Formulation and In-vitro Evaluation of Mucoadhesive Buccal Patches of Cyproheptadine Hydrochloride.

The goal of the present investigation was to design and evaluate mucoadhesive buccal patches of Cyproheptadine Hydrochloride (CPH) which is a sedating antihistamine with antimuscarinic, serotonin-antagonist, and calcium-channel blocking action. Buccal films were made with Hydroxy propylcellulose (HPC EF) and Hydroxy Propyl Methyl Cellulose (HPMC E15) as mucoadhesive polymers. Permeation of CPH was calculated ex vivo using porcine buccal membrane. The patches were evaluated for weight variation, thickness variation, surface pH, moisture absorption, in vitro residence time, mechanical properties, in vitro release, ex vivo permeation studies and drug content uniformity. The formulation F8 of HPMC E15 was found to give the better results and release of drug from the film followed Higuchi and Korsmeyer and Peppas models.

Development and evaluation of Meloxicam solid dispersion loaded buccal patches.

Meloxicam, a non-steroidal anti-inflammatory drug is widely used in the treatment of rheumatoid arthritis, ankylosing spondulytis and osteoarthritis. It is also indicated for the management of dental pain, Post-traumatic and post-operative pain, inflammation and swelling. Recently it is considered as a potential drug for prevention and treatment of colorectal polyps. One of the major problems with this drug is its low solubility in biological fluids, which results into poor bioavailability and GI-Side effects after oral administration. The present work was aimed at overcoming these limitations of the drug. The first problem i.e. Poor solubility of meloxicam was overcome by solid dispersion technique and the same was than published in a reputed online journal. The present study was the continuation of the published work, in this study buccal patches were prepared using varying percentage of carbopol 934p, chitosan (mucoadhesive polymers) and 50% W/W of propylene glycol (Plasticizer) by solvent casting technique, using 32 factorial design. Prepared blank buccal patches were evaluated for various physical and mechanical parameters, patches which comply with reported results were selected for meloxicam and its solid dispersion incorporation. Meloxicam solid dispersion incorporated buccal patches were prepared and evaluated for drug content, in-vitro diffusion, in-vivo release of meloxicam in rabbits and stability study. All solid dispersion loaded patches showed increased in-vitro drug release (i.e. between 95% to 99.95%) over an extended period of 8hrs as compared to plain drug loaded buccal patch. Whereas plain drug loaded buccal patch showed only 31.22% in-vitro drug release in 8hrs. Meloxicam solid dispersion loaded buccal patch (MSP1) containing meloxicam solid dispersion (meloxicam 150mg, PVP250mg, PEG6000 175mg and mixture of lactose and MCC(4:1)4gm) equivalent to 7.5mg of meloxicam, 1.5% of carbopol 934p, 2% of chitosan and 50% of polymer weight of propylene glycol in each 1cm2 of the patch showed highest in-vitro drug release i.e. 99.95% in 8hrs and it followed zero order release(r=0.9961, a=8.3124, b=5.0668). The r, a and b are correlation coefficient, slope and constant respectively for the best fit kinetic model. The in-vivo release of meloxicam from its solid dispersion loaded buccal patches was also studied using rabbit model. A good in-vitro in-vivo correlation was observed in MSP1 patch. All solid dispersion loaded buccal patches showed excellent stability under tested conditions. Finally it may be concluded that buccal patches were better for improvement of release of meloxicam and also to overcome the gastric side effects of drug.

Pharmacokinetics of tinidazole in saliva in healthy volunteers / 实用口腔医学杂志

Objective:To study the pharmacokinetic paramet er s of tinidazole in saliva. Methods:Tinidazole was separated on U ltrasphere ODS (C 18 column, 5 ?m,4.6 mm?25 cm)column with a mobile phas e of MeOH-2.33?10 -3 mol/L acetic acid 32∶68(v/v). The sample s were quantified with an ultraviolet detector operated at 310 nm. Resul ts:The saliva T max of the tinidazole tablets was (1.64?0.94) h,C max (69.23?11.39) ?g/ml,K e 0.059 6?0.013 2,T 1/2 (11.952?2.374) h,Auc (83.42?11.49) ?g?h/ml,Cl r 60.64? 8.56 and V r (2 704.45?601.42) ml respectively.Conclus ion:The method can be used for clinical monitoring of tinidazole in sali va.