Polyplasdone XL Research Articles

Formulation and Characterization of Oral Dispersible Tablet of Aprepitant

The oral route of drug administration is more common and convenient where tablets and capsules emerged as popular dosage form but many patients have dysphasia or difficulty in swallowing which is currently affecting 35% general population. Aprepitant is anti-emetic drug and used in the treatment of chemotherapy in cancer. Fast onset of action is required in this indication there for it was thought to prepare Oral Dispersible Tablet of Aprepitant which would help to avoid first pass metabolism and improve bioavailability also Aprepitant is insoluble in water so, to increase the solubility solid dispersion method (kneading method) was used. Here, Aprepitant ODT is prepared by direct compression method using Polyplasdone XL10 as superdisitegrant and optimized by 32 Full factorial design. Here, Polyplasdone XL10 (x1) and Mannitol(x2) is use as independent variable. while dependent variable are disintegration time and wetting time. Optimized formulation F8 batch showed drug content (98.41±0.91); disintegration time is (18.02±1.20) Wetting time (22.53±0.43). The formulation is stable at 40ºc/75% RH for 30days.

Formulation Development and Invitro Evaluation of Gliclazide Pellets using Superdisintegrants by Extrusion Spheronization Technique

Introduction: Gliclazide is a sulfonylurea derivative used for the treatment of type 2 Diabetes, it is an anti-diabetic drug it is marketed under the brand name Diamicron. It is taken orally and used when dietary changes, lack of exercise, and weight loss are not sufficient. 
 Aim: The principal objective of this work was to develop, formulate and evaluate the pellet formulations prepared with the incorporation of different super disintegrants in different ratios and in different combinations. In this research work, the drug gliclazide was chosen as a model drug and it was formulated into fast-dissolving pellets, which can be compressed into pelltabs and can also be filled into capsules. 
 Methods: Pellets were prepared by extrusion and Spheronization containing microcrystalline cellulose (MCC) and using gliclazide as a model drug with different super disintegrants namely croscarmellose sodium, crospovidone and sodium starch glycolate in different ratios, and in different combinations. Thus, in the present study, gliclazide pellets were developed using Extrusion-Spheronization for immediate drug delivery. The pellets were evaluated for percentage drug content, flow properties, friability, size analysis, shape analysis, disintegration test, and dissolution studies. Preformulation studies were then performed using solubility studies, partition co-efficient studies, infrared spectroscopy, and drug-excipients compatibility studies between the drug and selected excipients (croscarmellose sodium, crospovidone, and sodium starch glycolate) investigated.
 Results: Formulations containing MCC, super disintegrants, and drugs in different ratios of 60/0/40, 55/5/40, and 50/10/40 w/w of croscarmellose sodium, crospovidone, and sodium starch glycolate were found to show faster release of the drug for 9 hours. Croscarmellose sodium releases the drug as it disintegrates the 
 
 pellets. Sodium starch glycolate releases the drug by inducing swelling in the pellet 
 matrix. Unlike the other two super disintegrants, there was no apparent change in the swelling capability of the pellets of polymer crospovidone (Polyplasdone XL10) in water. The percentage increase in diameter for Ac-Di-Sol (croscarmellose sodium), Primojel (sodium starch glycolate), and Polyplasdone XL10 were 104%, 251%, and 29% in water.
 Conclusions: Various types of super disintegrants can be investigated for their suitability in formulating pellets. In vivo drug release rate, and bioavailability studies on animals and humans may be carried out to assess the superiority of the pellets over the tablet dosage form.

Design, Development and Evaluation of Gastroretentive Drug Delivery System of Antacids

