Formulation and Evaluation of Immediate Release Pregabalin Tablets

الموضوعات

طب

الملخص

Pregabalin is an anticonvulsant agent used for the peripheral and central neuropathic paintreatment, marketed as Capsule and Solution dosage forms. The purpose of this study is todevelop an immediate release Pregabalin Tablet, as a new dosage form in the Palestinianmarket that is bioequivalent to the FDA approved Reference Pregabalin Capsules (Lyrica).Pregabalin drug substance and the finished product during the time of development werenot described in either the British or US pharmacopoeia.The chemical and physical evaluation of bulk drug substance (Pregabalin) wasaccomplished following the manufacturer`s analytical method and specification. A newreversed-phase, isocratic LC method was developed and validated according to USPvalidation parameters, for the qualitative and quantitative determination of Pregabalin inpharmaceutical dosage forms using HPLC (LaChrome Elite) equipped with photodiodearray UV detector. Mobile Phase is a mixture of Phosphate Buffer pH 6.9, and acetonitrile(94:6).Chromatographic System is Column: C-18 ODS 5 to 10µm in diameter (25cm X 4.6 mmid), detector: UV set at wavelength 210 nm, Flowrate: 1.5 ml / min and Injection Volume:20 μL.Formula development was accomplished through a series of steps:Selection of excipients through compatibility studies, selection of manufacturing processand in-vitro comparison studies versus the reference product.Excipients compatibilities were studied by preparing a binary mixture of Pregabalin andexcipient (1:1) then sealed in neutral glass vials and incubated at 40±2 °C/75 ±5% RH for30 days. The mixtures were tested by means of FTIR for any possible interactions. Thefollowing excipients (Microcrystalline Cellulose, Pregelatinized Starch, Talc and MgStearate) were found to be compatible with Pregabalin.A series of pre formulation trials were composed and processed by direct compressionmethod. Selection of formula was based on:Powder characteristics: (such as compressibility ratio, flowability, bulk density and tappeddensity), which would allow for a simplified method of manufacture, friability, hardnessand disintegration of compressed tablets.The selected formulation was applied to prepare Pregabalin Tablets in two strengths, i.e.tablets containing 75mg/tablet and 300mg/tablet. They are prepared as dose weightproportional. The compressed tablets were film-coated with PVA based polymer by usingwater as solvent.The stability of film coated Pregabalin tablets were tested by incubating the finishedproducts in their final package (PVC-Alum) at different storage conditions i.e. 25 ± 2 °C /60 % ± 5% RH, 30 C ± 2 °C / 60% ± 5% RH and 40 C ± 2 °C / 75% ± 5% RH. Sampleswere tested biweekly for content of Pregabalin (assay), physical appearance, dissolutionrate, and degradation products.Pregabalin Tablets proved to be stable in all aspects for the period tested (1 month) at allstorage conditions.Biowavier study was performed between Pregabalin Tablets (75mg and 300mg) and theReference Pregabalin Capsules (Lyrica 75 and 300mg Capsules) using paddle methodrotated at 50 rpm in different dissolution media (0.06N Hydrochloric acid solution, Acetatebuffer pH 4.5 and phosphate buffer pH 6.8. It was found that either Reference or Testproducts release more than 85% of their Pregabalin content in 15 minutes. As PregabalinAPI, according to BCS is Class I drug and the dissolution profiles of Pregabalin Tablets issimilar to that of Reference Pregabalin Capsules (Lyrica) under the same test conditions,and all excipients used are not suspect of having any relevant impact on bioavailability it isstrongly believed that the developed Pregabalin Tablets are bioequivalent to the marketedLyrica Capsules.

روابط وملفات

التعريف والنوع

رقم الوثيقة

fbd4c7a5-ae5e-4cbe-b645-6b1b9525e9a7

رقم العقد

0

نوع الوسائط

Crawler

نوع المحتوى

الرسائل العلمية

صيغة المصدر

رسائل دكتوراة

نوع الملف

pdf text

أسماء الملفات

1696920_1.pdf

بيانات النشر

ترجمة العنوان

تطوير وتقييم شكل صيدلاني جديد بخاصية التحرر الفوري (أقراص بريغابالين)

ألقاب المؤلفين

[{"name_ar":"محمد سميح شفيق شناعة","title_ar":"اعداد","title_en":"Preparation"},{"name_ar":"نعمان مالكية","title_ar":"اشراف","title_en":"Supervision"}]

اللغة

English

المصدر والدورية

اسم المصدر

Formulation and Evaluation of Immediate Release Pregabalin Tablets

المحتوى والصفحات

عدد الصفحات

0

إشراف وإعداد

الإشراف

نعمان مالكية

الإعداد

محمد سميح شفيق شناعة

الاقتباسات الببليوغرافية