Optimization and In-vitro Evaluation of Coating Process for Film-Coated Tablets

2017 ◽  
Vol 13 (11) ◽  
Author(s):  
Marwan Abdelmahmoud Abdelkarim Maki ◽  
Palanirajan Vijayaraj kumar ◽  
Yeong Siew Wei
Keyword(s):  
Weight Gain ◽  
Scale Up ◽  
Film Coating ◽  
Inlet Temperature ◽  
Coating Process ◽  
Coating Quality ◽  
Tablet Coating ◽  
Spray Rate ◽  
Pan Coater

AbstractThe proper efficiency of the tablet-coating process often results in a coating within adequate quality, which might avoid the rejection of the film-coated tablets, minimize the operating expenses and production time. In general, the optimum coating system performance and coating conditions are important for achieving the desirable tablet-coating uniformity and manufacturing reproducibility. In this study, HPMC-aqueous-based tablet film coating successfully conducted in a perforated pan coater for process scale-up using the spray-coating technique. Certain process parameters such as spray rate, inlet air temperature, pan temperature, atomizing pressure as well as pan speed were maintained carefully and the optimum coating quality was achieved with acceptable film performance. At lower initial pan speed, the strength of the coated tablets was remarkably improved and the highest weight gain obtained. The smoothest and uniform film obtained at high spray rate, high pan speed, and low atomizing pressure. The results revealed that the optimum film-coating quality and uniformity achieved at a spray rate of 480 ml/min, atomizing pressure at 5 bar, inlet temperature at 85 to 90 °C, pan temperature at 58 °C, initial pan speed at 1.5 rpm and final pan speed at 4.0 rpm using side-vented pan coater. At initial pan speed of 1.5 rpm, the strength of the coated tablets remarkably improved with minimum edges erosion, which increases the weight gain up to 3.3%w/w.

A Scale-up Approach for Film Coating Process Based on Surface Roughness as the Critical Quality Attribute

2018 ◽  
Vol 19 (3) ◽  
pp. 1243-1253 ◽  
Author(s):  
Hiroyuki Yoshino ◽  
Yuko Hara ◽  
Masafumi Dohi ◽  
Kazunari Yamashita ◽  
Tadashi Hakomori ◽  
...  
Keyword(s):  
Surface Roughness ◽  
Scale Up ◽  
Film Coating ◽  
Coating Process ◽  
Quality Attribute ◽  
Critical Quality Attribute

Formulation Development of Metoprolol Succinate Controlled Release Tablets using Ethyl-cellulose-polyvinyl-pyrrolidone Coating

2015 ◽  
Vol 8 (2) ◽  
pp. 2851-2857
Author(s):  
Kiran Kumar Vangara ◽  
Kishore K. Konda ◽  
Shiva K. Ravula ◽  
Pradeep K Vuppala ◽  
Vijay K. Sripuram ◽  
...  
Keyword(s):  
Weight Gain ◽  
Controlled Release ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Film Coating ◽  
Release Profile ◽  
Water Soluble ◽  
Metoprolol Succinate ◽  
Water Soluble Drug

It is challenging to develop a controlled release (CR) formulation for a freely water soluble drug molecule without using rate controlling polymers in the core matrix. This study is aimed to develop and evaluate cost-effective ethyl cellulose (EC)-polyvinyl pyrrolidone (PVP) film coating that can effectively control the release of freely water soluble drug, metoprolol succinate (MS) and to match that of release profile with its marketed tablet. Simple core tables of MS were compressed and coated with a solution composed of hydrophobic rate controlling polymer, EC and water soluble pore forming polymer, PVP. The effect of formulation parameters such as the ratio of EC to PVP and tablet coating weight gain on the in-vitro drug release were evaluated. Release profile of the optimized formulation at different pH conditions was determined and the similarity factor (f2) with marketed release profile was calculated.It was observed that drug release rate increased with a decrease in the ratio of ethyl cellulose to PVP and decreased with increased weight gain of the coating membrane. Among all the formulations, the formulation with EC and PVP at a ratio of 60:40 %w/w and 9% weight gain showed matching release profile to marketed tablet with f2 value of 72.25. The optimized formulation showed pH independent in-vitro release. This study successfully demonstrated that EC-PVP film coating can effectively control the release rate of freely soluble drugs. Once a day CR formulation of metoprolol succinate pharmaceutically equivalent to marketed tablet was developed.  

