Journal of Literature Pharmacy Sciences

Biyoyararlanım ve Biyoeşdeğerliği Etkileyen Farmasötik Faktörler: Etkin Maddeye Ait Fiziksel ve Kimyasal Özellikler, Geleneksel Derleme
Pharmaceutical Factors Affecting Bioavailability and Bioequivalency: Physical and Chemical Properties of the Active Substance, Traditional Review
Esra DEMİRTÜRKa , Tilbe ÇEVİKELLİa , Deniz ONANb
aÇukurova Üniversitesi Eczacılık Fakültesi, Farmasötik Teknoloji ABD, Adana, Türkiye
bÇukurova Üniversitesi Eczacılık Fakültesi, Farmasötik Biyoteknoloji ABD, Adana, Türkiye
J Lit Pharm Sci. 2024;13(1):35-45
doi: 10.5336/pharmsci.2023-99867
Article Language: TR
Full Text
ÖZET
Katı oral dozaj şekillerinde biyoyararlanım ve biyoeşdeğerliğin değerlendirilebilmesi için uygulamadan sonra ilacın sırasıyla dağılması, sulu ortamda çözünmesi ve sistemik dolaşıma geçmesi gerekmektedir. Bu aşamalarda etkin maddeye ait fizikokimyasal özellikler, dozaj şekli tasarımına ait özellikler ve uygulama bölgesindeki anatomik ve fizyolojik özellikler uygulanan ilacın biyoyararlanım ve biyoeşdeğerliğine doğrudan etki eder. Dozaj şeklinin tipi, dağılma (dezentegrasyon), çözünme (disolüsyon), farmasötik eksipiyanlar ve üretim değişkenleri dozaj şekli tasarımına ait özellikler olmakla birlikte; partikül büyüklüğü, suda çözünürlük, dağılma katsayısı, tuz yapısı, iyonlaşma derecesi, iyonizasyon sabiti (pKa), ön ilaç formu, solvat-hidrat, polimorfizm özellikleri ise etkin maddeye ait fizikokimyasal özellikler olup, ilaç biyoyararlanım ve biyoeşdeğerliği üstünde birinci derece öneme sahiptir. Bu çalışmada, biyoyararlanım ve biyoeşdeğerliğe etki eden etkin maddeye ait fizikokimyasal özellikler için güncel literatür taranarak değerlendirilmesi yapılmış ve etkin maddenin fizikokimyasal kısıtlarından kaynaklanan biyoyararlanım sorununun iyileştirilmesi üzerine güncel yaklaşımlar sınıflandırılarak değerlendirilmiştir. Etkin maddenin biyoyararlanım ile biyoeşdeğerliğe etki eden ve biyoyararlanımı kısıtlayan fizikokimyasal özelliklerinin iyileştirilmesinde güncel yaklaşımların son yıllarda hız kazanarak ilaç araştırma ve geliştirme çalışmalarında geniş yer kazandığı ve Amerikan Gıda ve İlaç İdaresi tarafından artan onay oranları ile klinik kullanımda yaygın olarak yer almaya başladığı belirlenmiştir. Bu amaçla, konunun güncel literatür çalışmaları ile örneklendirilerek değerlendirilmesi amaçlanmıştır.

Anahtar Kelimeler: Biyoyararlanım; biyoeşdeğerlik; oral dozaj şekli
ABSTRACT
In order to evaluate the bioavailability and bioequivalence in solid oral dosage forms, the drug must be dispersed, dissolved in the aqueous medium and enter the systemic circulation, respectively, after administration. At these stages, the physicochemical properties of the active ingredient, the properties of the dosage form design, and the anatomical and physiological characteristics of the application area directly affect the bioavailability and bioequivalence of the administered drug. Although the type of dosage form, disintegration, dissolution, pharmaceutical excipients and production variables are the features of dosage form design; particle size, water solubility, dispersion coefficient, salt structure, degree of ionization, ionization constant (pKa), prodrug form, solvate-hydrate, polymorphism properties are the physicochemical properties of the active substance and are of primary importance on drug bioavailability and bioequivalence. In this study, the physicochemical properties of the active substance that affect its bioavailability and bioequivalence were evaluated by evaluating the current literature, and current approaches to improving the bioavailability problem arising from the physicochemical limitations of the active substance were classified and evaluated. It has been determined that current approaches to improving the physicochemical properties of the active substance, which affect bioavailability and bioequivalence and restrict bioavailability, have increased in recent years and gained wide coverage in drug research and development studies, and have begun to be applied in clinical use with increasing approval rates by the American Food and Drug Administration. For this purpose, it is aimed to evaluate the subject by exemplifying it with current literature studies.

Keywords: Bioavailability; bioequivalence; oral dosage form
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5. PROPRIETARY RIGHTS

5.1. The information accessed through this "SITE" or provided by the users legally and all the elements (including but not limited to design, text, image, html code and other codes) of the "SITE" (all of them will be called as studies tied to "Turkiye Klinikleri"s copyrights) belongs to "Turkiye Klinikleri". Users do not have the right to resell, process, share, distribute, display or give someone permission to access or to use the "Turkiye Klinikleri" services, "Turkiye Klinikleri" information and the products under copyright protection by "Turkiye Klinikleri". Within hereby "Terms of Use" unless explicitly permitted by "Turkiye Klinikleri" nobody can reproduce, process, distribute or produce or prepare any study from those under "Turkiye Klinikleri" copyright protection.

