Preparation and optimization of fast disintegrating tablets of isosorbide dinitrate using lyophilization method for oral drug delivery

2021 ◽  
Author(s):  
Mitra Alami-Milani ◽  
Sara Salatin ◽  
Elaheh Nasiri ◽  
Mitra Jelvehgari
Keyword(s):  
Isosorbide Dinitrate ◽  
Freeze Drying ◽  
Oral Drug Delivery ◽  
Aqueous Dispersion ◽  
Oral Dosage ◽  
Oral Drug ◽  
Disintegration Time ◽  
Orally Disintegrating Tablets ◽  
Solid Oral Dosage Form ◽  
Fast Disintegrating Tablets

Background: Orally disintegrating tablets rapidly disintegrate in saliva and then swallowed without the need for water. Materials & methods: The orally disintegrating tablets were prepared by freeze-drying of an aqueous dispersion of isosorbide dinitrate containing a matrix former (gelatin), a cryoprotectant (mannitol), a plasticizer (glycerin) and a dissolution enhancer (Tween/polyethylene glycol). Results: Results demonstrated that the selected formulation, Ft9, disintegrated within 1 min and showed faster dissolution rate compared with the commercial tablet. Conclusion: Having a fast disintegration time, the developed lyophilized tablet does not need to be swallowed as a whole. So, it is a convenient solid oral dosage form for the patients who have difficulty with swallowing such as the pediatric and elderly ones.

scholarly journals FAST DISSOLVING DRUG DELIVERY SYSTEMS: FORMULATION, PREPARATION TECHNIQUES AND EVALUATION

2018 ◽  
Author(s):  
Satbir Singh ◽  
Tarun Virmani ◽  
Reshu Virmani ◽  
Geeta Mahlawat ◽  
Pankaj Kumar
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Oral Drug Delivery ◽  
Dosage Forms ◽  
Delivery Systems ◽  
Oral Dosage ◽  
Oral Drug ◽  
Self Medication ◽  
Onset Of Action ◽  
Fast Disintegrating Tablets

The Fast Dissolving Drug Delivery Systems sets a new benchmark was an expansion that came into existence in the early 1980’s and combat over the use of the different dosage form like tablets, suspension, syrups, capsules which are the other oral drug delivery systems. Fast Dissolving Drug Delivery System (FDTS)  has a major advantage over the conventional dosage forms since the drug gets rapidly disintegrated and dissolves in the saliva without the use of water .In spite of the downside lack of immediate onset of action; these oral dosage forms have valuable purposes such as self medication, increased patient compliance, ease of manufacturing and lack of pain. Hence Fast Disintegrating Tablets (FDTS) technology has been gaining importance now-a-days with wide variety of drugs serving many purposes. Fast Disintegrating Tablets (FDTS) has ever increased their demand in the last decade since they disintegrate in saliva in less than a minute that improved compliance in pediatrics and geriatric patients, who have difficulty in swallowing tablets or liquids. As fast dissolving tablet provide instantaneous disintegration after putting it on tongue, thereby rapid drug absorption and instantaneous bioavailability, whereas Fast dissolving oral films are used as practical alternative to FDTS. These films have a potential to deliver the drug systemically through intragastric, sublingual or buccal route of administration and also has been used for local action. In present review article different aspects of fast dissolving  tablets and films like method of preparations, latest technologies, evaluation parameters are discussed. This study will be useful for the researchers for their lab work.  

scholarly journals A REVIEW ON PHARMACEUTICAL MINI TABLETS: NEW MODALITY TO ORAL DRUG DELIVERY

2020 ◽  
pp. 8-12
Author(s):  
NAVEEN TAJ S
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Drug Delivery ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Oral Drug ◽  
Solid Dosage ◽  
Therapeutic Benefits ◽  
Solid Oral Dosage Form

The purpose of any selected drug delivery system (DDS) is to deliver drug to target site and to get the desired drug concentration for effective therapy. The main purpose of designing controlled or sustained DDS is to decrease the frequency of dosing and maximizing its efficiency by confining the area of action of the drug to a selected region. It is well-identified that solid oral dosage form, particularly tablets, is the most satisfactory form of delivering medication. In addition, some new variations are emerging such as mini tabs which offer more formulation flexibility. Oral controlled release DDS are classified into two categories like single unit dosage forms which include tablets, capsules, and multiple-unit dosage forms include pellets, granules, or mini tablets. Mini tablets are a new development in solid dosage forms and more beneficial and great substitute for granules and pellets. Mini tablets defined as tablets which are having diameter <3 mm and promising patient friendly drug delivery system and more acceptable in small children’s and old age people as they are easy to swallow and offer therapeutic benefits such as manufactured relatively easy, dose and formulation flexibility, combination release pattern, coating, and less solvent requirement. Dose dumping and local irritation can be avoided using mini tablets. This review highlights the various advantages of mini tablets, manufacturing processes, formulation possibilities, and their challenges.