Magaldrate is an antacid have been widely used in the treatment of various gastric and duodenal disorders such as heartburn, reflux esophagitis, acid indigestion, gastritis, sour stomach, upset stomach, irritable stomach, gastric and duodenal ulcers. The conventional antacids dosage forms have a short duration of action which is about 2-3 hours due to gastric emptying process. A gastroretentive dosage form of antacid is needed since the healing of gastric ulcers occurs when gastric pH is kept above 3-4 during 24 hours. The present study was aimed at developing Gastro retentive bilayer drug delivery systems containing Magaldrate to minimize the side effect, improve the prolongation of action, to reduce the frequency of drug administration. A wet granulation technique was used to formulate 9 batches. Superdisintegrants like Polyplasdone XL-10, Ac-Di-Sol, and sodium starch glycolate was used for immediate release layer and HPMC K4 M, Ac-Di-Sol and lactose like polymers were used in floating layer. Preformulation studies were carried out to optimize the ratios required for various grades of polymers. The prepared floating tablets were evaluated for hardness, weight variation, thickness, friability, drug content uniformity, buoyancy lag time, total floating time, water uptake (swelling index), and in vitro dissolution studies. Successful formulation was developed having floating lag time as low as 30 sec and drug release was sustained up to 12 hrs. A biphasic drug release can be obtained by using bilayer tableting technology which involved compression of immediate and sustained release layer together. Bilayered floating tablets with release characteristics offer critical advantages such as, site specificity with improved absorption and efficacy. This technology can be inculcated to various medicaments which have stomach as the major site of absorption.
 Keywords: Magaldrate, Antacid, Gastroretentive dosage form, Bilayer floating tab, Superdisintegrant

Research the influence of excipients on the technological properties of captopril fast dissolving films

Drug-loaded films are of great interest among fast-dissolving drug-delivery systems. The creation of fast-dissolving films for the treatment of cardiovascular diseases is important.The first inhibitor of angiotensin-converting enzyme to appear on the world market was captopril, which is used to treat hypertension, chronic heart failure and others. Captopril has an antihypertensive effect, which manifests itself within 5–15 minutes after sublingual administration.
 The aim of our study was to develop the technology of captopril fast dissolving films by solvent casting method and analyze the influence of groups of excipients on technological properties of the films.
 The influence of the character of polymers, plasticizers, disintegrants and sweeteners on the technological properties of experimental batches of captopril fast dissolving films was studied. Such technological indicators as uniformity of weight, thickness, swelling index,tensile strength, elongationand disintegration time were studied.
 The influence of excipients' composition on the technological indicators of captopril fast dissolving films has been researched. It was found out that the effect of the type of polymer had the decisive influence on all parameters of films.The selected plasticizer determined the elasticity (films' elongation), film thickness and weight variation. Optimal values of the average weight and thickness of captopril films are provided by the use of a polymer in the combination of HPMC with PEG 4000 or a combination of HPMC with PEG 6000, as a plasticizer – glycerin or PEG 400. The best results of films' swelling were obtained with the introduction of HPMC brands Metolose® 90 SH 100 000 or Metolose® 65 SH 50, Polyplasdone XL-10 crospovidone, propylene glycol and sorbitol. The disintegration time less than 3 min was observed in all investigated film compositions, except those containing PVA. The highest value of tensile strength for captopril films was obtained using HPMC brand Metolose® 65 SH 50 or Metolose®90 SH 100 000.
 Using the desirability function, the optimal excipients within the studied groups were selected.It has been established that the optimal values of the technological parameters of captopril films can be achieved using Hydroxypropyl MethylcelluloseVivapharm® E15, polyethylene glycol 400, sodium starch glycolate and sorbitol.

Physico-Chemical and Pharmaco-Technical Characterization of Inclusion Complexes Formed by Rutoside with β-Cyclodextrin and Hydroxypropyl-β-Cyclodextrin Used to Develop Solid Dosage Forms

The aim of our study was to obtain rutoside (RUT) inclusion complexes in β-cyclodextrin (β-CD) and in hydroxypropyl-β-cyclodextrin (HP-β-CD), in a 1:1 molar ratio, using the lyophilization method of complexation in solution. The complexes were confirmed and characterized, in comparison with the raw materials and their simple physical mixtures, by SEM, DSC, and FT-IR analyses. The antioxidant activity of the compounds was assessed by using the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) and 2’-azino-bis(3-ethylbenzothiazolin-6-sulfonic) acid (ABTS) radicals, determining the radical scavenging activity, and by ferric reducing antioxidant power (FRAP) assay. The results revealed superior antioxidant ability for the inclusion complexes towards rutoside alone. The inclusion complexes were used as active ingredients in formulations of immediate-release tablets. The preformulation studies were performed on the powders for direct compression obtained after mixing the active ingredients with the excipients (Avicel PH 102, Polyplasdone XL-10, magnesium stearate, and talc). The materials were assessed for particle size, flowability, compressibility, and moisture content, establishing they are suitable for a direct compression process. The tablets were characterized regarding their pharmaco-technical properties and the results proved that the formulations lead to high-quality delivery systems, showing a good mechanical resistance with a low friability, excellent disintegration times, and satisfying dissolution rate. The performances were very similar for both formulations and the physico-mechanical properties of the tablets are not influenced by type of the used cyclodextrin, but the RUT- HP-β-CD tablets presented a higher dissolution rate.

