direct compression

Solubility is an important physicochemical factor for any drug molecule that affects its absorption along with its therapeutic effectiveness. Drug absorption is predominantly dependent upon its prompt dissolution. In the case of poorly water-soluble drugs, dissolution is the rate-limiting step in the process of drug absorption. Microspheres were prepared by solvent evaporation method using polymers namely Eudragit L100 and Eudragit RL100. Direct compression technique was used for the preparation of tablets. Tablets were prepared with MCC and PVP K-30 as polymers using an 8mm punch on a rotary press machine with a constant force. Microspheres and the prepared tablets were evaluated using various evaluation tests. The prepared microspheres showed >80% entrapment efficiency and percent yield. Batch F3 exhibited the highest drug release up to 98.30%. Fourier transform infrared (FT-IR) studies revealed no drug–polymer interaction. The results of SEM exhibited that the microspheres are spherical in shape with an average size 5µm. The result of all batches was within an acceptable limit. F2 batch tablet showed a higher drug release of 98.30% as compared with other batches. It was concluded that microcrystalline cellulose or PVP K-30, when used separately, caused retardation in drug release, whereas when used in combination (1:1) it achieved drug release in a controlled manner.

There has been an explosion of probiotic health-based products. Many reports indicated that there is poor survival of probiotic bacteria in these products. For oral delivery of probiotic, providing living cells with a physical barrier against adverse environmental conditions is considerable interest. The main goal of the study was to develop tablets made out of functional polymers in order to protect probiotic bacteria from gastric acidity, thus providing an easily manufacturing scale-up dosage form to deliver probiotics to the human intestinal. Tablets were produced by direct compression using Microcrystalline Cellulose )Avicel®( as main exipient. To optimize the formulation, using survival rate after both compressing and exposed pH: 2 acid medium were evaluated. Storage stability of lactobacilluse acidophiluse tablets was also performed by evaluation of viable cells throughout 3 months at 4 ºC. The highest viability was found in formulation 7 and 8 with %90.37 and 90.27% after compression pressure. Increasing amount of Avicel® in the tablet increase bacterial viability against pressure. 72.51% Survival was showed is related to formulation 3 after exposure acid. It can be concluded that The best protective qualities against artificial gastric juice were observed when tablets were prepared from compaction mixtures of lactic acid bacteria (LAB), sodium alginate, and Xanthan. A decrease of approximately one logarithmic cycle was observed after 3 month storage for formula 3 while untreated cell decrease 3.97 log. This preparation method and tablet formulation can be employed for intestinal delivery to ensure maximum viable cell release at intestine or colon and this product remains stable until the time of consumption.

Orally disintegrating tablets (ODTs) are a modern form of tablets that when placed in the oral cavity, disperses rapidly. These tablets have advantages, particularly good applications for children and old patients who have a complication in chewing or swallowing solid dosage forms.
The aim of this study was to design, formulate, and evaluate the physicochemical properties of 5 mg montelukast ODTs for the prevention of asthma and seasonal allergies.
Formulations were prepared with different amounts of super disintegrating agents and effervescent bases as disintegrant agents. Flowability and compressibility of mixed powders were evaluated. The prepared formulations were tested for hardness, thickness, friability, weight variation, drug content, wetting time, disintegration time, dissolution study, and moisture uptake studies.
The compressibility index and angle of repose were in the range of 15.87%–23.43% and 32.93–34.65, respectively. Hardness, thickness, friability, wetting time, and content uniformity of formulations were in the range of 33.7–37.1 N, 3.00–3.81 mm, 0.27%–0.43%, 31–50 s and 96.28%–99.90%, respectively. Disintegration time of the tablets prepared with super disintegrating agents, effervescent bases, and combination of two were in the range of 30–50, more than 60
and 20–36 s, respectively.
Mixture of powders and tablets passed all the specified tests. The results showed formulations prepared by super disintegrating agents and super disintegrating agents with effervescent bases had shorter disintegration time compared to formulations with effervescent bases alone.

