Bala Rajni, Khanna Sushil, Pawar Pravin K
Department of Pharmaceutics, Chitkara College of Pharmacy, Chitkara University, Rajpura, Patiala, Punjab, India.
J Adv Pharm Technol Res. 2013 Jul;4(3):151-9. doi: 10.4103/2231-4040.116785.
Clobazam is a newer 1,5-benzodiazepine used for the treatment of epilepsy. It is better tolerated and less sedating than other benzodiazepines. Absorption of the drug can be impacted by oral fast dissolving dosage form; this may have implications for epilepsy in pediatrics and those having difficulty in swallowing tablets/capsules resulting in improved patient compliance. The purpose of the present investigation was to formulate and optimize clobazam oro-dissolving tablets by direct compression method using response surface methodology (RSM). Oro-dispersible tablets of clobazam were prepared by direct compression method using crospovidone (2-6%) as a superdisintegrant, microcrystalline cellulose (MCC) (20-40%) was used as diluents along with directly compressible mannitol to enhance mouth feel. A 3(2) full factorial design was applied to investigate the combined effect of two formulation variables: amount of crospovidone and MCC over the independent variables disintegration time, wetting time and percent drug release. Disintegration time showed by all formulations was found to be in the range of 24.3-193 s based on evaluation parameters the formulation containing 6% of crospovidone and 30% of MCC showed promising performance against all other formulations. The results demonstrated that the RSM could efficiently be applied for the formulation of clobazam oro-dispersible tablets; therefore, constitute an advance in the management of epileptic attacks.
氯巴占是一种用于治疗癫痫的新型1,5 - 苯二氮䓬类药物。与其他苯二氮䓬类药物相比，它耐受性更好，镇静作用更小。该药物的吸收可能会受到口腔速溶剂型的影响；这可能对儿科癫痫患者以及吞咽片剂/胶囊有困难的患者有影响，从而提高患者的依从性。本研究的目的是采用响应面法（RSM）通过直接压片法来制备和优化氯巴占口腔崩解片。使用交联聚维酮（2 - 6%）作为超级崩解剂，微晶纤维素（MCC）（20 - 40%）作为稀释剂，并与直接可压性甘露醇一起使用以增强口感，通过直接压片法制备氯巴占口腔崩解片。采用3(2)全因子设计来研究两个配方变量（交联聚维酮和MCC的用量）对崩解时间、润湿时间和药物释放百分比等自变量的综合影响。根据评估参数，所有配方的崩解时间在24.3 - 193秒范围内，含有6%交联聚维酮和30%MCC的配方相对于所有其他配方表现出良好的性能。结果表明，RSM可有效地应用于氯巴占口腔崩解片的配方设计；因此，在癫痫发作的管理方面取得了进展。
