In vitro drug release profiles

One challenge that remains in biopharmaceutics research is that of correlating in vitro drug-release profiles with the in vivo pharmacokinetic data. TVIVC has been defined by the... 

Figure 2 Simulated in vitro drug-release profiles (panels a and b) and resultant plasma concentration—time profiles for a drug with a 1—hr half-life (panel c) and a 6—hr half-life (panel d).

Table 1 Comparison of Predicted Pharmacokinetic Parameters for Two Different Drugs with Identical In Vitro Drug Release Profiles, But Different Drug Disposition Characteristics (ty2 = 1 or 6 hr)...

Table 2 Fitted Weibull Parameters for the Three In Vitro Drug-Release Profiles Shown in Figure 3...

In order to obtain an in vitro-in vivo relationship two sets of data are needed. The first set is the in vivo data, usually entire blood/plasma concentration profiles or a pharmacokinetic metric derived from plasma concentration profile (e.g., cmax, tmax, AUC, % absorbed). The second data set is the in vitro data (e.g., drug release using an appropriate dissolution test). A mathematical model describing the relationship between these data sets is then developed. Fairly obvious, the in vivo data are fixed. However, the in vitro drug-release profile is often adjusted by changing the dissolution testing conditions to determine which match the computed in vivo-release profiles the best, i.e., results in the highest correlation coefficient. 

For an extended-release dosage form, at least three test time points are chosen to characterize the in vitro drug-release profile for the routine batch-to-batch quality control for approved products. Additional sampling times may be required for formulation development studies, biopharmaceutical evaluations, and drug approval purposes. An early time... 

Table 2—In vitro drug release profile of microcapsules and micromatrices...

Li Wan Po, Wong, L., and Gilligan, C. Characterization of commercially available theophylline sustained- or controlled-release systems In vitro drug release profiles. Int. J. Pharm. 66 111-130, 1990. 

The in vitro drug release profile (USP drug dissolution method, paddle type) of 5-amino salicylic acid from various grades of CMS-g-PAM matrix, in neutral dissolution medium is shown in Figure 5.12 [47]. 

In vitro Drug Release Profile of Composite Hydrogel... 

Figure 8.14 In vitro drug release profiles of electrospun RMp (1%), RMp (5%), RMp (10%), and RMp (20%) fibrous grafts. Each data point represents mean SD of three samples. Adapted from Ref. [101].

Schiavon G (1901) Constitution of citric acid derivatives. Gaz Chim Ital 31 536-544 Pramanick D, Ray TT (1990) In vitro drug release profile of bioerodable citric acid-glycerol copolymer. JAppl Polym Sci 40 1511-1517... 

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