Sustained Release

Methimazole is active pharmaceutical ingredient effectively utilized in hyperthyroidism. Methimazole inhibits peroxidase as well as iodine interactions with thyroglobulin to produce triiodothyronine with thyroxine. Methimazole shows very low protein binding (1-10%) bounds to plasma proteins and easily metabolized by liver. In this investigation, efforts given to develop a sustained release matrix tablet of Methimazole. Sustained release drug delivery systems are for a maximum of 24 hours clinical effectiveness. Such systems are primarily for the drugs of short elimination half-life. However, drugs with long half-life also qualify if a reduction in steady state fluctuation is desired. Matrix tablets of methimazole were prepared by utilizing direct compression method. HPMC along with Sodium carboxy methyl cellulose used to retard drug release from the dosage form. Matrix tablets of methimazole were evaluated for different quality control test to improve quality of the product. In vitro release study of methimazole matrix tablets shows that polymer percentage used in the formula is enough to extend the release of the drug for at least 12 hr. In dissolution study of matrix of methimazole formulation F2 shows maximum drug release 97.93 % at the end of 6 hours while F1 shows least 83.64 %.

The major objective of any dosage form development is to ensure the delivery of specific and reproducible amounts of pharmacologically active compounds to the body in the maximum amount possible. Today's most frequently used dosage forms are orally administered solids formulated such as tablets, capsules or powders. Timed-release products intend to improve delivery efficacy and/or effectiveness; for instance, the frequency of dosing can be reduced and, in certain cases, the actual daily dose can be reduced, offering the manufacturer a financial benefit. There have been many techniques developed for producing the variety of timed-release products. Ginger is a natural drug, which is used for nausea and vomiting, to treat bleeding disorders and rheumatism. In conventional dose is thrice a day, 8-10 gm which is not at all convenient for the patient. Increase the patient compliance is also a great challenge which is continuously improving by the novel drug delivery system. The main objective of the present work is to design Ginger root extract powder (5%w/w of 6-gingerol) timed release dosage form of the drug with the help of a novel clear transparent veggie capsule shell of ‘0’ size made up of cellulose and natural substance. The objective in formulating a sustained release dosage form is to be able to provide a similar blood plasma level pattern for up to desired hrs (12hrs) after oral administration of the drug. The formulation, optimization, destructive quantification parameters and in-vitro studies of the drug have focused in this research article. The presented work sought a futuristic research for the benefit of the patients.

In the present study, an attempt was made to prepare and evaluate matrix tablets of Ondansetron HCl using HPMC, EC and Eudragit for Sustained release of Ondansetron HCl. The matrix tablets were prepared by wet granulation method. All the formulations are evaluated for the Hardness, Friability, Weight variation, Drug Content, In-Vitro Drug Release. The weight variation and drug contents of all the tablets were found to be uniform with the low SD values. The FTIR study indicated that the drug is stable in the formulations. The prepared matrix tablets were capable of releasing the drug for 12 hours depending upon the formulation variables. The tablets prepared with HPMC and Eudragit combination have shown higher drug release Drug release mechanism followed non-Fickian transport from both the polymers matrices. The drug released from the formulation is depends on the concentration of the polymers.

Nateglinide, an oral hypoglycemic agent is having disadvantage of low systemic bioavailability, poor absorption in upper intestinal tract, and short biological half life (1.5hr) for increasing the resident time of this drug in stomach spray drying technique used for preparation of mucoadhesive microspheres consist of different polymers like Hydroxypropyl Methycellulose (HPMC), Hydroxypropyl cellulose (HPC), Polyvinylpyrrolidone (PVP), Sodium alginate and ethyl cellulose with Nateglinide. The surface morphology and particle shape were studied by scanning electron microscope (SEM). The microspheres were evaluated for their micro encapsulation efficiency. The micro encapsulation efficiency of microspheres evaluated. Mucoadhesive microspheres prepared were spherical in shape, size in the range of 2.6-5μm.In vitro drug release performed for all the formulation and in vivo study of optimum formulation (F3) and pure Nateglinide in normal healthy rabbits performed. The micro encapsulation efficiency was in the range of 76.75 % - 89.36 % and microspheres of formulations (F1, F2, F3, F4, F6, and F7) have shown good mucoadhesive property. F3 had shown significant hypoglycaemic effect upto period from 5 hrs to 19 hrs, whereas pure Nateglinide showed the reduction of 39.85% after a period of 3hrs and reached normal with in 6.5hrs.

The aim of this investigation was to develop and optimize Metformin HCl matrix tablets for sustained release application by response surface methodology based on two factor-three response factorial design. The effects of the amounts of polysaccharide from tamarind and polysaccharide from jackfruit in Metformin HCl matrix tablets on the properties of Metformin HCl sustained release matrix tablets drug release was analyzed and optimized. The observed responses were coincided well with the predicted values by the experimental design. The optimized Metformin HCl matrix tablets showed prolonged sustained release of Metformin HCl over 6 hours. These matrix tablets followed the first-order model with anomalous (non-Fickian) diffusion mechanism.