scholarly journals A REVIEW ON FAST DISSOLVING TABLET

2018 ◽  
Vol 8 (5) ◽  
pp. 50-55 ◽  
Author(s):  
RD Rahane ◽  
Punit R. Rachh
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Patient Compliance ◽  
Delivery System ◽  
New Technologies ◽  
Oral Drug Delivery ◽  
Oral Drug ◽  
Preparation Methods ◽  
Orally Disintegrating Tablets ◽  
Increasing Demand

The convenience of administration and improved patient compliance are important in the design of oral drug delivery system which remains the preferred route of drug delivery inspite of various disadvantages. Fast disintegrating tablets (FDTs) have received ever-increasing demand during the last decade, and the field has become a rapidly growing area in the pharmaceutical industry. The popularity and usefulness of the formulation resulted in development of several FDT technologies. These techniques render the disintegration of tablet rapidly and dissolve in mouth in five seconds without chewing and the need of water which is advantageous mainly for pediatrics, geriatrics and patients having difficulty in swallowing tablets and capsules. Formulation of a convenient dosage form for administration, by considering swallowing difficulty and poor patient compliance, leads to development of orally disintegrating tablets. Conventional preparation methods are spray drying, freeze drying, direct compression, Molding, and sublimation while new technologies have been developed for the production of orodispersible tablets. Keywords: Fast Dissolving Tablet, drug delivery system, fast disintegrating, fast melting.

REVIEW ON GASTRORETENTIVE DRUG DELIVERY SYSTEM

2020 ◽  
pp. 38-45
Author(s):  
MANDAR J BHANDWALKAR ◽  
PRASAD S DUBAL ◽  
AKASH K.TUPE ◽  
SUPRIYA N MANDRUPKAR
Keyword(s):  
Drug Delivery ◽  
Small Intestine ◽  
Drug Delivery System ◽  
Residence Time ◽  
Delivery System ◽  
Oral Drug Delivery ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Oral Drug ◽  
Low Solubility

In recent years, gastroretentive drug delivery system (GRDDS) has gained researcher’s interest in the field of oral drug delivery. Various GRDDS approaches can be utilized to retain the dosage forms in the stomach and to release the drug slowly for an extended period of time. GRDDS can be used to prolong the residence time of delivery system in the stomach. This results in targeting of drug release at a specific site for the systemic or local effects. GRDDS can be used to overcome challenges associated with conventional oral dosage forms and to release the drug at a specific absorption site to improve bioavailability of particular drug substance. The challenges include fast gastric emptying of the dosage form which results in the poor bioavailability of the drug. Prolongation of the retention of drugs in stomach those having low solubility at high intestinal pH improves the solubility of drugs. GRDDS has proved to be effective in systemic actions as well as in local actions to treat gastric or duodenal ulcers. Local activity in the upper part of the small intestine can be obtained by improving the residence time of delivery system in the stomach. The system is useful for drugs which are unstable in the intestine or having a low solubility/permeability in the small intestine. Various GRDDS approaches include high density (sinking) systems, low-density (floating systems), mucoadhesive, expandable, unfoldable, superporous hydrogel systems, and magnetic systems.

Design, Optimization and Evaluation of Lurasidone Hydrochloride Nanocrystals as Fast Disintegrating Tablets

2019 ◽  
Vol 4 (2) ◽  
pp. 121-129
Author(s):  
Satya Sankar Sahoo ◽  
Chandu Babu Rao
Keyword(s):  
Patient Compliance ◽  
Oral Drug Delivery ◽  
Particle Diameter ◽  
Water Soluble ◽  
In Vivo Studies ◽  
Oral Drug ◽  
Water Soluble Drugs ◽  
Fast Disintegrating Tablets ◽  
Lurasidone Hydrochloride