scholarly journals A Novel Scale Up Model for Prediction of Pharmaceutical Film Coating Process Parameters

2016 ◽  
Vol 64 (3) ◽  
pp. 215-221 ◽  
Author(s):  
Yasuhiro Suzuki ◽  
Tatsuya Suzuki ◽  
Hidemi Minami ◽  
Katsuhide Terada
Keyword(s):  
Process Parameters ◽  
Scale Up ◽  
Film Coating ◽  
Coating Process

scholarly journals OPTIMIZATION OF AQUEOUS-BASED FILM COATING PROCESS PARAMETERS CONTAINING GLUCOSAMINE SULFATE POTASSIUM CHLORIDE

2019 ◽  
pp. 251-257 ◽  
Author(s):  
NISHANT OZA ◽  
AKRUTI KHODAKIYA ◽  
SWATI SAGAR
Keyword(s):  
Factorial Design ◽  
Air Temperature ◽  
Process Parameters ◽  
Film Coating ◽  
Full Factorial Design ◽  
Coating Process ◽  
Coated Tablet ◽  
Spray Rate ◽  
Full Factorial ◽  
32 Full Factorial Design

Objective: The aim of the present work was to prepare film coated tablet of glucosamine sulfate potassium chloride and study the effect of coating process parameters which implicate more significant effects on an aqueous-based film coating process of tablets. Methods: The different batches of uncoated tablets were prepared by wet granulation method. Aqueous film coating was carried out by using opadry®II white 85F18422. A 32 full factorial design was employed to study the effect of spray rate (X1) and inlet air temperature (X2) on coating uniformity, coating process efficiency and % loss on drying. The surface characteristics of the aqueous based film coated tablet were studied using a SEM. Check point batch was prepared to validate the evolved model. Results: Preliminary trials indicated that individually process parameters affected the quality of coated tablets. Hence, studied the combined effect of these factors on the coating process required and 32 full factorial design was applied. In this study, it was seen that spray rate and inlet air temperature had a major effect on tablet coating process. It was observed from factorial batch that maximum drug release was found in batch F5. Conclusion: The results of full factorial design indicate both parameters spray rate (X1) and inlet air temperature (X2) have significant effect on coating process and batch F5 is stable for 3 mo at accelerated condition.

scholarly journals Effects of coating on the release profile of drug combination from hydrophilic matrix pellets

1970 ◽  
Vol 2 (2) ◽  
pp. 53-58
Author(s):  
Muhammad Shahidul Islam ◽  
Md Moniruzzaman ◽  
Ruknuzzaman Rony ◽  
Tasnuva Haque
Keyword(s):  
Ascorbic Acid ◽  
Ferrous Sulfate ◽  
Ferrous Sulphate ◽  
Film Coating ◽  
Release Profile ◽  
In Vitro Dissolution ◽  
Pharmaceutical Sciences ◽  
Coating Composition ◽  
Pan Coater