Formulation and study of nebivolol containing orodispersable tablets

Abstract In case of chronic diseases patient compliance to long-term treatment is of utmost importance. Patient compliance is generally higher for pharmaceutical forms dispersing in the oral cavity. One classic example for long-term therapy is hypertension. The aim of this study is to obtain nebivolol hydrochloride containing orally disintegrating tablets. As manufacturing technology, direct compression was chosen and rapid disintegration was aimed to be achieved using superdisintegrants. Various formulae have been developed, containing Kollidon and Polyplasdone in different concentrations, and the obtained dry powder mixtures were studied for their rheological properties. Afterwards these mixtures were compressed to obtain tablets. Active ingredient was embedded in the formulations with the shortest disintegration times (15 and 18 seconds) and the obtained tablets were studied for disintegration time, mechanical resistance, drug content and dissolution. Our results show that the pharmaceutical formulations containing Kollidon CL 5% or Polyplasdone XL 3% fulfill the requirements of orally disintegrating tablets, having a disintegration time under 3 minutes, proper mechanical resistance (greater than 80N) and the dissolution of the active ingredient is greater than 80% in 30 minutes.

FORMULATION AND EVALUATION OF ORODISPERSIBLE TABLETS OF LAMOTRIGINEUSING DISCRETE SUPER DISINTEGRANTS AND COPROCESSED EXCIPIENTS

Objective: The present study was designed to formulate and evaluate the orodispersible tablets of lamotrigine after enhancing its solubility.
 Methods: Lamotrigine was made into an inclusion complex with eudragit E 100 my kneading and mass extrusion method and later this mixture is compressed into orodispersible tablet using various super disintegrants and co-processed excipients to reduce the disintegration time for providing prompt action through rapid drug release.
 Results: Lamotrigine ODTs containing F-melt (F1-3%, F2-5%) dispersed in lesser time of (9±0.11) and (21±0.58) compared to formulations with polyplasdone XL-10 and primellose as super disintegrants respectively with F1 showing short wetting time. The water absorption was also was found to be more for formulation with 3% F-Melt.
 Conclusion: Lamotrigine orodispersible tablets were prepared by direct compression technique by using 3% and 5% of three super disintegrants (f-melt, primellose and polyplasdone XL-10). Disintegration time of F1 (3% f-melt) formulation was found to be least (7 sec).

Formulation Development and Evaluation of Immediate Release Tablet Dosage form of Sorafenib Tosylate

Immediate release drug formulation is a novel type of drug delivery system which disintegrates rapidly and gets dissolved to release the medicaments after administration. Sorafenib tosylate is kinase inhibitors, used to treat renal cell carcinoma. our work involves the formulation, optimization and post compressed evaluation studies of immediate release Sorafenib tosylate tablets. The direct compression method was employed for formulating tablets. Tablet composition contains Sorafenib tosylate as a filler. Explotab, Solutab and polyplasdone XL is a superdisintegrant, mannitol as sweeting agent magnesium stearate as a lubricant, talc as a anticaking agent. The prepared tablets were evaluated for physico-chemical properties and post evaluation studies such as drug content and in vitro dissolution. Further more, Finally, it was concluded that all the pre-formulation and post compression studies of sorafenib tablet met with required specifications and also showed comparably a good rate of dissolution like that of a commercial product. Among all the formulations F6 formulation containing, drug and Solutab showed good result that is 99.56% in 45 min. Hence from the dissolution data it was evident that F6 formulation is the better formulation.

FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF LORATADINE SOLID DISPERSION USING SUPER DISINTEGRANTS

The aim of the present investigation was to prepare solid dispersion (SD) of the water insoluble drug. Loratadine using super disintegrants as carrier and formulate it as fast dissolving tablets (FDTs) with an objective to improve solubility and enhance dissolution of drug. The SD’s of the drug were prepared by melt dispersion technique using polyethylene glycol (PEG) 6000 in diferent ratios 1 : 2.5, 1 : 5 and 1 : 7.5. The prepared SD formulations were characterized for equilibrium solubility, Fourier Transform Infrared spectroscopy (FTIR) and in vitro dissolution study. The batch containing SD formulation of loratadine showed fastest dissolution (99.87% drug release in 60 min). In this study, fast dissolving tablets were prepared by direct compression method using Croscarmellose sodium, sodium starch glycolate and polyplasdone XL as the super disintegrants. Effect of various super disintegrants on dissolution behavior of tablets was evaluated in phosphate buffer pH 6.8.

THE THE METHOD OF RANDOM BALANCE FOR STUDYING THE INFLUENCE OF EXCIPIENTSʼ QUANTITIES ON TECHNOLOGICAL PARAMETERS OF METFORMIN ORODISPERSIBLE TABLETS

Objective: The present investigation was undertaken with an objective of analyzing the influence of excipientsʼ amount on the technological parameters of metformin orodispersible tablets using the method of random balance.
 Methods: The tablets were prepared by using direct compression method. The formulations were designed according to the method of random balance. The technological parameters of metformin orodispersible tablets have been studied as a function of quantitative factors: crospovidone (Polyplasdone XL-10®), magnesium aluminometasilicate (Neusilin US2®), microcrystalline cellulose (MCC Sanaq® burst), lactose monohydrate, magnesium stearate (Tablube® MgSt micronized vegetable) and talc. 
 Results: The flowability results were ranging from excellent to good according to the quantities of Neusilin US2® and Polyplasdone XL-10® crospovidone, which used. Results of bulk density and tapped density of the powder mixtures for pressing depended from the quantities of Neusilin US2® and talc. The obtained tablets had uniform weight from 0.93 to 2.30 %. The increase in the amount of Polyplasdone XL-10® crospovidone and the decrease in the amount of talk improved the uniformity of tablets’ weights. All of the prepared tablets showed acceptable hardness and friability which were improved with decrease in the amount of MCC Sanaq®burst and increase in the amount of Neusilin US2®. The rapid disintegration and wetting time for all formulations of tablets were obtained by using the Polyplasdone XL-10® crospovidone and MCC Sanaq®burst.
 Conclusion: Oral disintegrating tablets of metformin were successfully prepared by direct compression method. The random balance method enabled us to identify the most significant quantitative factors and stabilize them at optimal values.

Development and Evaluation of Ondansetron Orally Disintegrating Tablets

Orally disintegrating tablet (ODT) has number of advantages like faster onset of action, ease of administration, rapid disintegration and dissolution etc. A novel attempt has been made to develop orally disintegrating tablets of Ondansetron by using two approaches, one is soluble hydrophilic matrix by superdisintegrant and other is effect of sweetener on the formulation. Direct compression method was employed for making orally disintegrating tablets. The formulated orally disintegrating tablets have rapid disintegration property for better patient compliance. Formulated tablets were evaluated for physical parameters along with wetting time, disintegration time, drug content and “in vitro” dissolution. In first approach it was found that batch F7 containing Crospovidone (Polyplasdone XL 10) 10 mg showed minimum disintegration time (i.e. approx. 7.00 seconds) with maximum drug release. Wetting time for batch F7 was found to beminimum (i.e. 12 seconds). In second approach of selection of sweetener batch F 10 containing Sodium saccharin was found better in terms of Impurity study (Relative Substances study).Impurity was found within the specified limit compared to other two sweeteners. Stability study was carried out on optimized formulation. Overall batch containing 10 mg Crospovidone (Polyplasdone XL 10) along with Sodium Saccharin was foundstable both physically and chemically.