Formulation of poorly water-soluble drugs for oral drug delivery has always been a difficult task for formulation scientists. Lurasidone hydrochloride is one such agent which is used to control bipolar depre-ssion. The objective of this study was to formulate and optimize lurasi-done nanosuspension, further formulating optimized nanosuspensions as fast disintegrating tablets for improved patient compliance. In the present study, lurasidone nanosuspension was prepared by nanomilling technique. Optimized nanosuspension has mean particle diameter of 248.9 nm, polydispersity index of 0.127 and zeta potential of 18.1 mV. The lyophilized optimized nanocrystals, optimize nanosuspension as granulating fluid and as top spraying dispersion for granulation in fluid bed granulator being used to formulate fast disintegrating tablets with suitable super disintegrant. Croscarmellose sodium was found to be best superdisintegrant compared to sodium starch glycolate and crospovidone, as its acts by both mechanism swelling and wicking. Its swells 4-8 folds in less than 10 s. Many folds increase in the rate of drug release observed compare to micronized lurasidone and marketed product. There was no change in crystalline nature after nanomilling as characterized by XRD and FTIR, and it was found to be chemically stable with high drug content. The developed fast disintegrating tablets would be an alternative better formulation than its conventional formulation to address its bioavailability issue and for improved patient compliance. However, this should be further confirmed by appropriate in vivo studies.

scholarly journals Design, optimization and evaluation of ibuprofen fast dissolving tablets employing starch succinate: A new superdisintegrant

2019 ◽  
Vol 9 (2) ◽  
pp. 270-279
Author(s):  
Rada Santosh Kumar ◽  
T. Naga Satya Yagnesh
Keyword(s):  
Oral Administration ◽  
Oral Drug Delivery ◽  
Immediate Release ◽  
Order Rate Constant ◽  
Oral Drug ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Drug Content ◽  
Dissolution Efficiency

The current scenario emphasize on oral administration. The main disadvantage in oral administration was difficulty in swallowing for pediatric and geriatric patients. To solve this problem in oral drug delivery system, the formulation of fast dissolving systems found to be the best alternatives.  The present investigation involves in the evaluation of starch succinate as a superdintegrant in the formulation of fast dissolving tablets of poorly soluble drugs employing 23factorial design. Starch succinate was synthesized by esterification process. The synthesized starch succinate was subjected to physical and micromeritic evaluation. All fast dissolving tablets were evaluated for drug content, hardness, friability, disintegration time and other dissolution characteristics like percent dissolved in 5 min (PD5), dissolution efficiency in 5 min (DE5%) and first order rate constant(K1). The starch succinate prepared was found to be fine, free flowing crystalline powder. Starch succinate exhibited good swelling in water. Fourier transform infrared spectra (FTIR) and Differential scanning calorimetry (DSC) study indicated the absence of interaction between ibuprofen and starch succinate. All the fast dissolving tablets formulated employing starch succinate were of good quality with regard to drug content (200±2%), hardness (3.6–4.0 kg/sq. cm), and friability (0.12-0.15%). The optimised formulation F8 has the least disintegration time i.e., 15±0. 02s. The in–vitro wetting time was less (i.e., 15s) in optimized formulation F8. The water absorption ratio of the formulated tablets was found to be in the range of 31.4±0.01 to 68.0±0.04%. The cumulative drug dissolved in the optimized formulation F8 was found to be 99.81± 0.22% in 5 min. Starch succinate was found to be a superdisintegrant which enhanced the dissolution efficiency with the ibuprofen and hence it could be used in the formulation of fast dissolving tablets to bring immediate release of the contained drug within 5 minutes. Keywords: Fast dissolving, Superdisintegrant, Starch succinate, Dissolution efficiency.

Natural Superdisintegrant: Opportunity in Oral Drug Delivery System

2021 ◽  
pp. 135-140
Author(s):  
Rina G. Maskare ◽  
Nitin H. Indurwade ◽  
Aparna O. Yadav ◽  
Ajita S. Kesharwani ◽  
Aishwarya A. Jain ◽  
...  
Keyword(s):  
Oral Drug Delivery ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Oral Drug ◽  
Plantago Ovata ◽  
Disintegration Time ◽  
Weight Variation ◽  
Complete Disintegration ◽  
Preformulation Studies

The present work concerned with formulation and evaluation of fast disintegrating tablet of Topiramate by using natural superdisintegrants like Trigonellafoenum graceum (fenugreek) powder, Plantago ovata powder, dehydrated banana powder, soy polysaccharide, linseed powder. Topiramate is an antiepileptic drug and also used in migraine. Preformulation studies like solubility, melting point were studied. Five formulations were prepared using different natural superdisintegrant with same concentrations by using direct compression method. All the formulations were evaluated for precompression parameters and all the parameters were found to be within the pharmacopoeial limits. Post compression parameters like hardness of the tablet, thickness of the tablet, friability test, weight variation, disintegration test, in-vitro dissolution test, drug content were performed. The formulation F-5 containing Trigonellafoenum-graceum (fenugreek) powder shown disintegration time of 12sec. Rapid disintegration of the Trigonellafoenum-graceum due to its rapid water absorbency swells in water to the extent of 200–300% disintegrates rapidly for quick and complete disintegration of the tablet. An accelerated stability study on optimized formulation was performed and it was found to be stable. It can be concluded that Trigonellafoenum-graceum (fenugreek) powder as Superdisintegrant showed better release than soy polysaccharide, plantago ovata powder, dehydrated banana powder and linseed powder.

