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Improvement of carvedilol dissolution rate through formation of inclusion complex with B-cyclodextrin
Pamudji J.S.a, Mauludin R.a, Lestari V.A.a
a School of Pharmacy, Institut Teknologi Bandung, Indonesia
[vc_row][vc_column][vc_row_inner][vc_column_inner][vc_separator css=”.vc_custom_1624529070653{padding-top: 30px !important;padding-bottom: 30px !important;}”][/vc_column_inner][/vc_row_inner][vc_row_inner layout=”boxed”][vc_column_inner width=”3/4″ css=”.vc_custom_1624695412187{border-right-width: 1px !important;border-right-color: #dddddd !important;border-right-style: solid !important;border-radius: 1px !important;}”][vc_empty_space][megatron_heading title=”Abstract” size=”size-sm” text_align=”text-left”][vc_column_text]Objective: Carvedilol is practically water-insoluble drug which has poor dissolution rate. These properties are associated with slow drug absorption leading to inadequate and unpredictable bioavailability. An inclusion complex is one of several methods to increase solubility and dissolution rate of an active pharmaceutical ingredient in water. The aim of this study is to improve dissolution rate of carvedilol by developing an inclusion complex with β-cyclodextrin. Methods: Preparations of the inclusion complex were performed by kneading, co-precipitation, and freeze drying methods. The variations of molar ratio of 1:1, 1:2, and 1:3 between carvedilol and β-cyclodextrin were carried out. The amount of carvedilol included in β-cyclodextrin was calculated based on the amount of included carvedilol in binary system and free carvedilol in solution. Evaluations of the inclusion complex were performed by infrared spectroscopy, X-ray difractometry (XRD) and Scanning Electron Microscopy (SEM). Furthermore, dissolution test was performed on pure carvedilol, physical mixture of carvedilol and β-cyclodextrin and all type of inclusion complexes. The amount of dissolved carvedilol in the medium were determined using UV spectrophotometer at λ = 286 nm. Results: The highest entrapment efficiency of inclusion complexes (89.68%) was obtained by freeze drying method with a molar ratio of 1:3. Infrared spectrum and SEM characterization revealed there are interaction between carvedilol and β-cyclodextrin. Meanwhile XRD evaluation showed a change on the crystalline status of carvedilol in all inclusion complexes. The results of one way ANOVA and LSD statistical test at 95% confidence level showed that the percentage of dissolved carvedilol at 10th minute and dissolution efficiency of carvedilol after 120 minutes were significantly different on all of those inclusion complexes. However, the obtained inclusion complex by freeze drying method with ratio molar of 1:3 revealed the highest percentage of the dissolved carvedilol within 120 minutes (87.68%). Conclusion: According to the evaluation on complex formation efficiency, characterization of the inclusion complex, percentage of the dissolved drug, and dissolution efficiency, the best formulation of the inclusion complex has been obtained by freeze drying method with molar ratio of 1:3.[/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”Author keywords” size=”size-sm” text_align=”text-left”][vc_column_text][/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”Indexed keywords” size=”size-sm” text_align=”text-left”][vc_column_text]Carvedilol,Coprecipitation method,Dissolution rate,Freeze drying method,Inclusion complex,Kneading method,β-cyclodextrin[/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”Funding details” size=”size-sm” text_align=”text-left”][vc_column_text][/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”DOI” size=”size-sm” text_align=”text-left”][vc_column_text][/vc_column_text][/vc_column_inner][vc_column_inner width=”1/4″][vc_column_text]Widget Plumx[/vc_column_text][/vc_column_inner][/vc_row_inner][/vc_column][/vc_row][vc_row][vc_column][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][/vc_column][/vc_row]