Rizatriptan benzoate is a potent and selective 5-HT1B/1D receptor agonist and is effective for the treatment of acute migraine. Difficulty in swallowing is common among all age groups, especially elderly and pediatrics. Orally disintegrating tablets may constitute an innovative dosage form that overcome the problem of swallowing and provides a quick onset of action. This study was aimed to formulate and evaluate an Orally Disintegrating Tablet (ODT) containing Rizatriptan while using semi-synthetic and natural superdisintegrants. Orodispersible tablets were prepared by direct compression using natural superdisntegrant (Plantago ovata mucilage) and semi-synthetic superdisntegrant (crospovidone). The prepared tablets were evaluated for hardness, friability, thickness, drug content uniformity, water absorption and wetting time. A 32 factorial design was used to investigate the effect of independent variables (amount of crospovidone and Plantago ovata mucilage) on dependent variables [disintegration time, wetting time and Q5 (cumulative amount of drug release after 5 minutes)]. A counter plot was also presented to graphically represent the effect of independent variable on the disintegration time, wetting time and Q5. The check point batch was also prepared to prove the validity of the evolved mathematical model. The systematic formulation approach helped in understanding the effect of formulation processing variable. According to the results of optimized batches, the best concentration of superdisintegrant were as follows: 9.4 mg Psyllium mucilage and 8.32 mg crospovidone gave rapid disintegration in 35sec and showed 99% drug release within 5 minutes. Plantago ovata mucilage, a natural superdisintegrant, gives a rapid disintegration and high release when used with synthetic superdisntegrant in formulation of orally disintegrating tablet of Rizatriptan.

The objective of present investigation was to formulate sustain release (SR) matrix tablets of Glipizide (GLZ) for treating type II Diabetes mellitus (T2DM). Different formulations were prepared by direct compression using Klucel HF (KLU HF) and Kollidon SR (KOL SR). Drug excipient interaction studies confirmed absence of any kind of interaction between the drug and the polymer. The powder blends were evaluated for their flow properties, compressibility, and particle size distribution. The tablets were evaluated for hardness, weight variation, friability and drug content uniformity. In vitro release of glipizide from the formulated tablets was performed in progressive pH media. These tablets were also evaluated for their swelling and erosion behaviour. Pharmacokinetic parameters of optimised formulation were compared with the immediate release and sustained release marketed formulations. Further, the formulations were evaluated for in vitro in vivo correlation and bioequivalence studies. The powder blends possessed good compressibility and flowability. The dissolution release profile demonstrated diffusion controlled release which was depicted from Higuchi and Korsmeyer Peppas model. However, swelling and erosion were also found to play profound role in the release kinetics. The in vivo studies along with in vitro in vivo correlation (IVIVC) elucidated that the optimized formulation was bioequivalent to the marketed formulation.

The purpose of this work was to develop once daily sustained release (SR) matrix tablets of naproxen, an anti-inflammatory agent. The tablets were prepared by wet granulation method along with hydrophilic matrix materials like Methocel K 15M CR and Methocel K 100M CR. The granules were evaluated for bulk density, angle of repose, compressibility index, total porosity and drug content. The tablets subjected to thickness, diameter, weight variation test, drug content, hardness, friability, and in vitro release studies in buffer medium (pH, 7.4). The granules prepared either by Methocel K 15M CR or Methocel K 100M CR did not show satisfactory flow properties and compressibility, and had difficulty in sieving and individual in drug release. On the other hand, tablet matrix prepared along with Methocel K 15M CR and Mehtocel K 100 LV CR polymers of the proposed formulation F-8 showed desired drug release up to 24 h. All the formulations followed first order release kinetics (except F-2 and F-4), exhibited diffusion dominated drug release when data plotted into Korsmeyer Peppas equation. The matrix tablet of naproxen using hydroxypropyl methylcellulose derivatives controls the drug release effectively for 24 h; hence, the formulation can be considered as once daily sustained release tablet of naproxen in order to improve patient compliance.