ВИБІР ДОПОМІЖНИХ РЕЧОВИН ДЛЯ ОТРИМАННЯ ТАБЛЕТОК L-ТРИПТОФАНУ З ТІОТРИАЗОЛІНОМ МЕТОДОМ ВОЛОГОЇ ГРАНУЛЯЦІЇ

Повідомлення 1. Вплив допоміжних речовин на однорідність дозування, процес пресування та зовнішній вигляд таблеток з L-триптофаном та тіотриазоліном, отриманих методом вологої грануляції.Мета роботи. Cтворення нового таблеткового лікарського засобу нейропсихотропної дії на основі L-триптофану та тіотриазоліну, підбір оптимальних допоміжних речовин, вивчення їх впливу на процес пресування, якість поверхні та однорідність маси дозування таблеток.Матеріали і методи. Діючі речовини – L-триптофан та тіотриазолін в співвідношенні 4:1, допоміжні речовини (наповнювачі, розпушувачі, зв’язуючі розчини, солюбілізатори). Таблетки пресували методом вологої грануляції. Вплив ДР речовин на таблетки, до складу яких входять L-триптофан та тіотриазолін, вивчали за такими показниками: однорідність дозування маси таблеток, процес пресування, зовнішній вигляд поверхні таблеток після виготовлення.Результати й обговорення. За результатами дисперсійного аналізу експериментальних даних було встановлено, що на процес пресування, зовнішній вигляд поверхні таблеток після виготовлення та однорідність дозування маси таблеток з L-триптофаном та тіотриазоліном впливає природа наповнювачів, розпушувачів, зв’язуючих розчинів, солюбілізаторів. Так, на процес пресування таблеток серед наповнювачів найкращий вплив має суміш таких ДР, як МКЦ 101+крохмаль картопляний+неусілін УФЛ, серед розпушувачів лідером є натрій крохмальгліколят.На якість поверхні таблеток L-триптофану з тіотриазоліном після виготовлення серед розпушувачів найбільший позитивний вплив має суміш МКЦ 101+ крохмаль картопляний + магній карбонат основний. На однорідність дозування маси таблеток серед зв’язуючих розчинів лідером є 5 % розчин ГПМЦ 5, серед розпушувачів перевага на боці поліплаздону ХЛ 10, серед наповнювачів лідером є суміш МКЦ 101 + крохмаль картопляний + магній карбонат основний, серед солюбілізаторів найбільший вплив має аеросил.Висновки. Вивчено вплив чотирьох груп допоміжних речовин на однорідність дозування, процес пресування та зовнішній вигляд таблеток з L-триптофаном та тіотриазоліном. Більшість із вивчених 16-ти ДР придатна для отримання таблеток на основі L-триптофану та тіотриазоліну методом вологої грануляції. За дослідженими показниками (процес пресування, якість поверхні таблеток, однорідність дозування) побудовані діаграми переваг рівнів 4-х вивчених факторів.

Selection of disintegrants for wet granulation method of “Angiolin” tablets

Every year there are about 9.4 million people who die from cardiovascular diseases. Among them, 51% of people are dying from stroke, and 45 % – from coronary heart disease. Today disease of the cardiovascular system is the number 1 problem in the world and in Ukraine. Annually cardiovascular disease kills more than 500 thousands of Ukrainians; it is about 1370 people every day. According to the State Statistics Service, about half of the deaths in 2016 in Ukraine had been caused by cardiovascular diseases. In comparison with 2015, the death rates have not changed in Ukraine. This shows low culture of prevention, diagnosis and treatment of cardiovascular disease among Ukrainians.Aim of our work is the selection of disintegrants to produce tablets “Angiolin” by wet granulation method with an active compound content of 200 mg.Materials and methods. 6 Disintegrants have been studied, most of which were presented in market only in recent years and were not used in the pharmaceutical tableting technology.Results. The disintegrants were studied in the experiment: a1 – potato starch, a2 – croscarmellose sodium, a3 – polyplasdone XL-10, a4 – carboxymethyl starch sodium, a5 – microcrystalline cellulose (MCC) burst, a6 – likotab P. The effect of disintegrants on the technological characteristics of “Angiolin” tablets has been studied and the possibility of their use by wet granulation method has been confirmed.Conclusion. The selected disintegrant, namely sodium croscarmellose has showed better results and will be used for “Angiolin” tableting by wet granulation method in the future.

Chronotherapeutically Modulated Pulsatile System of Valsartan Nanocrystals-an In Vitro and In Vivo Evaluation.

