methylcellulose and Hypesthesia

A buccal patch for systemic administration of carvedilol in the oral cavity has been developed using two different mucoadhesive polymers. The formulations were tested for in vitro drug permeation studies, buccal absorption test, in vitro release studies, moisture absorption studies and in vitro bioadhesion studies. The physicochemical interactions between carvedilol and polymers were investigated by Fourier transform infrared (FTIR) Spectroscopy. According to FTIR the drug did not show any evidence of an interaction with the polymers used and was present in an unchanged state. XRD studies reveal that the drug is in crystalline state in the polymer matrix. The results indicate that suitable bioadhesive buccal patches with desired permeability could be prepared. Bioavailability studies in healthy pigs reveal that carvedilol has got good buccal absorption. The bioavailability of carvedilol from buccal patches has increased 2.29 folds when compared to that of oral solution. The formulation AC5 (HPMC E 15) shows 84.85 + 0.089% release and 38.69 + 6.61% permeated through porcine buccal membrane in 4 hr. The basic pharmacokinetic parameters like the C(max), T(max) and AUC(total) were calculated and showed statistically significant difference (P<0.05) when given by buccal route compared to that of oral solution.

Topics: Administration, Buccal; Adrenergic beta-Antagonists; Adult; Animals; Area Under Curve; Biological Availability; Biomechanical Phenomena; Carbazoles; Carvedilol; Cellulose; Drug Carriers; Drug Delivery Systems; Drug Evaluation, Preclinical; Humans; Hypesthesia; Hypromellose Derivatives; Male; Methylcellulose; Mouth Mucosa; Propanolamines; Saliva; Solubility; Spectroscopy, Fourier Transform Infrared; Swine; Tensile Strength

Lagophthalmos and corneal hypaesthesia are amongst the most frequently encountered lesions in leprosy and they can easily give rise to blindness. Many measures (such as eye drops, protective conoid shields, muscle exercises, surgical treatment etc.) have been used to protect the eyes under such circumstances and this paper examines the protective role of methyl cellulose and conoid shields in 41 patients. All of them had lagophthalmos (5 mm or more) and corneal hypaesthesia. They were divided into three groups. Group one had 15 leprosy control patients (27 eyes) who did not use methyl cellulose or eye shields. Group two had 16 leprosy patients (28 eyes) and they used methyl cellulose and eye shields when they felt discomfort in their eyes. Group three had 10 leprosy patients (17 eyes) and they used methyl cellulose and eye shields regularly. Statistically significant improvement was seen in group three. Further studies on larger groups of patients including the effects of different concentrations of methyl cellulose, on Schirmer test and tear break up time, may be of value.

Topics: Adult; Corneal Diseases; Eye Protective Devices; Eyelid Diseases; Female; Humans; Hypesthesia; Leprosy; Male; Methylcellulose; Ophthalmic Solutions