Investigation of Drug-Excipient Compatibility Studies Using Validated RP-HPLC Method for Azelnidipine and Telmisartan Tablets

Aims: The Drug-Excipient compatibility testing was conducted at an early product development stage to determined that Excipients were compatible with drugs used in formulation and to distinguish as many degradation products as possible using validated gradient RP-HPLC method. Study Design: Drug-Excipient Compatibility study was conducted in glass vials at different stability conditions namely, at 300C + 20C/75% + 5% RH, 400C + 20C/ 75% + 5% RH for 04 weeks and another set of closed vials were stored in stability chamber at temperature 600C + 20C for 02 weeks. Methodology: Samples were analyzed by validated RP-HPLC method using Inertsil C-18 Column 150 × 4.6 mm ×5 µm, column oven temperature 40°C, flow rate 1.5 mL/min, Injection volume 10 µL with run time 12.0 minutes at 254 nm using Acetonitrile and buffer as mobile phase in gradient mode. Results: The developed method meets all system suitability parameters and found specific to determine the drug in the presence of Excipient as no interference was observed at the Retention time (Rt) of analyte. Conclusion: There was no physical and chemical incompatibility observed with Drug-Excipient and did not observe significant increase in the related substances.

Formulation and Evaluation of Transdermal Patch of Blonanserin

The objective of the present study was to formulate and evaluate transdermal patch of Blonanserin. Blonanserin transdermal patches were prepared by solvent casting method using natural and synthetic polymer. Various plastisizer were screened along with polymers. Drug excipient compatibility studies concluded that the drug and excipient are compatible with each other. The prepared patches were evaluated for physico-chemical parameters to justify their suitability for transdermal use. Formulations containing Xanthan Gum with plasticizer propylene glycol gives best drug release in 8 hours. More than 90% drug release found after 8 hours in formulation F5. Hence F5 formulation is considered as optimized batch. F5 batch was found stable during stability study. Blonanserin transdermal patches were successfully prepared by solvent casting method using Xanthan Gum natural polymer.

Formulation and Invitro evaluation of immediate release tablets containing febuxostat

In the present research work, Febuxostat Immediate Release Tablet was prepared by direct compression method using varying concentrations of Lycoat, Crospovidone& Croscarmellose sodium as disintegrants. The formulations prepared were evaluated for precompression& post-compression parameters. From the drug excipient compatibility studies, we observe that there are no interactions between the pure drug (Febuxostat) and optimized formulation (Febuxostat+ excipients) which indicates there are no physical changes. Post compression parameters were found to be within the limits. Among the formulation prepared the tablet containing 12mg of CCS shows 98.13% of the drug release within 45 min & follows first-order kinetics.

Drug-Excipients Compatibility Studies in Proniosomal Formulation: A Case Study with Resveratrol

Proniosomal drug delivery system is one of the advancements in nanotechnology. Similarly to traditional dosage forms, chemical and physical compatibility of proniosomes components with the active ingredient(s) is a key step in the preformulation process of such systems. In this work, the compatibility of resveratrol with selected excipients in the development of proniosomal formulation was investigated by thermal and spectroscopic techniques. To evaluate the drug-excipient compatibility, different techniques such as differential scanning calorimetric study, attenuated total reflectance Fourier transform infrared spectroscopy study and powder X-ray diffraction were adopted. The results showed that the excipients used in the formulation were compatible with resveratrol.

Fabrication and Characterization of Lercanidipine Hydrochloride Solid Dispersions by Fusion Technique

The authors aimed to design solid dispersions with Lercanidipine Hydrochloride (LCD) with PVP K-30, Poloxamer-188, and HPMC K4M as carriers. Various mixtures of LCD and Polymers (PVP K-30, Poloxamer-188, and HPMC K4M) were made in 1:1, 1:3, 1:5 and 1:7 ratios, and the solid dispersion was prepared by melting tactic, later compressed into tablets. Drug excipient compatibility studies were examined by DSC and FTIR studies. LCD was found to compatible with carriers used. The LCD solid dispersion was measured for physicochemical quality both in solid dispersions SD, and tablet states. The LCD solid dispersions found to have excellent flow possessions and compression assets. The yield of prepared solid dispersion was observed to be more than 90%), and the formulation LPOX-3 has showed a good yield of 98.9±1.95%, The tablets which were compressed from solid dispersions were found to have a uniform in size, shape, color, and consistency. The tablets were observed to have a uniform in thickness, and weight and ranged from 300.2±1.64 to 301.7±1.64 mg. The loss on friability was less than 1%, and the hardness was more than 4 Kg/cm2 indicates significant mechanical strength and the LCD content was also found to be uniform (96.8±1.35 to 99.9±2.34). The solubility of LCD was found to be good in 0.1N HCl and diminished with an increase in pH of the buffer. LCD released from the tablets were firstly by eruption followed by zero order. The dissolution was found to be good in solid dispersions with LCD: Poloxamer-188 at the ratio of 1:5. The results obtained were satisfactory. The study concludes that LCD solid dispersions (LPOX-3) with 1:5 ratios of LCD and Poloxamer-188 was found to be a better carrier than PVP K-30, and HPMC K4M in increasing the solubility of LCD from the solid dispersions.

