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Abstract The present study is aimed to formulate steroidal oral mucoadhesive gels of dexamethasone sodium phosphate and betamethasone sodium phosphate. Six gel formulations each of dexamethasone sodium phosphate and betamethasone sodium phosphate prepared using two different polymers carboxymethyl cellulose sodium and hydroxypropyl methylcellulose, in variable proportions. All the formulations subjected for assessment of various physicochemical parameters and mechanical properties. The formulations BSP5 and DSP5, both containing 1.25 % carboxymethyl cellulose sodium, 1.25 % hydroxypropyl methylcellulose, exhibiting mucoadhesive strength of 12.300 ± 0.004 and 12.600 ± 0.01, adhesiveness of 28.04 ± 00 and 30.02 ± 00, cohesiveness of 28.04 ± 00 and 30.02 ± 00, drug release of 86.869 ± 0.380 % and 88.473 ± 0.457 % respectively were considered as promising ones and were further subjected for stability studies and in vivo study in male albino rats. Formulation DSP5 upon oral application for 4 months in arecoline induced oral submucous fibrosis rats, showed more than 80 % reduction in fibrosis as compared with BSP5 which showed nearly 50 % reduction. These results were concluded on the basis of histopathological profile and weight gain among the experimental animals during in vivo study. Hence, DSP5 by minimizing the painful injuries and morbidities justifies being suitable noninvasive model for OSMF treatment.
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Animals , Male , Rats , Oral Submucous Fibrosis/drug therapy , Betamethasone/analysis , Dexamethasone/analysis , Chemistry, Physical/classification , Benchmarking/methods , Gels/classification , Adhesiveness , Drug LiberationABSTRACT
Objective:To compare the protective effect of corneal protectant hydroxypropyl methylcellulose (HPMC) and balanced salt solution (BSS) on corneal epithelium in vitreous body surgery for proliferative diabetic retinopathy (PDR).Methods:A randomized controlled clinical trial was conducted.Fifty eyes of 50 patients with PDR who underwent minimally invasive vitrectomy in Xuzhou First People's Hospital from September 2018 to January 2019 were enrolled and randomly divided into HPMC group and BSS group, with 25 eyes in each group.All eyes underwent three-channel minimally invasive vitrectomy under non-contact wide-angle lens, and 2% HPMC and BSS were applied to keep the ocular surface moist according to grouping during the operation.The combination of cataract surgery, operation time, application times of 2% HPMC or BSS and the grade of corneal epithelial edema before and after operation were recorded.The patients were followed up for 1 month.Corneal fluorescein sodium staining and tear film break-up time (BUT) test were performed before operation and at 1 day, 3 days, 10 days and 1 month after operation.Schirmer Ⅰ test (SⅠt) and ocular surface disease index (OSDI) questionnaire were carried out before operation and at 1 month after operation.The study protocol adhered to the Declaration of Helsinki and was approved by an Ethics Committee of Xuzhou First People's Hospital (No.xyyⅡ[2018]005). Written informed consent was obtained from each patient prior to any medical examination.Results:The average frequency of application of eye drops in the HPMC group was (5.00±1.56) times, which was significantly less than (50.56±17.00) times in the BSS group ( t=-13.071, P<0.01). The postoperative corneal edema score of the HPMC group was 1.0 (1.0, 1.0) point, which was lower than 2.0 (2.0, 2.0) points of BSS group, and the difference was statistically significant ( Z=-4.909, P<0.01). There were statistically significant differences in postoperative corneal fluorescein sodium scores among 1 day, 3 days, 10 days and 1 month in the two groups (HPMC group: χ2=36.040, P<0.01; BSS group: χ2=50.892, P<0.01). The 1-, 3- and 10-day postoperative corneal fluorescein sodium scores in the HPMC group were significantly lower than those in the BSS group (all at P<0.05). One-day, 3-day, 10-day and 1-month postoperative BUT values were (6.15±2.20), (6.95±2.46), (6.16±2.11) and (5.81±2.92) seconds in the HPMC group, respectively, and were (3.89±1.87), (5.32±2.59), (5.01±2.12) and (4.97±2.10) seconds in the BSS group, respectively.There were significant differences in BUT between the two groups at different time points ( Fgroup=5.240, P<0.05; Ftime=2.846, P<0.05). The preoperative and 1-month postoperative SⅠt values in the BSS group were (12.24±5.55)mm and (9.96±4.53)mm, respectively, showing a statistically significant difference ( t=3.863, P=0.001). The postoperative OSDI score in the BSS group was (51.00±12.04) points, which was significantly higherly than the preoperative value of (47.89±10.95) points, and the difference was statistically significant ( t=-2.111, P<0.05). Conclusions:Compared with BSS, 2% HPMC in minimally invasive vitreous surgery has better protective effect on corneal epithelium of PDR, reduces the frequency of eye drop use during the surgery and shortens the repair time of ocular surface tissue after surgery.
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Objective To investigate effect of hydroxypropyl methyl cellulose (HPMC) to in vitro release characteristics of cefaclor sustained-release tablets.Methods Collected 10 batches of HPMC from different manufacturers.Determined the viscosity, molecular weight and the distribution of molecular weight of HPMC.HPMC from different manufacturers was used as blocking agent for the preparation of cefaclor sustained-release tablets according to the same prescription.Results The molecular weight was positively related to the viscosity of HPMC.The more molecular weight was, the slower the drugs release rate was,the better controlled released.Conclusion HPMC from different manufacturers show different quality stability and effect in vitro release of cefacor sustained-release tablets.
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[Objective]To study the influence of hydroxypropyl methyl cellulose(HPMC) on injectability of calcium phosphate cements(CPC).[Method]Calcium phosphate cement(ICPC) with different content of HPMC(0～4%) was prepared.Injectability coefficient and consistency were tested to evaluate the injectability of the cements.[Result]Injectability increased as HPMC content increased.CPC injectability coefficient reached to 95% with lowest consistency when HPMC increased to 2%.CPC with 2% HPMC could be injected from syringe completely.Injectability began decrease when HPMC beyond 3%.Injectability decreased to 90% as HPMC increased to 4%,2% HPMC increased the injectability and decreased the consistency significantly,without any influence of setting time.[Conclusion]Rheology and injectability of CPC can be improved by HPMC significantly,Injection of CPC with 2% HPMC can be used for mini-invasive orthopedic surgery.
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Object To study the preparation and technology on sinomenine (SM) release from Sinomenine Sustained-release Tablets (SSTs) in which hydroxypropyl methyl cellulose (HPMC) was used as the primary excipients. Methods SSTs were prepared with different HPMC viscosity of K4M, K15M, and K100M, different HPMC content, and preparing technology. Results Little effect was observed on the releasing rate of SM with different HPMC viscosity when the content of HPMC was 30%. SM releasing rate increased with the decreasing of proportion of HPMC while the content of HPMC was less than 30%. But the releasing velocity slowed down while the content of HPMC increased and the effect on the releasing rate was not found as the content of HPMC was over 30%. When the ratio of SM and HPMC was 1∶1.5, the releasing rate decreased with the increasing of tablet weight from 280 mg to 360 mg. The releasing rate was insensitive to the particle size of HPMC and hardness of SSTs in this study. Conclusion It is necessary to control the tablet weight and choose the proper quantity of HPMC in the preparation of SSTs.