting. Fast dissolving tablets of Promethazine.HCl were prepared using five superdisintegrants viz; sodium starch glycolate, crospovidone, croscarmellose, L-HPC and pregelatinised starch. The precompression blend was tested for angle of repose, bulk density, tapped density, compressibility index and Hausner’s ratio. The tablets were evaluated for weight variation, hardness, friability, disintegration time (1 min), dissolution rate, content uniformity, and were found to be within standard limit. It was concluded that the fast dissolving tablets with proper hardness, rapidly disintegrating with enhanced dissolution can be made using selected superdisintegrants. Among the different formulations of Promethazine.HCl was prepared and studied and the formulation S2 containing crospovidone, mannitol and microcrystalline cellulose combination was found to be the fast dissolving formulation. In the present study an attempt has been made to prepare fast dissolving tablets of Promethazine.HCl, by using different superdisintegrants with enhanced disintegration and dissolution rate. 


Author(s):  
C Suja ◽  
Sismy C

The goal of this study was to formulate and evaluate norfloxacin sustained release tablets. Norfloxacin sustained release tablets were prepared by wet granulation method using two polymers such as HPMC K 100 M (hydrophilic polymer) and guar gum (natural polymer) and with three polymer ratios (0.5, 1.0 and 1.5). The prepared granules were evaluated to preformulation studies such as angle of repose, bulk density, tapped density, bulkiness, compressibility index and Hauser’s ratio. All the parameters shows that the granules having good flow properties. Then the formulated tablets were taken to evaluation studies such as hardness, weight variation, friability, drug content and thickness. All the parameters were within the acceptable limits. IR spectral analysis showed that there was no interaction between the drug and polymers. The in vitro release study was performed in phosphate buffer pH 7.4 at 293 nm. The in vitro release study showed that if the polymer ratio is increased, then the release of the drug is prolonged. HPMC K 100M shows a prolonged release when compared to guar gum.


Author(s):  
Mayuri B. Patil ◽  
Avish D. Maru ◽  
Jayshree S. Bhadane

The aim of the present study was to design and evaluate bilayer tablets of metformin hydrochloride as sustained release form for the treatment of Type-II diabetes mellitus. The basic aim of any Bi-layer tablet formulation is to separate physically or chemically incompatible ingredients and to produce repeat action or prolonged action of tablet. They are many drugs for treating type-II diabetes. Sulphonyl urea and biguanides are used commonly by a wide section of patients. Melt granulation process was used for the formulation of sustained comprising metformin layer and wet granulation of immediate comprising layer of glimepiride. The precompression studies like bulk density, tapped density, angle of repose, compressible index and post formulation studies includes weight variation, hardness, thickness, friability and dissolution study. The in-vitro release profile of Glimepiride was dissolved within 45 min, and Metformin Hydrochloride was able to release more than 12 hrs. They all the formulation was optimized formula due to its higher rate of dissolution and collate all other parameters with the official specifications.


Author(s):  
Mohammed Sarfaraz ◽  
Surendra Kumar Sharma

ABSTRACTObjective: The main objective of this research was to formulate Fast disintegrating tablets of Flurbiprofen incorporating superdisintegrants, isolated from natural sources like Plantago ovata (PO) seeds, Lepidium sativum (LS) seeds and agar-agar.Methods: Superdisintegrants were isolated from their natural sources using reported methods. Swelling index and hydration capacity was determined for the natural superdisintegrants to know their disintegration capacity. The tablet formulations were designed using isolated natural superdisintegrants. The powder blends were evaluated for pre-compressional parameters like angle of repose, bulk density, tapped density, carr’s index, and hausner’s ratio. Fast disintegrating tablets were prepared by direct compression method. The compressed tablets were characterized for post compression parameters.Results: All formulations had hardness, friability, weight variation and drug content within the pharmacopoeial limits. The wetting time was 84 to 254 sec, in vitro disintegration time was between 59.2 to 221 sec, and in-vitro drug release was as low as 11.80% (LS1) to a maximum of 98.99% (PO4) after 4 min of study. Among all, optimized formulation was PO4, as it showed good wetting time (84 sec), fastest disintegration time (59.2 sec), dispersion time (135 sec) and drug release of 98.99.% within 4 min.Conclusion: Flurbiprofen FDT’s were successfully developed using isolated natural disintegrants. The natural disintegrants isolated showed promising results and can prove as effective alternative for synthetic disintegrants.


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