In this work zinc sulfate, ferrous sulfate and ascorbic acid was formulated on the same pellet by combination pelletization technique and their and in vitro dissolution studies were performed by using United States Pharmacopoeia (USP) apparatus type II. In addition, effect of different types of polymers, formulation variables and variations in coating composition on the release of drug were studied. The desired release profile for ferrous sulfate was 35% for 1st hour, 45-75% for 2nd hour and 60-85% for third hour and not less than 85% for 4th hour. The release rate controlling polymer used was various concentrations of Methoccel K15M CR with different concentrations of Microcrystalline cellulose (Avicel PH 101). The maximum release percentage of Ferrous Sulphate was obtained from 2.5 % of Methocel K15M CR and 30 % Avicel PH 101 containing pellets (F-4) and it was 92.32%. And the minimum release percentage of Ferrous Sulphate was obtained from 10 % of Methocel K15M CR and 35.7% Avicel PH 101 containing pellets (F-1) and it was 86.36%. The release profile from other formulations containing 35.4% Methocel K 15M CR & 7.5% Avicel (F-2) and 32% Methocel K 15M CR & 4% Avicel (F-3) were also within desired range. The effect of Eudragit coating (enteric) and the presence of PEG and HPMC in the film coating composition on the drug release were also investigated. Hydrophobic matrix pellets prepared using lower concentrations of Methocel K15M CR were found to be best suited for modulating the delivery of the ferrous sulphate from the combination.  Key words: Non Pariel Seeds (NPS); Pan Coater; Ascorbic acid; Methocel K15M CR; Pelletization; PEG; Avicel PH 101; Xanthan gum.DOI: 10.3329/sjps.v2i2.5824Stamford Journal of Pharmaceutical Sciences Vol.2(2) 2009: 53-58

Formulation and Evaluation of Atenolol and Indapamide SR Matrix Tablets for Treatment of Hypertension

2014 ◽  
Vol 7 (2) ◽  
pp. 2450-2458
Author(s):  
Sarika Pundir ◽  
Ashutosh Badola
Keyword(s):  
Kinetic Studies ◽  
Film Coating ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Simultaneous Estimation ◽  
Matrix Tablet ◽  
Release Agent ◽  
Disintegration Time ◽  
Weight Variation

In the present study we have formulated (F1 to F6) matrix tablets of atenolol and indapamide for the management of hypertension. As in simultaneous estimation of these drugs it was found that a confined release can be formulated. In the formulation of SR matrix tablet by using different concentration of delayed release agent DCP and pregelatinized starch as disintegrant we prepared tablets by wet granulation method. For sustained release action HPMC polymers were used for film coating. Preformulation studies were performed prior to compression. The compressed SR matrix tablets were evaluated for weight variation, hardness, friability, drug content, disintegration time and in vitro drug release using USP dissolution apparatus type 2 (paddle). It was found that the optimized formulation showed 49.33%, 48.90%, 48.52%, 47.65%, 46.84% and 46.51% release for atenolol in 12 hours respectively. However, indapamide released 49.62%, 49.39%, 48.72%, 48.27%, 47.59% and 47.36% at the end of 12 hr. The IR spectrum study revealed that there is no disturbance in the principal peaks of pure drugs atenolol and indapamide. This confirms the integrity of pure drugs and no incompatibility of them with excipients. The stability studies were carried out for the optimized batch for one months and it showed satisfactory results. The kinetic studies of the formulations revealed that diffusion is the predominant mechanism of drug and release follows Zero-order, Super case II transport.

scholarly journals Reduction of body-weight gain enhances in vitro embryo production in overfed superovulated dairy heifers

Reproduction ◽  
2006 ◽  
Vol 131 (4) ◽  
pp. 783-794 ◽  
Author(s):  
S Freret ◽  
B Grimard ◽  
A A Ponter ◽  
C Joly ◽  
C Ponsart ◽  
...  
Keyword(s):  
Weight Gain ◽  
Dietary Intake ◽  
Live Weight ◽  
Reproductive Hormones ◽  
Embryo Production ◽  
Live Weight Gain ◽  
Dairy Heifers ◽  
Period 2 ◽  
Significant Difference