The objective was to improve the dissolution of valsartan by developing valsartan nanocrystals and design a pulsed release system for the chronotherapy of hypertension. Valsartan nanocrystals were prepared by sonication-anti-solvent precipitation method and lyophilized to obtain dry powder. Nanocrystals were directly compressed to minitablets and coated to achieve pulsatile valsartan release. Pharmacokinetic profiles of optimized and commercial formulations were compared in rabbit model. The mean particle size and PDI of the optimized nanocrystal batch V4 was reported as 211nm and 0.117, respectively. DSC and PXRD analysis confirmed the crystalline nature of valsartan in nanocrystals. The dissolution extent of valsartan was markedly enhanced with both nanocrystals and minitablets as compared to pure valsartan irrespective of pH of the medium. Core minitablet V4F containing 5% w/w polyplasdone XL showed quickest release of valsartan, over 90% within 15min. Coated formulation CV4F showed two spikes in release profile after successive lag times of 235 and 390min. The pharmacokinetic study revealed that the bioavailability of optimized formulation (72.90%) was significantly higher than the commercial Diovan tablet (30.18%). The accelerated stability studies showed no significant changes in physicochemical properties, release behavior, and bioavialability of CV4F formulation. The formulation was successfully designed to achieve enhanced bioavailability and dual pulsatile release. Bedtime dosing will more efficiently control the circadian spikes of hypertension in the morning.

Rapimelts of Venlafaxine Hydrochloride- An Approach to Formulation and In-vitro Evaluation

The present research workwas designed to manufacture venlafaxine hydrochloride rapimelts using different super disintegrants by direct compression method. The superdisintegrants used were sodium starch glycolate Primogel croscarmellose sodium Ac-Di-Sol and crospovidone Polyplasdone XL10 in varying concentrations of 2-5. In total nine formulations of venlafaxine hydrochloride rapimelts were prepared. The preformulation studies were conducted for the prepared blends and were found satisfactory. The formulated tablets of venlafaxine hydrochloride were evaluated for parameters like friability hardness disintegration time wetting time water absorption ratio disintegration time drug content and drug release. All the evaluated parameters were found within the limits. Amongst therapimelts prepared R-IX containing 5 of crospovidone showed 100 of drug release within 20 min and was optimized as the best formulation. The rapimelts of optimized formulation was subjected for accelerated stability studies as per ICH guidelines for a period of 180 days and then evaluated for hardness wetting time water absorption ratio and in vitro dispersion time. No significant changes in the evaluated parameters indicate that the formulation was found functionally stable.

Optimization of composition and technology for tablets containing aspen bark extract

Summary. Influence of quantitativefactorsof basic quality parameters has been investigated for tabletscontainingextractofaspenbark, receivedbydirect pressingmethodand mathematicalplanningof experiment.To set the optimal composition of tablets containingaspen bark extract the proportion ofProsolv 90, Ludiflash and Polyplasdone XL 10 has been studied. The relationship between the studied factors and parameters of tablets’ regression models has been described. As a result tablets containing aspen bark extractwith mentioned above formula match necessary pharmaco-technological parameters of State Pharmacopoeia of Ukraine.Introduction.Peptic and duodenal ulcer are serious problems in modern medicine. According to statistics this disease is found in 12,83 % of the adult population in Ukraine [1]. Among the remedies for treatment and prevention of peptic ulcers we can find herbal medicines that may be used in the treatment of pre-peptic conditions and during an acute period as a means of adjuvant therapy in combination with strong remedies [2]. An antacid, cytoprotective, anti-inflammatory and reparative actions of aspen bark extract were proved by the researches of domestic and foreign scientists [3, 4].Previously, we researched the mutual influence of excipients on the main indicators of quality of aspen bark extract tablets obtained by direct compression method. Due to these researches the best excipientshave been selected. It is necessary to establish the optimal quantitative proportion of excipients in order to obtain the tablets with suitable parameters that satisfy the requirements of the State Pharmacopoeia of Ukraine (SPU) [5, 6].Rational selection of excipients requires wide range of studies to obtain the optimal composition of the tablets containing aspen bark extract. Using mathematical planning of the experiment gives the possibility to reduce the number of experiments and to obtain the most detailed results of researches about effects of excipients on the basic parameters of tablet quality.The aim of investigation.In the previous stages of the experiment, we studied the effect of quantitative factors on pharmaco-technological parameters of tablets. To further study were selected Prosolv 90, Ludiflash and Polyplasdone XL 10.The aim of investigation was to set and study the proportion of excipients selected for developing optimal formula of tablets containing aspen bark extract.Materials and methods.The tablets based on aspen bark extract, obtained by direct compression method, have beenselected as research object. In the development of technology and tablet form,dry aspen bark extract, obtained by the Department of Pharmacognosyof the National University of Pharmacy,has been used [7]. The dry aspen bark extract is hygroscopic fine powder with particles of anizodiametric shape.Namely, from the group of samples of microcrystalline cellulose (MCC) – Prosolv 90 (Silicified MCC, manufactured by JRS Pharma GMBH & Co KG., Germany), from the group structure-based substances sugars – Ludiflash (combination of mannitolCrospovidone, Povidone and polyvinyl acetate, manufactured by BASF Corp., USA) and from the group of disintegrants – Polyplasdone XL 10 (homopolymer of vinyl pyrrolidone, manufactured by manufactured by Ashland Inc., USA). At establishment of optimal composition of the tablets based on aspen bark extract three excipientsinfluence, and also their correlation in composition of tabletshas been studied [8].Results and discussion.The optimal formula of selected excipients has been set and their proportions in tablet dosage form at the shorter intervals have beendetermined. The study of each researched factor has been carried out according to 5 levels. As a result of studies we found the optimal number of excipients for tablet formula: Prosolv 90 – 0,054 g, Ludiflash – 0,03 g, Polyplasdone XL 10 – 0,025 g, MCC 102 – 0,0835 g, magnesium stearate – 0,0025 g in one unit of dose medication. As a result tablets of aspen bark extract with mentioned above formula have necessary pharmaco-technological parameters that meet the requirements of SPU: resistance to crushing – 130 H, abrasion – 0,04 % mass uniformity of tablets – ± 2,85%, disintegration – 6 min [9].ConclusionsDue to mathematical planning the quantitative impact of significant excipients on pharmaco-technological parameters of tablets based on aspen bark extract: Prosolv 90, LudiflashтаPolyplasdone XLhave been studied.Due to the regression analysis optimal composition of tablets based on aspen bark extract : dry aspen bark extract – 0,05 g, Prosolv 90 – 0,054 g, Ludiflash – 0,03 g, Polyplasdone XL 10 – 0,025 g, MCC 102 – 0,0835 g,Neusilin US 2 – 0,0025 g, talc –0,0025 g, magnesium stearate – 0,0025 ghas been determined. As a result tablets of aspen bark extract with mentioned above formula have necessary pharmaco-technological parameters that meet the requirements of SPU.

