Orodispersible Tablets in Psychiatric and Mood Disorder Management: Clinical Value, Pharmacokinetics, and Patient-Centric Formulation Strategies

Objectives: Olmesartan medoxomil (OM) is employed for treating patients who are intolerant of ACE inhibitors. The challenge to the researchers is because of its poor oral bioavailability and poor solubility. The approach for this problem is to use a hydrophilic carrier in formulation of oro-dispersible tablet (ODT) which presents a suitable way to improve the bioavailability by using quality by design (QbD) techniques with design of experiments (DoE) using definitive screening design (DSD) which produce a robust and rugged formulation. Methods: The focus of the research was to formulate OM/PVP solid dispersion (SD) and formulation of an Oro dispersible tablet (ODT) by QbD techniques. The main focus of this research is to provide a rugged and robust formulation using QbD concept with the application of Definitive screening design for optimization. Results: The dissolution studies of OM/PVP K30 1:1% w/w showed full release within 30 min which may be attributed due to the hydrogen bond formation between OM and PVP K30 in the FTIR spectra which enhanced the solubility. The disintegration and dissolution results were found to be satisfactory and meeting the desired quality target product profile (QTPP). Conclusion: The present research highlights a thorough understanding of the dosage form development with the knowledge of the critical risks involved in formulation to have an impact on critical quality attributes (CQAs). The critical material attributes (CMAs) were refined by DoE using definitive screening design (DSD) to develop design space. Key words: Critical material attributes (CMAs), Critical quality attributes (CQAs), Definitive screening design (DSD), Quality by design (QbD), Design of experiments (DoE).

Formulation and evaluation of orodispersible tablet of taste masked doxylamine succinate using ion exchange resin

Background: This study aimed to develop and optimize an orodispersible herbal tablet incorporating Achyranthes aspera Linn extract. Sodium Starch Glycolate and Crospovidone were employed as superdisintegrants to promote rapid tablet disintegration, while β-cyclodextrin was utilized to enhance the solubility of specific constituents within the extract. The optimized formulation exhibited a rapid disintegration time of 1.805 seconds and achieved a cumulative drug release of 98.04%, indicating improved dissolution and potential enhancement in oral bioavailability. Methodology: Orodispersible tablets were formulated using Design of Experiments (DOE) software, with crospovidone and sodium starch glycolate as independent variables, and time of disintegration and cumulative drug release as dependent variables. The formulation was evaluated for weight variation, uniformity, hardness, wetting time, and in vitro dispersion time. Result & Discussion: The optimized F6 batch of orodispersible herbal tablets demonstrated the following characteristics: hardness of 2.98 kg/cm², friability of 0.58%, weight variation of 3.319%, disintegration time of 13.805 seconds, wetting time of 34.4 seconds, content uniformity of 99.5%, water absorption of 36%, and cumulative drug release of 98.04%, all within the permissible limits as per official pharmacopoeialstandards. Conclusion: The study concludes that crospovidone and sodium starch glycolate effectively reduce disintegration time and improve cumulative drug release. These findings validate the reliability of the model, with minor deviations attributed to experimental variability.

Orodispersible tablet (ODT) provides rapid disintegration in the oral cavity. ODT improves the efficacy of using medicines especially in term of compliance in a patient with dysphagia. The major challenge of ODT is a bitter taste of active pharmaceutical ingredient (API); they can lead the patients to refuse medication. This study focused on the developing of the orodispersible disc (ODD) with a taste masking property by preparation of API particle that was taste-masked by polymers. The co-precipitation technique was used for the taste masking. Acetaminophen (APAP) taste-masked particles prepared with different grades of crospovidone were investigated for the taste-masking property. Kollidon® CL-SF exhibited the lowest drug release. An increasing amount of Kollidon® CL-SF caused increasing of APAP release. Particles consisted of APAP:crospovidone at ratio 3:1 showed the lowest drug release. It was probably due to the complexation which was shown by the FT-IR and DSC. Taste-masked particles were compressed as ODD by a hydraulic press machine. The disintegrating time of ODD was at the range of 12.62-17.35 s. The dissolution of ODD was focused on the taste-masking zone (drug release in 1 min). The ODD with ratio 3:1 particle (APAP: Kollidon® CL-SF) showed the highest taste-masking performance, the lowest drug release. All disc formulations completely released APAP after 30 min. Therefore, the preparation of ODD contains taste-masked particles was promising to improve patient compliance of bitter APIs.