COLOCASIA ESCULENTA STARCH: NOVEL ALTERNATIVE DISINTEGRANT FOR PHARMACEUTICAL APPLICATION

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (02) ◽  
pp. 41-53
Author(s):  
Ujjwala Y. Kandekar ◽  
Mayuri H. Tapkir ◽  
Priyanka H. Bhalerao ◽  
Nikita B. Rukhe ◽  
Shubhada K. Kad ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Research Work ◽  
Colocasia Esculenta ◽  
Oral Drug ◽  
Wet Granulation ◽  
Disintegration Time ◽  
Pharmaceutical Application ◽  
Oral Drug Delivery System

Oral drug delivery system has always been the most prevalent route of administration and continuous efforts are made to improve the drug delivery by this route. Tablets are one of the most extensively used dosage forms and various excipients have been developed for their formulation. The purpose of the current research work was to isolate and study the physicochemical properties of the Colocasia esculenta starch and further compare its disintegration ability with maize starch. Starch was isolated from C. esculenta corms by aqueous extraction method and possesses characteristics that are typical of starches. It was further evaluated for the presence of other foreign matter and phytoconstituents. Results showed that the isolated sample was free from foreign organic matter and the total ash value was found to be 0.4%. Tablets were prepared by the wet granulation method by varying concentrations in the range of 2.5 to 10% w/w for both the starches. Pre and post-compression parameters were studied and were found to be within the pharmacopoeial limits. Disintegration tests showed that disintegration time decreases with increasing concentration of both the starches. At 10% w/w concentration, disintegration time was found to be lowest, hence it was selected as an optimized formulation Stability studies were performed on F4 batch and it was found to be stable. The determination of disintegration efficiency indicates that C. esculenta starch exhibits disintegrating potential.

scholarly journals APPLICATION OF LIQUISOLID TECHNOLOGY TO ENHANCE THE DISSOLUTION OF CEFIXIME FROM ITS ORAL CAPSULES

2018 ◽  
Vol 10 (5) ◽  
pp. 214
Author(s):  
Zainab H. Mahdi ◽  
Nidhal K. Maraie ◽  
Zahraa Amer Al-juboori
Keyword(s):  
Oral Drug Delivery ◽  
Oral Route ◽  
Oral Drug ◽  
Content Uniformity ◽  
Disintegration Time ◽  
Promising Technology ◽  
Weight Variation ◽  
R Value ◽  
Optimum Formula

Objective: Oral drug delivery is the most desired route for drug administration for its well-known features. Therefore, many attempts were implemented to improve the poor solubility of many active ingredients in order to enhance their dissolution and absorption via the oral route. From these, the liquisolid system is a very promising technology for enhancing solubility and bioavailability of poorly soluble drugs.Methods: In this research, oral capsules of cefixime were prepared by liquisolid technique after mixing different concentrations of the drug with propylene glycol (non-volatile solvent), followed by their addition to different proportions of microcrystalline cellulose and aerosil i.e. different carrier: coating (R-value). The liquisolid capsules were evaluated for In vitro disintegration and dissolution in addition to content uniformity and weight variations. Furthermore, solubility studies, scanning electron microscope (SEM) were performed to the optimum formula. Finally, the release profile of the optimum formula was compared with the marketed cefixime capsules.Results: Liquisolid formula (F3) with 70% cefixime and R-value equals 10 was selected as the optimum formula having higher % release in 45 min (99.5%±0.53) compared to other formulas with faster release rate in the first 20 min than marketed capsules. It had an acceptable disintegration time (25 min±0.76), content uniformity (197.6±0.92) and weight variation (698.04±0.16). Results of solubility study, SEM assured enhancement in solubility and dispersibility of the drug.Conclusion: This research proved that liquisolid system is a promising technology in improving the solubility and dissolution of cefixime from its capsules and hence it may improve its absorption and oral bioavailability.

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