Data from: Influence of acetylation levels on dual-modified corn starch in colon-targeted Budesonide tablet formulation
Data files
May 24, 2024 version files 51.35 KB
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Degree_of_substitution_(DS)_and_acetyl_content_of_native_and_derived_corn_starches.xlsx
9.87 KB
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Dissolution.xlsx
12.93 KB
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Hardness_Friabiity_DT.xlsx
10.48 KB
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README.md
5.23 KB
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Swelling_and_Solubility.xlsx
12.84 KB
Abstract
Although starch is an affordable and safe biodegradable polymer, its rapid breakdown in the upper gastrointestinal tract renders it an unsuitable excipient for colon-targeted oral tablets. The current study examined the influence of varying degrees of acetylation on dual-modified (retrograded and acetylated) corn starch as a polymer in the formulation of colon-targeted tablets, emphasizing drug release and suitability for direct compression, utilizing Budesonide as a model drug. Starch acetylation was performed using acetic anhydride as the acetylating agent and water or acetic acid as the solvent to prepare starch with low, medium, and high degrees of substitution. Analysis techniques confirmed the presence of acetyl groups, revealed changes in crystalline structure, and illustrated morphological alterations post-acetylation. Among the various degrees of substitution (DS) studied, it was evident that starch acetylated to a high degree offered the most promising attributes as an excipient for colon-targeted drug delivery. Specifically, tablet formulation with a high DS of 2.01±0.03 (F4) demonstrated optimal mechanical strength, hardness, and desirable physical properties for achieving controlled drug release in the colon. Dissolution studies indicated F4's effectiveness, releasing 15.24% of the drug in pH 1.2 within 2 hours, followed by 37.58% and 22.53% in pH 7.4 and pH 6.8 phosphate buffers, covering the ileo-colonic region. In conclusion, the study emphasized the significance of the degree of substitution (DS) in acetylation for dual-modified starch in colon-targeted tablet formulations, highlighting its potential as an ideal option for drug delivery applications by achieving controlled drug release in the targeted ileo-colonic region.
README: Data from: Influence of acetylation levels on dual-modified corn starch in colon-targeted Budesonide tablet formulation
https://doi.org/10.5061/dryad.69p8cz99n
Description of the data and file structure
The dataset consists of four .xlsx files. In all of these files, four types of tablet formulation were evaluated which contain native starch (NCS) formulation F1, low substituted corn starch (LDSCS) formulation F2, medium substituted corn starch (MDSCS) formulation F3, and high degree of substitute corn starch (HDSCS) formulation F4, respectively. These files with corresponding variables are described below:
1. File name: "Hardness_Friabiity_DT”, which supports Table 2 (Post-compression assessment of different starch tablet formulations) in the manuscript. Variable name and description:
a) Hardness (3 observations)-Tablet hardness measured in Kg/cm2
b) Mean Hardness- Mean of three observations of hardness expressed as Mean ± Standard deviation
c) Friability (3 observations) measured by the formula Friability (%) = [(W1 – W2)/ W1] X 100
d) Mean Friability (%)- Mean of three observations of friability expressed as Mean ± Standard deviation
Where, W1 = Weight of Tablets (Initial / Before Tumbling) & W2 = Weight of Tablets
e) Disintegration time (3 observations)- Tablet disintegration time measured in minutes.
f) Mean Disintegration Time (min)- Mean of three observations of disintegration time expressed as Mean ± Standard deviation
2. File name: "Degree_of_substitution_(DS) and_acetyl_content_of_native_and_derived_corn_starches", which supports Table 2 (Post-compression assessment of different starch tablet formulation) in the manuscript. Variable name and description:
a) Starch Type- Type of starch prepared i.e., LDSCS, MDSCS or HDSCS
b) Acetyl Content (%)- Acetyl content of the starch calculated as per the formula mentioned in the manuscript (3 observations)
c) Mean Acetyl Content (%)-Mean of three observations of Acetyl Content (%) expressed as Mean ± Standard deviation
d) Degree of Substitution- Degree of Substitution of the starch calculated as per the formula mentioned in the manuscript (3 observations)
e) Mean Degree of Substitution -Mean of three observations of Degree of Substitution expressed as Mean ± Standard deviation
3. File name: "Swelling_and_Solubility", which supports Figure 4 (Swelling and solubility study of starch samples) in the manuscript.
A) The swelling power worksheet represents the results of the swelling study. Variable name and description:
a) Sample-Starch type (NCS/LDSCS/MDSCS/HDSCS)
b) At room temperature (3 observations)-Observations taken at room temperature
c) Mean at room Temperature- Mean of three observations at room temperature expressed as Mean ± Standard deviation
d) At 50⁰C (3 observations)- Observations taken at 50⁰C
e) Mean at 50⁰C- Mean of three observations at 50⁰C expressed as Mean ± Standard deviation
f) At 70⁰C (3 observations)- Observations taken at 50⁰C
g) Mean at 70⁰C- Mean of three observations at 70⁰C expressed as Mean ± Standard deviation
h) At 90⁰C (3 observations)- Observations taken at 50⁰C
i) Mean at 90⁰C- Mean of three observations at 90⁰C expressed as Mean ± Standard deviation
B) Solubility worksheet represents results of solubility study. Variable name and description:
a) Sample-Starch type (NCS/LDSCS/MDSCS/HDSCS)
b) At room temperature (3 observations)-Observations taken at room temperature
c) Mean at room Temperature- Mean of three observations at room temperature expressed as Mean ± Standard deviation
d) At 50⁰C (3 observations)- Observations taken at 50⁰C
e) Mean at 50⁰C- Mean of three observations at 50⁰C expressed as Mean ± Standard deviation
f) At 70⁰C (3 observations)- Observations taken at 50⁰C
g) Mean at 70⁰C- Mean of three observations at 70⁰C expressed as Mean ± Standard deviation
h) At 90⁰C (3 observations)- Observations taken at 50⁰C
i) Mean at 90⁰C- Mean of three observations at 90⁰C expressed as Mean ± Standard deviation
4. File name: "Dissolution", which supports Figure 6 (Drug release behavior of different formulations during simulated in-vitro GI transit) in the manuscript. LSDCS worksheet represents Cumulative % drug release profile for LSDCS. MSDCS worksheet represents Cumulative % drug release profile for MSDCS. HSDCS worksheet represents Cumulative % drug release profile for HSDCS.
Variable name and description in each worksheet:
a) Time: Duration of drug release from beginning of study in hours
b) Cumulative % drug release (3 observations)- Calculated as: (amount of drug released/Total drug taken) X 100
c) Mean Cumulative % drug release- Mean of three observations of Cumulative % drug release for a specific duration expressed as Mean ± Standard deviation