Patel, Khushman V. Asodaria, Hetal P. Patel and Dinesh R. Surat, Gujarat , India. Keywords:Controlled release osmotic pump tablets, glipizide, poloxamer , solid dispersion.
|Genre:||Health and Food|
|Published (Last):||12 December 2007|
|PDF File Size:||4.10 Mb|
|ePub File Size:||18.88 Mb|
|Price:||Free* [*Free Regsitration Required]|
Drugs are more frequently taken by oral administration. The solubility of Glipizide enhanced with different ratios of CCS by the kneading method. In-vitro release profile of solid dispersion obtained in Ph 6. These solid dispersions were directly compressed into tablets using sodium starch glycolate, crosspovidone and pregelatinised starch in different concentrations as a superdisintegrants.
The prepared tablets containing the solid dispersion of Glipizide had sufficient strength of 1. The disintegrated in the oral cavity within 21 sec. Keywords: Glipizide, CCS, solid dispersion, Superdisintegrants, Mouth dissolving tablet INTRODUCTION: An ideal dosage regimen in the drug therapy of any disease is the one, which immediately attains the desire therapeutics concentration of drug in plasma or at the site of action and maintains it constant for the entire duration of treatment.
It is considered most natural, uncomplicated, convenient, safe means of administering drugs, greater flexibility in dosage form design, ease of production and low cost.
Since the introduction of mouth dissolving tablet MDT in s, it has become one of the fastest growing segments of oral drug delivery. Techniques that have commonly been used to improve dissolution and bioavailability of poorly water-soluble drugs, in general, include micronization, the use of surfactant and the formation of solid dispersion SD 1. The SD approach has been widely and successfully applied to improve the solubility, dissolution rates, and consequently, the bioavailability of poorly water soluble drugs.
A number of drugs have been shown to improve their dissolution character, which converted to SDs. To date, some reports on the formulation of these systems have appeared An obstacle of SD technology in pharmaceutical product development is that a large amount of carrier, i. This high percentage of carrier causes consistency of product performance at the time of manufacturing.
This is a major consideration in that the number of market products arising from this approach has been less than expected. Among the various carriers used in the formation PEG is most commonly used. CCS are semicrystalline polymers that have been used extensively in the SDs preparation for their solubilizing and surface active properties The non-ionic surfactant Tween 80 was used as the third component in the ternary SD system Mouth dissolving tablets of itraconazole 16, valdecoxib 17, diazepam 18, glyburide 19, clonazepam 20 and rofecoxib 15 were prepared using SD technique.
Glipizide is a class-II antidiabetic drug which is purely insoluble in water. Rate of bioavailability of GLP is highly variable due to their low aqueous solubility. One of the major problems with drug is its very low solubility in biological fluids and its short biological half-life of 2 h Thus, these two factors act as the rate determining step or the barrier to rapid onset of action upon oral ingestion of GLP.
Moreover, it was also attempted for the incorporation of optimized SD formulation for the development of mouth dissolving tablets of GLP. All other chemicals used were of analytical grade. Construction of Standard Calibration Curve: Glipizide can be estimated spectrophotometrically at Aliquot of standard drug solution ranging from 0.
Absorbance of each solution was measured at nm against pH 6. A plot of concentrations of drug versus absorbance was plotted. The linear regression analysis was done on absorbance data points and given in Figure 1. Solubility Determination: The apparent solubility of Glipizide was determined in distilled water and buffer of pH 6. Each preparation equivalent to 10 mg was added to 10 ml of solvent in glass vials with rubber closers.
The solution was then filtered through 0. Solid dispersion formulation given in table 3. The potassium bromide KBr disk method was used for preparation of sample. The spectrum was compared with the infrared spectra of plain drug and polymer and checked for the drug-polymer interaction.
In vitro Dissolution Rate Study Dissolution rates from different solid dispersions were determined in ml of pH 6. A 5 ml aliquot of dissolution medium was withdrawn at 5, 10, 15, 30, 45, 60, 90, , min with a pipette.
The samples were suitably diluted and assayed spectrophotometrically at nm. Each dissolution rate test was repeated 3 times. Results are reported in Table 4, Figure 5 shows the dissolution profiles of solid dispersions. Tablet Formulation: Mouth Dissolving Tablets of Glipizide:CCS solid dispersions were prepared using direct compression method after incorporating different disintegrants like crosspovidone, SSG, Pre-gelatinized starch and microcrystalline cellulose MCC in different concentrations.
The methods of preparation, amount of solid dispersions equivalent to drug, and other tabletting excipients were kept constant to avoid the influence of these on the results. Solid dispersions and mannitol were mixed thoroughly in a glass mortar using a pestle. Disintegrants were mixed in the powder mixture, finally the talc and magnesium stearate were added as lubricants.
Compression force was kept constant for all formulations. The composition of the tablet is as shown in Table 5. Precompression parameter: Angle of Repose The angle of repose was determined by the funnel method.
The accurately weighed powder was taken in a funnel. The height of a funnel was adjusted in such a way that its tip just touches the apex of the heap of the powder. The powder was allowed to flow through funnel freely on to the surface. The diameter of the powder heap was measured and angle of repose was calculated using following equation.
Moisture Sorption Capacity Moisture sorption study was performed using programmable environmental test chamber Remi Labs, Mumbai One gram of powdered blend was taken in a petri dish and spread uniformly. The moisture sorption was calculated by recording weight difference of the sample before and after exposure to programmable environmental test chamber. Hydration Capacity H. Then 10 ml of distilled water was added to it and allowed to centrifuge for 10 minutes. After the centrifugation process the tarred centrifuge tube was taken out and inverted to remove the supernatant.
The decanted tube then weighed on digital balance shimadzu and the hydration capacity was calculated using following equation. Powdered 2 gm was poured into calibrated measuring cylinder 10 ml and noted initial volume. Then the cylinder was allowed to fall under its own weight onto the hard surface from the height of 2. The tapping was then continued until no further change in volume was noted. Tablet friability was measured using friability tester Roche friabilator.
Hardness of tablet was measured by Monsanto hardness tester. The data is shown in Table 7. Wetting Time The method reported by Mutasem was followed to measure tablet-wetting time. A piece of tissue paper folded twice was placed in a small petri dish ID 6.
A tablet was put on the paper, and the time for complete wetting was measured. Three trials for each were performed. Time required for complete disintegration of tablet was recorded. The test sample was filtered membrane filter, 0. The data is shown in Table 8.
Development of Controlled Release Osmotic Pump Tablet of Glipizide Solid Dispersion
Formulation and in vivo hypoglycemic effect of glipizide solid dispersion.