Invitro Designing of Fluvastatin Chrono Formulation

The objective was to improve fluvastatin prescribed pulsatile release formulation to get the disintegrative and ruptured lag-time mechanism with a fixed time delay which matches the chronotherapeutics (hypercholesteroidal disorder). Pre formulation studies UV, FTIR (Drug excipient compatibility), solubility studies and flow properties were evaluated for blend and drug. All the values were within the limit. 12 core tablets were prepared with two novel disintegrants, i.e. ludiflash, lycoat in different concentrations after doing the post-compression parameters & drug release F8 was optimized & then coated with PH sensitive polymers HPMC K200M & Ethylcellulose in different concentrations. An evaluation was carried out for all six formulations, and all the values were within the limit. Based on In-vitro dissolution studies, swelling index and rupture test C5F8 is optimized and compared with the marketed product for 10 hours. As per the ICH guidelines optimized formulation (C5F8), stability tests were conducted for three months and was found to be stable. Optimized formulation (C5F8) contains 3:2 polymers (HPM K200M: Ethylcellulose) demonstrates an outstanding pulsatile drug delivery relative to the branded version (Lexcol XL) compared to all other formulations.

Development of Emulgel Delivery of Mupirocin for Treatment of Skin Infection

Aim:: To design controlled release topical delivery of mupirocin for the treatment of skin infection. Background:: Mupirocin is an antibacterial drug. Mupirocin works to kill the bacteria, which include strains of Staphylococcus aureus and Streptococcus pyogenes. It is also used for the treatment of inflammation of a hair follicle. The half-life of mupirocin is only 20-40 min. It has very slight solubility in water. Patent literature had shown work on ointment, antibiotic composition, nasal and topical composition. Emulgel is a duel control release system for the topical delivery of hydrophobic drugs. Objective:: The objective was to formulate emulgel with controlled delivery of mupirocin using Sepineo P 600. Methods:: Soya oil, tween 80 and polyethylene glycol 400 (Oil:Surfactant:Cosurfactant) were used for emulsion formulation. Emulgel was optimized by 32 factorial design. Sepineo P 600 and hydroxy propyl methyl cellulose K4M were used as independent variables. Drug excipient compatibility analysis was carried out by FTIR, UV and DSC spectra. Emulgel was evaluated for its physical characterization, in vitro release, ex vivo release, antimicrobial and anti-inflammatory study. Results:: DSC, UV and FTIR analysis confirmed drug excipient compatibility. FE SEM showed a size range between 228-255 nm. Zeta potential was found to be -25.1 mV, which showed good stability of the emulsion. Design expert software showed F2 as an optimized batch. Release studies indicated that the controlled release of drugs forms Sepineo P 600 gel due to its higher gelling capacity. Batch F2 showed comparable results with marketed formulation against Staphylococcus aureus. For batch F2, 40 μg/ml was the minimal inhibitory concentration. Conclusion:: Antimicrobial and anti-inflammatory study proved successful development of stably controlled release mupirocin emulgel.

Assessment of Structural Compatibility of Saxagliptin in Physical Mixtures with some excipient by Using HPLC

Introduction: Saxagliptin hydrochloride is an oral hypoglycemic agent used for the treatment of type 2 diabetes mellitus. Saxagliptin is unstable because it undergoes an intra-molecular cyclisation reaction to form a cyclicamidine in both solution and solid states. In pharmaceutical development of saxagliptin it is important to select the excipients which are compatible and help to minimize the formation of cyclicamidine. In excipient compatibility study for saxagliptin it is essential to identify the formation of cyclicamidine and other related substances. Materials and Methods: In the current work, the method for quantification of saxagliptin, cyclicamidine and its related substances by high performance liquid chromatographic was developed and validated. This method was used as screening technique for assessing the compatibility of saxagliptin with some pharmaceutical excipients. These were evaluated by analyzing the pure saxagliptin and saxagliptin- excipient in physical mixture, which were stored under different conditions at 40°C/75% Relative Humidity (RH) for one month. The method was successfully validated as per ICH guidelines. Results and Conclusion: The results of compatibility study demonstrate the suitability of saxagliptin with Methocel, Polyethylene Glycol (PEG), Opadry Red, Opadry pink, Opadry white, and Opadry Pink.