Gliclazide tablet prescription and Preparation Process_1014

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Gliclazide tablet prescription and Preparation Process_1014

Gliclazide tablet prescription and Preparation Process

     Author: Xu Jun PENG Wang Lu Hua Zhao Defang

     Abstract Objective To study and selection of gliclazide Preparation of dispersible tablets and prescription. Methods

    filter through a series of experiments the collapse of auxiliary agents to determine the prescription and preparation process, compared dispersible tablets and ordinary tablets in the dissolution of the main drugs. The results determined in order to cross-linked carboxymethyl cellulose sodium, cross-

    linked polyvinylpyrrolidone as a disintegrant in tablet prescription; tablet dissolution rate as compared with ordinary tablets. Conclusion Gliclazide tablet prescription reasonable and technology is feasible, in line with the

    requirements of dispersible tablets.

     Key words gliclazide tablet prescription Preparation

     Abstract: ObjectiveTo optimize the preparation technology and the formula of Gliclazide dispersible tablets. MethodsThe formula and preparation process were optimized by a series of experiments. The dissolution rates of the principal agent in dispersible tablets and conventional tablets were determined and compared. ResultsSodium carboxymethyl starch and crospolyvinylpyrrolidone were optimized as the disintegrants

    of the dispersible tablet formula; the dissolution rates of the dispersible tablets were faster than those of the conventional tablets. ConclusionThe prepared gliclazide dispersible tablet is reasonable in formula, feasible in technology and it meets the quality standards.

     Key words: Gliclazide; Dispersible tablets; Formula; Preparation technologies

     Gliclazide is a second-generation oral sulfonylurea

    hypoglycemic agents, the role of strong, its mechanism is selectively acts on islet β-cells, promoting insulin

    secretion, and increase insulin release after the consumption of glucose, so that glycogen formation and the output is inhibited, for non-insulin-dependent diabetes mellitus (?)


     At present, gliclazide tablets listed species are mainly [3], capsules [4,5] and so on. Dispersible tablets in recent years developed an oral immediate-release dosage forms, which

    can rapidly collapse into a uniform viscous suspension. Because of its convenient to take, especially suitable for

    old, young, and patients with difficulty swallowing solids, coupled with the absorption of its fast and high bioavailability [6], the preparation process the same as ordinary tablets, which have become an increasing concern.

     This experiment, the author appearance, hardness, disintegration time, uniformity and dissolution rate dispersion as an indicator of the composition and preparation process prescriptions were screened studies to determine the tablet of the prescription and preparation process.

     1 Materials and equipment

     1.1 Materials gliclazide (Tianjin Zhongxin Pharmaceutical Group, New New pharmaceutical); lactose (Shanghai dairy products factory); powder silica gel (Zhejiang Huzhou foods & chemicals); cross-linked carboxymethyl cellulose sodium

    (Shanghai Chemical Yuan-hong Co., Ltd.); cross-linked

    polyvinylpyrrolidone (Shanghai Yuan Wang Chemical Co., Ltd.); Poloxamer (Shenyang Pharmaceutical University Pharmaceutical Factory); magnesium stearate (Shanghai Pharmaceutical

    Excipients plant).

     1.2 Instrument Dissolution Tester (Tianjin Guo-ming

    Medical Equipment Co., Ltd.); high-speed milling machine

    (Zhangjiagang City, New Electrical and Mechanical Co., Ltd.); Smart collapse Instrument (Fa Technology Co., Ltd. Tianjin,

    Tianjin University and Tianjin); TDP Single Punch Tablet Press (Shanghai United Pharmaceutical Equipment Co., Ltd.); tablet hardness tester (Shanghai Yellow doping Instruments Co.,

    Ltd.); electronic balance (Beijing Sartorius Instrument Systems Co., Ltd.).

     2 Methods and Results

     2.1 The prescription and Technology

     2.1.1 Prescription Gliclazide 40 g, lactose 80 g, powder silica gel 39 g, microcrystalline cellulose 95 g, cross-linked

    sodium carboxymethyl cellulose 20 g, cross-linked

    polyvinylpyrrolidone 20 g, parking losha Beam 5 g, magnesium stearate 1 g, 30% ethanol amount.

