口腔速崩片的研制与评价

目的：研制及评价口腔速崩片。方法：选用微晶纤维素（MCC）和低取代羟丙基纤维素（L-HPC）作为崩解剂，通过湿法制粒压片工艺制备口腔速崩片。并考虑速崩片的性质，如硬度、润湿时间、吸水率、崩解时间来初步阐明其润湿及崩解的特性。此外，选用萘生为模型药物，考察其含量对崩解时间的影响及润滑剂硬脂酸镁的含量对崩解时间的影响，同时也测定了速崩片在口腔内的崩解时间。结果：当MCC/L-HPC的比例从3：7至9：1时，其体外崩解时间均在10s以内，体内崩解时间均在30s以内。随着萘普生和硬脂酸镁的含量增大，其崩解时间相应延长，但也都在30s以内。结论：当MCC/L-HPC的比例为9：1时，崩解时间最短，润湿时间最短。疏水性药物萘普生和疏水性润滑剂硬脂酸镁的含量分别增大至50%和5%，其崩解时间分别在13s和28s以内，仍具有速崩片（在30s内崩解）的特性。     

罗通定口腔崩解片的研制

目的研制在唾液中迅速崩解,含高剂量活性成分37.5%(W/W)的片剂。方法分别通过直接压片、湿法制粒和模制法制备含罗通定、崩解剂和其它赋形剂的口腔崩解片。应用单因素实验选择使用不同的崩解剂和赋形剂以确保最佳崩解。同时按照常规药典方法和润湿时间测定方法测定崩解时间。结果通过直接压片得到的硬度40kg·mm-2的片剂(80mg)在健康志愿者口腔中于15秒内快速崩解;湿法制粒所得片剂也具足够硬度,崩解时间稍长但可接受(口腔中25秒内);模制法所得片剂在口腔中40秒内崩解,但硬度低(2kg·mm-2)。三种不同制备方法所得片剂的崩解时间与各自的润湿时间相似。体外崩解时间和润湿时间均和体内崩解时间相似,后者和口腔内崩解时间显示更好的相关性。结论可以通过上述三种方法和片剂制备中的常用赋形剂制备口腔崩解片。体外崩解时间和润湿时间是评价口腔崩解片体外崩解时间的必要指标。     

苯甲酸利扎曲普坦口腔速崩片的制备

目的 制备苯甲酸利扎曲普坦口腔速崩片.方法 选用微晶纤维素(MCC)和低取代羟丙基纤维素(LHPC)作为崩解剂,通过粉末直接压片工艺制备口腔速崩片.考察速崩片的性质.结果 当MCC/LHPC的比例为9:1时,其体外崩解时间在20 s以内,体内崩解时间在30 s以内.结论 所制片剂口感良好,优化的工艺可以工业化生产.     

双氯芬酸钠-β-环糊精包合物口腔速崩片的处方及制备工艺研究

目的:制备双氯芬酸钠-β-环糊精包合物的口腔速崩片,确立其处方及制备工艺。方法:以崩解时间为指标,分别对5种崩解剂、2种润滑剂、3种片剂硬度范围和2种压片方法进行筛选得出最佳处方及制备方法,并进行验证。结果:以交联聚维酮为崩解剂,微粉硅胶和滑石粉为润滑剂,硬度为20～30N,采用湿法制粒压片所制得的口腔速崩片,在60s内可完全崩解。结论:双氯芬酸钠经β-环糊精包合后再制成口腔速崩片,制备方法简单,质量合格,且适合工业化生产。     

枸橼酸西地那非速崩舌下片的制备及质量评价

目的制备枸橼酸西地那非速崩舌下片,并评价其质量。方法采用升华剂为致孔剂,采用外加致孔刺法压制舌下片,并以真空干燥除去升华剂获得快速崩解的舌下片,对速崩舌下片以崩解时间、润湿时间、吸水比、体外溶出度等指标评价处方。结果以升华剂为致孔剂制备的枸橼酸西地那非速崩舌下片,均在30 s内崩解,且各样品均在6 min内即可达到全部溶出,其他各检测指标均符合速崩舌下片的指标。结论采用升华剂为致孔剂制备枸橼酸西地那非速崩舌下片工艺可行,制备的速崩舌下片崩解时间短,溶出速率快。     

