Preparation and evaluation of 1-deoxynojirimycin sustained-release pellets vs conventional immediate-release tablets

This study aimed to develop a novel sustained release pellet of loxoprofen sodium (LXP) by coating a dissolution-rate controlling sub-layer containing hydroxypropyl methyl cellulose (HPMC) and citric acid, and a second diffusion-rate controlling layer containing aqueous dispersion of ethyl cellulose (ADEC) on the surface of a LXP conventional pellet, and to compare its performance in vivo with an immediate release tablet (Loxinon®). A three-level, three-factor Box-Behnken design and the response surface model (RSM) were used to investigate and optimize the effects of the citric acid content in the sub-layer, the sub-layer coating level, and the outer ADEC coating level on the in vitro release profiles of LXP sustained release pellets. The pharmacokinetic studies of the optimal sustained release pellets were performed in fasted beagle dogs using an immediate release tablet as a reference. The results illustrated that both the citric acid (CA) and ADEC as the dissolution- and diffusion-rate controlling materials significantly decreased the drug release rate. The optimal formulation showed a pH-independent drug release in media at pH above 4.5 and a slightly slow release in acid medium. The pharmacokinetic studies revealed that a more stable and prolonged plasma drug concentration profile of the optimal pellets was achieved, with a relative bioavaibility of 87.16% compared with the conventional tablets. This article provided a novel concept of two-step control of the release rate of LXP, which showed a sustained release both in vitro and in vivo.

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Bilayer tablets with sustained-release metformin and immediate-release sitagliptin: preparation and in vitro/in vivo evaluation

Journal of Pharmaceutical Investigation ◽

10.1007/s40005-021-00533-z ◽

2021 ◽

Author(s):

Ngoc Nha Thao Nguyen ◽

Duy Toan Pham ◽

Duc Tuan Nguyen ◽

Thi Thu Loan Trinh

Keyword(s):

Sustained Release ◽

Immediate Release ◽

In Vivo Evaluation ◽

Bilayer Tablets

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Preparation and evaluation of sustained-release azithromycin tablets in vitro and in vivo

Asian Journal of Pharmaceutical Sciences ◽

10.1016/j.ajps.2014.03.003 ◽

2014 ◽

Vol 9 (3) ◽

pp. 155-161 ◽

Cited By ~ 4

Author(s):

Le Sun ◽

Weixiang Zhang ◽

Xiaohong Liu ◽

Jin Sun

Keyword(s):

Sustained Release ◽

Preparation And Evaluation

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Development of a Scalable Process of Film-Coated bi-Layer Tablet Containing Sustained-Release Metoprolol Succinate and Immediate-Release Amlodipine Besylate

Pharmaceutics ◽

10.3390/pharmaceutics13111797 ◽

2021 ◽

Vol 13 (11) ◽

pp. 1797

Author(s):

Nguyen Thi Linh Tuyen ◽

Le Quan Nghiem ◽

Nguyen Duc Tuan ◽

Phuoc Huu Le

Keyword(s):

Sustained Release ◽

Manufacturing Process ◽

High Speed ◽

Immediate Release ◽

New Drugs ◽

Batch Size ◽

Average Weight ◽

Amlodipine Besylate ◽

Metoprolol Succinate ◽

Dry Mixing

The development of new drugs that combine active ingredients for the treatment hypertension is critically essential owing to its offering advantages for both patients and manufacturers. In this study, for the first time, detailed development of a scalable process of film-coated bi-layer tablets containing sustained-release metoprolol succinate and immediate-release amlodipine besylate in a batch size of 10,000 tablets is reported. The processing parameters of the manufacturing process during dry mixing-, drying-, dry mixing- completion stages were systematically investigated, and the evaluation of the film-coated bi-layer tablet properties was well established. The optimal preparation conditions for metoprolol succinate layer were 6 min- dry mixing with a high-speed mixer (120 rpm and 1400 rpm), 30-min drying with a fluid bed dryer, and 5-min- mixing completion at 25 rpm. For the preparation of amlodipine besylate layer, the optimal dry-mixing time using a cube mixer (25 rpm) was found to be 5 min. The average weight of metoprolol succinate layers and bi-layer tablets were controlled at 240–260 mg and 384–416 mg, respectively. Shewhart R chart and X¯ charts of all three sampling lots were satisfactory, confirming that the present scalable process was stable and successful. This study confirms that the manufacturing process is reproducible, robust; and it yields a consistent product that meets specifications.

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PREPARATION AND EVALUATION OF SUSTAINED-RELEASE DICLOFENAC SODIUM TABLETS

Zagazig Journal of Pharmaceutical Sciences ◽

10.21608/zjps.2008.162612 ◽

2008 ◽

Vol 17 (2) ◽

pp. 1-5

Author(s):

Hussein Sayed ◽

Mamdouh Ghorab ◽

Tamer Hamed

Keyword(s):

Sustained Release ◽

Diclofenac Sodium ◽

Preparation And Evaluation

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Formulation, Development and Evaluation of Bilayer Floating Tablet of Gemfibrozil

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v9i4-s.3401 ◽

2019 ◽

Vol 9 (4) ◽

pp. 574-578

Author(s):

Mohammad Faizan Mohammad Gufran ◽

Sailesh Kumar Ghatuary ◽

Reena Shende ◽

Prabhat Kumar Jain ◽

Geeta Parkhe

Keyword(s):

Drug Release ◽

Sustained Release ◽

Hydroxypropyl Methylcellulose ◽

Immediate Release ◽

In Vitro Dissolution ◽

Log P ◽

Physical Parameters ◽

Direct Compression ◽

Formulation Development ◽

Compression Technique

Formulation development is an important part of drug design and development. Bioavailability and bioequivalence are totally dependent on formulation development. Now-a-days formulation development is done by following QbD (Quality by Design).The aim of present study is to formulate Gemfibrozil (Gem) sustained release (SR) and immediate release (IR) bilayer tablet by different concentration of Hydroxypropyl methylcellulose (HPMC) and HPMC K 100 M to control the release pattern. The sustained release layer of Gem was prepared by using different grades of HPMC like, HPMC K-15, HPMC K-4 along with other excipients by direct compression technique. The immediate release layer of Gem was prepared by Cross carmellose sodium, Crospovidone and Sodium starch glycolate by direct compression technique. The powders were evaluated for their flow properties and the finished tablets were evaluated for their physical parameters. The both immediate release and sustained release layers of Gem were characterized by FT-IR and in vitro dissolution studies. The drug release study of Gem was evaluated using USP-II paddle type dissolution apparatus. The release rate of Gem in immediate release layer was studied for 15 min in 0.1 N HCL media and that of Gem in sustained release layer was studied for 12 h in 0.1 N HCL. From the nine batches F6 batch showed good release behaviour 99.85% of drug is released over 12 hours. Gem belongs to BCS Class II (log P 3.6) with poor solubility and high permeability resulting in limited and variable bioavailability. Total four trial batches of each drug have been manufactured to optimize and develop a robust and stable formulation, the stability studies of the products also comply with ICH guideline. Keywords: Bilayer floating tablets, Gemfibrozil, Biphasic drug release, HPMC K 15.

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