Bosentan is a drug used to treat pulmonary hypertension via dual endothelial receptor antagonism. Bosentan has a restricted oral bioavailability, a problem that's mostly due to poor solubility and hepatic metabolism. It is extensively used for the elderly and children who require a friendly dosage form like orodispersible tablets. So, the goal of this research work was to hasten the dissolution rate of bosentan to produce an orodispersible tablet with immediate drug release. Bosentan was exposed to ethanol-assisted kneading with a rise of xylitol or menthol concentrations (1:1 and 1:2 molar ratio of bosentan with excipient). In addition to observing the dissolution behavior, the resulting dry products were investigated using Fourier transform infrared spectroscopy (FTIR), differential thermal analysis (DTA), and X-ray diffraction (XRD). The FTIR reflected possible hydrogen bonding with xylitol and menthol. DSC studies reflected a reduction in the enthalpy and Tm. These results with XRD data reflected partial co-amorphization in the case of xylitol and eutaxia in the case of menthol. These modifications were related to an accelerated dissolving rate. The developed systems were fabricated as orodispersible tablets which exhibited immediate release of bosentan. Thus, the current study offered simple co-processing for the preparation of orodispersible bosentan tablets.

In present study Orodispersible tablets (ORDT) of Loratadine were prepared and optimized. Solid dispersion of Loratadine- β cyclodextrin complex were prepared and used in preparation of Orodispersible tablets. Various super-disintegrating agent like Cross carmellose sodium, Cross povidone and Kyron T-314 were employed for faster disintegrating effect. The 24 factorial and Box-Behnken design were utilized to optimize the tablet formulation. The Orodispersible tablet of Loratadine was optimized by Box Behnken Design, where concentrations Kyron T-314, CRP and Pearlitol SD200 were employed and its effect on Disintegration time (DT), Wetting time (WT) and % drug release at 20 min (Q20) was evaluated. Precompression parameters like angle of repose, bulk density, % compressibility, Hausner’s ratio was studies. The different batches of Orodispersable tablets were prepared and evaluated for disintegration time, friability, wetting time and drug release studies. Different batches prepared showed disintegration time in the range of 23 ± 2.52 to 59 ± 2.64, wetting time in between 27± 0.57 to 66.3 ± 3.4, drug release (Q 20) in between 86.1 ± 0.6 to 96.7 ± 0.4 in 20 min., friability less than 1 % and hardness 3.4 to 4.2 Kg/cm2. The optimized formula when compared with marketed product it showed faster disintegration time and rapid drug dissolution in phosphate buffer 6.8. The solid dispersion of Loratadine not only helped improve in solubility but may also help in taste masking. Keywords: Orodispersible tablets, Loratadine, β cyclodextrin Solid dispersion

In a challenge to prepare a stable Oro-dispersible tablet (ODT) of Desloratadine, using dry resin was incorporated into a fast-disintegrating matrix to prepare an optimized ODT that achieved the desired criteria of stabilization and patient acceptance. In this study, the critical process parameters (CPPs) and critical material attributes (CMAs) were determined via risk assessment methods within the framework of Quality by Design (QbD). The results showed that resin (Amberlite IRP64®) can be used as a dry stabilizer and the selected variables in the optimization phase have a strong influence on the blend flowability, disintegration time, and wetting time of the ODTs. Furthermore, by comparing the optimized formula with the marketed one, the optimized formula showed a significantly lower disintegration, lower wetting time, and an almost similar dissolution profile.

Amlodipine is a BCS (biopharmaceutical Classification System) class I drug with high permeability and high solubility. It has a long half-life of 30-50h. It is a suitable model drug for formulating orodispersive tablets, as the orodispersive tablets can release the drug immediately. thus, formulation of amlodipine into orodispersible tablets will help in improved delivery of the drug at a faster rate. to achieve this, the orodispersive tablets were prepared by sublimation technique and the concentration of the sublimating agents was optimized by central composite design. based on the results, it was concluded that camphor and thymol when used at optimum concentrations can be used in the formulation of orodispersive tablets, the drug delivery systems for drugs with long half-life. they are potential delivery systems to improve palatability also for model drugs like amlodipine.

Background: Lovastatin, a BCS Class II drug, exhibits poor aqueous solubility and dissolution-limited bioavailability, which may reduce therapeutic effectiveness. Solid dispersion using hydrophilic carriers is an effective approach to enhance solubility and dissolution. Orodispersible tablets (ODTs) further improve patient compliance and provide rapid drug release. Aim: The present study aimed to develop and optimize lovastatin solid dispersions using PEG 6000 and formulate the optimized dispersion into ODTs for improved dissolution and potential bioavailability. Method: Solid dispersions were prepared by fusion method and optimized using Central Composite Design by studying temperature, stirring speed, and drug addition rate on drug content, drug release, and dissolution efficiency. The optimized formulation was characterized using FTIR. The optimized solid dispersion was formulated into ODTs by direct compression and evaluated for physicochemical properties, dissolution, release kinetics, and stability. Results: The optimized formulation at 69.99°C and 499.38 rpm showed 99.23% drug content, 96.52% drug release, and 84.67% dissolution efficiency (desirability 0.904). FTIR confirmed absence of interaction, while DSC showed amorphous conversion. ODTs showed acceptable parameters with rapid disintegration (27 sec) and drug release (96.21% at 30 min). Drug release followed first-order kinetics with Fickian diffusion. Stability studies confirmed formulation stability. Conclusion: The developed ODTs significantly improved dissolution and may enhance oral bioavailability of lovastatin.