Contrasting the crospovidones functionality as excipients for direct compression

Specific values of technological properties of excipients allow the establishment of numerical parameters to define and compare their functionality. This study investigates the functionality of Polyplasdones XL and XL10. Parameters studied included tablet disintegration profiles, compactibility profiles and powder flow. The results allowed the establishment of quantitative surrogate functionalities of technological performance, such as absolute number, and as a value relative to the known microcrystalline cellulose type 102. Moreover, the establishment of an explicit functionality to improve the technological performance of two diluents and a model drug was investigated, as was setting up of these functionalities, as quantitative values, to determine the input variables of each material and its probable functionality in a drug product. Disintegration times of pure Polyplasdone XL and its admixtures were around half that of Polyplasdone XL10. The improvement in tablet compactibility was 25-50% greater for Polyplasdone XL10 than Polyplasdone XL. Crospovidones proportions of up to 10% have little effect on the flow properties of other powders, although pure Polyplasdone XL10 and its admixtures display compressibility indexes about 20% greater than Polyplasdone XL. The observed results are in line with a smaller particle size of Polyplasdone XL10 compared to Polyplasdone XL.

The Use of Synthetic Polymers (Superdisintegrants) in Technology Tablets Containing Ethanol Dry Extract from Asparagus officinalis

Dry extracts are now frequently used in medicine as an alternative to synthetic drugs. In the case of tablet technology with dry plant extracts, the proper selection of disintegrants (superdisintegrants) is particularly important. Objectives. The aim of this study was to evaluate the usefulness of the polymers constituting superdisintegrants (Vivasol®, Vivastar®, Polyplasdone XL) in uncoated tablet formulation of alcoholic extracted from Asparagus officinalis. Dry the ethanol extract of Asparagus officinalis, Vivasol®, Vivastar®, Vivapur®, Kollidon VA64, Polyplasdone XL, magnesium stearate. Direct compression. Paddle method was carried out to study pharmacopoeial parameters and pharmaceutical availability. The calculation of equivalency factors: similarity [f2] and the difference [f1]. Approximation results. Tablets brownish-green, with a smooth and uniform surface, without stains, chipping and damage. The determined average weight of the tablets compiled with the standards. The test friability and crushing strength revealed that the most mechanically strong tablets contained Vivasol, Vivastar, Polyplasdone XL. These tablets also have a longer disintegration and dissolution time compared with tablets containing only Vivasol. These differences are also confirmed by the calculated f2 and f1. The addition of a mixture of Polyplasdone XL and Vivastar to Vivasol significantly increases the mechanical strength of the tablets (crushing strength, resistance to crushing). The addition of a mixture of Polyplasdone XL and Vivastar to Vivasol paradoxically increases the disintegration time of tablets (11.1 min). Single superdisintegrant breaks up the tablet more effectively than a mixture of superdisintegrants.