卡马西平口腔速崩片处方筛选和制备工艺研究

目的为了方便老人、儿童和吞咽困难的患者服药,提高卡马西平的生物利用度,优化处方制备卡马西平口腔速崩片（CBZ—ODT）。方法筛选恰当的崩解时间测定方法,以崩解时间和口感为主要评价指标,通过实验选择最佳制备工艺及配方,并通过单因素试验选取对崩解时间影响大的成分的含量为变量进行三因素四水平的L16（43）正交试验设计,确定最优处方。结果采用全粉末直接压片法,用乳糖作为填充剂,硬脂酸镁做为润滑剂,交联羧甲基纤维素钠（CCNa）作为崩解剂,以崩解时间、硬度和口感为评价指标筛选出最佳处方组合压制三批卡马西平口腔速崩片,片面光洁圆整,无斑点,经测试,崩解时间在（21±3）s。结论采用全粉末直接压片法压片,工艺简单且能满足要求。采用崩解仪改良法测量崩解时间更为接近于人体口腔内的测定结果,所制备的卡马西平口腔崩解片崩解时间短,硬度适中,口感好,具备临床应用价值。     

咪达那新口腔崩解片的制备及处方优化

目的 研究咪达那新口腔崩解片的处方与制备工艺.方法采用粉末直压 升华干燥制备法,以崩解剂的种类与用量、助崩解剂用量、升华剂用量等为考察因素,以物料休止角、片剂润湿时间、崩解时间等为考察指标,通过单因素试验进行处方筛选,确定最优处方.在最优处方的基础上考察片剂硬度对口崩片崩解时间的影响,从而制得孔隙率较高脆碎度较好的咪达那新口腔崩解片.结果处方以甘露醇为填充剂,微晶纤维素40%、交联聚维酮5%为崩解剂,另加入10%的碳酸氢铵为升华剂,压制硬度4.0～6.0 kg的咪达那新口腔崩解片,于60 ℃真空恒温干燥箱干燥90 min.结论该优选的制备工艺简单可行.     

灯盏花素口腔速崩片的研制

目的　以灯盏花素为模型药物制备口腔速崩片。方法　以沉降容积比及崩解时间为指标,单因素法筛选片剂的处方组成及工艺,并优化制备工艺。结果　灯盏花素口腔速崩片以甘露醇、明胶、阿司帕坦与薄荷香精为辅料,经冷冻干燥法制备,口感良好,崩解时间为4 s,体外溶出度4 min达98.72%。结论　灯盏花素口腔速崩片可迅速崩解于口腔内,制备工艺可行。     

压片法制备口腔速崩片的因素考察

目的:研制口腔速崩片,为国内口崩片的设计和制备提供参考及思路。方法:以崩解时限为指标考察影响速崩片的因素。结果:崩解剂、润滑剂的种类、用量、压片的压力等对速崩片的崩解时限有影响。结论:采用国内现有设备,运用适宜的赋形剂及工艺可制出合格的口腔速崩片。     

阿司匹林口崩片的制备

目的用正交实验法优选阿司匹林口腔崩解片的最佳处方和制备工艺。方法以崩解时间为主要评价指标,选择最佳制备工艺及配方,通过单因素试验选取变量,进行正交试验设计,确定最优处方,通过粉末直接压片制备样品。结果以崩解时间为评价指标筛选出了最佳处方组合,制得3批阿司匹林口腔速崩片,片面光洁圆整、无斑点,崩解时间为21±3 s。结论制备的阿司匹林口腔崩解片崩解时间短、硬度适中、口感好,具备临床应用价值。     

氯氮平口腔崩解片的研制

目的以氯氮平为模型药物制备口腔崩解片。方法以沉降容积比及崩解时间为指标,单因素法筛选片剂的处方组成及工艺,并优化制备工艺。结果氯氮平口腔崩解片以甘露醇、明胶、阿司帕坦与薄荷香精为辅料,经冷冻干燥法制备,口感良好,崩解时间为5 s,体外溶出度3 m in达94%。结论氯氮平口腔崩解片可迅速崩解于口腔内,制备工艺可行。     

布洛芬口腔崩解片的研制

目的制备布洛芬口腔崩解片。方法采用正交设计考察了十二烷基硫酸钠、微晶纤维素、羧甲基淀粉钠及枸橼酸对布洛芬口腔崩解片崩解时间的影响,筛选并优化了处方和工艺。结果及结论试验结果表明所制备的布洛芬口腔崩解片崩解时间为35s,口感良好,溶出速度明显优于布洛芬普通片。     

Preparation and evaluation of taste-masked dextromethorphan oral disintegrating tablet

