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In Vivo and in Vitro Studies of Formulation and Consistency Evaluation of Generic Drugs

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In the consistency evaluation of generic drugs, it is very important to take effective measures to accurately evaluate the in vivo and in vitro relevance of drugs. Appropriate in vivo and in vitro correlation models can accurately predict the action characteristics of the drug in vivo, thereby guiding and optimizing the formulation design, establishing more representative dissolution test rules, and rationally adjusting the preparation process, which has far-reaching significance for drug safety and preparation development.

The blood concentration and action time of the effective part are the basis for the efficacy of the drug. However, the internal process is complex and changeable and cannot be monitored in real time. Changes in intestinal volume, peristalsis, PH value, transit time, intestinal villi area and other factors, Will lead to changes and differences in dissolution. Relying solely on in vivo experiments to obtain data is cumbersome and requires high experimental requirements. Therefore, it is extremely important to simulate the in vivo environment and use in vitro experiments to accurately predict the in vivo behavior of drugs. The quality difference of generic drugs can directly affect the safety and effectiveness of drugs. In the consistency evaluation of generic drugs, the in vivo and in vitro correlation (IVIVC) model of generic drugs is built to evaluate generic drugs in order to develop the consistency of generic drug treatment and efficacy. Sex evaluation provides a reference for reference, which can reduce the risk of clinical drug inequity to a certain extent.

The development of in vitro and in vivo correlation models for formulations enables people to use in vitro data to predict in vivo formation. If a researcher compares the dissolution profile and bioequivalence of the imported reference preparation naproxen tablets and the domestic imitation naproxen tablets, and evaluates the quality consistency of the two [1], it is the prescription and technology of the domestic naproxen tablets. Optimize and make reasonable suggestions. Researchers used Gastro PlusTM software combined with in vitro dissolution data to establish a correlation model of naproxen tablets in vivo and in vitro to evaluate the bioequivalence of imported naproxen tablets and imitation naproxen tablets. The study found that the in vivo and in vitro correlation model established in this experiment can well reflect the dissolution in vivo. The quality of 8 domestic imitation naproxen tablets and imported reference preparations are quite different, and the formulation and process need to be optimized.

Although my country is a big country of generic drugs, compared with the original research drugs, domestic generic drugs have shortcomings in terms of technology development, production technology and key quality control technologies. The quality consistency evaluation of generic drugs clearly proposes to comprehensively improve the quality of generic drugs. Medicilon Biopharmaceuticals has successfully completed a number of quality consistency evaluation cases in terms of the quality consistency evaluation of generic drugs, and has rich experience in generic drug research and development. , Able to provide customers with professional consistency evaluation services.

The research on the in vivo and in vitro correlation of drugs is often used in the development of oral solid preparations. The purpose of establishing the correlation model is to predict the absorption of drugs in the human body through the results of in vitro release tests. If a researcher evaluated the in vivo and in vitro correlation of isosorbide mononitrate sustained-release tablets, the researchers used dry powder direct compression technology to prepare isosorbide mononitrate sustained-release tablets with hypromellose K200M as the sustained-release material[ 2]. The reference preparation (60 mg) was used as a control to compare the similarity of the in vitro release curves of the two. Results The calculated value of the similarity factor (f2) of the release curves of the two in water was 85, so it was judged that the in vitro release behaviors of the two were similar. The pharmacokinetic characteristics of the self-made preparation and the reference preparation in Beagle dogs and the correlation between in vitro release and in vivo absorption were further compared. The paired t test showed that there was no statistical difference between the pharmacokinetic parameters of the self-made and reference preparations (P>0.05); the AUC0→24 h, tmax and cmax of the self-made sustained-release tablets and the reference preparation were (5.74± 0.54) and (5.42±0.34) h•mg•L-1, (3.00±0.32) and (3.00±0.32)h, (1.11±0.13) and (1.14±0.09) mg/L. In addition, the in vitro release of the self-made preparations and the reference preparations have a very significant correlation with the in vivo absorption of Beagle dogs.

In short, in the evaluation of the consistency of generic drugs, a good model of the relationship between in vitro dissolution and in vivo absorption of the drug can be established, and the in vitro dissolution data can be used to predict the in vivo absorption process of the drug, thereby reducing the economic burden brought by the BE test and shortening the drug It can reduce the risk of bio-inequivalence of preparations.

[1] Evaluation of the similarity of the dissolution profile of naproxen tablets and the correlation between in vivo and in vitro [J].

[2] In vivo and in vitro correlation evaluation of isosorbide mononitrate sustained-release tablets[J].

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