tegkmurthy's blog

Topics for the month

Myself : 1)Chronotherapeutic vs colon drug delivery systesms 2)Chronotherapeutic vs pulsatile drug delivery systems G.Sailesh 1) Technology transfer (lab to commercial scale) 2) Stability testing V.Vijaya kumar 1) Effects of poor bioavailability 2) Reasons for poor bioavailability

Modified excipients

There are several reports indicating that the peformance of a pharmacuetical dosage form is influenced by the changes in suppliers of the same excipient due to the variations in physicochemical properties and quality of excipient. There is increased demand for excipients with pre-determined specifications to control the physical properties of excipients like size, shape, tecture, density and moisture content. Spray dried excipients improves the flow property and freeze dried excipients enhances the dissolution rate.

CO-PROCESSING EXCIPIENTS

Co-processing excipient is an excipients mixture containing more than one excipient and not prepared by simple physical mixing. These materials are formulated with co-crystallization, co-grinding, co-precipitation, spray drying and common solvent evaporation techniques. The physical properties such as particle size, shape, density may differ from one excipient to another excipient and results segregation and non uniformity. In case of co-processed excipients, the physical properties are well controlled.

Topics for the month of May

Leader (Myself): 1) Co-processed excipients 2) modified excipients M.Kishore babu : 1) Discriminative dissolution methods significance 2) Correlation of the college lab experiment with the industry - a necessity G.Sailesh : 1) Antibiotic drug resistance - Super bug 2) Enhancement of dissolution using multiparticulates V.Vijaya kumar: 1) Sterility testing

Coating technique for controlled release

Coating technique is used to modify the site, rate and extent of release. It can be applied for single unit dosage forms such as tablets/capsules and multiple unit dosage forms like pellets, granules. Aqueous based and organic based solvents can be used for coating. Coating technique can also be applied to achieve a drug release after a set lag time. Coating on multiparticulate system reduces the dose duping compared to single unit system.

Coating technique for stabilization

Coating technique is useful to improve the physical, chemical and biological stability and protects the drug against environmental factors. The insoluble drugs are often presented in the form of amorphous solids which may undergo crystallization over time to attain most stable form. To retain the drug in amorphous form i.e., most soluble form and to inhibit surface crystallization, the amorphous form may be coated with an ultra thin poly-electrolyte coating or alternatively with bio-compatible materials.

strategies to overcmome dose dumping

Solubility of polymer in gastric fluid and the solvent employed for administration of the formulation are to be considered in design of controlled drug delivery systems. The polymer with least solubility in these fluids avoids the possible dose dumping. pH independent polymers and pH dependent polymers soluble in intestinal polymers are preferable to prevent the dose dumping risk. Diffusion controlled systems are preferable compared to dissolution controlled systems go prevent dose dumping. Matrix controlled system are best suited rather than membrane controlled systems.

Dose Dumping - USFDA Regulatory perspective

There were many reasons for dose dumping of an extended release dosage form like improper design of dosage form, drug excipient interactions, crushing or chewing by patient1, intake of food or alcohol2 of which dose dumping due to alcohol is of more concern. Dose dumping due to alcohol was initially identified in palladone capsules that contain hydromorphone used to treat pain2. It is a potent narcotic with the dose of 12mg.

Dose dumping - technical perspective

Dose dumping is defined as "Unintended, rapid drug release in a short period of time of the entire amount or a significant fraction of the drug contained in a modified release dosage form1." A sustained/extended/controlled release dosage form is intended to release the drug in desired concentrations for a prolonged period of time. A dosage form is said to be dose dumped when there is an excess release of drug at a particular time interval other than the stated or required amount. This results in higher systemic drug concentrations that may result in toxicity.

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