This study was aimed at preparing and evaluating oral disintegrating tablets (ODTs) using a strongly cationic resin, Amberlite(?) IRP-69, to mask the bitter taste of a delivered drug, i..e. dextromethorphan hydrobromide. The drug was loaded into the resin (referred to as resinate) or physically mixed with the resin (referred to as physical mixture), and was then incorporated into ODTs by direct compression. A variety of formulae was developed to acquire the optimal formulations of taste-masked ODTs that had acceptable hardness and mouth feel (grittiness). The optimized ODTs were further evaluated for thickness, diameter, weight, friability, disintegration time, wetting time, wetting rate, drug content, drug release and degree of bitter taste, respectively. The thickness, diameter, weight and friability of the tablet with resinate were slightly higher than those with physical mixture. The tablet with resinate had a longer disintegration time, corresponding with its slower wetting time and rate. Both tablets with resinate and physical mixture provided a sustained pattern of drug release. However, only tablets with resinate successfully masked the bitter taste of the drug. In conclusion, the combination of drug and ion exchange resin as resinate could increase the palatability and acceptability of ODTs containing bitter drugs.     

盐酸昂丹司琼口腔崩解片的制备以及崩解时间影响因素的考察

目的考察影响盐酸昂丹司琼口腔崩解片崩解时间的因素。方法采用湿法制粒压片法制备盐酸昂丹司琼的口腔崩解片,浆法测定崩解时间,考察了口腔崩解片的硬度、交联聚维酮（PVPP）和微晶纤维素（MCC）的用量对崩解时间的影响。结果片剂硬度与崩解时间成正比,交联聚维酮和微晶纤维素的用量与崩解时间成反比。调节片剂硬度为4．6kg／mm、交联聚维酮的用量为15～20mg／片和微晶纤维素的用量为50-70mg／片,可获得较理想的崩解时间和良好的片剂性质。结论湿法制粒压片法简便易行;制备的盐酸昂丹司琼口腔崩解片符合质量要求。     

多潘立酮口腔崩解片的处方优化及体外评价

目的:优化多潘立酮口腔崩解片的处方并评价其质量。方法:以直接粉末压片法制备多潘立酮口腔崩解片,采用HPLC法测定其含量,以崩解时限和体外溶出度为指标优化处方。结果:以6%的交联聚维酮作为崩解剂,制备的多潘立酮口腔崩解片外观圆整光洁,硬度为(3.3±0.8)kg/cm2,脆碎度<1%,体外崩解时限和口腔内崩解时限分别为(9.00±0.56),(17.00±2.00)s,15min的累积溶出度为(99.22±0.38)%。结论:按最优处方制备的多潘立酮口腔崩解片符合《中华人民共和国药典》2010年版的要求,质控方法准确可靠。     

阿托伐他汀钙口腔崩解片的制备工艺研究及含量控制

目的制备阿托伐他汀钙口腔崩解片,并评价其质量。方法采用正交设计方法优选出制备的最佳条件,以微晶纤维素、交联聚维酮为崩解剂,制备阿托伐他汀钙口腔崩解片。利用高效液相色谱法测定崩解片中阿托伐他汀钙的含量。结果阿托伐他汀钙口腔崩解片崩解时间在30 s内,含量稳定。结论该制备工艺简单易行,可用于阿托伐他汀钙口腔崩解片的制备及质量控制。     

Formulation and <Emphasis Type="Italic">in vivo</Emphasis> evaluation of ondansetron orally disintegrating tablets using different superdisintegrants

The aim of this study was to formulate cost effective taste-masked orally disintegrating tablets of ondansetron, a bitter drug using different superdisintegrants by a wet granulation technique. Microcrystalline cellulose (Avicel) as a diluent and disintegrant in addition to aspartame as a sweetener were used in all formulations. The prepared tablets were evaluated for weight variation, thickness, hardness, friability, drug content, water content, in vitro disintegration time and in vitro drug release. The tablets’ hardness was maintained in the range of 2–3 kg and friability was <1% for all batches. All tablet formulations disintegrated rapidly in vitro within 5.83 to 33.0 sec. The optimized formulation containing 15% Polyplasdone XL-10 released more than 90% of drug within 5 min and the release was comparable to that of a commercial product. In human volunteers, optimized formulation was found to have a pleasant taste and mouth feel and they disintegrated in the oral cavity within 12 sec. The stability results were also satisfactory. A pharmacokinetic study with the optimized formulation was performed in comparison with a reference (Zofer MD 8®) and they were found to be bioequivalent. In conclusion, a cost effective ondansetron orally disintegrating tablet was successfully prepared with acceptable hardness, desirable taste and rapid disintegration in the oral cavity.     

聚维酮碘口腔速崩片的研制

以片剂的崩解时间为主要指标,用单因素法优化聚维酮碘口腔速崩片的处方及工艺.按优化工艺制得的片剂口感良好,约在23s崩解.