ASSESSMENT OF PHARMACEUTICAL QUALITY AND RELEASE KINETICS OF METOPROLOL TARTRATE EXTENDED RELEASE TABLETS AVAILABLE IN TURKISH DRUG MARKET

Yıl 2020, Cilt: 9 Sayı: 2, 179 - 189, 30.07.2020

Ayşe Gençer , Emrah Akgeyik , Mustafa Sinan Kaynak , Mustafa Çelebier , Murat Sami Berkman , Selma Şahin

https://doi.org/10.18036/estubtdc.661691

Cited By: 1

Öz

Cardioselective β-adrenergic blocker metoprolol tartrate, is used in the treatment of different diseases such as cardiac arrhythmias, hypertension, heart failure, angina pectoris, migraine, and hyperthyroidism. Beside dosage forms of the parenteral ampoule and conventional tablets of different manufacturers, there are extended release tablets of metoprolol tartrate in the Turkish Drug Market. In this research work, comparative quality control studies of metoprolol tartrate extended release tablets (original and generic) produced by two different pharmaceutical companies in the Turkey were carried out and evaluated according to the related guidelines. Thickness and diameter, hardness, weight variation, friability, content uniformity and dissolution rate were examined as quality control parameters. A new validated HPLC method for the quantification of metoprolol tartrate has been developed. An ACE column (C18, 5 µm, 250x4.6 mm) and acetonitrile:phosphate buffer (30:70, v/v) mobile phase were used for the determination of metoprolol tartrate. The tablets showed extended release for 8 hours (70.74% release from drug A, 76.87% from the drug B). Both products have acceptable hardness, friability and weight variation values. Content of the active ingredient of the tablets was consistent with label claim (99.45% for drug A and 96.45% for drug B). The dissolution data were evaluated by model dependent and model independent methods using DDSolver program. The obtained results showed that release kinetics of both drugs were well fitted with the Korsmeyer-Peppas model.

Anahtar Kelimeler

Metoprolol tartrate, Modified release, Pharmaceutical quality control, Release kinetics, DDSolver

Teşekkür

Ayse Gencer was supported by TUBITAK 2211-A grant. This study is the part of Ayşe Gencer’s graduation project.

Türk İlaç Pazarında Mevcut Olan, Metoprlol Tartarat Uzatılmış Salımlı Tabletlerinin Salım Kinetiklerinin ve Farmasötik Kalitelerinin Değerlendirilmesi.

Öz

Kardiyoselektif β-adrenerjik bloker olan metoprolol tartrat, kardiyak aritmiler, hipertansiyon, kalp yetmezliği, anjina pektoris, migren ve hipertiroidizm gibi farklı hastalıkların tedavisinde kullanılmaktadır. Parenteral ampul formu ve farklı üreticilerin konvansiyonel tabletlerinin yanı sıra, Türkiye İlaç Pazarında uzatılmış salımlı metoprolol tartrat tabletleri bulunmaktadır. Bu çalışmada, Türkiye'de iki farklı ilaç şirketi tarafından üretilen metoprolol tartrat uzatılmış salımlı tabletlerin (orijinal ve jenerik) karşılaştırmalı kalite kontrol çalışmaları yapılmış ve ilgili kılavuzlara göre değerlendirilmiştir. Kalınlık ve çap, sertlik, ağırlık değişimi, kırılganlık, içerik tekdüzeliği ve çözünme hızı kalite kontrol parametreleri olarak incelenmiştir. Metoprolol tartaratın miktar tayini için yeni bir valide edilmiş HPLC yöntemi geliştirilmiştir. Metoprolol tartaratın miktar tayini için bir ACE kolonu (C18, 5 um, 250x4.6 mm) ve asetonitril: fosfat tamponu (30:70, v / v) mobil faz kullanılmıştır. Tabletler 8 saat boyunca uzatılmış salım göstermiştir (ilaç A'dan% 70.74 salım, ilaç B'den% 76.87). Her iki ürün de kabul edilebilir sertlik, ufalanabilirlik ve ağırlık değişim değerlerine sahiptir. Tabletlerin aktif bileşeninin içeriği, etiketlerinde belirtilen miktarlar ile tutarlıdır (ilaç A için% 99.45 ve ilaç B için% 96.45). Çözünme verileri DDSolver programı kullanılarak modele bağlı ve model bağımsız yöntemlerle değerlendirilmiştir. Elde edilen sonuçlar her iki ilacın salım kinetiğinin Korsmeyer-Peppas modeli ile iyi bir şekilde uyduğu gösterilmiştir.

Anahtar Kelimeler

Metoprlol Tartrate, DDSolver, Değiştirilmiş Salım, Farmasötik Kalite Kontrol, Salım Kinetiği

Kaynakça

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