The aim of our study was to test whether a reduction in dietary intake could improve in vitro embryo production in superovulated overfed dairy heifers. Cumulus–oocyte complexes of 16 Prim’ Holstein heifers (14 ± 1 months old) were collected by ovum pick-up (OPU), every 2 weeks following superovulation treatment with 250 μg FSH, before being matured and fertilized in vitro. Embryos were cultured in Synthetic Oviduct Fluid medium for 7 days. Heifers were fed with hay, soybean meal, barley, minerals and vitamins. From OPU 1 to 4 (period 1), all heifers received individually for 8 weeks a diet formulated for a 1000 g/day live-weight gain. From OPU 5 to 8 (period 2), the heifers were allocated to one of two diets (1000 or 600 g/day) for 8 weeks. Heifers’ growth rates were monitored and plasma concentrations of metabolites, metabolic and reproductive hormones were measured each week. Mean live-weight gain observed during period 1 was 950 ± 80 g/day (n = 16). In period 2 it was 730 ± 70 (n = 8) and 1300 ± 70 g/day (n = 8) for restricted and overfed groups respectively. When comparing period 1 and period 2 within groups, significant differences were found. In the restricted group, a higher blastocyst rate, greater proportions of grade 1–3 and grade 1 embryos, associated with higher estradiol at OPU and lower glucose and β-hydroxybutyrate, were observed in period 2 compared with period 1. Moreover, after 6 weeks of dietary restriction (OPU 7), numbers of day 7 total embryos, blastocysts and grade 1–3 embryos had significantly increased. On the contrary, in the overfed group, we observed more <8 mm follicles 2 days before superovulation treatment, higher insulin and IGF-I and lower nonesterified fatty acids in period 2 compared with period 1 (no significant difference between periods for embryo production). After 6 weeks of 1300 g/day live-weight gain (OPU 7), embryo production began to decrease. Whatever the group, oocyte collection did not differ between period 1 and 2. These data suggest that following a period of overfeeding, a short-term dietary intake restriction (6 weeks in our study) may improve blastocyst production and embryo quality when they are low. However, nutritional recommendations aiming to optimize both follicular growth and embryonic development may be different.

scholarly journals Identification of the Active Ingredient and Beneficial Effects of Vitex rotundifolia Fruits on Menopausal Symptoms in Ovariectomized Rats

Biomolecules ◽  
2021 ◽  
Vol 11 (7) ◽  
pp. 1033
Author(s):  
Ji Hwan Lee ◽  
Sullim Lee ◽  
Quynh Nhu Nguyen ◽  
Hung Manh Phung ◽  
Myoung-Sook Shin ◽  
...  
Keyword(s):  
Weight Gain ◽  
Body Weight Gain ◽  
Animal Experiments ◽  
Ovariectomized Rats ◽  
Biological Functions ◽  
Menopausal Syndrome ◽  
Active Constituents ◽  
Mcf 7

Estrogen replacement therapy is a treatment to relieve the symptoms of menopause. Many studies suggest that natural bioactive ingredients from plants resemble estrogen in structure and biological functions and can relieve symptoms of menopause. The fruit of V. rotundifolia, called “Man HyungJa” in Korean, is a traditional medicine used to treat headache, migraine, eye pain, neuralgia, and premenstrual syndrome in Korea and China. The aim of the present study was to confirm that V. rotundifolia fruit extract (VFE) exerts biological functions similar to those of estrogen in menopausal syndrome. We investigated its in vitro effects on MCF-7 cells and in vivo estrogen-like effects on weight gain and uterine contraction in ovariectomized rats. Using the polar extract, the active constituents of VFE (artemetin, vitexicarpin, hesperidin, luteolin, vitexin, and vanillic acid) with estrogen-like activity were identified in MCF-7 cells. In animal experiments, the efficacy of VFE in ameliorating body weight gain was similar to that of estrogen, as evidenced from improvements in uterine atrophy. Vitexin and vitexicarpin are suggested as the active constituents of V. rotundifolia fruits.

scholarly journals Extraction and Fractionation Effects on Antiplasmodial Activity and Phytochemical Composition of Palicourea hoffmannseggiana

2021 ◽  
Vol 8 (01) ◽  
pp. e34-e42
Author(s):  
Leticia Hiromi Ohashi ◽  
Douglas Costa Gontijo ◽  
Maria Fernanda Alves do Nascimento ◽  
Luciano Ferreira Margalho ◽  
Geraldo Célio Brandão ◽  
...  
Keyword(s):  
Growth Inhibition ◽  
Scale Up ◽  
Indole Alkaloid ◽  
Ethanol Extract ◽  
Parasite Growth ◽  
In Vitro Activity ◽  
Acid Base ◽  
Leaf Extracts ◽  
Leaf Powder

