Preparation of solid pharmaceutical forms of celecoxib with immediate-release and sustained-release by using wet granulation techniques and evaluation of their in vitro characteristics

doi:10.5246/jcps.2022.07.047

中国药学(英文版) ›› 2022, Vol. 31 ›› Issue (7): 536-544.DOI: 10.5246/jcps.2022.07.047

Preparation of solid pharmaceutical forms of celecoxib with immediate-release and sustained-release by using wet granulation techniques and evaluation of their in vitro characteristics

Ahmed Alkhodri, Svetlana Suslina^*()

Department of General Pharmaceutical and Biomedical Technology, Medical Institute, Peoples' Friendship University of Russia, Street Miklukho-Maklaya 6, Moscow 117198, Russia

收稿日期:2022-02-14 修回日期:2022-04-23 接受日期:2022-05-06 出版日期:2022-07-31 发布日期:2022-07-31
通讯作者: Svetlana Suslina
作者简介:
+ Tel.: +7-926-692-31-88, E-mail: ahmedalkhodri@g-mail.com

Preparation of solid pharmaceutical forms of celecoxib with immediate-release and sustained-release by using wet granulation techniques and evaluation of their in vitro characteristics

Ahmed Alkhodri, Svetlana Suslina^*()

Department of General Pharmaceutical and Biomedical Technology, Medical Institute, Peoples' Friendship University of Russia, Street Miklukho-Maklaya 6, Moscow 117198, Russia

Received:2022-02-14 Revised:2022-04-23 Accepted:2022-05-06 Online:2022-07-31 Published:2022-07-31
Contact: Svetlana Suslina

摘要/Abstract

摘要：

In the present study, we aimed to formulate matrix tablets of celecoxib with immediate-release (IR) and sustained-release (SR) and evaluate the influence of different types and concentrations of polymers on drug release characteristics in vitro. All formulations were prepared by using the wet granulation technique. One formulation (F5) with the traditional release was composed without release-control polymers. In contrast, four formulations (F1–F4) with prolonged action were designed by using different cellulosic polymers, such as hydroxypropyl methylcellulose polymers (HPMC-K100M and HPMC-Е6), hydroxypropyl cellulose with high viscosity grade (HPC_h), carboxymethyl cellulose (CMC), and ethylcellulose (EC-10 cps). All tablet formulations contained sodium lauryl sulfate (SLS), polyvinylpyrrolidone (PVP-k30), microcrystalline cellulose (MCC), and lactose monohydrate. The MCC and PVP-k30 were used in a fixed quantity in all formulations except for formulation F5, which contained 10% and 2.7% of them, respectively. The effects of polymer viscosity grade and its quantity on celecoxib release from two formulations containing the same polymer were studied. Drug release in vitro was evaluated in phosphate buffer (pH = 7.4). The amount of celecoxib released in phosphate medium was calculated by preparing a standard series. In vitro profile indicated that formulations F1 (HPMC-K100M) and F2 (HPMC-E6) extended the drug release for 18 h (82%) and 10 h (96.001%), respectively. Formulations F3 and F4 released 72.09% and 59.8% of their contents during 18 h, respectively, and thus their effects could last for more than a day. However, IR formulation (F5) released more than 90% of its content within 1–2 h. MS Excel was used to analyze the dissolution profile data for drug release kinetics, such as first-order, Zero-order, Higuchi, and Korsmeyer-Peppas models. The release mechanism of all formulations was Case II relaxation release. This study showed that cellulosic derivative polymers could successfully prolong IR of matrix tablet formulation.

关键词: Immediate release, Sustained release, Celecoxib, HPMC, Wet granulation, Dissolution profile

Abstract:

Key words: Immediate release, Sustained release, Celecoxib, HPMC, Wet granulation, Dissolution profile

Supporting:

Ahmed Alkhodri, Svetlana Suslina. Preparation of solid pharmaceutical forms of celecoxib with immediate-release and sustained-release by using wet granulation techniques and evaluation of their in vitro characteristics[J]. 中国药学(英文版), 2022, 31(7): 536-544.

图/表 7

Table 1. Compositions of celecoxib IR and SR tablet formulations.

Table 2. Technological characteristics of granule formulations after adding lubricant.

Table 3. Physicochemical of IR and SR tablet formulations.

Table 4. Standard series in alkaline medium (pH = 7.4).

Figure 1. Standard series of celecoxib in alkaline medium (pH 7.4).

Figure 2. In vitro drug release profile of IR and SR tablet formulations at pH = 7.4.

Table 5. Profile drug release kinetic formulations.

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Preparation of solid pharmaceutical forms of celecoxib with immediate-release and sustained-release by using wet granulation techniques and evaluation of their in vitro characteristics

Preparation of solid pharmaceutical forms of celecoxib with immediate-release and sustained-release by using wet granulation techniques and evaluation of their in vitro characteristics

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