5.2. Within hereby "Terms of Use", "Turkiye Klinikleri" reserves the rights for "Turkiye Klinikleri" services, "Turkiye Klinikleri" information, the products associated with "Turkiye Klinikleri" copyrights, "Turkiye Klinikleri" trademarks, "Turkiye Klinikleri" trade looks or its all rights for other entity and information it has through this website unless it is explicitly authorized by "Turkiye Klinikleri".

6. CHANGES IN THE TERMS OF USE

"Turkiye Klinikleri" in its sole discretion may change the hereby "Terms of Use" anytime announcing within the "SITE". The changed terms of the hereby "Terms of Use" will become valid when they are announced. Hereby "Terms of Use" cannot be changed by unilateral declarations of users.

7. FORCE MAJEURE

"Turkiye Klinikleri" is not responsible for executing late or never of this hereby "Terms of Use", privacy policy and "USER Contract" in any situation legally taken into account as force majeure. Being late or failure of performance or non-defaulting of this and similar cases like this will not be the case from the viewpoint of "Turkiye Klinikleri", and "Turkiye Klinikleri" will not have any damage liability for these situations. "Force majeure" term will be regarded as outside of the concerned party's reasonable control and any situation that "Turkiye Klinikleri" cannot prevent even though it shows due diligence. Also, force majeure situations include but not limited to natural disasters, rebellion, war, strike, communication problems, infrastructure and internet failure, power cut and bad weather conditions.

8. LAW AND AUTHORISATION TO FOLLOW

Turkish Law will be applied in practicing, interpreting the hereby "Terms of Use" and managing the emerging legal relationships within this "Terms of Use" in case of finding element of foreignness, except for the rules of Turkish conflict of laws. Ankara Courts and Enforcement Offices are entitled in any controversy happened or may happen due to hereby contract.

9. CLOSING AND AGREEMENT

Hereby "Terms of Use" come into force when announced in the "SITE" by "Turkiye Klinikleri". The users are regarded to agree to hereby contract terms by using the "SITE". "Turkiye Klinikleri" may change the contract terms and the changes will be come into force by specifying the version number and the date of change on time it is published in the "SITE".

 

30.03.2014

Privacy Policy

We recommend you to read the terms of use below before you visit our website. In case you agree these terms, following our rules will be to your favor. Please read our Terms of Use thoroughly.

www.turkiyeklinikleri.com website belongs to Ortadoğu Advertisement Presentation Publishing Tourism Education Architecture Industry and Trade Inc. and is designed in order to inform physicians in the field of health

www.turkiyeklinikleri.com cannot reach to user’s identity, address, service providers or other information. The users may send this information to the website through forms if they would like to. However, www.turkiyeklinikleri.com may collect your hardware and software information. The information consists of your IP address, browser type, operating system, domain name, access time, and related websites. www.turkiyeklinikleri.com cannot sell the provided user information (your name, e-mail address, home and work address, phone number) to the third parties, publish it publicly, or keep it in the website. Gathered information has a directing feature to be a source for the website’s visitor profile, reporting and promotion of the services.

www.turkiyeklinikleri.com uses the taken information:

-To enhance, improve and maintain the quality of the website

-To generate visitor’s profile and statistical data

-To determine the tendency of the visitors on using our website

-To send print publications/correspondences

-To send press releases or notifications through e-mail

-To generate a list for an event or competition

By using www.turkiyeklinikleri.com you are considered to agree that;

-Ortadoğu Advertisement Presentation Publishing Tourism Education Architecture Industry and Trade Inc. cannot be hold responsible for any user’s illegal and immoral behavior,

-Terms of use may change from time to time,

-It is not responsible for other websites’ contents it cannot control or the harms they may cause although it uses the connection they provided.

Ortadoğu Advertisement Presentation Publishing Tourism Education Architecture Industry and Trade Inc. may block the website to users in the following events:

-Information with wrong, incomplete, deceiving or immoral expressions is recorded to the website,

-Proclamation, advertisement, announcement, libelous expressions are used against natural person or legal identity,

-During various attacks to the website,

-Disruption of the website because of a virus.

Written, visual and audible materials of the website, including the code and the software are under protection by legal legislation.

Without the written consent of Ortadoğu Advertisement Presentation Publishing Tourism Education Architecture Industry and Trade Inc. the information on the website cannot be downloaded, changed, reproduced, copied, republished, posted or distributed.

All rights of the software and the design of the website belong to Ortadoğu Advertisement Presentation Publishing Tourism Education Architecture Industry and Trade Inc.

Ortadoğu Advertisement Presentation Publishing Tourism Education Architecture Industry and Trade Inc. will be pleased to hear your comments about our terms of use. Please share the subjects you think may enrich our website or if there is any problem regarding our website.

info@turkiyeklinikleri.com