Orodispersible tablet (ODT) containing microcapsules is an advanced and convenient drug delivery system that offers advantages of easy administration, and increased bioavailability. Metronidazole is an antiprotozoal, with a bitter and metallic taste as its major drawback. A taste masking is required since the tablet will disintegrate in the oral cavity releasing the drug into close proximity to the taste buds. The purpose of the study is to design and evaluate metronidazole microcapsules for formulation of taste masked orally ODT metronidazole tablets. Taste masked metronidazole microcapsules were prepared by emulsion polymerization method with sodium alginate as polymer using different drug to polymer ratio. The microcapsules were evaluated for drug loading, entrapment efficiency, drug-polymer interaction by FTIR spectrometry, DTA, and flow properties. Batches B4 and B5 were formulated into orally disintegrating tablet by direct compression method. The results of FTIR spectrometry and DTA characterization of microcapsules revealed absence of drug-polymer interaction. Evaluation of the microcapsules showed fairly good flow properties and increase in entrapment efficiency as the polymer concentration increased. Evaluation of the directly compressed ODTs showed acceptable weight variation, and average disintegration time less than 60 sec. The average tablet crushing strength range from 18 to 19 N, and the drug release profiles showed greater than 80% release of metronidazole within 10 min. The successful microencapsulation of metronidazole, fast disintegration, rapid drug release profile, and evidence of compatibility between metronidazole and the process polymer demonstrates the suitability of the microcapsules for formulation of orally disintegrating tablet for convenient delivery of metronidazole.Keywords: Orally disintegrating tablets, microencapsulation, taste masking

The purpose of this research was to mask the intensely bitter taste of aceclofenac (ACF) and to formulate oro dispersible tablet (ODT) of the taste-masked drug. Taste masking was done by complexing aceclofenac with Hydroxypropyl-β-Cyclodextrin (HPβCD) by different methods. Phase solubility studies indicated complex with possible stoichiometry of 1:1 and a stability constant of 221.11 M−1. The complexes were characterized by Fourier transform infrared spectroscopy, X-ray diffraction, and differential scanning calorimetry studies. The characterization studies confirmed inclusion of the ACF within the nonpolar cavity of HPβCD in the neutralization method (NM). Remarkable improvement in the in vitro drug release profiles in pH 6.8 phosphate buffer was observed with all complexes, especially the neutralization. The complexes of ACF–HPβCD (1:1) was compressed into tablet and properties of tablets such as tensile strength, wetting time, in vitro disintegration time, and disintegration in the oral cavity were investigated to elucidate the wetting and disintegration characteristics of tablets. Polyplasdone XL-10 7% wt/wt gave the minimum disintegration time. Tablets of batch F4 containing Avicel 200 and 7% wt/wt Polyplasdone XL-10 showed faster disintegration, within 12 s, than the marketed tablet (128 s). Good correlation between in vitro disintegration with in-house developed method and in the oral cavity was recognized. Taste evaluation of ODT in human volunteers revealed considerable taste masking with the degree of bitterness below threshold value. Thus, results conclusively demonstrated successful masking of taste and rapid disintegration of the formulated tablets in the oral cavity.

Ofloxacin is a synthetic chemotherapeutic antibiotic used for treatment of a variety of bacterial infections, but therapy suffers from low patients’ compliance due to its unpleasant taste. This study was aimed to develop taste masked microspheres of ofloxacin using Eudragit and to prepare orodispersible tablets of the formulated microspheres using natural superdisintegrant. Taste masking Eudragit E100 microspheres were prepared by solvent evaporation technique with an entrapment efficiency ranging from 69.54 ± 1.98 to 86.52 ± 2.25%. DSC revealed no interaction between the drug and polymer. Microspheres prepared at a drug/polymer ratio of 1:4 and 1:5 revealed sufficient flow properties and better taste masking as compared to other ratios. Drug loaded microspheres were formulated as orodispersible tablets using locust bean gum as a natural superdisintegrant offering the advatages of biocompatibility and biodegrad-ability. The wetting time, water absorption ratio and in-vitro disintegration time of the tablets were found to range between 19 ± 2 to 10 ± 3 seconds, 59.11 ± 0.65 to 85.76 ± 0.96 and 22 ± 2 to 10 ± 2 seconds, respectively. The in-vitro ofloxacin release was about 97.25% within 2h. The results obtained from the study suggested the use of eudragit polymer for preparing ofloxacin loaded microspheres with an aim to mask the bitter taste of the drug and furthermore orodispersible tablets could be formulated using locust bean gum as a natural superdisintegrant.

