Oral solid dosage has been a predominant form to provide Active Pharmaceutical Ingredients (APIs) to a patient. The disintegration of the drug through oral dosage forms has been a cause of major bioavailability problems in the past. Therefore, the mechanism is carefully controlled in pharmaceutical products. Oral dosage usually refers to the category of drugs administered to the patient in the form of tablets, capsules and other orally administered forms.
This is a specifically critical process for Immediate-release dosage forms. Immediate-release tablets are such that they completely disintegrate and dissolve within a short time period of 2.5 to 10 minutes when exposed to physiological fluids. Such fast disintegration is even more required for Orally-dispersible tablets that disintegrate in the mouth immediately after coming in contact with the saliva before being swallowed. Also, the quick disintegration of the drug is required in case of the need for rapid onset of action, For example - Analgesics.
Another form of tablets is the Modified-release tablets. In such dosages, API release may be designed to be slow for gradual or selective absorption in the Gastro-Intestinal (GI) tract, or for resulting in delayed onset time. This gradual disintegration can be obtained by- embedding API in a polymer matrix having slower dissolving rate than the drug, or by coating the API with a suitable polymer coating that functions as a mass transfer limiting barrier.
Usually, therapeutic dose of a drug is administered to the patient. In that case, API is combined with the excipients to obtain the required full volume of the dosage, hence, facilitating the compression of the powder mixture into desired tablet size. APIs can lead to several processing limitations such as - difficulty in blending, unwanted adhesion to surfaces of tablet punches and feeder walls, or poor flowability. These processing limitations of APIs occur due to their small particle size and needle-like morphology.
To overcome these limitations, selecting proper process routes like glidants, lubricants and surfactants are crucial in order to ensure a high-quality product. However, embedding of a drug in a complex matrix usually reduces its bioavailability. It delays the onset of dissolution in case of Immediate-release tablets.
Therefore, it is required to add disintegration agents to enhance breaking up of tablets in small granules and constituent particles and thus, facilitate quick disintegration of drug particles from the matrix of the tablet so as to increase the surface area for dissolution.
The API near the tablet surface will dissolve, leaving the API in the matrix in the absence of disintegration. Hence, complete disintegration of the tablet upon exposure to the dissolution medium is very crucial to obtain a dependable clinical performance of the dosage form.
Another form of tablets is the Modified-release tablets. In such dosages, API release may be designed to be slow for gradual or selective absorption in the Gastro-Intestinal (GI) tract, or for resulting in delayed onset time. This gradual disintegration can be obtained by- embedding API in a polymer matrix having slower dissolving rate than the drug, or by coating the API with a suitable polymer coating that functions as a mass transfer limiting barrier.
Usually, therapeutic dose of a drug is administered to the patient. In that case, API is combined with the excipients to obtain the required full volume of the dosage, hence, facilitating the compression of the powder mixture into desired tablet size. APIs can lead to several processing limitations such as - difficulty in blending, unwanted adhesion to surfaces of tablet punches and feeder walls, or poor flowability. These processing limitations of APIs occur due to their small particle size and needle-like morphology.
To overcome these limitations, selecting proper process routes like glidants, lubricants and surfactants are crucial in order to ensure a high-quality product. However, embedding of a drug in a complex matrix usually reduces its bioavailability. It delays the onset of dissolution in case of Immediate-release tablets.
Therefore, it is required to add disintegration agents to enhance breaking up of tablets in small granules and constituent particles and thus, facilitate quick disintegration of drug particles from the matrix of the tablet so as to increase the surface area for dissolution.
The API near the tablet surface will dissolve, leaving the API in the matrix in the absence of disintegration. Hence, complete disintegration of the tablet upon exposure to the dissolution medium is very crucial to obtain a dependable clinical performance of the dosage form.
Get subject wise printable pdf documentsView Here
Thanks for the knowledge sharing.
ReplyDeleteWhat about extended release? Would you write an article about the pharmaceutical technologies to achieve a prolonged release?
Surely I shall write it very soon. Keep visiting.
DeleteCan you please guide us with the in house calibration performed in formulation plant like RPM of machines CFM calculation, Inprocess equipments like DT and friability etc.
DeleteYes, I have written all calibrations on my blog. Please do search.
Deleteplease write on filter validation and cleaning validation in injectable dosage form
ReplyDeleteInteresting read. Thank you
ReplyDeleteInteresting!
ReplyDelete