Preformulation consideration and application in development of dosage form I Introduction
1.3 هزار بار بازدید -
4 سال پیش
-
Preformulation evolved in the late
Preformulation evolved in the late 1950s and early 1960s as a result of a shift in emphasis in industrial pharmaceutical product development. It was improvement in analytical methods that spurred the first programs that might bear the name “preformulation”. The overall objective of preformulation testing is to generate information useful to the formulator in developing stable and bioavailable dosage forms which can be mass-produced.
During the early development of a new drug substance, the synthetic chemist, alone or in co-operation with specialists in other disciplines including preformulation, may record some data which can be appropriately considered as preformulation data.
Before starting the preformulation studies we should know the properties of the drug, potency relative to the competitive products and the dosage form, literature search providing stability and decay data, the proposed route of drug administration, literature search regarding the formulation approaches, bioavailability and pharmacokinetics of chemically related drugs. It also includes preliminary investigations and molecular optimization by the drug should be tested to determine the magnitude of each Suspected problem area (Step I), if a deficiency is detected, a molecular modification should be done(Step II). To overcome this deficiency molecular modification is done be salts, prodrugs, solvates, polymorphs or even new analogues. The dissolution rate of a salt form of a drug is generally quite different from that of the parent compound. Sodium and potassium salts of weak organic acids and hydrochloride salts of weak organic bases dissolve much more readily than do the, respective free acids or bases. For Example Ephedrine base is very poorly water soluble molecules that characterized by low solubility and dissolution rates. So, it is modified in the form of the salt Ephedrine HCL that is ionized and offer higher water solubility and dissolution rate. Prodrug formation is the formation of synthetic derivatives of the drug (e.g. esters or amides) that liberate the active drug in-vivo. Prodrug may or may not have a pharmacological activity.
#preformulationstudies #drvikaspharmacy
During the early development of a new drug substance, the synthetic chemist, alone or in co-operation with specialists in other disciplines including preformulation, may record some data which can be appropriately considered as preformulation data.
Before starting the preformulation studies we should know the properties of the drug, potency relative to the competitive products and the dosage form, literature search providing stability and decay data, the proposed route of drug administration, literature search regarding the formulation approaches, bioavailability and pharmacokinetics of chemically related drugs. It also includes preliminary investigations and molecular optimization by the drug should be tested to determine the magnitude of each Suspected problem area (Step I), if a deficiency is detected, a molecular modification should be done(Step II). To overcome this deficiency molecular modification is done be salts, prodrugs, solvates, polymorphs or even new analogues. The dissolution rate of a salt form of a drug is generally quite different from that of the parent compound. Sodium and potassium salts of weak organic acids and hydrochloride salts of weak organic bases dissolve much more readily than do the, respective free acids or bases. For Example Ephedrine base is very poorly water soluble molecules that characterized by low solubility and dissolution rates. So, it is modified in the form of the salt Ephedrine HCL that is ionized and offer higher water solubility and dissolution rate. Prodrug formation is the formation of synthetic derivatives of the drug (e.g. esters or amides) that liberate the active drug in-vivo. Prodrug may or may not have a pharmacological activity.
#preformulationstudies #drvikaspharmacy
4 سال پیش
در تاریخ 1399/06/17 منتشر شده
است.
1,339
بـار بازدید شده