Development of fast dispersing tablets of nebivolol: experimental and computational approaches to study formulation characteristics

Formulation of FDT (fast dispersing tablets) of nebivolol was optimized and evaluated using simplex lattice design (SLD). The influence of type and concentration of three disintegrants viz.,Ac-Di-Sol, Primojel and Polyplasdone XL on hardness, friability and disintegration time of tablet was studied. Response surface plot and the polynomial equations were used to evaluate influence of polymer on the tablet properties. Results were statistically analyzed using ANOVA, and a p < 0.05 was considered statistically significant. Results reveal that fibrous integrity and optimal degree of substitution in Primojel and Ac-Di-Sol are mainly responsible for the hardness of the tablet. Use of Polyplasdone in higher percentage in tablet formulation may result in high friability. Increase in concentration of Ac-Di-Sol increases the disintegration time but increased concentration of Primojel in the tablet formulation decreases the disintegration time. This is also evident from model terms for disintegration time with a high 'F' value of 14.69 and 'p' value of 0.0031 (<0.05). The reason could be that Primojel has higher swelling properties and an optimum hydration capacity, which favors fast disintegration of a tablet. In conclusion, careful selection of disintegrant for FDT could improve their properties. Use of Simplex Lattice Design for formulation development could simplify the formulation process and reduce the production cost.

RIZATRIPTAN BENZOATE FAST DISSOLVING TABLETS FOR QUICK RELIEVE OF MIGRAINE: DESIGN, DEVELOPMENT AND CHARACTERIZATION

Objective: Rizatriptan benzoate (RB) is a new generation anti-migraine drug. After oral administration, the peak plasma concentrations (tmax) occur in about 1 to 2.5 hrs depending on the formulation and the bioavailability which is about 40 to 45%. Food may delay the tmax by about 1 hour. The aim of this work was to design and develop fast dissolving tablets of RB to improve the bioavailability and patient compliance applying the Mixture Experimental Design. Methods: Twenty formulations were prepared by direct compression each containing 14.53 mg of RB equivalent to 10 mg Rizatriptan with different proportions of superdisintegrants (X1-X3) according to the experimental design. The independent factors selected were the percentages of: Croscarmellose sodium (X1), Explotab (X2) and Polyplasdone XL 10 (X3). The dependent variables investigated were: hardness (Y1), disintegration time (Y2) and cumulative % drug release after 10 minutes (Y3). The formulations were evaluated for the pre-compression parameters to assess the powder compressibility and flowability (bulk and tapped density, Hausner’s ratio, Carr’s index and angle of repose) as well as the post-compression parameters (weight variation, friability, hardness, disintegration time, wetting time, water absorption ratio, drug content and in-vitro drug release). The optimized formulation was prepared and evaluated in the same manner. Results: All the evaluated parameters, either for powder blend or for the compressed tablets, were within the acceptable limits. The values of dependent variables ranged between 3.13-3.68 kg/cm2; 12.23-21.81 sec; and 94.44-99.83% for Y1, Y2 and Y3 respectively. Polynomial regression equations for the variables (Y1-Y3) were generated and the quantitative effects of X1-X3 at different levels on Y1-Y3 could be predicted. Surface response and contour plots were plotted. The optimal ratios of different disintegrants were used to prepare the optimized formulation. The difference between the predicted and the observed data for the optimized formula were minimal. Conclusions: The use of direct compression technique and the mixture experimental design succeeded to produce fast dissolving tablets of RB with optimal hardness, minimal disintegration time and maximal in vitro drug release. The quantitative effects of the selected factors tested on the different variables were explored. Based on the obtained results, fast dissolving tablets of RB could be a potential dosage form for quick relieve of migraine patients.