Influence of Excipients and Processing Conditions on the Development of Agglomerates of Racecadotril by Crystallo-Co-Agglomeration.

Influence of excipients and processing conditions on the development of agglomerates of racecadotril by crystallo-co-agglomeration.

Int J Pharm Investig. 2012 Oct; 2(4): 189-200
Garala K, Patel J, Patel A, Raval M, Dharamsi A

The purpose of the present investigation was to improve the flow and mechanical properties of racecadotril by a crystallo-co-agglomeration (CCA) technique. Direct tableting is a requirement of pharmaceutical industries. Poor mechanical properties of crystalline drug particles require wet granulation which is uneconomical, laborious, and tedious.The objective of this work was to study the influence of various polymers/excipients and processing conditions on the formation of directly compressible agglomerates of the water-insoluble drug, racecadotril, an antidiarrheal agent. The agglomerates of racecadotril were prepared using dichloromethane (DCM)-water as the crystallization system. DCM acted as a good solvent for racecadotril as well as a bridging liquid for the agglomeration of the crystallized drug and water as the nonsolvent. The prepared agglomerates were tested for micromeritic and mechanical properties.The process yielded ~90 to 96% wt/ wt spherical agglomerates containing racecadotril with the diameter between 299 and 521 ?. A higher rotational speed of crystallization system reduces the size of the agglomerates and disturbs the sphericity. Spherical agglomerates were generated with a uniform dispersion of the crystallized drug. CCA showed excellent flowability and crushing strength.Excipients and processing conditions can play a key role in preparing spherical agglomerates of racecadotril by CCA, an excellent alternative to the wet granulation process to prepare intermediates for direct compression. HubMed – drug


Formulation and evaluation of carvedilol melt-in-mouth tablet using mucoadhesive polymer and PEG-6-stearate as hydrophilic waxy binder.

Int J Pharm Investig. 2012 Oct; 2(4): 183-8
Dangi AA, Zalodiya PB

The demand for melt-in-mouth tablets (MMTs) has been rapidly growing during the last decade, especially for the elderly and children who have swallowing difficulties, to avoid first-pass metabolism and quick drug entry into the systemic circulation.In this work, a new approach has been tried to prepare MMTs using a hydrophilic waxy binder [polyethylene glycol (PEG)-6-stearate]. Carvedilol MMTs were prepared by direct compression method using different mucoadhesive polymers such as hydroxypropyl methylcellulose (HPMC), chitosan, and sodium carboxymethyl cellulose (Na-CMC) at various concentrations (range: 0.5-5%) to reduce the flushing action of saliva and to increase mucosal absorption. All the formulations were evaluated for various physiochemical parameters, and the formulations containing the maximum amount of polymer (F4, F7, and F10) were selected for further stability study.The deaggregation time of the tablets was found to be rapid, and the dissolution test revealed that carvedilol was dissolved from the formulation within the compendia limits. This data confirmed that the polymer concentration (0.5-5%) was within acceptable limits. It was also concluded that avicel PH101, pearlitol SD 200, and croscarmellose sodium (CCS) were the appropriate excipients and formulated in the right proportion.As a result, mouth dissolving administration of carvedilol formulated with appropriate excipients and especially with chitosan seems a promising alternative to traditional routes. HubMed – drug


Formulation and optimisation of raft-forming chewable tablets containing H2 antagonist.

Int J Pharm Investig. 2012 Oct; 2(4): 176-82
Prajapati ST, Mehta AP, Modhia IP, Patel CN

The purpose of this research work was to formulate raft-forming chewable tablets of H2 antagonist (Famotidine) using a raft-forming agent along with an antacid- and gas-generating agent.Tablets were prepared by wet granulation and evaluated for raft strength, acid neutralisation capacity, weight variation, % drug content, thickness, hardness, friability and in vitro drug release. Various raft-forming agents were used in preliminary screening. A 2(3) full-factorial design was used in the present study for optimisation. The amount of sodium alginate, amount of calcium carbonate and amount sodium bicarbonate were selected as independent variables. Raft strength, acid neutralisation capacity and drug release at 30 min were selected as responses.Tablets containing sodium alginate were having maximum raft strength as compared with other raft-forming agents. Acid neutralisation capacity and in vitro drug release of all factorial batches were found to be satisfactory. The F5 batch was optimised based on maximum raft strength and good acid neutralisation capacity. Drug-excipient compatibility study showed no interaction between the drug and excipients. Stability study of the optimised formulation showed that the tablets were stable at accelerated environmental conditions.It was concluded that raft-forming chewable tablets prepared using an optimum amount of sodium alginate, calcium carbonate and sodium bicarbonate could be an efficient dosage form in the treatment of gastro oesophageal reflux disease. HubMed – drug


Formulation strategies for drug delivery of tacrolimus: An overview.

Int J Pharm Investig. 2012 Oct; 2(4): 169-75
Patel P, Patel H, Panchal S, Mehta T

Tacrolimus (FK 506) is a potent macrolide lactone immunosuppressive agent used for prophylaxis of organ rejection after transplantation and graft-versus-host disease after bone marrow transplantation in patients. Moreover, tacrolimus is a drug of choice in the treatment of atopic dermatitis for decreasing side effects associated with the use of topical corticosteroids. In spite of its success in ensuring graft survival, therapeutic use of tacrolimus is complicated due to its narrow therapeutic index (between 5 and 15 ng/ml). Tacrolimus has a large inter-/intra-patient variability in pharmacokinetics profile and a poor oral bioavailability because of its poor solubility, P-gp efflux, marked pre-systemic metabolism by CYP3A in the enterocytes and liver first pass effect. Several formulation approaches such as oily solution, solid dispersions, complexation with cyclodextrins, liposomes etc., have been investigated to improve oral delivery of FK 506. In this review, we have discussed various formulation approaches that have been undertaken by various researchers to solve the problems related to the drug delivery of tacrolimus. HubMed – drug


Photoletter to the editor: Botryomycosis in an immunocompetent woman.

J Dermatol Case Rep. 2013 Mar 30; 7(1): 29-30
Barreiros HM, Cunha H, Bártolo E

Botryomycosis is a chronic, granulomatous infection of the skin, soft tissue and viscera. It is uncommon and mainly occurs in immunocompromised patients. Splendore-Hoeppli phenomenon represents an immunological host reaction to antigens of infectious and non-infectious agents. We report a case of a 64-year-old immunocompetent woman presented at our department with a 2-month history of abdominal papules and discharging nodules. She was treated with several antibiotics with no success. Skin biopsy showed granular bodies in the dermis with a Splendore-Hoeppli phenomenon. Microbiologic study isolated a Staphylococcus aureus. Patient was successfully treated 4 weeks with oral clindamycin 300 mg bid. Lack of drug penetration into the “encapsulated-like” microcolonies could explain the therapeutic challenge of this case. HubMed – drug



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