A Novel Approach of Formulation & Evaluation of Tablet in Capsule Device for GI Protection Pain Management
Abstract
This research article presents a novel approach in the formulation and evaluation of a tablet in capsule device aimed at providing GI protection and effective pain management. Key aspects include the development of Aceclofenac Extended-Release tablets and Misoprostol Immediate Release tablets, enclosed in a hard gelatin capsule. The study covers preformulation, formulation development, in-process quality control checks, and stability studies. Results indicate the combination dosage form offers advantages in safety, patient compliance, and therapeutic efficacy.
Introduction
Historically, the most convenient and commonly employed route of drug delivery has been by oral ingestion. Oral drug delivery has been known for decades as the most widely utilized route of administration among all the routes that have been explored for the systemic delivery of drugs via various pharmaceutical products of different dosage forms. It is considered the most natural, uncomplicated, convenient, and safe route. Among the different oral dosage forms, tablets and capsules stand out as the most preferred options by pharmaceutical manufacturers, physicians, and patients (1). Tablets, which are solid dosage forms containing medicinal substances with or without suitable diluents, offer several advantages such as excellent physicochemical stability, accurate dosing, and ease of mass production with robust quality controls. Similarly, capsules, which are solid dosage forms where the drug is enclosed within a hard or soft soluble shell, provide versatile drug delivery options for powders and non-powder fillings such as tablets, capsules, and pellets (1, 2).
Solid oral dosage forms, such as tablets and capsules, have distinct advantages over other forms of medication. They are the most stable dosage form in terms of physical, chemical, and microbiological attributes, providing accurate, stable doses with the greatest precision and least content variability. They are also user-friendly, easy to handle, and carry, and have an attractive, elegant appearance. The manufacturing cost of tablets is relatively low, and their production speed is quite high, making them suitable for large-scale production. Furthermore, the packaging and shipping of tablets are comparatively easy and cost-effective. Tablets and capsules can also mask the unpleasant taste and odor of medications, reduce incompatibilities and deterioration due to environmental factors, and offer various branding possibilities through colored film coatings, different shapes, sizes, or logos (3).
However, solid oral dosage forms also come with certain disadvantages. Drugs that are amorphous in nature or have low-density characteristics are difficult to compress into tablets. Hygroscopic drugs are not suitable candidates for compressed tablets, and drugs with poor wetting properties, slow dissolution profiles, and high optimal gastrointestinal absorption may be challenging to formulate as tablets (4). Additionally, drugs with bitter tastes and objectionable odors require special treatments like coating or encapsulation, which may increase production costs. Capsules are not suitable for extremely soluble materials such as potassium chloride or highly efflorescent or deliquescent fill materials. Despite these challenges, the continued development and optimization of tablet and capsule formulations ensure that they remain a cornerstone of effective and reliable drug delivery systems (5).
The aim of this study is to formulate a combination dosage form of Aceclofenac Extended-Release tablets (200 mg) and Misoprostol Immediate Release tablets (200 mcg) enclosed in Size ‘0’ elongated Hard Gelatin Capsules. This involves conducting a preformulation study to assess the compatibility of Aceclofenac and Misoprostol with various excipients, followed by the preparation of compact Aceclofenac ER tablets using hydrophilic polymers HPMC and Ceolus KG 1000, and Misoprostol IR tablets by direct compression. Comprehensive quality control checks and an accelerated stability study will be performed to ensure the efficacy, safety, and stability of the combination product under specified conditions.
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Table 1: Drug– Excipient Compatibility
| S.No | Drug-Excipient | Ratio | Initial | Initial | Appearance |
|---|---|---|---|---|---|
| Assay % | WC | ||||
| 1 | MI-MCC Type 102 | 1:1 | 97.29 | 4.75 | White powder |
| 2 | MI-Crospovidone | 1:0.25 | 98.90 | 3.81 | White powder |
| 3 | MI-Cabosil | 1:0.25 | 96.58 | 2.79 | White powder |
| 4 | MI-Stearic acid | 1:0.25 | 98.05 | 1.25 | White to off white powder |
| 5 | AC-MCC KG 1000 | 1:0.5 | 98.05 | 4.32 | White powder |
| 6 | AC -HPMC E50 | 1:0.5 | 96.07 | 3.12 | White powder |
| 7 | AC-Stearic acid | 1:0.25 | 99.30 | 0.10 | White to off white powder |
Jupalli santhipriya, Bhimavarapu. Gamya, Mitta. Anil, Bobbili.dharani, Chilukuri.vydhehi, Syed .Malin, Meeraja. Abubakar, A Novel Approach of Formulation & Evaluation of Tablet in Capsule Device for GI Protection Pain Management, doi: 10.48047/AFJBS.6.13.2024.5321-5337
Read also our introduction article:
CPHI Milan 2024 – with a focus on excipients