     2.1.2 process the original, auxiliary backup over 100 mesh sieve, according to the amount of said prescription to take the original, auxiliary materials, will gliclazide and

    lactose mixing, and placing high-speed milling machine crushed

    1 min, were added to silica gel powder, microcrystalline cellulose, crosslinked polyvinylpyrrolidone and crosslinked sodium carboxymethyl cellulose, so that mixing, poloxamer 30%

    ethanol solution of the system of soft material, 18 mesh sieve system of particles, the wet granules at 80 ? for drying 4 h,

    16 Whole mesh sieve, add lubricant magnesium stearate mixing, tabletting, that is too.

     2.2 Prescription and screening to determine

     2.2.1 formulation design according to "Chinese Pharmacopoeia" on the requirements of dispersible tablets: dispersible tablets must be within 3 min and can collapse on the 2nd through the sieve (24 mesh). In addition, the need to have better dissolution. According to these requirements, I designed using a prescription comparison of different combinations of prescription trial to compare tablets disintegrated within 3 min in the case, as well as the determination of dissolution results of screening to determine

    the best use of prescription combination. Reposted elsewhere in the paper for free download http://

     The author according to the requirements of dispersible tablets and this product characteristics, design of this product on-chip weight about 300 mg, the appropriate

    combination of accessories to take the same preparation technique to observe the preparation process and the collapse

    of the problems in a decentralized situation, formulation design Table 1. Table 1 Prescription Design (abbreviated)

     Trial during the following problems: 1 ~ 3 by adding a prescription wetting agent 90% ethanol, granulating effect is better, but fragile particles after drying, it should lower the ethanol concentration; prescription by adding 90% ethanol

    at 4 dry granulation, powder more particles less pressure films hat serious phenomenon tablet machine is unable to continue operating, thus, the formulation design is unreasonable to be eliminated.

     Four kinds of prescription tablets to suppress the

    determination of disintegration time and the tablet hardness testing. The results in Table 2. Table 2 Prescription test results (omitted)

     From Table 2 experimental results, the prescription of two better. Prescription a longer disintegration time, its

    hardness, one-sided finish is poor, needs to be improved.

     2.2.2 Prescription adjustment and to determine the appropriate adjustment of prescription, preparation ibid, prescription design in Table 3. Table 3 Adjusted prescription Design (abbreviated)

     Prescriptions for more than five groups, forming after the disintegration time, hardness, dissolution test and other tests, the results in Table 4. Table 4 prescriptions designed to test results (omitted)

     The results we can see from table 4: two sets of

    prescription prescription 8,9 suppression of its

    disintegration time and hardness of tablets, dissolution have better results. In particular, the combination of nine prescription only an increase in the solvent also reached a good dissolution, film-sided light, and the prescription of a minimum of components in components. Taking all factors, after selection and choose a prescription prescription prescription for the final nine.

     3 Discussion

     Gliclazide of raw materials and excipients lactose mixed

    high-speed milling, the powder fine grind (through 200 mesh sieve), conducive to gliclazide drug dissolution may be related to the formation of solid melts were related, need to be further validation.

     In this study, using the poloxamer dissolved in 30%

    ethanol solution (Lueke heated to accelerate dissolution), the soft material is conducive to the system will be fully poloxamer solubilizer uniformly distributed in soft materials, the increased glibenclamide Qi Special drug dissolution.

     Through the above analysis of experimental results can be seen, the prescription preparation of dispersible tablets of gliclazide rapid disintegration, dissolution high, in line with dispersible tablet formulation requirements, and its

    preparation process is simple, suitable for industrial mass production, has good prospects for development and application of .


     [1] Zeng Yan Cai, Sheng-based, Li Rulin, et al. The

    quality of life in patients with type ? diabetes research

    [J]. Chinese Journal of Public Health, 1997,16 (5): 267.

     [2] Yang WY, Gampe true, Jin Yan, et al. Gliclazide effects on diabetic microangiopathy [J]. Zhonghua Endocrinology Metabolism, 2001,17 (3): 114.

     [3] Sun Jianguo, Gao Ling, Wang Guang-Ji, et al.

    Gliclazide tablets in human pharmacokinetics and relative bioavailability studies [J]. Journal of China Pharmaceutical University, 1998,29 (3): 217.

     [4] LI Cen, Zhang Bin, Zheng, et al. Gliclazide capsules

    human pharmacokinetics and relative bioavailability studies [J]. Chongqing Medical University, 2003,28 (3): 307.

     [5] Theresa Fu Jun, Zhong Liping. Gliclazide capsules bioequivalence study [J]. Jiangxi Medical College Journal, 2001,41 (3): 3.

     [6] Mr Richard Pearson-ming. Dispersible tablet

    prescription, technological characteristics and progress of the [J]. Drug Evaluation, 2005,2 (3): 230. Reposted elsewhere in the paper for free download http://

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