Dual strategy to enhance domperidone dissolution: mechanochemically synthesized multicomponent salts in orodispersible tablets.

Different tablet dosage forms were prepared to be administered for patients with dysphagia (swallowing difficulties) like buccal, sublingual and orodispersible tablets, however, they possesses certain constrains like taste masking difficulties, limitations in drug and dose selection and friability. Hence, in an attempt to overcome these constrains, a new easily swallowed immediate release tablets containing (160mg) Valsartan were prepared, and designed to be slippery upon contact with saliva giving an easy swallowing of the intact tablet (without water) with efficient taste masking effect, thus, they called Oroslippery tablets (OSTs). Core tablets were prepared by direct compression using different superdisintegrants, followed by dipping in special coating dispersion containing different proportion of kollicoat IR (film former) and xanthan gum (slipperiness inducer) at different coating levels. These OSTs were optimized for their physical properties, in-vitro disintegration and release in addition to in-vivo slipperiness and taste masking effect. It was found that F12 containing 6% crosscarmellose sodium double coated with 15% kollicoat IR and 0.3% xanthan gum possessed a good mechanical strength (hardness=5.69±0.58 Kg/cm2, friability=0.09%±0.79), suitable in-vivo slipperiness and taste masking times (8±1.45 and 58±2.18 seconds) respectively, with longer disintegration time (5.57±1.36 minutes) but similar release profile to the commercial conventional tablet Diovan® with similarity factor (f2= 68.4±1.07) and difference factor (f1= 1.39± 0.95). Therefore, this study developed a new easily swallowed tablet with an efficient taste masking property, high loading capacity and adequate mechanical strength that can be used as an alternative to buccal, sublingual and orodispersible tablets.

ألخلفية: ألبريدنيزولون هو كورتيكوستيرويد ذو طعم شديد ألمرارة يعمل كدواء مضاد للإلتهاب و مثبط للمناعة يستعمل في أي مرحلة عمرية. ألهدف: لتحسين تقبل ألمريض للدواء بواسطة إكساء ألطعم ألمر للدواء ليتم إيصاله كقرص متشتت بالفم. ألطريقة: طريقة ألتبلور الأيوني ألخارجي, حيث إستخدم ألجينات ألصوديوم (0.5%) و كلورايد ألكالسيوم (1%) بوجود (0.5%) غم/ مل من ألكاربابول 940 لتحضير خرز مكسوة ألطعم محملة بالبريدنيزولون ليتم كبسها كأقراص متشتتة بالفم. ألنتائج: تم إكساء ألطعم ألمر للبريدنيزولون بواسطة تحضير خرز متكونة من 1:1:1 (ألجينات ألصوديوم, كاربابول 940, بريدنيزولون) والتي حررت فقط 0.77% من ألبريدنيزولون في وسط يشبه ألوسط ألفموي. تم تحضير ألقرص ألمتشتت في ألفم بواسطة طريقة ألكبس ألمباشر بأستعمال كمية من ألدواء ألمكسو ألطعم المكافئ ل 5 ملغم من ألبريدنيزلون, 3% كروسبوفيدون, 2% بولي فينيل ألكحول, 1% تالك, 1% سترات ألمغنيسيوم ومزيج من ألأفسيل PH 102 وألمانيتول بنسبة 1:1 وكان ألتصييغ ألمختار T6 يملك صلابة 3.9± 0.32, هشاشة 0.45%, سمك 2.5 ± 0.05 mm, نسية محتوى ألدواء 98.2% ± 1.8, ألوقت أللازم للترطيب 18.7 ± 1.3 ثانية, نسبة امتصاص الماء 41 ± 2.1%, ألوقت أللازم للتشتت15.3 ± 0.5 ثانية وكانت نسبة تحرر ألدواء في ألوسط ألمشابه للوسط ألفموي هي فقط .75% ± 0.010 من ألبريدنزلون خلال دقيقة واحدة ( وهذا يدل على ألإكساء ألجيد) بينما إستمر تحرر ألدواء في ألوسط ألحامضي ألمشابه لوسط ألمعدة وألوسط ألقاعدي ألمشابه لوسط ألأمعاء لمدة ساعتين لكل وسط. ألأستنتاج: يمكن ألإستنتاج بنجاح طريقة ألتبلور ألايوني ألخارجي في إكساء ألطعم ألمر للبريدنيزولون وأيضا يمكن تصييغه كقرص متشتت بالفم مكسو ألطعم بواسطة طريقة ألكبس ألمباشر.