AbstractThe present study on Palicourea hoffmannseggiana, which was collected at Marapanim, state of Pará, Brazil, comprises the preparation of different stem and leaf extracts and fractions. Ethanol, hydroethanol, and water extracts were prepared by several methods and evaluated for in vitro activity against resistant Plasmodium falciparum (W2 strain), disclosing a low parasite growth inhibition effect (< 50%). Dereplication by UPLC-DAD-ESI−MS of the leaf ethanol extract showed the presence of two known alkaloids, lyalosidic and strictosidinic acids, along with a sinapoyl ester of lyalosidic acid, with m/z 719.33 [M+H]+, which is possibly a new monoterpene indole alkaloid representative. Sequential liquid-liquid acid-base alkaloid separations from the leaf ethanol extract as well as directly from leaf powder afforded fractions of increased parasite growth inhibition, reaching up to 92.5±0.7%. The most bioactive fractions were shown to contain the β-carboline alkaloids harmane and 4-methyl-β-carboline, along with N-methyl-tryptamine and N-acetyl-tryptamine, while monoterpene indole alkaloids were detected in inactive fractions of these processes. The present results demonstrate that these preliminary fractionation methods can lead to significantly active fractions supporting an adequate scale-up to carrying out the isolation of anti-plasmodial compounds.

Studies on the phytate: zinc molar contents in diets as a determinant of Zn availability to young rats

1979 ◽  
Vol 41 (3) ◽  
pp. 591-603 ◽  
Author(s):  
N. T. Davies ◽  
S. E. Olpin
Keyword(s):  
Weight Gain ◽  
Fixed Amount ◽  
Sodium Phytate ◽  
Egg Albumin ◽  
Zn Content ◽  
Egg Albumen ◽  
Zn Status ◽  
Textured Vegetable Protein ◽  
Zn Availability

1. Studies were carried out in vitro to examine the effects of phytate on the solubility of the trace elements zinc, copper and manganese. Appropriate volumes of a solution of sodium phytate were added to a mineral solution to achieve phytate: Zn values of from 0: 1 to 45:1. In a second series the same values for phytate: Zn were achieved by varying the amount of added Zn at a fixed phytate concentration.2. In both experiments > 85% of the Zn was rendered insoluble at pH 6.5 even at the lowest value for phytate:Zn (5:1). The effect of phytate on Zn solubility was greater than effects on Cu or Mn.3. In a dietary study, rats were offered a semi-synthetic egg-albumin-based diet with added phytate. Two series of diets were prepared, the first had a constant Zn content (18.5 mg Zn/kg) and the amount of sodium phytate varied so as to achieve values for phytate: Zn of from 0:1 to 40:1 (series 1). In the second series, the same values for phytate:Zn were achieved by adding a fixed amount of phytate (7.4 g phytic acid/kg) while the amount of Zn was varied (series 2).4. Dietary phytate caused significant reductions in growth rates, plasma Zn concentrations and hair Zn concentrations and greying of the coat at values for phytate:Zn of 15:1, 10:1, 10:1 and 15:1, respectively.5. While phytate was apparently slightly more effective in reducing Zn status when phytate:Zn values were achieved at the lower absolute levels of phytate and Zn (series I diets), the differences at equivalent phytate:Zn values were small. It was concluded that phytate:Zn values can be used as an indicator of Zn availability from phytate-rich diets.Rats offered three diets containing soya-bean-based textured-vegetable-protein (TVP) exhibited low rates of weight gain compared with rats offered an egg-albumen-based diet of similar Zn content (14.5 mg Zn/kg). Additional Zn supplied in drinking-water (25 mg Zn/l) was without effect on rats consuming the egg-albumin diet but significantly improved the weight gain of rats on the TVP diets.7. It was concluded that phytate naturally present in TVP behaves similarly to phytate added to an otherwise phytate-free diet and that the reduced availability of Zn in TVP diets can be accounted for entirely by their phytate contents.

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